TW201245154A - Substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals - Google Patents

Abstract

The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Description

201245154 6. Description of the Invention: [Technical Field of the Invention] The present invention relates to a compound of formula I,

Among them, A, D, E, L·, G, R10, R30, R40, R50 and R60 have the meanings indicated below, and are valuable pharmaceutically active compounds. It is an inhibitor of protease cathepsin A and can be used to treat diseases such as atherosclerosis, heart failure, kidney disease, liver disease or inflammatory diseases. The invention further relates to a process for the preparation of a compound of formula I, to its use and to pharmaceutical compositions comprising the same. [Prior Art] Cathepsin A (EC = 3.4.16.5; gene symbol CTSA) is a protease also known as lysosomal carboxypeptidase A or a protective protein. It belongs to the family of serine carboxypeptidase which contains only two other mammalian representatives, retinoid-induced serine carboxypeptidase and yolk carboxypeptidase protein. Cathepsin A resides in the lysosome in the cell and forms a high molecular weight complex with β-galactosidase and neuraminidase. The interaction of cathepsin oxime with these glycosidases is necessary to correct the lysosome and protect it against proteolysis in the lysosome. Cathepsin A deficiency caused by multiple mutations in the ctsa gene, resulting in secondary β-galactosidase and neuraminidase deficiency, which appears as an autosomal dominant lysosomal storage disorder galactose sialic acid generation 4 201245154 Xie disease (see A. d'Azzo et al., in " The Metabolic and

Molecular Bases of Inherited Disease", vol. 2 (1995), 2835-2837). Most of the confirmed mutations in ctsa are missense mutations that affect protein folding or stability. It has not been shown to occur at the active site of the enzyme (G. Rudenko et al., Proc. Natl. Acad. Sci. USA 95 (1998), 621-625). Accordingly, lysosomal storage disorders can be corrected with catalytically inert cathepsin A mutations (N. J. Galjart et al., J.

Biol. Chem. 266 (1991), 14754-14762). The structural function of cathepsin A can therefore be separated from its catalytic activity. This point was also emphasized by observation of mice lacking the ctsa gene, and mice with catalytically inert mutations in the ctsa gene did not develop human disease with galactose sialic acid metabolism (RJ Rottier et al., Hum). Mol. Genet. 7 (1998), 1787-1794; V. Seyrantepe et al., Circulation 117 (2008), 1973-1981). Cathepsin A exhibits renegductase activity at acidic pH and exhibits deaminase and esterase activity at neutral pH against a variety of naturally occurring bioactive peptides. In vitro studies indicated that cathepsin A converts angiotensin I to angiotensin 1-9 and bradykinin to bradykinin 1-8, which is a ligand for the bradykinin B1 receptor. It hydrolyzes endothelin, neurokinin and oxytocin, and deamination of substance p (see M Hiraiwa,

Cell. Mol. Life Sci. 56 (1999), 894-907). The detection of local cathepsin A activity in the urine is suggested to be associated with the degradation of tubular bradykinin (M. Saito et al) Int. J. Tiss. Reac. 17 (4995), 181-190). Enzymes can also be released from platelets and lymphocytes and expressed in anti-201245154 original cells where they may be involved in antigen processing (WL Hanna et al., J. Immunol. 153 (1994), 4663-4672; H. Ostrowska, Thromb Res. 86 (1997), 393-404; M. Reich et al., Immunol. Lett, (online Nov. 30, 2009)). Immunohistochemistry of human organs revealed prominent expression in renal tubular epithelial cells, bronchial epithelium Cells, interstitial cells of the testis, and large neurons of the brain (〇. Sohma et al., Pediatr. Neurol. 20 (1999), 210-214). They regulate upward during monocyte differentiation into macrophages (Ν · M. Stamatos et al., FEBS J. 272 (2005), 2545-2556). In addition to structural and enzymatic functions, 'Cathepsin A confirms binding to neuraminidase and alternative spliced β-galactosidase Formation of cell-surface adhesion and elastin receptor complexes in fibroblasts, smooth muscle cells Chondrocytes, white blood cells, and certain cancer cell types (A. Hinek, Biol. Chem. 377 (1996), 471-480). The importance of cathepsin A in regulating the amount of local bradykinin in animal models of hypertension It is demonstrated that the pharmaceutical inhibition of cathepsin A activity increases the amount of kallikrein and prevents salt-induced hypertension (H. Ito et al., Br. J. Pharmacol. 126 (1999), 613-620). It can be achieved via an antisense oligonucleotide that inhibits the expression of cathepsin A (I. Hajashi et al., Br. J. Pharmacol. 131 (2000), 820-826). In addition to high gold pressure, the benefit of slow stimulation The effects are demonstrated in a variety of other cardiovascular and other diseases (see J. Chao et al., Biol. Chem. 387 (2006), 665-75; P. Madeddu et al., Nat. Clin. Pract. Nephrol. 3 (2007), 208-221). The main factor of cathepsin A inhibitors 6.201245154 Indications include atherosclerosis, heart failure, heart infarction, cardiac hypertrophy, a tube hypertrophy, left ventricular dysfunction, especially Is left ventricular dysfunction after myocardial infarction, kidney disease such as renal interstitial fibrosis, renal failure Inadequate renal function; liver diseases such as liver fibrosis and liver sclerosis, diabetic complications such as nephropathy, as well as organs such as the heart and kidneys of organ protection. As described above, cathepsin A inhibitors can prevent the production of the bradykinin B1 receptor ligand bradykinin M (M Sait〇 et al, Im)

Reac. 17 (1995), 181-190). This provides an opportunity to treat pain, particularly neuropathic pain, and inflammation with cathepsin A inhibitors, as evidenced by bradykinin B1 receptor antagonists (see jp Marceau et al., Nat.

Rev. Drug Discov. 3 (2004), 845-852). Cathepsin A inhibitors can also be used as antiplatelet agents, which can be demonstrated via a proponolide derivative of the cathepsin A inhibitor, ebexerone B (ebelactone B), which inhibits platelet aggregation in hypertensive animals (H. 0str 〇wska et al., J. Cardiovasc. Pharmacol. 45 (2005), 348-353). In addition, like other serine proteases such as prostaglandin, elastase or proteolytic enzymes, cathepsin A can stimulate the amiloride-sensitive epithelial sodium channel (ENaC) and thus the fluid volume through the epithelial membrane. Regulation (see C. Planes et al., Curr. Top. Dev. Biol. 78 (2007), 23-46). Accordingly, respiratory diseases such as cystic fibrosis, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infection, and lung cancer can be improved by using a cathepsin A inhibitor. Cathepsin A regulation in the kidney can be used to promote diuresis and thus initiate hypotensive effects. 201245154 In addition to the above-mentioned compound ebelactone B, the inhibitory effect of cathepsin A was found in certain dipeptide phenylalanine derivatives which are disclosed in ^2005/145839. Other compounds are required to inhibit the group, Protease A and provide an opportunity to treat the above diseases and other diseases in which tissue protease A is involved. The present invention satisfies this need by providing an oxygen-substituted 3_heteroaryl-propionic acid derivative as defined by Formula I below. It is disclosed that certain compounds may be present in the 3-heteroarylamino-propionic acid group. For example, the amine derivatives disclosed in WO 2006/076202, which modulate the activity of steroid nuclear receptors, carry a heteroaryl fluorenyl group on the nitrogen atom of the amine functional group and a broadly defined other group. A widely defined amino acid derivative is disclosed in US 2004/0072802, which carries a thiol group on the β-amino group and is an inhibitor of matrix metalloproteinases and/or tumor necrosis factors. In w〇2〇〇9/〇8〇226 and W0 2009/080227, which are antagonists of platelet ADp receptor P2Y] and inhibit platelet aggregation, revealing that bis-oxazolidinyl-substituted carboxylic acid is derived. But it has an additional carboxylic acid derivative group on the carbon atom bearing the pyrazolylamine group. Other compounds substituted with a oxazolidine group are attached to the gas atom of the moon. The ring system, which is an inhibitor of the blood coagulation enzyme Factor Xa and/or the Vila factor, is disclosed in WO 2004/056815. SUMMARY OF THE INVENTION The present invention is a compound of the formula I which is in any stereoisomerism 8 .201245154 a mixture of forms or stereoisomeric forms in any proportion, or

Wherein A is a series selected from the group consisting of QR1) and N; D is a series selected from the group consisting of C(R2) and N; E is a series selected from the group consisting of C(R3) and N; L is selected from C(R4) and a series consisting of N, wherein at least one and at most two A, D, E or L are N; G is selected from the group consisting of R71-〇-C(0)-, R72_N(R73)_c(〇) and four 〇 sitting_ a series consisting of 5 groups; R1 is selected from the group consisting of hydrogen, _ group, (CrC6)-alkyl, HO-, (QQ)-alkyl-0-, CrC6)-alkyl-s(0)m- and NC- a series consisting of; R2 is selected from the group consisting of hydrogen, halo, (eve?)-alkyl, (CrC6)-alkyl-oxime-, (CrC6)-alkyl-CO-, (crc6)-alkyl-CO- a series consisting of HN-, NR12R13, Het, (C3-C7)-cycloalkyl-CsH2s- and Ar-CsH2s-, wherein s is an integer selected from the group consisting of ruthenium, 1, 2 and 3; R3 is selected from the group consisting of hydrogen and halogen Base, (CrC6)-alkyl, (CrC6)-alkyl-SCOU-,

a series consisting of Het4-(0)t-, -NR12R13, Het2, Rn-0-, R12-N(R13)-C(0)-0- and Het2-C(0)-0- and NC-, wherein s is an integer selected from the group consisting of oxime, ib 2 and 3 and wherein t is an integer selected from 〇 and 1; R 4 is selected from the group consisting of hydrogen, halo, (CrC6)-alkyl, (CrC6)-alkyl-oxime-, 201245154 series of HO-, NR12R13, Het2; R1G is selected from hydrogen, halo, (CVC6)-alkyl, (CrC6)-alkyl-oxime, alkyl-S(0)m-, HO-, a series of -NR12R13, Het2, phenyl-CsH2s-(0)r, wherein s is an integer selected from 0, 1, 2 and 3 and wherein t is an integer selected from 0 and 1; or R1 and R2 or R2 And R3 forms an acridinyl group; or R1 and R2 are -C((CrC3)-alkyl)=NN((CrC3)-alkyl)-; or R2 and R3 are -NH-CH=N-; One of R1, R2, R3, R4 or R1G is a cyclic substituent; R11 is a series selected from the group consisting of hydrogen, R14, (C3-C7)-cycloalkyl, Ar and Het3; R12 and R13 are independently selected from each other. a series consisting of hydrogen and R15; R14 is (CrC1())-alkyl optionally substituted one or more of the same or different selected from halo, HO-, R16-0-, keto, (C3-C7 )-cycloalkyl, Ar, Het1, Het3, NC-, H2N-C ( 0)-, (CrC4)-alkyl-NH-C(O)-, di((CVQ)-alkyl)NC(O)·, HetLqO)·, (CrC4)_alkyl-C(0)- Substituted by a substituent of the NH- and (CrC4)-alkyl-S(0)m-composition series; R15 is a (Ci-C6)-alkyl group optionally randomly selected from halo groups by one or more of the same or different , HO- and (C-C6)-substituted substituents of the series of alkyl groups; R16 is (CrC6)-alkyl group, which is optionally selected from one or more of the same or different selected from HO-, (C1-C4) Replacement with a substituent consisting of a group consisting of a group of -O- and NC-; 201245154 R30 is a column selected from the group consisting of R31, (C3-C7)-cycloalkyl, R32-Cuh2u_ and Het3_CuH2u_ where u is selected From the integers of 0, 1, 2 and 3; R3 is (Ci-Cw)-alkyl group which is optionally one or more of the same or different selected from halo, (C3-C7)-cycloalkyl, HO- , (CrC6)·alkyl-hydrazine-, (CrC6)-alkyl-S(0)m-&----substituent substitution of NC-series; R32 is selected from phenyl and aromatic 5-member or 6 a member comprising a monocyclic heterocyclic group consisting of one, two or three ring heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and linked via a ring carbon atom wherein the phenyl and heterocyclic groups are all Desirably one or more of the same or different selected from halo, (Crc6)-alkyl, (C3-C7)-cycloalkyl, R33, HO-, (CVQ)-formyl·〇_, r33_〇_ , R33-(Ci_C4)-hospital-Ο-, -O-CH2-O-, -O-CF2-O-, (C^-C^)-alkyl-S(0)m-, H2N-S (0) 2_, (C1-C4)-alkyl-NH-S(0)2_, bis((CrC4)-alkyl)NS(0)2-, H2N-, (CrC6)-alkyl-NH- , bis((CrC6)-alkyl)N-, Het1, (Ci-C4)-alkyl-C(0)-NH-, Ar-C(0)-NH·, (CrC4)-alkyl-S (〇) a substituent substituted by a series of 2-NH- and NC-; R33 is a series consisting of a phenyl group and an aromatic 5-member or a 6-membered monocyclic heterocyclic group, which contains one, two or three Ring heteroatoms which are the same or different from nitrogen, oxygen and sulfur and which are bonded via a ring carbon atom, wherein the phenyl and heterocyclic groups are all optionally randomly selected from one or more of the same or different selected from halo, ((VQ) -alkyl, (C3-C7)-cycloalkyl, HO·, (Ci_C6)-alkyl-hydrazine-, (Ci-C6)_alkyl-S(0)m-, H2N-S(0)2 -, (CVC4)-alkyl-NH-S(0)2-, bis((CrC4)-alkyl)NS(0)2- and substituents of the NC-series series; 201245154 R40 is selected from hydrogen And (Q-CO-alkyl group Or R30 and R40 are (CHA optionally substituted by one or more identical or different (CrC4)-alkyl substituents, wherein X is an integer selected from 2, 3, 4 and 5; R50 is a series selected from the group consisting of hydrogen, (CrC6)-alkyl, HO- and (CrC6)-alkyl; R6G is a series selected from the group consisting of hydrogen and (CrC6)-alkyl; or R50 and R60 are (CH2) y , optionally substituted by one or more identical or different (Cl-C4)-alkyl substituents, wherein y is an integer selected from 2, 3, 4 and 5; R71 is selected from hydrogen and (CpCs) a series of alkyl groups optionally substituted with one or more substituents of the same or different series selected from the group consisting of (CrC6)-alkyl-oxime- and (crC6)-alkyl-c(o)-o- Substituted; R72 is selected from the group consisting of hydrogen, (CrC6)-alkyl, (C3-C6)-cycloalkyl, -CH2-(CH2)b-(C3-C6)-cycloalkyl, Het4 and -(CH2)b a series consisting of -Het4 wherein the alkyl or cycloalkyl group is optionally one or more selected from the group consisting of halo, HO-, HOOC-, (C"C6)-alkyl-oxime- and (cvc6) - a substituent substituted by a series of a group of -C(0)-〇·, Nc-, N((Cl_C4)_alkyl)2 and b is 0, 1 or 2; R73 is selected from hydrogen, (crc6) -alkyl a series of constituents; or R 2 and R 73 together with the nitrogen atom to which they are bonded form a saturated 4_ member to 7-membered monocyclic heterocyclic group optionally containing a heterocyclic ring selected from the group consisting of nitrogen, oxygen and sulfur An atom optionally substituted with one or more substituents selected from the group consisting of halogen 12 201245154, (Ci-C4)-alkyl, HO- and (Ci-C#)-homoquinone;

Ar, independently of the other Ar groups, is selected from the group consisting of phenyl and aromatic 5-membered or 6-membered monocyclic heterocyclic groups containing one, two or three rings of the same or different selected from the group consisting of nitrogen, oxygen and sulfur. The heteroatoms are bonded via a ring carbon atom, wherein the phenyl and heterocyclic groups are all optionally randomly selected from one or more of the same or different selected from halo, (CVC6)-alkyl, HO-(CrC6)-alkyl, Het4. ,-(CH2)X-phenyl, (CrC6)-alkyl-oxime-, (C3-C7)-cycloalkyl-(CH2)x-0-'-CF3, -CO-(CrC6)-alkyl Substituted with a series of substituents of -NR12R13, Het2, -CO-NR12R13, CO-Het2, (CVC6)-alkyl-S(0)m-, h2N-S(0)2-, and NC-; Phenyl can be via -CH=CH-CH=CH stomach, -OCH2-0-, -0-CH2-CH2-0-, -0-CF2-0- or -Ν(((ν(:3)-alkane) Base) -CH=CH- substituted;

Het, independently of the other Het groups, is a saturated or unsaturated 4-membered to 8-membered monocyclic heterocyclic group containing a ring nitrogen atom and Heti is linked thereto and optionally one or two identical or different Other ring heteroatoms from gas, oxygen and sulfur, optionally at one or more of the same or different selected from halo, (CrC4)-alkyl, HO-, (CrC4)-alkyl, keto and NC- Substituted by a series of substituents;

Het2 is a saturated 4- to 7-membered monocyclic heterocyclic group containing a ring nitrogen atom and Het2 is bonded thereto and optionally a ring hetero atom selected from nitrogen, oxygen and sulfur, optionally passing through a ring. Or a plurality of substituents of the same or different substituents selected from the group consisting of a halogen group, a (CrC4)-alkyl group, a HO- and (CrC4)·alkyl group, and a ruthenium group;

Het3' is independent of each other and is a 4-membered to 7-membered monocyclic heterocyclic group containing one or two other heteroatoms of the same or different nitrogen, oxygen and sulfur and via a ring carbon. An atomic linkage, optionally substituted with a plurality of substituents of the same or different substituents selected from the group consisting of fluorine, (CrC4)-alkyl and keto groups;

Het4, independently of the other Het4 groups, is a saturated or unsaturated 4 to 8 membered monocyclic heterocyclic group containing from one to four other ring heteroatoms of the same or different selected from the group consisting of nitrogen, oxygen and sulfur. Substituting one or more substituents of the same or different substituents selected from the group consisting of halo, (CVQ)-alkyl, HO-'CCrCO-alkyl-oxime, keto, and NC-; m, with other numbers m is independently of each other and is an integer selected from the group consisting of ruthenium, 1 and 2; wherein all of the cycloalkyl groups are independently, independently of one another, one or more substituents of the same or different substituents selected from the group consisting of fluorine and (CrC4)-alkyl groups. Substituent; wherein all of the alkyl, CsH2s, CuH2u, (CH2)X and (CH2)y are independent of each other, and independently of any other substituent, are optionally substituted with one or more fluorine substituents. If a structural element such as a group, a substituent or a number may occur several times in a compound of formula I 'all of them are independent of each other and may have any indicated meaning in each case, and it may be the same in each case or Unlike any other this element. For example, in the dialkylamino group, the alkyl groups may be the same or different. The alkyl group, which is a saturated hydrocarbon group, may be a linear (straight chain) or a branched 201245154 chain. This also applies if the groups are substituted or part of other groups, such as alkyl-0-(alkyloxy, alkoxy) or HO-substituted alkyl (hydroxyalkyl). The number of carbon atoms in the alkyl group may be, for example, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10' or 1, 2, 3, 4, 5, 6, 7 depending on the definition. Or 8, or 1, 2, 3, 4, 5 or 6' or 1, 2, 3 or 4, or 1, 2 or 3, or 1 or 2, or 1. In a particular embodiment of the invention, the (crc10)-alkyl group present in the compound of formula I is (CrC8)-alkyl, in another embodiment is (CrC6)-alkyl, in another specific In the examples is (crc4)-alkyl, in another embodiment (crc3)-alkyl, in another embodiment (crc2)-alkyl, in another embodiment ( C2-c3)-alkyl, in another embodiment is a fluorenyl group. In a particular embodiment of the invention, the (crc8)-alkyl group present at any position in the compound of formula I is (crc6)-alkyl, and in another embodiment is (crc4)-alkyl, in another In one embodiment is (crc3)-alkyl, in another embodiment (CVC2)-alkyl, in another embodiment is (c2-c3)-alkyl, in another embodiment In the exemplified are fluorenyl groups, wherein any (crc8)-alkyl group present in the compound of formula I may be a group of any of these specific embodiments independently of the other (crc8)-alkyl groups. In a particular embodiment of the invention, the (crc6)-alkyl group present at any position in the compound of formula I is (crc4)-alkyl, and in another embodiment is (crc3)-alkyl, in another In a particular embodiment is (crc2)-alkyl, in another embodiment is (c2-c3)-alkyl, in another embodiment is methyl, wherein is present in compound 15 201245154 of formula I Any (CrC6)-alkyl group which may be independently of each other (CrC6)-alkyl group is a group of any of these specific examples. In a particular embodiment of the invention, the (CrC4)-alkyl group present in any position in the compound of formula I is (Ci-C3)-alkyl, and in another embodiment is (CrC2)-alkyl, In another embodiment is a (C2-C3)-alkyl group, and in another embodiment is a fluorenyl group, wherein any (C1-C4)-alkyl group present in the compound of formula I can be combined with other (CVC4) - The yards are independent of each other and are the basis of any of these specific embodiments. Examples of alkyl groups are methyl, ethyl, propyl including propyl (i.e., n-propyl) and isopropyl, butyl including butyl (i.e., n-butyl), t-butyl, isobutyl, and The third butyl group and the pentyl group include a pentyl group (ie, n-pentyl group), a 1-decyl butyl group, an isopentyl group, a neopentyl group, and a third pentyl group, and the hexyl group includes a hexyl group (ie, a n-hexyl group), 3, 3-dimethylbutyl and isohexyl, heptyl includes heptyl (ie, n-heptyl), octyl includes octyl (ie, n-octyl), fluorenyl includes fluorenyl (ie, n-decyl), The sulfhydryl group includes a sulfhydryl group (ie, a ruthenium group). Examples of alkyl-hydrazine- are methoxy, ethoxy, propoxy (i.e., n-propoxy), isopropoxy, butoxy (i.e., n-butoxy), isobutoxy, Third butoxy, pentyloxy (ie, n-pentyloxy). Examples of alkyl-s(0)m- are methylsulfanyl-(CH3-S-), sulfinyl-(CH3-S(0)-), sulfonyl (CH3-S) 0) 2-), ethylsulfanyl-(CH3-CH2-S-), ethanesulfinyl-(CH3-CH2-S(0)-), ethylsulfonyl (CHrCH2-S(0) 2-), 1-mercaptoethylsulfanyl-((CH3)2CH-S-), 1-mercaptoethanesulfinyl-((CH3)2CH-S(0)-), 1-曱Ethyl sulfonyl ((CH3)2CH-S(〇)2-). In one embodiment of the invention, the number 16 201245154 words m is selected from 〇 and 2, wherein all numbers m are independent of each other and may be the same or different. In another embodiment, the number m at which it appears is 〇 independent of other occurrences. In another embodiment, the number m at which it appears is 2, independent of other occurrences. The substituted alkyl group can be substituted at any position. The prerequisite is that each compound is sufficiently stable and suitable as a pharmaceutically active compound. The various groups and compounds of formula I are prerequisites for their stability and suitability as pharmaceutically active compounds, and are generally applicable to the definition of all groups in the compounds of formula I. In a particular embodiment of the invention, any alkyl group in the compound of formula I and individual carbon atoms in other groups such as cycloalkyl and heterocyclic groups, independently of any other carbon atom, are not more than one A substituent bonded to an oxygen atom, a nitrogen atom or a sulfur atom, for example, HO-, (CrQ)-alkyl-〇- or (crC4)-alkyl-S(0)m-substituent. The alkyl group optionally subjected to one or more fluorine substituents may be unsubstituted, that is, without a fluorine substituent, or for example, one, two, three, four, five, six, seven, eight, nine, ten Or substituted with eleven fluoro substituents, or substituted with one, two, two, four, five, six or seven fluoro substituents, or substituted with one, two, three, four or five fluoro substituents, or one Substituted with two or three fluorine substituents, which can be located at any position. For example, in a fluorine-substituted alkyl group, one or more fluorenyl groups may each have three fluoro substituents and be present as a trifluoromethyl group, and/or one or more fluorenylene groups (CH2) may each have two Fluorine substituent and present as difluoromethylene. The description of each fluorine-substituted group also applies if the group additionally carries other substituents and/or another group 17 201245154, such as alkyl-o-. Examples of fluoro-substituted alkyl groups are trifluoromethyl, 2-fluoroethyl, 1-oxyethyl, 1,1-difluoroethyl, 2,2,2-triseoethyl, five-rat ethyl 3,3,3-dimethylpropyl, 2,2,3,3,3-pentapropyl, 4,4,4-trifluorobutyl and heptafluoroisopropyl. Examples of the fluorine-substituted alkyl group are a trifluoromethoxy group, a 2,2,2-trifluoroethoxy group, a pentafluoroethoxy group, and a 3,3,3-trifluoropropoxy group. Examples of fluoro-substituted alkyl-S(〇)m- are trifluoromethylsulfanyl-(CFs-S-), trifluoromethylsulfinyl-(CFrS(0)-) and trifluoro Mercaptosulfonyl (cf3-s(o)2-). The above description regarding the alkyl group correspondingly applies to the alkanediyl group (divalent alkyl group) including the divalent groups CsH2s, CuH2u, (CH2)x&(CH2)y. The alkyl moiety of the substituted alkyl group can also be considered as a divalent group. Accordingly, the alkanediyl group may also be straight-chain or branched, and the bond to an adjacent group may be at any position and may start from the same carbon atom or a different carbon atom, and it may be substituted with a fluorine substituent. Examples of the alkanediyl group include a group (: fluorene and CuH2u and as long as it constitutes a polyindenylene chain, the group ((: 乂 is -匚仏-, -CH2-CH2-'-CH2-CH2-CH2- '-CH2-CH2-CH2-CH2-'-CH2-CH2-CH2-CH2-CH2-, -CH(CH3)-, -C(CH3)2-, -CH(CH3)-CH2-, -CH2- CH(CH3)-, -C(CH3)2-CH2-, -CH2-C(CH3)2. Examples of fluorine-substituted calcined bases, which may contain one, two, three, four, five or six Fluorine substituents, or one, two, three or four II substituents or one or two fluorine substituents, are -CHF-, -CF2-, -CF2-CH2-, -CH2-CF2-, -CF2 -CF2-, -CF(CH3)-, -C(CF3)2-, -C(CH3)2-CF2-, -CF2-C(CH3)2-. Ring in (C3_C7)-cycloalkyl The number of carbon atoms may be 3, 201245154 5, 6 or 7. Examples of cycloalkyl groups are cyclopropyl, cyclobutyl, cyclodecyl, cyclohexyl and cycloheptyl. As for cycloalkyl via one or more ( CVC4)- a random substitution of an alkyl substituent which may be unsubstituted, ie without an alkyl substituent, or for example one, two, three or four' or one or two identical or different (CrC4)-alkyl substituents such as decyl substituted three The group may be in any position. Examples of the alkyl-substituted cycloalkyl group are 1-methylcyclopropyl, 2,2-dimethylcyclopropyl, methylcyclopentyl, 2,3-dimethyl Cyclopentyl, methylcyclohexyl, 4-nonylcyclohexyl, 4-isopropylcyclohexyl, 4-tert-butylcyclohexyl and 3,3,5,1 tetramethylcyclohexyl. Random substitution of one or more fluorine substituents, which may be unsubstituted, that is, without a fluorine substituent, or for example, one, two, three, four, five, six, seven, eight, nine, ten or a ten-fluoro substituent, or one, two, three, four, five or six fluorine substituents, two, three or four fluorine substituents, or substituted by one or two fluorines may be present in the fluorine substituent The cycloalkyl group may also be at any position on the cycloalkyl group or the substituent substituted by a mono group. An example of the 11-substituted Wei group is 1-fluoro% <propyl, 2,2-di Fluorocyclopropyl, 3,3-difluorocyclobutyl, 1-fluorocyclohexyl, 4,4·difluorocyclohexyl and 3,3,4,4,5,5-hexafluorocyclohexyl.cycloalkyl Also: a case in which an alkyl group substituted with (CrC7)_cycloalkyl group is substituted by fluorine and an alkyl group, It may represent, for example, R11 or R3, which is propyl fluorenyl, cyclobutyl fluorenyl-, cyclopentyl fluorenyl _, cyclohexyl fluorenyl... cycloheptyl fluorenyl, 1-1⁄4 propyl ethyl... 2- Cyclopropylethyl-, 1-cyclobutylethyl-, 2-cyclobutylethyl-, 1, cyclopentylethyl...2-cyclopentylethyl, cyclohexylethyl-, 2- Cyclohexylethyl_, 丨-cycloheptylethyl... 2 cycloheptylethyl. 19 201245154: The description of the alkyl group corresponding to the divalent cycloalkyl group (cycloalkane) ' can occur if the two groups r30 40 or (d) together are the y. The substituent moiety can be considered as a Wei-diyl group. Accordingly, for example, a cycloalkyl group, a bond attached thereto to an adjacent group, may be located at any position and: starting from a 3t-like carbon atom, as in the case of a cycloalkanedi group, such as R and R together is (CH2)x or two groups R50 and R60 are (in the case of CHJy, or start from a different ring carbon atom. In the substituted stupid group, the substituent may be in any position. In the case of a valence substituent - 〇-ch2-〇-(indenylenedioxy) and -〇_CFV〇(difluoromethylenedioxy), it may be present on a phenyl group and an aromatic heterocyclic group. The two oxygen atoms are adjacent ring carbon atoms bonded to the phenyl or aromatic heterocyclic group and replace the two hydrogen atoms of the parent system. In the monosubstituted phenyl group, the substituent may be in the 2-position, 3 - position or 4 stomach position. 'Substituents in a disubstituted phenyl group may be in the 2,3-position, 2,4-position, 2,5-position, 2,6-position, 3,4-position or 3,5-position. In the trisubstituted phenyl group, the substituent may be in the 2,3,4-position, 2,3,5-position, 2,3,6-position, 2,4,5· position. , 2, 4, 6-position or 3, 4, 5-position. If the phenyl group has four substituents' It may be, for example, a fluorine atom, and the substituent may be at the 2, 3, 4, 5-position, 2, 3, 4, 6-position or 2, 3, 5, 6-position. If the polysubstituted phenyl group has a different a substituent, each substituent may be in any suitable position' and the invention includes all positional isomers. The number of substituents in the optionally substituted phenyl group may be one, two, three, four or five. In one embodiment of the invention, the 'optionally substituted phenyl group' is independently of any other randomly substituted phenyl group in the compound of formula 20 201245154, with one, two or four, in another specific In one embodiment, one, two or one, in another embodiment one or two, in another specific embodiment is one, the same or different substituents, and in another embodiment It is unsubstituted. Similarly, among the substituted heterocyclic groups, it includes aromatic 5_members and single-rings. Heterocyclic groups can represent r32, r33 and saturated and unsaturated spears 4- To a 8-membered monocyclic heterocyclic group which may represent a 1, and a saturated member to a 7-membered monocyclic heterocyclic group which may represent this 2 And W, a substituent may be present at any position and may be present on a ring carbon atom and a suitable ring nitrogen atom. The invention includes all positional isomers which may be present in a substituted heterocyclic group of a compound of formula I. The number of bases depends on the size of the ring, the number of materials, and the extent of the type of the residue. In this, the number of identical or different substituents on any heterocyclic group in the compound of the formula! And the number of substituents of any other group present on the other heterocyclic group in the hydrazine compound is independent of each other, and is -, -, - interesting one, two, four or five, in another specific ^ 1 Lieutenant one, two, three or four 'in another specific embodiment = one, two or three' in another embodiment - or two, f another - specific implementation is - One. The net of the substituent optionally includes a ring nitrogen J in which the ring is not bonded via a saturated heterocyclic ring, and a 5-shell aromatic heterocyclic ring such as a pyrrole, imidazole or triazole nitrogen atom. The parent heterocyclic ring carries a hydrogen atom. 21 201245154 Substituent oxime on any of the ring nitrogen atoms of one of the present invention, selected from the group consisting of substituents indicated at the definition of each group bonded via a carbon atom, for example Selected from (Ci.CM, (cvc7)-cycloalkyl and R' in another embodiment is selected from (CrC6)-homo and (CrC7)-cycloalkyl, which may represent R32 In the case of a heterocyclic ring, it is selected from the group consisting of %-(:6)-homoxyl group and in the case of an aromatic heterocyclic ring which may represent r33, from (CVC7)·cycloalkyl, in the case of an aromatic heterocyclic ring which may represent Ar In the case where 疋 is selected from (C丨-C6)-alkyl and in the case of Heti, Het2 and Het3, (, from (crc4)-filament, through t, except optionally with the derogatory in each group & In addition to the substituents, the 32.t nitrogen atom, especially the aromatic heterocyclic group in the heterocyclic group of the compound of the formula 1, for example, may represent a heterocyclic group of R, R & Ar, for example. The ring nitrogen in the bite group may also have an oxo group and a ruthenium oxide. It may represent g, Het2 H and a ruthenium monocyclic heterocyclic group and a combination of Any suitable two-set == group::dimer, Stable and suitable as a doctor

In a specific embodiment of the present invention, in the heterocyclic ring of formula I, the solid-ring hetero atom cannot exist in the phase = J! The two ring heteroatoms having a hydrogen atom or a fluorene group have a ring atom single bond The ruthenium atom and the s atom in the adjacent hetero fluorenyl group cannot exist in the adjacent ring position of 22 201245154. In the aromatic heterocyclic ring, the choice of the ring hetero atom and its position are limited by the fact that the ring is a prerequisite for aromaticity, that is, it contains a ring system of six non-localized π electrons. Accordingly, for example, in an aromatic monocyclic 6-membered heterocyclic ring, only a nitrogen atom may appear as a ring hetero atom, and in an aromatic monocyclic 5-membered heterocyclic ring, only one selected from a hydrogen atom or A ring hetero atom of a substituent of a 0 atom, an S atom, and a ruthenium atom series. The heterocyclic group which may represent Het1 may be aromatic, for example, in the case of a pyrrolyl group, an imidazolyl group or a triazolyl group, which is bonded via a ring nitrogen atom and may represent Het1, or is non-aromatic and contained in the ring. There are one or two double bonds that can exist anywhere. In a particular embodiment, the 4-membered heterocyclic group representing hydrazine cannot be unsaturated. Heterocyclyl groups can each be bonded via any ring f atom or via any suitable ring nitrogen atom, as described in the definition of each group. Het1 can be 4-, 5-, 6- or 7- or 8-member. Het2 and Het3 can be 4-, 5, 6 or 7 members. Examples of aromatic heterocycles may represent R32, R33 and Ar and are as suitable as possible for any one or more of the aromatic 5-membered and 6-membered monocyclic heterocyclic groups. In a specific embodiment of 2, the Het1 is From (4), material "cembran", imidazole, pyrazole, carbazole ([U] drink azole), carbazole ([1,2] carbazole ^ saliva ([1,3] 嗟嗤), isoindole Saliva ([12] ten sittings), [to three saliva, (1) three saliva, [1,3,4 oxadiazole "bipyridine, tarenged" pyridine and its material, all of which are via any ring carbon atom or via Any suitable cyclic nitrogen, =, and all of which are optionally substituted as described above for the compound of formula I or any of the specific examples above and below. An example of a group: R32, R33 and Ar and as far as possible ^ 23 201245154 Any one or more aromatic 5-membered and 6-membered monocyclic heterocyclic groups, in a specific embodiment of the invention, Het1 is selected from pyrrole small groups, 0 is more than -3, the base, the mouth is kein-2-yl, the mouth is mouth South, and the volume is '_〇甘μμ

嗒-4-yl, pyrimidin-2-yl, pyrimidine-4-yl and pyridin-2-yl, all of which are analogous to the general compounds of formula I or any of the above and below specified.

Examples of saturated heterocyclic and non-aromatic unsaturated heterocyclic rings, in one embodiment of the present invention, Het1, Het2, Het3, and 4 are selected from any one or more of them, for the size of the ring and The degree of saturation is as follows, which is 'azetine, propylene, thiazepine, pyrrolidine, 2,5-dihydro-1H-pyrrole, tetrahydrofuran, tetrahydrothiophene, pyrazole, imidazole Pyridine, 4,5-dihydro-1H-imidazole, [L3]dioxolane, oxazolidinetrithiazolidinium, hexahydropyridine, 1,2,3,6-tetrahydropyridine, tetrahydropyran, tetra Hydrogen thiopyran, hexahydro (tetra), [(3) two gang, ^] akisaki, sulphon, sulphon, azepane, oxepane, thioheptane, 24 201245154 [1, 3] diazepine, (10) diazepine, (10) oxepane, [1,4], heterocyclic, and nitrogen, and all of which are like the general compound of formula I or above And arbitrarily substituted as described in any of the specific examples below (4). Examples of saturated heterocyclic and non-aromatic unsaturated heterocyclic ring-specific groups, in one embodiment of the invention, 孖", Het2, Het3, and Het4 are independently selected from any one or more of them, for a ring The size, degree of saturation, and the type of atom to which the group is bonded are as applicable as possible, and are azacyclobutan-1-yl, oxetan-3-yl, thietane-3-yl, pyrrolidinyl, Pyrrolidinyl-2-yl-pyrrolidinyl-3-yl, 2.5-dihydro-1H-pyrrol-1-yl, tetrahydrofuranyl, tetrahydrofuranyl, tetrakishen-2-yl, tetrahydro-septene-3- Base, π is β-supplemented, β-pyrazin-4-yl, imidazolidinyl, imidazolidin-2-yl, imidazolidinyl, 4.5-dihydro-1Η-imidazol-2-yl, 1, 3-dioxolan-2-yl, 1,3-dioxolan-4-yl, guan-2-yl, guanidine-3-yl, 啐cr sigma-4-yl, π|oxazolidine-5-yl, thiazolidin-2-yl, thiazolidin-3-yl, thiazolidinyl, thiazolidin-5-yl, hexahydropyridin-1-yl, hexahydropyridin-2-yl, Hexahydroazin-3-yl, hexahydropyridin-4-yl, 1,2,3,6-tetrahydropyridin-1-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl Tetrahydropyran-4- , tetrahydrothiopyran-2-yl, tetrahydrosulfurium σ-pyranyl 3-yl, tetrahydrothiona-pyranyl-4-yl, hexahydropyrene, hexamidine, hexahydropyrylene-2-yl, [1,3] Diterpenoid-2-yl, [1,3]diπ-alkyl-4-yl, [1,3]dioxan-5-yl, anthracene, 4]dioxane-2- Base, fraternity. Lin-2-yl, flufen-3-yl, morpholine-4-yl, thiomorphin-2-yl, thiophene-3-yl, thiophene- 4-yl, azepan-1-yl, azepan-2-yl, azepan-3-yl, azepan-4-yl, oxe-2-a 201245154, Oxecycloheptan-3-yl, oxepan-4-yl, diazepane, [1,4]diazepine, [14]oxetan and (1)4] thiophene Aza-heptyl-l-yl, and all of which are optionally substituted as described in the general formula or any of the specific examples specified above and below. Halo is fluoro, chloro, bromo or iodo. In one embodiment of the invention, any of the dentate groups present in the compound of formula I, independently of one another, are fluorine, gas or bromine, and in another embodiment, fluorinated or sulphur, in another embodiment a specific embodiment Is a fluorine. A keto substituent, that is, an oxygen atom bonded via a double bond, when attached to a carbon atom, replaces two hydrogen atoms on the carbon atom of the parent system to which it is attached. Accordingly, if CH2 is substituted with a ketone group, It becomes a carbonyl group (c(〇), C Ο). The keto substituent cannot exist on the carbon atom of the aromatic ring. In addition to the carbon atom, the 'keto substituent may also be present on the ring sulfur atom of Heti. In particular, if Het1 is saturated, and in Het3, if a keto substituent is present on the sulfur atom, the ring member s(〇) (S-0, also known as a subunit) is obtained, or if two ketone groups are substituted The base is present on the sulfur atom to give the ring member S(0)2 (S(=0)2, which is the sulfone group). An example of a heterocyclic ring which may represent Het1 and Het3 and which has a cyclic sulfur atom of a keto substituent is 1,1-di-yl-tetrahydroneptene, 'as is the general compound of formula I or above and below Any of the specific examples specified herein are described as being "optionally substituted with other substituents such as (Cj-C4)-alkyl substituents. The present invention includes all stereoisomeric forms of the indole compounds, and examples 26 201245154 include all para-isomers and non-paraffinomers including cis/trans isomers. The invention likewise includes mixtures of two or more stereoisomeric forms, such as a palmo isomer and/or a non-paraffinomer, including a mixture of cis/trans isomers in all ratios. Included in the asymmetric center of the compound of formula I, for example in an unsubstituted or substituted alkyl group, may all have an S configuration or an R configuration independently of one another. The present invention relates to palmar isomers, left-handed and right-handed. An antipode, a form that is pure in the palm of the isomerism and a form that is substantially pure to the palm of the isomer, such as two palmomers with a molar ratio of 994 or higher, and racemic The form of the substance is in the form of a mixture of two pairs of palmomers in all ratios. The present invention is also directed to mixtures of non-powder isomers and two or more non-paraffinomers in pure form and in substantially pure form of the non-palphaliomer. The invention also includes all cis/trans isomers of the compound of formula I in pure form and in substantially pure form, such as cis/trans isomers and cis isomers having a molar ratio of 99:1 or higher. a mixture of the substance and the anti-isomer in all proportions. The cis/trans isomer can occur in the substituted ring. If it is desired to prepare individual stereoisomers, the dissociation of the mixture can be carried out according to conventional methods, for example via chromatography or crystallization, or via stereochemically identical starting compounds or stereoselective reactions in the synthesis. . Desirably, the derivatization can be carried out before the separation of the stereoisomers. The separation of the mixture of stereoisomers can be carried out at the stage of the compound of formula I or at the intermediate stage of the synthesis. The invention also includes all tautomeric forms of the compounds of formula I. Physiologically acceptable salts of the compounds of formula I, including the salts which are pharmaceutically acceptable, are generally non-toxic in nature. It may contain inorganic or organic salt components. This salt can be formed, for example, from a compound of the formula I containing an acidic group such as a sulfonic acid group (hydroxycarbonyl group, HO-C(O)-) and a non-toxic inorganic or organic test. Suitable tests are, for example, metal test compounds or soil test metal compounds such as sodium hydroxide, potassium hydroxide, sodium carbonate or sodium hydrogencarbonate, or ammonia, organic amine based compounds and quaternary ammonium hydroxide. The reaction of a compound of formula I with a base for the preparation of a salt is usually carried out in a conventional manner in a solvent or a diluent. Examples of the salts of the acidic groups are accordingly sodium, potassium, magnesium or calcium or ammonium salts which may also carry one or more organic groups on the nitrogen atom. A hydrazine compound containing a basic, ie protonatable group, such as an amine group or a basic heterocyclic group, may be present as a physiologically acceptable addition salt thereof, for example with hydrogen acid, hydrogen Salts of acid, acid, sulfuric acid, acetic acid, benzoic acid, methanesulfonic acid, p-toluenesulfonic acid, which can generally be prepared from a compound of formula I by reaction with an acid in a solvent or diluent according to conventional methods. If the compound of formula I contains both acidic and basic groups in the molecule, the present invention also includes internal salts (betaine, zwitterion) in addition to the salt forms mentioned. The invention also includes the compounds of formula I = all axes' which, because of their low physiological tolerance, are not directly suitable for use as a medicament, but are suitable as intermediates for chemical reactions or for the preparation of physiologically acceptable substances, for example via anion exchange or Cation exchange. The present invention also encompasses the compounds of formula I and all of their solvents: 匕4, L includes physiologically acceptable solvates, such as hydrates, that is, adducts of hydrazine with water, and with alcohols such as allyols. An adduct and an active metabolite of a compound of formula I and a guanidine compound 28 201245154 A prodrug, that is, a compound which does not require pharmacological activity in a test tube, but which is converted in vivo to a pharmacologically active compound of formula I, such as a compound It is converted to a compound of formula I via metabolic hydrolysis, such as a compound wherein the carboxylic acid group is present in esterified form or in the form of decylamine. In a particular embodiment of the invention, the group A is CXR1), and in another embodiment A is N. In a particular embodiment of the invention, the group D is selected from N, in another specific In one embodiment, it is selected from C(R2). In one embodiment of the invention, the group E is selected from N, and in another embodiment is selected from C(R3), in a particular embodiment of the invention In the examples, the group L is selected from N, and in another embodiment is selected from C(R4), with the proviso that one or two groups A, D, E, L are N. In another embodiment of the invention, the group A is N and the groups D, E and L are C(R2), C(R3) and C(R4). In another embodiment of the invention, the group D is N and the groups A, E and L are CXR1), C(R3) and C(R4). In another embodiment of the invention, the group E is N and the groups A, D and L are C^R1), C(R2) and C(R4). In another embodiment of the invention, the group L is N and the groups A, D and E are QR1), C(R2) and C(R3). In another embodiment of the invention, groups A and D are N and groups E and L are C(R3) and C(R4). In another embodiment of the invention, groups A and E are N and groups D and L are C(R2) and C(R4). 29 201245154 In another embodiment of the invention, the groups A and L are N and the groups D and E are C(R2) and C(R3). In another embodiment of the invention, the groups D and E are N and the groups A and L are C^R1) and C(R4). In another embodiment of the invention, the groups D and L are N and the groups A and E are C^R1) and C(R3). In another embodiment of the invention, the groups E and L are N and the groups A and D are qR1) and C(R2). With respect to the formula derived from Formula I via incorporation of A, D, E or L, in one embodiment of the invention, any one or more of Formulas 1-1 to 1-7, such as a compound of Formula 1-1 Or a compound of formula 1-2, or a compound of formula 1-3, or a compound of formula 1-4, or a compound of formula 1-5, or a compound of formula 1-6, or a compound of formula 1-7 in any of its stereoisomeric forms Or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, wherein in the compounds of formula 1-1 to 1-7, groups A, D , E, G, R1, R2, R3, R10, R3Q, R4G, R5G and R6G are as defined for the general compounds of formula I or as described in any of the specific examples above and below.

30 201245154

1-3

In a specific embodiment of the Renfeng invention, the group G is selected from the group consisting of C(〇)-R72-N(r73), and four# bases, and in another specific implementation, the money is selected from the group consisting of r7l0_c and r72_n ( R73)_c(〇), in another embodiment G is selected from r71〇_c(〇)_, and in another embodiment 〇 is selected from r'n(r73)_c(〇) _. In a specific embodiment of the invention, the group r1 is selected from the group consisting of hydrogen, halo, (CrC6), alkyl, H0, (Ci C6)-alkyl, and NC, in another embodiment. Is selected from the group consisting of hydrogen, secret, (Ci_c6)-alkyl, (frC6)-alkyl-oxime- and NC_, and in another embodiment is selected from the group consisting of hydrogen, halo, (CrC6)-alkyl and Nc_, In another embodiment, the oxime is selected from the group consisting of hydrogen, secret, (crC6) alkyl, H 〇 and (c "c6) alkyl 31 201245154 - Ο -, in another embodiment selected from hydrogen, halo (CrCJ-alkyl and (CrC6)-alkyl-oxime-, in another embodiment selected from the group consisting of hydrogen, halo and (CrC6)-alkyl, in another embodiment selected from hydrogen And an il group, in another embodiment, is selected from the group consisting of hydrogen, fluorine, and gas, and in another embodiment R1 is hydrogen. In one embodiment of the invention, (CrC6) occurs at R1. The alkyl group is (CrC4)-alkyl, in another embodiment is a (CrC2)-alkyl group, and in another embodiment is a fluorenyl group. In one embodiment of the invention, R2 is selected from (Ci-C;)-Alkyl and (C3-C7) -cycloalkyl-CsH2s-, in another embodiment selected from (C3-C7)-cycloalkyl-CsH2s- and Ar-CsH2s-, in another embodiment R2 is (CrC7)-alkane In another embodiment, R2 is (C3-C7)-cycloalkyl-CsH2s-, and in another embodiment R2 is Ar-CsH2s-, in one embodiment, s is from 0. The integers of 1 and 2 are 0 and 1 in another embodiment, 1 and 2 in another embodiment, and s is 0 in another embodiment, and in another embodiment s is 1. In a particular embodiment of the invention, R2 is Ar-CsH2s- and s is 0, that is, R2 is Ar and D is accordingly N(Ar). In a particular embodiment, divalent alkane The di-based CsH2s is a linear group. In a particular embodiment, the (CrC7)-alkyl group representing R2 is (CrC7)-alkyl, and in another embodiment is (C3-C6)-alkyl. In a particular embodiment, the (C3-C7)-cycloalkyl group present at R2 is (C3-C6)-cycloalkyl, and in another embodiment is (C5-C6)-cycloalkyl, In another embodiment, it is a cyclopropane 32 2〇1245154 group. In one In the embodiment, the μ which is present at R2 is a ruthenium and an aromatic 5-member or a 6-membered heterocyclic ring which contains - or two identical or different ring heteroatoms selected from the group consisting of gas, oxygen and sulfur and which are via The ring carbon atom fast knot, in another embodiment, is selected from the group consisting of phenyl and aromatic 6-membered heterocyclic rings containing or two I atoms as ring heteroatoms, and in another embodiment, fluorene is selected from benzene. The base, thiophenyl group, pyridyl group and pyrimidinyl group are selected from the group consisting of a phenyl group and a thiophenyl group in another embodiment, and in another embodiment, the invention is selected from the group consisting of a stupid group, a 吼η group and a base group. In another embodiment, 2 is selected from the group consisting of stupid and pyridyl, and in another embodiment Ar in the R is stupid, and all of them are of the general formula! The compound is optionally substituted as described above in any of the specific examples specified above and below. In a particular embodiment, Ar occurring at R2 is optionally substituted with one' two or three identical or different substituents, and in another specific embodiment it is optionally one or two identical or different Substituent substitution, in another embodiment it is optionally substituted with one substituent, in another embodiment it is substituted with one, two or three identical or different substituents, in another specific In the examples it is substituted with one or two identical or different substituents, and in another embodiment it is substituted with one substituent. In a specific embodiment, the substituent optionally present on Ar of R2 is selected from the group consisting of halo, (CVC6)-alkyl, (CVQ)-alkyl-hydrazine-, (CrC6)-alkyl-s(9)^ And NC_, in another embodiment selected from the group consisting of halo, (Ci_c6)-alkyl, (CrC6)-alkyl-0- and (crc6)-alkyl-S(〇)m-, in another In a particular embodiment is selected from the group consisting of a dentate group, (CrC6)-alkyl and (Crc6)-alkyl 33 201245154 -s(o)m-, in another embodiment selected from a halo group and (crc6)- The alkyl group, in another embodiment, is selected from the group consisting of halo, in another embodiment selected from the group consisting of fluorine and chlorine, and in another embodiment selected from the group consisting of fluorine, chlorine and methyl. In a particular embodiment of the invention, the (CrC6)-alkyl group present at R2 is (CrC4)-alkyl, and in another embodiment is (crc2)-alkyl, in another embodiment It is a base. An example of Ar that may occur at R2, and in one embodiment of the invention, Ar, which is present at R2, is selected from any one or two, and is phenyl, 2-f-phenyl, 3-fluoro-benzene. Base, 4-fluoro-phenyl, 2-oxo-phenyl, 3-chloro-phenyl, 4-a-phenyl, 3-> odor-phenyl, 4-> odor-phenyl, 2, 3-diqi-phenyl, 2,4-di-phenyl-, 2,5-dichloro-phenyl, 2,6-di-phenyl-, 3,4-di-phenyl, 2, 3-disorder-local, 2,4-di-r-phenyl, 2,5-difluoro-phenyl, 2,6-difluoro-phenyl, 3,4-difluoro-phenyl, 2- Gas-6-fluoro-phenyl, 3,4,5-trifluoro-phenyl, 2-methyl-phenyl (o-tolyl), 3-methyl-phenyl (m-fluorenylphenyl), 4-methyl-phenyl (p-tolyl), 2,3-dimethyl-phenyl, 2,4-dimethyl-phenyl, 2,5-dimethyl-phenyl, 2,6 - dimethyl-phenyl, 3,4-dimercapto-phenyl, 2-ethyl-phenyl, 3-ethyl-phenyl, 4-ethyl-phenyl, 3-isopropyl-benzene , 3-tert-butyl-phenyl, 4-tert-butyl-phenyl, 3-trifluorodecyl-phenyl, 4-trifluorodecyl-phenyl, 2-fluoro-5-fluorenyl -phenyl, 3-chloro-2-indolyl-phenyl, 5-gas-2-indolyl-phenyl' 5-a-2- Fluoro-3-indolyl-phenyl, 2-fluoro-3-trifluoromethyl-phenyl, 2-fluoro-5-trifluorodecyl-phenyl, 4-fluoro-3-trifluorodecyl-benzene , 5-fluoro-3-trifluorodecyl-phenyl, 3- gas-4-difluoroindolyl-phenyl, 5-chloro-2-dimethylhydrazine-phenyl, 5-gas-3- Difluorodecyl-phenyl, 2-methoxy 34 201245154 -phenyl, 3-decyloxy-phenyl '4-decyloxy-phenyl, 3-ethoxyphenyl-phenyl, 3-propoxy -Phenyl, 3-isopropoxy-phenyl, 4-tert-butoxy-phenyl, 3-difluorodecyloxy-phenyl, 4-trifluorodecyloxy-phenyl, 3-(( 2,2,2-trifluoroethoxy)-phenyl, 5-vapor-2-methoxy-phenyl, 3-ox-4-oxo-phenyl, 5-fluoro-3-isopropyl Oxy-phenyl, 2-fluoro-3-trifluoromethoxy-phenyl, 4-decyloxy-3,5-dimercapto-phenyl, 3-decyloxy-5-trifluorodecyl -phenyl, 2,3-indenylenedioxy-phenyl, 2,3-difluoroarylene dioxy-phenyl, 3,4. methylenedioxy-phenyl, 3,4·2 Fluoride, dioxy-phenyl, 3-methylsulfanyl-phenyl, 3-ethylsulfanyl-phenyl, 3-trifluorodecylsulfanyl-benzyl, 3-mer Base-phenyl, 3-ethylidene-phenyl, 3-amine-phenyl-phenyl, 2-cyano-benzene , 3-cyano-phenyl, 4-cyano-phenyl, thiophen-2-yl, thiophen-3-yl, 3-a-thiophen-2-yl, 4-chloro-thiophen-2-yl, 5 -chloro-thiophen-2-yl, 4,5-diox-thiophen-2-yl, 5-carbo-thiophen-3-yl, 2,5-dichloro-thiophen-3-yl, 4-indenyl- Thiophen-2-yl, 5-methyl-thiophen-3-yl, 4,5·didecyl-thiophene-2-yl, pyridin-2-yl, pyridin-3-yl, 0-biti-4-yl , 2-gas-. Than 3-amino, 5-gas-° ratio bit-2-yl, 6-chloro to 0--3-yl, 2-chloro-pyridin-4-yl, 2,6-di-pyridine-3 -yl, 6-decyloxy-pyridin-3-yl, 2·gas-6-decyloxy-pyridin-3-yl. In a particular embodiment of the invention, R3 is selected from the group consisting of hydrogen, halo, ((VC6)-alkyl, (qQ)-alkyl-0- and NC-, and in another embodiment is selected from Hydrogen, mercapto, (CrC6)-alkyl and NC-, in another embodiment selected from the group consisting of hydrogen, halo, (CrC6)-alkyl and (Ci-C6)-alkyl--0- In another embodiment, it is selected from the group consisting of hydrogen, halo, and (CVC6)-alkyl, and in another embodiment is selected from the group consisting of hydrogen and 35 201245154 halo, and in another embodiment is selected from hydrogen and (Q-C6)-alkyl, in another embodiment selected from the group consisting of hydrogen, fluorine and chlorine, in another embodiment R3 is hydrogen, and in another embodiment R3 is (Q-C6 - Alkyl. In one embodiment of the invention, the (CrC6)-alkyl group present at R3 is (CrC4)-alkyl, and in another embodiment is (CVQ)-alkyl, in another In one embodiment, it is a fluorenyl group. In one embodiment of the invention, R1G is selected from the group consisting of Ru-〇- and r12-n(r13)-c(o)-o-, in another embodiment Is selected from R12-N(R13)-C(0)-0- and Het2-C(0)-0-, and in another In a particular embodiment R1G is Rn-0-. In a particular embodiment, Het2, which may be present at R2, R3, R4 or R1G, is a saturated 4-member to 6-member, in another embodiment 5-member or 6-member, in another embodiment is a 5-membered monocyclic heterocyclic group optionally containing other nitrogen, oxygen and sulfur in addition to the ring nitrogen to which Het2 is attached Ring heteroatoms. In a particular embodiment, Het2 may be present at R2, R3, R4 or R10, except for the ring nitrogen to which Het2 is attached, without other ring heteroatoms. In a particular embodiment, The Het2 present at R2, R3, R4 or R1() is selected from the group consisting of lysine, hexahydro σ, and morphine. In a specific embodiment, arbitrarily present may occur in R2, R3. The number of substituents on Het2 of R4 or R1Q is one, two, three or four, in another embodiment one, two or three, and in another embodiment one or two, In another embodiment, one is, and in another embodiment the Het2 is not taken 36 201245154 generation. In a particular embodiment, the substituent optionally present on Het2 which may occur on R2, R3, R4 or R10 is selected from the group consisting of fluorine, (C丨-c4)-alkyl, HO- and (CrC4)-alkyl- In another embodiment, it is selected from (Ci-C4)-alkyl, HO- and (CrC4)-alkyl-oxime-, and in another embodiment is selected from (CVC0-alkyl) H0· and (CrC4)-alkyl-0-' is in another embodiment a (CrC4)-alkyl substituent, and in another embodiment it is a H0-substituent. In a particular embodiment of the invention, R11 is selected from the group consisting of hydrogen, R14, (CVC:7)-cycloalkyl and Het3, and in another embodiment is selected from hydrogen and R14, in another embodiment The middle is selected from the group consisting of hydrogen, R14 and (Cs-C7)-cycloalkyl, which in another embodiment is selected from the group consisting of (C3-C7)-cycloalkyl, Ar and Het3, in another embodiment From (CyC7)-cycloalkyl and Het3' in another embodiment R" is hydrogen' in another embodiment R11 is, and in another embodiment R" is Ar. In a particular embodiment, Ar representing R11 is phenyl which is optionally substituted as described in the general formula or as described in any of the specific examples specified above and below. In a particular embodiment, Ar representing R11 is optionally substituted with one, two or three identical or different substituents, and in another embodiment it is optionally substituted by one or two identical or different The base substitution, in another embodiment, is optionally substituted with one substituent. In a specific embodiment, the substituent optionally present on Ar representing Rn is selected from the group consisting of halo, (CrC4)-alkyl, (crc4)-alkyl-oxime- and NC-, in another embodiment In one embodiment is selected from the group consisting of halo, (Ci_c4)-alkyl and 37 201245154 (Q-C4)-alkyl-〇-, in another embodiment selected from halo and ((VC0-alkyl. In a particular embodiment, the (c3-c7)-cycloalkyl group representing r11 is (c3-c6)-cycloalkyl. In a particular embodiment, Het3 representing R11 is a saturated 4-member to 6-member. Monocyclic heterocyclic groups which contain one or two identical or different ring heteroatoms 'in another embodiment are a ring heteroatom selected from nitrogen, oxygen and sulfur' in another embodiment thereof Containing a ring heteroatom selected from nitrogen and oxygen' in another embodiment containing a ring heteroatom selected from the group consisting of oxygen and sulfur, and in another embodiment containing an oxygen atom as a ring heteroatom, Wherein the heterocyclic ring is bonded via a ring carbon atom and optionally passed through one, two, three or four, in another embodiment one or two, selected from fluorine , (cvc4)-alkyl and keto groups substituted with the same or different substituents, another embodiment is selected from the group consisting of fluorine and crc4). A. In one embodiment of the invention, R12 and R13 are each other. Independently selected from hydrogen and R15' is, in another embodiment, R15 and Ar' and in another embodiment R15 is the same or different. In one embodiment, R12 and R13 One is selected from the group consisting of R15 and Ar' and the other is R15. In a specific embodiment, Ar representing R12 or R13 is a phenyl group which is optionally passed through one or two, and in another embodiment is selected Substituted from the same or different substituents of a halo group and an alkyl group, and in another embodiment an unsubstituted phenyl group. In one embodiment of the invention, (Ci-Ci〇) representing R14 - Alkyl is (CrQ).alkyl, in another embodiment 38 201245154 (Crc7)-alkyl, in another embodiment (CVC4)-alkyl'. In another embodiment Is (CVC3)-alkyl, in another embodiment is (Crc2)-alkyl, in another embodiment In the case of a methyl group, in another embodiment is a (c4-c8)-alkyl group, in another embodiment a (c4-c7)-alkyl group, in another embodiment (c5) -c7)-alkyl, in another embodiment is a c6-alkyl group, wherein all of these alkyl groups are straight or branched as are suitable for alkyl groups generally in the compounds of formula I, and are as in general formula I The compound is optionally substituted with one or more of the same or different substituents as described above in any of the specific examples specified above and below. In a particular embodiment of the invention, the substitution in the alkyl group representing R14 The number of bases is one, two, two or four, in one embodiment one, two or three, in another embodiment one or two 'in another embodiment is one . In a particular embodiment, the alkyl group representing R14 is substituted, and in another embodiment it is substituted with one, two, three or four substituents, and in another embodiment Two or three substituents are substituted, in another embodiment substituted with one or two substituents, and in another embodiment substituted with a specified substituent. In a particular embodiment, the (CrC7)-cycloalkyl group which is represented by a substituent in the alkyl group represented by the formula is a (CrQ)-cycloalkyl group, and in another specific embodiment it is a cyclopropyl group. In a particular embodiment, the Ar which is represented by a substituent in the alkyl group representing R]4 is a phenyl or an aromatic 5-membered or 6-membered monocyclic heterocyclic group which contains a nitrogen, oxygen and sulfur selected from the group consisting of nitrogen, oxygen and sulfur. One or two identical 39 201245154 or different ring heteroatoms, and in another embodiment containing one nitrogen atom as a ring heteroatom and in the case of a 5-membered heterocyclic ring containing one selected from the group consisting of nitrogen, oxygen and sulfur Other ring heteroatoms, and in another embodiment, the substituents present in the alkyl group representing rM are selected from the group consisting of phenyl, decyl, isoxazolyl and thiazolyl, all of which are as The general compounds of formula I are optionally substituted with one or more of the same or different substituents as described above and in any of the specific examples specified hereinafter. In a particular embodiment, the number of random substituents of Ar present as a substituent in the alkyl group representing rM is one, two or three, and in another embodiment one or two, in another embodiment In one embodiment is one. In a particular embodiment, the optionally present substituent of Ar which is represented by a substituent in the nodal group representing R is selected from the group consisting of _ group, (C1-C4), and (C1-C4)-alkyl- 〇- and NC-, in another embodiment, are selected from the group consisting of halo, (CVC4)-alkyl and (crc4)·alkyl-oxime, and in another embodiment are selected from halo and ( Ci_C4)_S base' and in another embodiment it is a (CrC4)-alkyl group. In a particular embodiment, 'Het, which appears as a substituent in the leuco group representing Han 14, is a saturated or unsaturated 4- to 6-membered heterocyclic ring, and in another embodiment is a 5-member or a 6-membered heterocyclic ring containing a ring nitrogen atom to which H e t1 is bonded and optionally other ring heteroatoms selected from nitrogen, oxygen and sulfur, as in the general compound of formula I or above and below; Optionally substituted as described in any particular embodiment. In a specific embodiment, the substituent is present in the alkyl group representing R14 and contains no other ring heterocycle 201245154 atoms other than the ring nitrogen atom to which Het1 is attached. In a particular embodiment, Het1 which is present as a substituent in the alkyl group representing rh is saturated, and in another embodiment it is not saturated. In a particular embodiment, the number of substituents present in Het1 present in the alkyl group representing R14 as a substituent is one, two, three or four, and in another embodiment one, two or three In another embodiment, one or two 'in another embodiment, one, in one particular embodiment, is optionally present in Het1 where a substituent is present in the alkyl group representing R14. The substituent is selected from the group consisting of halo, (CrC4)-alkyl, HO-, (CrQ)-alkyl hydrazine, and a contact group, and in another embodiment is selected from the group consisting of fluorine, (CrC4)-alkyl, H〇_ and a keto group, in another embodiment, are selected from the group consisting of fluoro, (CrC4)-alkyl and keto groups, and in another embodiment are selected from (Ci-C#)·alkyl and keto groups. And in another embodiment it is a keto substituent. In a specific embodiment, the number of substituents of Het present in the alkyl group representing R14 in the substituent is not more than two, and in another specific embodiment, it is not more than one. In a particular embodiment, the substituent HeP-CXO)- appearing on the alkyl group representing rh is a 4-member to 6-membered heterocyclic ring, and in another embodiment 5-member or 6- a heterocyclic ring which is saturated or unsaturated and which contains a ring nitrogen atom to which Het1 is bonded and optionally other ring heteroatoms selected from nitrogen, oxygen and sulfur, as in the general formula or above and below Optionally substituted as described in any particular embodiment. In a particular embodiment, the Het1 of the substituent Het1-C(0)- appearing on the alkyl group representing rh, except for the ring nitrogen atom to which Heti is attached, 201245154 = does not contain any other ring heteroatoms. In a particular embodiment, the milk: Het1 of the substituent Het丨-C(O)- on the alkyl group representing R14 is 苴/or contains one double bond in %, and in another embodiment two Department,. In a specific embodiment, the number of substituents optionally present in the substituent Heti_C(0)_Het1 present on the alkyl group representing the group is one, two, three or four, in another embodiment The number is one, one or three, in one embodiment one or two, and in another embodiment one. In a specific embodiment, optionally, the substituent present in the substituent Hetl-C(0)~Het1 present on the alkyl group representing R!4 is selected from a halogen group, (CVC4)-alkyl group, HO -, (Cr(:4)-alkyl-oxime- and keto group, in another embodiment selected from the group consisting of gas, (CrC4)-alkyl, H0- and fluorenyl, in another embodiment The middle is selected from the group consisting of fluorine, (CrC4)., and the ketone group. In another specific embodiment, the oxime is selected from the group consisting of (Ci-C4)-alkyl and ketone groups. In another embodiment, the ketone group is Substituent' and in another embodiment is a (CrC4)-alkyl substituent. In a particular embodiment, the substituent Heti_c (0> Het1) present randomly on the alkyl group representing R14 The number of keto substituents is no more than two, and in another embodiment is no more than one 'and in another embodiment no keto substituents are present in this Het1. In a particular embodiment, Het3, which is represented by a substituent in the alkyl group representing R!4, is a saturated 4-membered to 6-membered monocyclic heterocyclic group which contains one or two identical or different children. The atom 'and in another embodiment contains a ring heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, and the system 42 201245154 is bonded via a ring carbon atom and is as conventional a compound of the formula or above and below Optionally substituted as specified in any particular embodiment. In one embodiment, the ring heteroatom of Het3 present in the stimulus representing RW in a substituent is selected from nitrogen and oxygen, in another specific In the two cases, it is selected from the group consisting of oxygen and sulfur, in another embodiment it is a nitrogen atom, and in another specific embodiment it is an oxygen atom. In a specific embodiment, it is optionally present in place of The number of substituents of Het3 present in the base representing Ru is one, two, three or four, and in another specific Bega case, one, one or two, in another embodiment One or two, in another embodiment, is one. In a specific embodiment, the substituent which is optionally present in the alkyl group represented by a substituent in the alkyl group representing rM is selected from the group consisting of fluorine and (CrC4). )-alkyl, in another embodiment It is selected from (CrC4)-alkyl and keto groups, in another embodiment it is a (CrC4)-alkyl substituent, and in another embodiment it is a keto substituent. In a specific embodiment Among them, P is presently present in the number of stems of the thiol substituent of Het3 which appears as a substituent in the group representing R14, not more than two, and in another and in the embodiment, not more than one. In a particular embodiment, the substituent optionally present in the alkyl group representing Ri4 is selected from the group consisting of halo, HO, R16-〇, keto, (C3_c7)-cycloalkyl, Ar, Het1, Het3 , H2N-C(0)·, (CrC4)-alkyl-NH-C(O)-, bis((CrC4)-alkyl)NC(0)- and Hef-CXO)-, in another embodiment In the examples, it is selected from the group consisting of halo, HO-, R16-〇, keto, (C3-C7)-cycloalkyl, Het1, Het3, H2N-C(0)-, (CrC4)-alkyl 43 201245154 - NH-C(O)-, di((C"C4)-alkyl)NC(O)- and Hef-CXO)-, in another embodiment selected from halo, H〇-, r16- 〇-, keto, (CrC7)-cycloalkyl, Het1, Het3, bis((CrC4)-alkyl)NC(O)- and HeP-CXO)-, in another embodiment Selected from halo, HO-, R16-0-, keto, (C3-C7)-cycloalkyl, Het1 and Het3, in another embodiment selected from halo, h〇-, r16-〇 a keto group, (C3-C7)-cycloalkyl, Ar, Het1 and Het3, in another embodiment selected from the group consisting of HO-, R16-〇-, keto, (C3-C7)-cycloalkane The group, Ar, Het1, bis((CrC4)-alkyl)NC(O)- and Het^qO)·, in another embodiment is selected from the group consisting of HO-, R16-0-, keto, (CrC7) -cycloalkyl, Ar, bis((CrC4)-alkyl)NC(O)- and Het^qo)-, in another embodiment selected from the group consisting of HO-, R16-0-, keto, (C3-C7)-cycloalkyl and Ar, in another embodiment selected from the group consisting of HO-, R16-0-, keto, (C3-C7)-cycloalkyl, bis((CrC4)-alkane Bases NC(O)- and Het^C^O)-, in another embodiment selected from the group consisting of HO-, R16-0-, keto, (C3-C7)-cycloalkyl, Het1 and Het3 In another embodiment, it is selected from the group consisting of HO-, R16-0-, keto, (CrC7)-cycloalkyl, and Het3, and in another embodiment is selected from the group consisting of HO-, keto, (C ^-C:7)-cycloalkyl and Het3' are in another embodiment From HO-, keto and (CrC7)-cycloalkyl, in another embodiment selected from the group consisting of HO-, keto and Het3', in another embodiment selected from HO- and keto groups, in In another embodiment, it is selected from the group consisting of HO-, R-0-, (CVC7)-cycloalkyl and Het3' is, in another embodiment, selected from the group consisting of HO-, (q-C7)-cycloalkyl and Het3, in another embodiment of 201245154, is selected from the group consisting of HO- and CHEN, and in another embodiment is selected from the group consisting of HO- and Het3, and in another embodiment, it is a HO-substituent, And in another embodiment it is a keto substituent. In a specific embodiment, the number of keto substituents optionally present in the alkyl group representing Ri4 is not more than two, and in another specific embodiment is not more than one. In a particular embodiment, the halogen atom present in the alkyl group representing R14 with a substituent is selected from the group consisting of fluorine and a gas atom, and in another embodiment it is a fluorine atom and is substituted by other substituents. In the latter specific embodiment, the alkyl group representing R14 is optionally substituted by a fluorine substituent, as is the alkyl group which is suitable for use in the general compound of formula I. An example of a group which may represent R14, and in a specific embodiment of the invention, R14 is selected from any one or more, and is thiol, ethyl, propyl, isopropyl, butyl, iso Butyl, cyclopropylmethyl, benzyl, 2-hydroxy-ethyl, 2-hydroxy-propyl, 2-hydroxy-butyl, 2-hydroxy-2-indole-propyl, 2-hydroxy-2 _Methyl-butyl, 2-hydroxyindoleyl-butyl, 2-hydroxyl-2,3-dimethyl-butyl, 2-hydroxy-3-tridecylbutyl, 2-ethyl-2-hydroxyl -butyl, 2-hydroxy-2,3, decyltrimethylbutyl, 2ethyl-2-hydroxyl-3-yl-butyl-butyl, 2-ethyl-2-hydroxy-3,3-dimethyl -butyl, 2-cyclopropyl. 2-hydroxy-ethyl, 2-cyclopropylhydroxy-propyl, indole cyclopropyl-2-hydroxy-butyl, 2-keto-propyl, 2-ketone Base-butyl, 3-indolyl-2-keto-butyl, 3,3-dimercapto-2-keto-butyl, cyclopropyl-2-keto-ethyl. If on behalf of the pit group substituted by R14, including the group of the above-mentioned group 45 201245154, which contains a palmitic carbon atom, the compound of formula i may exist in any stereoisomeric form for the slave atom, ie In the R configuration or s configuration 'or a mixture of stereoisomeric forms in any ratio 'for example, a mixture of two stereoisomeric forms at a molar ratio of 1:1' applies to all of the compounds of formula I Carbon atoms. In a particular embodiment of the invention, the compound of formula I has a 'pure stereochemical configuration of a palmitic carbon atom at R14, whether it is an R configuration or an S configuration' or a substantially pure stereochemical configuration, For example, the molar ratio of the two configurations is 99: 1 or higher. In a particular embodiment of the invention, the (CrC6)-alkyl group representing R15 is (CVC0-alkyl, in another embodiment (CrC2)-alkyl) in another embodiment 曱a group wherein all of these alkyl groups are optionally substituted with one or more of the same or different substituents as described in the general compound of formula I or any of the specific examples specified above and below. In a particular embodiment of the invention In the examples, the number of random substituents in the alkyl group representing R15 is one or two, and in another embodiment is one. In one embodiment, the alkyl group representing R15 is unsubstituted. In a particular embodiment, the substituent optionally present in the alkyl group representing R15 is selected from the group consisting of HO- and (CrC4)-alkyl-oxime-. In one embodiment of the invention 'represents R16(CrC6) · Topographical (Ci-C4)-alkyl, in another embodiment (C1-C3)-alkyl, in another embodiment (c2_C3)-alkyl, in another embodiment In the case of an ethyl group, in another embodiment it is a methyl group in which all of these groups are as normal The compound of formula I is optionally substituted with one or more identical or different substituents as described above and any of the specific embodiments specified in 46 201245154. In one embodiment of the invention, in the representation of R16 The number of random substituents in the alkyl group is one or two, and in another embodiment is one. In one particular embodiment, the alkyl group representing R14 is unsubstituted, in another embodiment it Substituted by one or two identical or different substituents, in another embodiment substituted by a substituent. In a particular embodiment, the substituent optionally present in the alkyl group representing R!5 is Selected from HO- and (C "C core-based" in another embodiment, which is a HO substituent, in another embodiment, its ketone-oxime-substituent, and in another In the specific embodiment of the present invention, 'R30 is selected from R31, (曰院基* Het, CuH2u·, in another embodiment) In the case, the 疋 is selected from (C3^ 环丝, r32_CuH2j WcA, and the other (four) body is implemented. Since R32. cuH2u_ and Het3_cuH2u_, in two with money _ towel r3. It is r32_Cuh2u·, and in another specific embodiment, R3° is R31. In a specific embodiment, u is an integer selected from 0'1 and 2' is selected from 0 and 1 in another embodiment, and is selected from 1 and 2 in another embodiment. In another embodiment, u is G 'and in another embodiment, in a specific embodiment, R3° is ... UH2U and u is 0, that is, in this embodiment, R30阜, & "Λ R疋 is selected from phenyl and aromatic 5-membered or 6-membered monocyclic heterocyclic groups containing -, two or three identical 201245154 or different rings selected from nitrogen, oxygen and sulfur Heteroatoms and are attached via a ring carbon atom, wherein the phenyl and heterocycle are all optionally substituted as described for the general compound of formula I or any of the specific examples specified above and below. In a particular embodiment, The divalent alkanediyl CuH2u is a linear group. In a particular embodiment, the c3-c7)-cycloalkyl group representing r3G is (c3-c6)-cycloalkyl, in another embodiment ( C5-c6)-cycloalkyl, in another embodiment is a cyclopropyl. In a particular embodiment, Het3, which is present at R3(), is a saturated 4-membered to 6-membered monocyclic heterocyclic group. In another embodiment is a saturated 5- or 6-membered ring heterocyclyl, and in another embodiment is a saturated 6-membered ring heterocyclyl containing one or two identical or different a ring heteroatom, and in another embodiment containing a ring heteroatom selected from nitrogen, oxygen, and sulfur, and attached via a ring carbon atom, and as generally a compound of formula I or specified above and below Optionally substituted as described in any particular embodiment. In one particular embodiment, the ring heteroatom in Het3 restricted to R3() is selected from nitrogen and oxygen, and in another embodiment is selected from Oxygen and sulfur, in another embodiment, are nitrogen atoms, and in another embodiment are oxygen atoms. In one embodiment, the number of substituents optionally present in Het3 of R3Q is present. Is one, two, three or four, in another embodiment one, two or three, in another embodiment one or two, in another embodiment one, and in In another embodiment, Het3 is limited to R3〇. Substituted. In a particular embodiment, the substituent optionally present in Het3 limited to R3G is selected from the group consisting of fluorine and (CrC4)-alkane 48 201245154, and in another embodiment (Cl_c Alkyl substituent. In one embodiment of the invention, the (Crc10)-alkyl group representing R31 is (CVC: 8)-homoxyl, and in another embodiment is (CrC4)-alkyl, In another embodiment, it is (Ci_c3)-alkyl, in another embodiment (crc2)-alkyl, in another specific embodiment is a fluorenyl group, in another embodiment The base, in another embodiment, is (C5_C8)-alkyl, wherein all of these alkyl groups are optionally subjected to one or more as described in the general compound of formula I or any of the specific embodiments specified above and below. Substituted by the same or different substituents. In a particular embodiment of the invention, the number of random substituents representing the base of R31 is ", two or three in another embodiment - or two, in another specific In the embodiment, in one embodiment, the alkyl group representing r31 is unsubstituted, and in another embodiment it is substituted by -, two or three = substituents. In a particular embodiment, the substitution by 1 is 'in another embodiment, by a specified substitution=two: in a specific embodiment, in the representative of the base of 1131: and from the base, ( Crc7) · ring-shaped group, ") - ray base =, in another embodiment is selected from the group i, (C3_C7) - in another embodiment is selected from a halogen group and (CVC7) _ a halogen atom in the ring group, and in the other (c3-c7)-ring system, wherein the halogen atom of the second group is selected from fluorine and chlorine atoms, and in another embodiment, it is fluorine. Atom, and in addition to being substituted by a 49 201245154 = substituent, in the latter embodiment, the alkyl group is represented as applicable to the compound of formula j The radical is optionally substituted with a fluoro substituent. In a particular embodiment, the fluorenyl group is present in the alkyl group representing R30 (CrO cycloalkyl is (c3-c6)-cycloalkyl, in another embodiment Wherein is (C5_Q)-cycloalkyl, in another embodiment cyclopropyl. Μ A In a specific embodiment of the invention, R32 is selected from phenyl and aryl 5 members $6_ A monocyclic heterocyclic group which contains - or two identical or different rings, an atom, in another embodiment - contains a ring heteroatom which is selected from the group consisting of nitrogen, oxygen and sulfur, and is via a ring carbon Atom linkage, in another embodiment, the towel is selected from the group consisting of a phenyl group and a 6-membered monocyclic heterocyclic group containing - or two nitrogen atoms as a ring hetero atom, and the phenyl group and the f ring are all as normal. The compound of formula 1 or optionally exemplified by the examples specified above and below is the same or different: In a particular embodiment, the aromatic atom representing R32 is selected from the group consisting of nitrogen and hydrazine, in another Specific implementation two = two In a specific embodiment, R32 is selected from the group consisting of benzene... is selected from the group consisting of phenyl, bowl, and other In the embodiment, it is selected from the group consisting of stupid bases and 吼' and ^ bases in another one, r is a phenyl group, and in another one concrete one: two ones are all like a general formula 巾 compound towel " As described in the Examples, it is substituted with c and the following two == or a plurality of the same or different 201245154 substituents. In a specific embodiment, the substituents are optionally present in the phenyl group representing the R32 and the aromatic heterocyclic ring. The number is one, two, three or four, in one embodiment one, two or three, in another embodiment one or two, and in another embodiment one. In a particular embodiment, the substituent optionally present in the phenyl group representing R32 and the aromatic heterocyclic ring, particularly in the phenyl group, is selected from the group consisting of halo, (CrC6)-alkyl, (Crc7)-cycloalkyl, R33 , (Ci_c6)alkyl, R33-0-, R33-(CrC4)-alkyl-oxime-,-0-CH2-0-,-0-CF2-0-, (CrC6)-alkyl-s(0 M-, h2n_s(o)2-, (crc4)·alkyl-NH_S(0)2-, di((Crc4)-alkyl)ns(o)2-, (c丨-c6)-alkyl -NH-, bis((QQ)-alkyl)N-, Het1, (CVQ)·alkyl-C(0)-NH_, Ar_C(0)-NH-, ( (VQ)-Alkyl-S(0)2-NH- and NC- 'in another embodiment is selected from the group consisting of halo, (CrC6)-alkyl, (C3-C7)-cycloalkyl, R33 ,(crC6)-Alkyl-0-, R33-〇-, R33-(CrC4)-alkyl_〇-, -〇-CH2-0- '-O-CF2-O- ' (CrC6)-alkyl -s(0)m-, H2N-S(0)2-, (Ci-CU)-alkyl-nh-s(o)2-, di((CrC4)_alkyl)NS(0)2- (CrCJ-alkyl-NH-, bis((CrC6)-alkyl)N-, Het1 and NO, in another embodiment selected from halo, (CrC6)-alkyl, (C3-C7) )-cycloalkyl, R33, (CrC6)-alkyl-0-, R33-〇-, 尺 33_((^-(:4)-alkyl·0-,-0-CH2-0-, _0- CFr0-, (CVC6)-alkyl-S(0)m-, (CrC6)-alkyl-NH-, bis((c"c6)-alkyl)N-, Het1 and NC-, in another specific In the examples, it is selected from the group consisting of halo, (CrC6)-alkyl, R33, (CrC6)-alkyl-oxime-, 51 201245154 R33_〇-,-0-CH2-0-,-0-CF2-0- , (crc6)-alkyl-S(0)m-,

Het1 and NC-, in another embodiment, are selected from the group consisting of halo, 33 (CrC6)-alkyl, R, (C1-C6)-alkyl_〇_, r33_〇_, -0-CH2- 0-, -〇-CF2-0- and NC-, in another embodiment selected from the group, (Ci-C6)-alkyl, R33, (crc6)_alkyl_〇_, r33_ 〇_ and NC-, in another embodiment, are selected from the group consisting of halo, (Cl_C6)-alkyl, (C3-C7)-cycloalkyl, R33, (crC6)-alkyl·〇_, r33_ 〇_, R33-(C "C4)-alkyl-〇-, -〇-CH2-〇-, -〇_cf2-〇_, (c^-C^)-院基-S(0)m- , bis((C1-C4)-homo)n_s(〇)2_, h2N-, di((CrC6)-alkyl)N-, Het1, (crc4)-alkyl_C(0)-NH-,

Ar-C(0)-NH- and NC- 'in another embodiment is selected from the group consisting of halo, (rcc6)-alkyl, (c3-c7)-cycloalkyl, R33, (Ci_C6)alkyl- Ο-, R33-0-, R33-(CrC4)-alkyl group_〇_, 〇_CH2_〇_, •0-CF2-0·, (CrC6)-alkyl_s(0)m_, two ( (Ci_c4)alkyl)NS(0)2-, H2N-, di((CVC6)-alkyl, Het1 and NC-, in another specific embodiment is selected from halo, (Ci_c6)-alkyl , (j-C7)-cycloalkyl, R33, (CrC6)alkyl_〇_, r33〇-, R -(CVC4)-hospital-〇-,_〇_ch2-〇_,_0_CF2_0...(Ci_C6 _ alkyl-S(0)m;, bis((crC4)-alkyl)N_s(〇)2_, bis((Ci_c6)_alkyl)N-, Het and NC-, in another embodiment Is selected from the group consisting of halo, (c"c6)-alkyl, (C3_c7), ring-based, r33, (Ci-c6)alkyl-hydrazine-, R33-o., m(CrC4)-alkyl hydrazine, (Cl c6) alkyl, one ((Cl-C4) 'alkyl) NS (〇) 2-, two ((CrC6)-alkyl) N-, Het1 and NC-, in another embodiment Selected from halo, -alkyl 52 201245154, R33, (crC6)_alkyl_〇_ and R'〇_, in the example, selected from the group consisting of a dentate group, (cvc6)-alkyl group, heart and (CVc city base) ^ Two other - In a specific embodiment, it is selected from the group consisting of halo, (CVc6), and the like, and in another embodiment, is selected from the group consisting of halo and (C1_C6)-alkyl. In the specific example, 'if the substituent is selected From ~, alkyl, R, R _ 〇 _, r33 _ (Ci C4) alkyl hydrazine, 〇 c% 〇 ·, m'retii am: (g) Lu 'do not exceed this substituent = exist in the representative The phenyl and aromatic heterocyclic rings of R are in the other and in the case of = no more than one such substituent exists, without a substituent or with any other substituent. l, he substituted in the specific embodiment The phenyl group and the aryl group = riCK: 6) which are represented by R32 are ("nuclear group, in another specific (ci-C3)-alkyl group, in another embodiment, summer) m)_alkyl, in another embodiment is methyl. In a miscellaneous 2, the two are used to take the money to represent the r32 silk and the aromatic:: (10) ring is (c, burning base) In another embodiment, (c3_c5)·cyclohexyl, in another embodiment 疋(CVQ)-cycloalkyl group, in another embodiment, the ring is in the same Specific f-finance, appearing in the stupid base ^% representing r32 It is selected from the group consisting of phenyl and aromatic 5 or 6 member heterocyclic rings and contains:: two identical or different ring heteroatoms, and in another embodiment, a ring hetero atom selected from nitrogen, oxygen and Sulfur, which is linked via a = atom, and which is carried out on another ride. The group is all like a compound of formula I or any of the specific embodiments of 53 201245154 specified above and below. Replace it arbitrarily. In a particular embodiment, the number of random substituents present in the phenyl and aromatic heterocycles representing R32 is one or rain, and in another embodiment is - and the random substituent is Selected from halo, (Crc4)-alkyl, (Ci-C4)-alkyl_〇_, (C"C4)-alkyl-S(0)m• and NC-, in another specific embodiment Is selected from the group consisting of halo, (Ci-C4)-alkyl and (CrC4)-alkyl-indole- in another embodiment selected from halo and (crc4)-alkyl, and in another In a particular embodiment, this Ar is unsubstituted. In a particular embodiment, Het1 which is represented by a substituent on the phenyl or aromatic heterocycle representing R32 is a saturated or unsaturated 4_member to 6-membered single ring. A heterocyclic group, in another embodiment, is a 5- or 6-membered heterocyclic group which contains a ring nitrogen atom through which He t1 is attached and optionally one or two other ring heteroatoms, in another In a particular embodiment is a further ring heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, as described in the general compound of formula I or any of the specific examples specified above and below. In a particular embodiment, Het1, which appears as a substituent on a stupid or aromatic heterocycle representing R32, does not contain any other _ atom except for a ring nitrogen atom to which Heti is attached. In the examples, Het1 which is represented by a substituent on a phenyl group or an aromatic heterocyclic ring representing r32 is saturated, and in another specific embodiment, it is unsaturated. In a specific embodiment, it is optionally present in The number of substituents in Hetl on the phenyl or aromatic heterocyclic ring representing R32 is one, two or four, and in another embodiment - two or three In another embodiment, there are - or two, one in another embodiment of 54 201245154, and in another embodiment the Het1 is unsubstituted. In a particular embodiment, optionally present The substituent in Het1 which is represented by a substituent on the phenyl group or the aromatic heterocyclic ring representing R32 is selected from a halogen group, a (CrC4)-alkyl group, a H0...(CrC4)-alkyl group and a ketone group, in another In one embodiment, it is selected from the group consisting of fluorine, (ci-C4).alkyl, HO- and keto, in In one embodiment, it is selected from the group consisting of fluorine, (CrC4)-alkyl and keto groups, and in another embodiment is a (Ci-C4)-alkyl group substituent. Examples of 32 R, in the present invention In a specific embodiment, R32^ is selected from any one or more of the group consisting of phenyl, 2•fluoro-phenyl, 3-fluoro-phenyl, 4-fluoro-phenyl, 2·gas-phenyl, 3 _Chloro-phenyl, 4-chloro-phenyl, 3-di: stupid, 4-di-phenyl, 2,3-di-phenyl, 2,4 2;: '-chloro-benz, 2,6-Dichloro-phenyl, 3,4-di-phenyl-, 2,3-difluoro-phenyl, 2,4-difluoro-phenyl, 2,5-difluoro-phenyl, 2,6-difluoro-phenyl, 3,4-difluoro-phenyl, 2_gas_6|phenyl, 3,4,5 tri-p-phenyl, decyl-phenyl (o-quinone) Stupid base), 3_fluorenyl-phenyl (m-phenylene), 4-2-yl-phenyl (p-nonylphenyl), 2 3 -didecyl-phenyl, 2,4-didecyl ^, 2,5-dimercapto-styl, 2,6-diindolyl, 3,4-didecyl-phenyl, 2-ethyl-phenyl, 3-ethyl-phenyl, 4-ethylphenyl, 3-isopropyl-phenyl, 3-t-butyl-phenyl, 4-tert-butyl-phenyl, 3-tris-methyl-phenyl, 4-trifluoroanthracene Base-phenyl, 2_fluoro·5_ Base_phenyl, 3_^2-indenylphenyl, 5·gas_2_methyl·phenyl, 5·gas_2_qi-3-mercapto-phenyl, 2-fluoro-3-di Fluorinyl-phenyl, 2-fluoro-5-trifluoromethyl-phenyl, 4-vapor-3-trifluoromethyl-phenyl, 5-fluoro-3-trifluoromethyl-phenyl, 3 _气冬55 201245154 Difluoromethyl-benyl, 5-non-2-difluoromethyl-phenyl, 5-gas-3-trifluoromethyl-phenyl, 2-methoxy-phenyl, 3-methoxy-phenyl, 4-ρoxy-phenyl, 3-ethoxy-phenyl, 3-propoxy-phenyl, 3-isopropoxy-phenyl, 4-third Butoxy-phenyl, 3-trifluoromethoxy-phenyl, 4-trifluoromethoxy-phenyl, 3-(2,2,2-trifluoroethoxy)phenyl, 5_ Gas_2_methoxy-phenyl, 3-vapor-4-methoxy-phenyl, 5-fluoro-3-isopropoxy-phenyl, 2-fluoro-3-trifluoromethoxy- Phenyl, 4-methoxy-3,5-dimethyl-phenyl, 3-decyloxy-5-trifluoromethyl-phenyl, 2,3-methylenedioxy-phenyl, 2 , 3-difluoroarylene dioxy-phenyl, 3,4-methylenedioxy-phenyl, 3,4-difluoromethylenedioxy-phenyl, 3-methylsulfanyl- Phenyl, 3-ethylsulfanyl-yl, 3-dimethylthiosulfanyl-phenyl, 3-methylthiol , 3_ethanesulfonyl-phenyl, 3-aminesulfonyl-phenyl, 2-cyano-phenyl, 3-cyano-phenyl, 4-cyano-phenyl, thiophene-2-yl ,. Benzene _3_yl, 3-chloro-thiophen-2-yl, 4-oxo-thienyl, 5-chloro-thiophen-2-yl, 4,5-diox thiophen-2-yl, 5-gas -thienyl, 2,5-diox-thiophene-3-yl, 4-nonyl-thiophen-2-yl, 5-nonyl-thiophene-3-yl, 4,5-dimethyl-thiophene-2- Base, pyridin-2-yl, pyridine-3-yl, pyridine-4-yl, 2-pyridyl-3-yl, 5-halo-2-yl, 6-gas·π ratio bite_3_yl, 2- Chloroquinone bite _4 base, 2'6-dichloro ratio bite _3_ group, 6_ methoxy group _π than bite _3_ group, 2_ gastooxy group than bite-3-yl group. In a particular embodiment of the invention, R33 is selected from the group consisting of phenyl and aromatic 6 membered monocyclic heterocyclic groups containing - or two identical or different bad heteroatoms' in another embodiment It is a ring heteroatom which is selected from the group consisting of nitrogen, oxygen and sulfur and is linked via a ring carbon atom, 56 in 201245154. The phenyl a and the heterocycle are all optionally substituted by one or more of the same | different substituents as described in the general formula or any of the specific examples specified above and below. In a particular embodiment, the ring heteroatom in the R33(R) aromatic heterocycle is selected from the group consisting of nitrogen and sulfur, and in another -3 = the specific embodiment is a nitrogen atom. In a specific embodiment, R is selected from the group consisting of phenyl and an aromatic 6-membered heterocyclic ring according to the definition, and in another embodiment, the thiophene is converted from phenyl and 6 贞 to contain - or two nitrogen atoms. As a ring heteroatom, in another embodiment R33 is a 6-membered monocyclic heterocyclic group according to the definition, and in another embodiment it is an aromatic 6-membered heterocyclic ring which contains one or two nitrogen atoms. As a ring heteroatom, in another embodiment R33 is selected from the group consisting of phenyl, thiophenyl and pyridyl, and in another embodiment is selected from phenyl and pyridyl, in another embodiment R33 Is a phenyl group, and in another embodiment R33 is a pyridyl group, all of which are optionally the same or different, as described in the general formula or any of the specific examples set forth above and below. Substituted for the substituent. In a particular embodiment, the number of substituents optionally present on the phenyl and aromatic heterocycles representing R33 is one, two or three, and in another embodiment one or two 'in another In one embodiment is one. In a particular embodiment, the substituents optionally present on the phenyl and aromatic heterocycles representing R33 are selected from the group consisting of halo, (Ci_c6), (C3-C7)-cycloalkyl, HO-, (Crc6)_Alkyl-0_, (Crc6)·Alkyl-S(〇)m-, H2N-S(0)2-, I((CVC4)-alkyl)NS(〇)2- and NC- In another embodiment, it is selected from the group consisting of halo, (c)-c-alkyl, 57 201245154 (C3-C7)-cycloalkyl, HO-, (crc6)-alkyl-o-, h2n-s (o) 2-, di((CrC4)-alkyl)NS(0)2- and NC-, in another embodiment selected from halo, (CrC6)-alkyl, (C3-C7) -cycloalkyl, HO-, (CrC6)-alkyl-0- and NC-, selected from halo, (CrC4)-alkyl, (CVC4)-alkyl-0-, (CrC4)-alkyl -S(0)m- and NC-, in another embodiment selected from the group consisting of halo, (CVC4)-alkyl, (CrQ)-alkyl-0- and NC-, in another embodiment The intermediate is selected from the group consisting of halo, (C1-C4)-alkyl and (C1-C4)-- in another specific embodiment is selected from halo and (crc4)-alkyl. In a specific embodiment Among them, a (CrC6)-alkyl group which is represented by a substituent on the phenyl group representing R33 and an aromatic heterocyclic ring is ( CrC4)-alkyl, in another embodiment is (CrC3)-alkyl, in another embodiment is (crc2)-alkyl, and in another embodiment is fluorenyl. In the examples, the (C3-C7)-cycloalkyl group which is represented by a substituent on the phenyl group representing R33 and the aromatic heterocyclic ring is (C3-C6)-cycloalkyl group, and in another embodiment ( C3-c5)-cycloalkyl, in another embodiment is a (c3-c4)-cycloalkyl group, in another embodiment it is a cyclopropyl group. In a particular embodiment of the invention, R40 is selected from hydrogen and (rcc2)-alkyl, in another embodiment selected from hydrogen and methyl, and in another embodiment r4Q is hydrogen. If r3G and r4Q are different and have r3G And the carbon atom of r4G is accordingly palmar. In a specific embodiment of the invention, the compound of formula I having the carbon atom is a pure stereochemical configuration, which is one of R configuration or S configuration, or Is a substantially pure stereo chemical configuration, for example, the molar ratio of the two configurations is 58 201245154 99 : 1 or more. If R30 is R32_CuH2u_ and u is 〇, which is R30 a phenyl group or an aromatic heterocyclic ring as defined above, r4 is a gas and rS0 is hydrogen. In one embodiment of the invention, the compound of formula I having the slave atom with r3〇 and R is a pure Group S State, or a substantially pure S configuration, such as S configuration to the R configuration molar ratio of 99: 1 or higher. ' If R and R40 are a divalent group (CH2)x, the two groups R and R and the carbon atom bearing the two together form a ring selected from cyclopropyl, cyclobutane, cyclopentene and A cyclohexane ring having a group _c(〇)_NH and -C(R5Q)(R6Q)-G which are described on the same ring carbon atom in the formula. In one embodiment of the invention, the number of (C1-C4)-alkyl substituents optionally present on (CH2)X is -, two, two or four, in another embodiment One or two, and in another embodiment, no alkyl substituent is present on (CH2)x. In a particular embodiment, the (CrC4)-alkyl group which is represented by a substituent on (CH2)x is a methyl group. In a specific embodiment, the integer χ is selected from 2, 4, and 5, in another embodiment is selected from 4 and 5, and in another embodiment χ is 2, and in another embodiment In X疋4. In one embodiment of the invention, r3〇 and 尺4〇 together cannot be (CH2)x, and in this particular embodiment, r3〇 and r4〇 can only have other meanings as defined. In a particular embodiment of the invention, R5 is selected from the group consisting of hydrogen, (CrC4)-alkyl and HO-, and in another embodiment is selected from the group consisting of hydrogen and (CrC4)-alkyl, in another In a particular embodiment, it is selected from the group consisting of hydrogen and 59 201245154 (CrC: 2)-alkyl, in another embodiment selected from the group consisting of hydrogen and sulfhydryl, and in another embodiment selected from hydrogen and HO-, And in another embodiment R5G is hydrogen. In a particular embodiment of the invention, r6G is selected from the group consisting of hydrogen and (C1-C4)-alkyl group, and in another embodiment is selected from the group consisting of hydrogen and (Ci-C3)-alkyl group in another specific In one embodiment is selected from the group consisting of hydrogen and (CrQO-alkyl, in another embodiment selected from hydrogen and methyl) and in another embodiment R60 is hydrogen. In one embodiment of the invention R5G and R6G are all hydrogen. If R5G and R6 are different and the carbon atom bearing R50 and R60 is accordingly palmitic, in a particular embodiment of the invention, the compound of formula I having this carbon atom is A pure stereo chemistry configuration, either one of the R configuration or the S configuration, or a substantially pure stereo chemistry configuration. For example, the molar ratio of the two configurations is 99: 1 or higher. If R50 and R60 Starting from a divalent group (CH2)y, the two groups R and R together with the carbon atom bearing the two form a cycloalkane ring selected from the group consisting of cyclopropane, cyclobutane, cyclopentane and cyclohexane. , having the group _C(r3〇)(r4〇) and 〇 described on the same ring carbon atom in the formula ^. In one embodiment of the invention, optionally present (CH2, (the number of Ci-ao-alkyl substituents is one, two, three or four, y in another embodiment - or two 'and in another embodiment) No substituent is present on (CH2)y. In a particular embodiment, the (ci A) filament present on (CH2)y as a substituent is a methyl group. In a particular embodiment, the integer x is selected from 2, 4 and 5, in another embodiment 201245154 is selected from 4 and 5, in another embodiment y is 2, and in another embodiment y is 4. In one embodiment of the invention, r50 and r6G together cannot be (CH2)y, if at the same time R30 and R4G are together (CH2)X. In one embodiment of the invention 'R71 is selected from hydrogen and (CrC6) The alkyl group, in another embodiment, is selected from the group consisting of hydrogen and (CrC4)-alkyl, and in another embodiment is selected from the group consisting of hydrogen and (Ci-C:;)-alkyl, in another In a particular embodiment is selected from the group consisting of hydrogen and (CrC2)-alkyl, in another embodiment R71 is hydrogen, and in another embodiment R71 is (CrC6)-alkyl' in another embodiment R71 (CrC4)-alkyl, in another embodiment R71 is (CVC3)-alkyl, and in another embodiment R71 is (CrC2)-alkyl, wherein all of these alkyl groups are as in general formula I The compound is optionally substituted as described above in any of the specific examples specified above. In one embodiment, the number of substituents optionally present on the alkyl group representing R71 is one or two, in In another embodiment, one is, and in another embodiment, the alkyl group representing R71 is unsubstituted. In a particular embodiment, the alkyl group optionally present on behalf of R7! is (CrC6)-alkyl-oxime-substituted, and in another embodiment is (C1-C4)-alkyl--0-substituted The base, in another embodiment, is a (C1-C3)-alkyl-O-substituent, and in another embodiment is a (Ci-C6)-alkyl-C(0)-0-substituent In another embodiment, (CrC4)-alkyl-C(0)-0-substituent' is in another embodiment (C1-C3)-alkyl-C(0)-0- Substituent. 201245154 In a specific embodiment, R72 is selected from the group consisting of hydrogen, (CrC6)-alkyl, (C3-C6)-cycloalkyl-CH2-(CH2)b-(C3_C6)-cycloalkyl and -(CH2) b-Het4, wherein the alkyl or cycloalkyl is optionally one or more of the same or different selected from halo, HO-, HOOC-, (CrCJ-cro--0- and (CrC6)-alkyl-C Substituting (0)-0-, NC-, N((CrC4)-alkyl)2 and b is 0, 1 or 2 and R73 is selected from hydrogen, (CrC6)-alkyl. In the examples, R72 and R73 together with the atomic atoms to which they are bonded form a saturated 4- to 7-membered monocyclic heterocyclic group optionally containing a ring heteroatom selected from the group consisting of nitrogen, oxygen and sulfur. It is optionally substituted with one or more substituents which are the same or different selected from the group consisting of halo, (CrC4)-alkyl, HO- and (C1-C4)-alkyl--0-. In another embodiment , R72 is selected from the group consisting of hydrogen, (Crc6)-, (C3-C6)-cycloalkyl, Het4, and -CH2-Het4, wherein the thiol or the choline is optionally one or more identical or different Selected from _ group, H〇_, H00C-, (CrQ)-alkyl-oxime- and (CrC6)-alkyl group_c(〇)_〇_, NC-, N((C"C4)-alkyl 2) Substituted and R73 is selected from the group consisting of a gas, (Ci_C6)-alkyl group. In another embodiment, R72 and R73 form a saturated 5-member to 6-membered monocyclic heterocycle together with the nitrogen atom to which they are bonded. a radical containing a ring heteroatom selected from nitrogen, oxygen, and sulfur, which is selected from the group consisting of halo, (CrC4), alkyl, and (Ci) Substituted by a substituent of -C4)-alkyl-O-. In a particular embodiment, R72 is selected from the group consisting of hydrogen, (CVC6)-fluorenyl, (C3_C6)-cycloalkyl and -CHyHet4' wherein the alkyl or ring烧美 is 62 201245154 self-halogen, HO-, • alkyl-c(o)-o-, and R73 is selected from hydrogen and optionally oxidized by one or more of the same or different HOOC-, (Ci_C6)_ Substituent (Ci-C^)-alkyl group substituted with a substituent of the group NC-, NKCi-C4)-alkyl). In another embodiment, the nitrogen atoms of the ruthenium 72 and R73 together form a saturated 5-member to 6 - a member of its own bond, ''° 娘 娘 heterocyclyl optionally containing a ring heteroatom selected from nitrogen, oxygen and sulfur, optionally free from one or more of the same or different selected from halo , (CrC4)_Siumei and (CVQ)-Alkyl-〇- Substituent substitution. 1 In a specific embodiment, R72 is selected from the group consisting of hydrogen, 2,2-diindolyl-but-3-yl, 2,2-diindolyl-prop-3-yl, pent-3- Base, propyl-2-yl, 2-mercapto-propan-2-yl, butan-1-yl, but-2-yl, 2-indolyl-butyl-3-yl, 2-indenyl-but-2- - group, -CH2CHF2, -CHCF3, CH2CN, _CH2CH2〇CH3, -CH(CH2OH)CH(CH3)2, -CH2C(CH3)2-CH2OH, CH(C2H5)CH2OCH3, CH2CH2CH2N(CH3)2, cyclopropyl , cyclobutyl, cyclopentyl, cyclohexyl and -CH2-Het4 and R73 is hydrogen. In another embodiment, R72 and R73 together with the nitrogen atom to which they are bonded form a ratio of p. It is optionally substituted by HO-. In another specific embodiment, R72 is selected from the group consisting of hydrogen, (Cl_C6)-alkyl, wherein the alkyl group is HO-substituted one or more times and r73 is nitrogen. In one embodiment of the invention, the feet 72 and R are independently selected from the group consisting of hydrogen and (rcc2)-alkyl, and in another embodiment are selected from the group consisting of hydrogen and sulfhydryl. In one embodiment, one of 'r7 and R is hydrogen and the other is selected from hydrogen and (Ci-C4)-alkyl, and in another embodiment 63 201245154 is selected from hydrogen and (c"c The 2)-alkyl group, in another embodiment, is selected from the group consisting of hydrogen and methyl, and in another embodiment, both r72 and R73 are hydrogen. In one embodiment of the invention 'Het4, Other Het4 independent of each other, are saturated or unsaturated 4_ to 8-membered monocyclic heterocyclic groups containing one to four other ring heteroatoms selected from nitrogen, oxygen and sulfur, which are followed by one or more Substituting the same or different substituents selected from the group consisting of dentate, (C1_C4)-alkyl, H0-, (Cl-c4)-alkyl-hydrazine-, keto, and NC. In another embodiment, Het4, Other Het4 are independent of each other and are saturated or unsaturated 5- to 6-membered monocyclic heterocyclic groups which contain one to four other heteroatoms selected from the group consisting of gases, oxygen and sulfur, which are optionally subjected to one or more The same or different substituents selected from the group consisting of halo, (CrC4)-alkyl, HO-, (CVC4)-alkyl, keto and NC_. In another embodiment, 'Het4, with other H Et4, independently of each other, is an unsaturated 5-member to 6-membered monocyclic heterocyclic group containing from one to four other ring heteroatoms selected from nitrogen, oxygen and sulfur, optionally at one or more of the same or different Substituent substitutions selected from the group consisting of I#, (CVC4)-alkyl, HO-, (CrC4)-alkyl-oxime- and NC-. In another embodiment, Het4, independent of other Het4' is It is selected from the group consisting of 1,2-anthracenyl, tetrasaltyl, pyridyl, guanidino, pyridyl, pyrimidinyl, optionally substituted by methyl. In a specific embodiment of the invention, in formula j Any occurrence of Ar' in the compound, independently of each other, is selected from the group consisting of phenyl and aromatic 5-membered or 6-membered monocyclic heterocyclic groups containing one or two ring heteroatoms of the same or different 64 201245154, In another embodiment, a ring heteroatom is selected which is selected from the group consisting of nitrogen, oxygen and sulfur, and which are attached via a ring carbon atom, and in another embodiment Ar is selected from the group consisting of phenyl and aromatic 6- a heterocyclic ring containing one or two nitrogen atoms as a ring hetero atom, and in another embodiment Ar is selected from the group consisting of a phenyl group, a thiophenyl group, and a pyridyl group. In another specific embodiment, it is selected from the group consisting of phenyl and thiophenyl, in another embodiment selected from phenyl and pyridyl, and in another embodiment Ar is phenyl and in another In a particular embodiment, Ar is pyridinyl, wherein the strepyl and all heterocycles are optionally substituted as described in the general compounds of formula I or any of the specific examples set forth above and below. In a particular embodiment The number of substituents optionally present on Ar, independently of each other, is one, two, three or four, and in another embodiment one is two or three, in another embodiment In one embodiment, one or two, in another embodiment, is one, and in another embodiment, Ar is unsubstituted. In a specific embodiment, if selected from -CH=CH-CH=CH-, -〇_CH2-CH2-0-, ·Ν(((^-<:3)-alkyl)-CH=CH The substituent of -, -〇-CH2-〇- and -〇-CF2-0- is present on Ar of the fluorene group, and there are no more than two such substituents, and in another specific embodiment, there is no more than One such substituent is, without any other substituent or with any other substituent. In one embodiment, the substituent optionally present in Αι·, independently of each other, is selected from a halo group. , (Cl_C6)-alkyl, H〇_(CrC6)^, Het4, -(CH2)X-phenyl, (CrC6)_alkyl 〇, (c3_C7) ring 65 201245154 alkyl _(ch2) Xo-, -cf3, -co-(crc6)-alkyl, -NR12R13, Het2, -CO-NR12R13, CO-Het2, (CrC6)-alkyl-S(0)m-, H2N-S(0) 2- and NC-. In another embodiment, it is selected from the group consisting of halo, (Ci-C6)-alkyl, (CVC6)-alkyl-hydrazine-, (CrQ)-alkyl-s(0)m - and NC-, in another embodiment selected from the group consisting of halo, (Cl-C6)-alkyl, (Ci-C6)-alkyl--0- and NC-, in another embodiment Selected from halo, ( Crc6)-alkyl and (CrQ)-alkyl-oxime-, in another embodiment selected from halo, (crc4)-alkyl and (CrC4)-alkyl-0-, in another specific In the examples, it is selected from the group consisting of halo and (CrCd-alkyl. The subject of the invention is that all of the compounds of formula I wherein any one or more, structural elements such as groups, substituents and amounts are according to any given specific embodiment or The definition of an element or the definition of one or more of the specified meanings is referred to herein as an example of an element in which one or more specified specific embodiments and/or definitions and/or all combinations of the specific meanings of the elements Is the subject of the present invention, and as regards all of the compounds of the formula I, all of their stereoisomeric forms and stereoisomeric forms in any proportion of the mixture 'and its physiologically acceptable salts, and any of its physiologically acceptable Accepted solvates are also the subject of the present invention. As an example of a compound of the invention, any structural element is defined in accordance with the specific embodiment specified by the invention or the definition of this element, a compound of formula I may be mentioned wherein G is Selected from r7L〇-C(0)- and R72-N(R73)-C(0)-; 〇30 β P32 ^ τ R疋K -CuH2u-, where u is an integer selected from 〇 and 1; 66 201245154 R32是a phenyl group and an aromatic 6 member monocyclic heterocyclic group having one or two nitrogen atoms as a hetero atom (CVC6)alkyl, (C3_C7)cycloalkyl, R33, HO-, (Cl-C6)-alkyl 〇, R'〇_, R33_(CrC4)·alkyl-ο-, -o-ch2 -o-, -0_cf2-0_, (c broad Q)alkyl_s(0)m... bis((Crc4)-alkyl)Ns(o)2-, H2N-, di((Crc6)_alkyl )Ν·,

Het1, (CrC4)_alkyl_C(0)_NH_, Ar_c(〇) NH and nc• substituents are substituted; R疋 is selected from phenyl and aromatic 6-S monocyclic heterocyclic groups containing - or two A nitrogen atom as a % hetero atom's all of which are optionally substituted by one or more of the same or different ones selected from the group consisting of halo, (Ci_C6)-filament, (C3_C7)-cycloalkyl group HO-, (crc6) - burnt base - 〇 _, (Ci_c6) yard base, H2N-s (〇) 2 ·, : ((CrC4)_ burnt base) ns (〇) 2_ and [take the substitution; r4 () is hydrogen. A = another example of a compound of the invention, which is defined with respect to any structural morpheme according to the specific embodiment specified by the invention or the definition of this element, and the compound of formula I which may be mentioned is G in the form of R71-〇-C (0)_ ; 八 R is R32-CuH2u-, wherein u is 〇; 32 R 疋 疋 k from the present group, wherein the phenyl group is optionally one or more of the same or different oximes selected from the group 1, (C -C6)_Alkyl, (C3-C7)-cycloalkyl, R33, HO-, (Crc6)-院基_〇_, R33_〇, R33_(Ci_C4)•烧基_〇, -0_CH2- 〇-, _〇_CF2_〇_, (Ci C6) alkyl _s(〇)m, two ((Ci 〇67 201245154 alkyl)NS(0)2-, H2N-, two ((CVQ)- Alkyl) N-, Het1, (CrC4)-alkyl-C(0)-NH-, Ar-C(0)-NH- and NC-; R33 is selected from phenyl, wherein the phenyl is optionally One or more of the same or different selected from the group consisting of halo, (CrC6)-alkyl, (C3-C7)-cycloalkyl, HO-, (CVC6)-alkyl-0-, (c--c6)- Substituted by a substituent of an alkyl group, H2N-S(0)2-, bis((CrCO-alkyl)NS(0)2- and NC-; R4() is hydrogen. As another example of the compound of the present invention, Any structural element is referred to according to the invention a specific embodiment or a definition of this element, a compound of formula I may be mentioned, t R5C) is hydrogen; r6() is hydrogen. As another example of a compound of the invention, it is according to the invention with respect to any structural element A specific embodiment or a definition of this element is defined, and a compound of formula I may be mentioned wherein Formula I is selected from the group consisting of Formula 1-1 to 1-7.

68 201245154 1-3

As another example of the compound of the present invention, it is defined with respect to any structural element according to the specific embodiment specified by the present invention or the definition of this element.

Wherein R2 is Ar-CsH2s-, wherein s is an integer selected from 0; R3 is selected from the group consisting of hydrogen, 4, alkyl and (CrC6)-alkyl; preferably HO- and (CrC6)-alkyl; R4 Is hydrogen; 69 201245154 R10 θ Total hurricane. As another example of the compound of the present invention, it is defined with respect to any structural element according to the specific embodiment specified by the present invention or the definition of this element, the compound of the formula 1-1.

Wherein R1 is hydrogen; R is selected from the group consisting of hydrogen, i group, (CrQ)-alkyl, (crc6)-alkyl-s(0)m-, phenyl CsH2s-(0)r, Het4-(0)t -, -NR丨V3, Het2, Rii-O-, R12-N(R13)-C(0)-0- and Het2-C(0)-〇- and NC-, where s is selected from 〇, 1 An integer from 2 and 3 and wherein t is an integer selected from 〇 and 1; R 4 is hydrogen; R 〇 is selected from the group consisting of hydrogen, dentate, (CrQ)-alkyl, (Ci-Q)-alkyl-0. , (C1-C6)-hospital-S(〇)m-, HO-, -NR12R13, Het2, phenyl_CsH2s-(〇)t- ' where s is an integer selected from 〇, 1, 2 and 3 And wherein t is an integer selected from 0 and 1. A subject of the invention is also a compound of formula I which is selected from any of the specific compounds of formula I disclosed herein, or one of the compounds of any particular formula 1 disclosed herein, whether disclosed as a free form compound and/or as a specific or physiological An acceptable salt, or any solvate thereof, which is physiologically acceptable in 201245154, wherein the compound of formula i is in any of its stereoisomeric forms or mixtures of stereoisomeric forms in any ratio is the subject of the present invention. For example, the subject of the invention is a compound of formula I which is selected from the group consisting of (S)-3-[(5-hydrazinyl-6-phenyl-[rho]but-2-yl)-amino]-3- o-Phenylphenyl-propionic acid (S)-3-(2,4-diaza-phenyl)-3-[(5-methyllacyl-6-phenyl-0-pyridin-2-yl) )-amino]-propionic acid (S)-3-[(6-chloro-5-methoxyl σ sec-2-yl)-amino]-3-o-indole phenyl-propionic acid ( S)-3-{[3-(4,6-dioxaoxy-pyrimidin-2-yloxy)-«bipyridine-2-carbonyl]-amino}-3-o-tolyl-propionic acid ( S)-3-[(6->Smell-5-曱乳--0 σσ定-2-$Carbonyl)-Amino]-3-o-tolyl-propionic acid (S)-3- {[4-(Pyridine-2-ylsulfanyl)-. (β)-3-[(6-phenyl-° ratio α定-2 -_carbyl)-amino] -3 -o-decyl-propionic acid (S)-3-[(5-phenylpyridin-2-carbonyl)-amino]-3-o-tolyl-propionic acid (S)-3- {[5-(2- gas-phenyl)-0 ratio °-3-weiki]-amino]·_3-o-indole-propionic acid (S)-3-{[5-(2 ,3-dioxa-phenyl)-acridin-3-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[5-(2,3-didecyl) -phenyl)-acridin-3-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)-3-o-indolephenyl-3-[(6-meta-methyl) -0 ratio ° -2 -yl)-amino]_ 71 201245154 Propionic acid (S)-3-{[6-(2-chloro-phenyl)^pyridinyl-2-carbonyl]-aminob 3_o-indole phenyl-propionic acid (S)-3-{[6-(2-fluoro-phenyl) "specific bite 2_yl] aminyl 3 o-tolyl-propionic acid (S -3{[6-(2,3-Difluoro-phenyl)pyridinyl-2-carbonyl]-aminodibu 3_o-tolyl-propionic acid (S)-3- {[6-( 2,5-monofluoro-phenyl)-«»Bistyl-2-yl]-amino}-3-o-tolyl-propionic acid (S)-3-{[6-(4-fluoro- 2-indenyl-phenyl)-indole- 2-yl]-amino}-3-o-phenylene-propionic acid (S)-3-{[6-(2,3-didecyl) -phenyl)_σpyridinyl-2-carbonyl]-amino}_3_o-tolyl-propionic acid (S)-3-{[6-(5-fluoro-2-methyl-phenyl)_η比〇定_2-藏基]-aminopyr 3_o-tolyl-propionic acid (S)- 3_{[6-(2.Methoxy-4-methyltrienyl)-phenyl)-acridine-2-carbonyl]-amino}-3-o-indole-propionic acid (3)-3 -{[6-(4-Gas_2_曱-oxy-phenyl)-0-pyridyl-2_yi-yl]-amino}_3· o-tolyl-propionic acid Λ (S)-3_{[6_ (2_Fluorine_5_decyloxy-styl) 0-pyridyl-2_ylamino]aminopyr 3·o-indolephenyl-propionic acid (S)-3-{[6_(2-fluoro- Phenyl)_5_methoxy-0pyridinyl-2-carboxyl]•Aminodi 3_o-indolephenyl-propionic acid (S)-3-{[6-(2-fluoro-5-fluorenyl)- Phenyl)-acridine_2.carbonyl]•Aminobutano 72 201245154 -Phenylphenyl-propionic acid (S)-3-[(5-methoxy-6-phenyl)pyridin-2-carbonyl )-Amino]-3-p-tolyl-propionic acid (S)-3-[(5-decyloxy-6-o-tolylpyridinyl-2-carbonyl)-amino]•孓对_ Phenylphenyl-propionic acid (S)-3-{[5-methoxy-6-(2-trifluoromethyl-phenylpyridinylcarbonyl)-amino}-3-p-indole phenyl·c Acid (S)-3-{[6-(3-Fluoro-phenyl)-5-methoxyl-acridine-2-carbonyl]-aminodi 3_p-tolyl-propionic acid (S)-3 -{[5-decyloxy-6-(2-decyloxy-phenyl)·»»Biidine_2-carbonyl]-amino}-3-p-tolyl-propionic acid (S)-3-{[6-(2-chloro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino)·3_p-tolyl-propionic acid (S)-3- {[6-(2-1-phenyl)-5-decyloxybiidine_2-carbonyl]-aminodi 3_p-tolyl-propionic acid (S)-3-{[6-(2, 4-difluoro-phenyl)-5-methoxypyridinyl-2-ylcarbonyl]-amino}-3-p-nonylphenyl-propionic acid (S)-3-{[6-(2,3 -diqi·stupyl)-5-decyloxypyridinyl-2-carbonyl]-amino}_3-p-phenylene-propionic acid (S)-3-{[6-(2-gas-5 -trifluoro-1methyl-phenyl)-5-methoxyl_B than 唆_2_罗炭基]-amino}-3·p-·p-phenyl-propionic acid (S)-3-{ [6-(3-Fluoro-2-indolyl-phenyl)-5-decyloxy--bito-2-amino]]amino}-3-(2-fluoro-phenyl)-propionic acid ( S)-3-{[6-(2-Ga-5-trifluoromethyl-phenyl)-5-decyloxy·π ratio.定_2_罗炭73 201245154 基]-Amino}-3-(2-gas-phenyl)-propionic acid (S)-3-{[6-(2,3-difluoro-phenyl)- 5-decyloxypyridin-2-carbonyl]-amino}-3-p-indolephenyl-propionic acid (S)-3-{[6-(2,5-difluoro-phenyl)-5 -曱oxy-n-pyridin-2-carbonyl]-amino}-3-p-indolephenyl-propionic acid (S)-3-{[6-(2,5-dichloro-phenyl)- 5-decyloxypyridin-2-carbonyl]-amino}-3-p-nonylphenyl-propionic acid (S)-3-{[6-(3,5-diindolyl-isoxazole- 4-yl)-5-decyloxy-pyridine-2-carbonyl]-amino}-3-p-tolyl-propionic acid (S)-3-{[6-(4-fluoro-2-indenyl) -phenyl)-5-decyloxy-acridin-2-carbonyl]-amino}-3-p-indolephenyl-propionic acid (S)-3-{[6-(2,3-dioxin) Phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3·p-nonylphenyl-propionic acid (S)-3-[(3,2-propoxy-[ 2,3'] in combination with 11 fluorenyl-6-alkyl)amino]_3. p-nonylphenyl-propionic acid (8)-3·{[6-(5-fluoro-2·indolyl)phenyl ··5-decyloxypyridinyl-2-yl]-amino}-3·p-tolyl-propionic acid (8)_3-{[6-(4-a-2-oxooxyphenyl)- 5-decyloxy-ton bite·2_rocarbyl]-amino}-3-p-tolyl-propionic acid (S)-3-{[6-(5-fluoromethoxy-phenyl) _5_曱oxy_D than pyridine·2_carbonyl]-amino}-3-pair- Phenyl-propionic acid (S)-3-{[6-(2-fluoro-5-methyl-phenyl)-5-methoxy-π-pyridyl-2-carbonylamino-4-py-p-phenylene _propionic acid canine soil (3)·3·{[6-(3-gas·2_mercapto-phenyl)_5_methoxy_D is a pyridyl group]_ 201245154 Amino} - 3 -pair-曱Phenyl-propionic acid (S)-3-{[6-(3-fluoro-2-indolyl-phenyl)-5-decyloxy-0-pyridin-2-yl]-amino}_3 -p-Phenylphenyl-propionic acid (S)-3-{[6-(5-Gas-2-fluoro-phenyl)-5-decyloxy-acridin-2-carbonyl]-amino}- 3-(p-tolyl-propionic acid (S)-3-(2-fluoro-phenyl)-3-[(5-decyloxy-6-phenyl-acridin-2-carbonyl)-amino] -propionic acid (S)-3-{[6-(2,4-dichloro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-(2-fluoro-benzene ()-propionic acid (S)-3-(2-a-phenyl)-3-[(5-methoxy-6-o-indolephenyl-α-pyridin-2-ylcarbonyl)-amino] - (S)-3-(2-Fluoro-phenyl)-3-{[5-decyloxy-6-(2-trifluoromethyl-phenyl)-propionate. ratio.定-2->Carbonyl]-amino hydrazine-propionic acid (S)-3-(2-fluoro-phenyl)-3-{[5-methoxy-6-(2-methoxy- Phenyl)-indoleyl]-amino}-propionic acid (S)-3-{[6-(2-chloro-phenyl)-5-decyloxyl sigma-2-yl]-amine (3-)-(2-rho-phenyl)-propionic acid (S)-3-(2-fluoro-phenyl)-3-{[6-(2-fluoro-phenyl)-5-methyl milk Base-α ratio biting-2-carbonyl]-amino}-propionic acid (S)-3-{[6-(2,4-disorder-phenyl)-5-decyloxy-° ratio- 2-(yl)-amino}-3-(2-a-phenyl)-propionic acid (S)-3-{[6-(2,3-di-phenyl)-5-decyloxy -α ratio α-den-2-weilyl]-amino]·_3-(2-a-phenyl)-propionic acid (S)-3 - {[6-(2,3-di-phenyl-phenyl) -5-decyloxy-° ratio biting-2-weiyl]-amine 75 201245154 】}-3-(2-fluoro-phenyl)-propionic acid (S)-3-{[6-(2,5 -difluoro-phenyl)-5-methoxyl^pyridin-2-carbonyl]-amino}-3-(2-fluorophenyl)-propionic acid (S)-3-{[6-( 4-fluoro-2-methyl-phenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid (S)-3-{ [6-(3,5-Dimercapto-isoxazol-4-yl)-5.methoxy-acridin-2-carbonyl]-amino}-3-(2-fluoro-phenyl)- (S)-3-{[6-(2,3-Dimercapto-phenyl)-5-methoxy-acridin-2-carbonyl]-amino}-3-(2-fluoro-propionate) Phenyl)-propionic acid (S)-3_[(3 , 2'-dimethoxy-[2,3']biacridinyl-6-carbonyl)-amino]-3-(2-phenyl)-propionic acid (S)-3-{[6 -(5-fluoro-2-indolyl-phenyl)-5-methoxy-acridin-2-carbonyl]-amino}-3-(2-fluoro-phenyl)propionic acid (S)_3 ][6-(4-Fluoro-2-methoxy-phenyl)-5-methoxy-η-pyridin-2-carbonyl]-amino}_3-(2-fluoro-phenyl)-propionic acid (δ)·3-{[6-(5-fluoro_2_decyloxy-phenyl)_5_decyloxy-0-pyridyl-2-carbonyl]-amino}-3-(2-fluorobenzene ())-propionic acid (S)-3-{[6-(2-fluoro-5-indolyl-phenyl)-5.nonyloxy_D-pyridyl·2·carbonyl-hydroxyl-}-3-( 2-fluoro-phenyl)·propionic acid (S)-3_{[6_(3·Ga 2_indolyl_phenyl)_5_methoxybipyridine-2carbonyl]_月女基}-3· (2-Fluoro-phenyl)-propionic acid (S)_34[6-(5-Gas-2-fluoro-phenyl)-5-methoxyl-bite-2-carbonyl]-Amineyl 3-(2 -Fluoro-phenyl)-propionic acid (3)3 {[6-(3-Gas_2_ disordered phenyl)_5_methoxy-π ratio bite_2_yl]]amine 76 201245154 】}-3-( 2-mur-phenyl)-propionic acid (S)-3-(2-muro-phenyl)-3-{[5-methyl,oxy-6-(2-indolyl-?-fusan-3- Base)_. 〇定定-2 - 叛基]-amino}-propionic acid (S)-3-{[6-(2-chloro-3-methyl-phenyl)-5-decyloxy-acridine-2 -carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid (S)-3-(2-a-phenyl)-3-[(5-decyloxy-6-phenyl) (bi)-2-carbonyl)-amino]-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,4-dichloro-phenyl)-5- Oxy-吼σ定-2-绿基]-amino}-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(4-fluoro-phenyl)-5 -decyloxypyridin-2-carbonyl]-aminopropionic acid (S)-3-{[5-decyloxy-6-(3-trifluorodecyl-phenyl)-pyridin-2- Carbonyl]-amino}·_3-o-indolephenyl-propionic acid (S)-3-{[6-(2,4-dichloro-phenyl)-5-methoxy-0-pyridin- 2-(yl)-amino}-3-o-indolephenyl-propionic acid (S)-3-{[6-(4-fluoro-phenyl)-5-indole-based-to-bit-2 -Prison base]-Amino}-3_ O-Phenylphenyl-propionic acid (S)-3-{[6-(4-Gas-phenyl)-5-decyloxy-0 σ 定 -2- Alkyl]-amino}-3_o-nonylphenyl-propionic acid (S)-3-[(5-decyloxy-6-p-indolylphenyl-acridin-2-carbonyl)-amino] -3-o-indole phenyl-propionic acid (8)-3-{[6-(3-a-phenyl)-5-indole-based-buty-2-yl]-amino}- 3-o-indolephenyl-propionic acid (S)-3-{[5-decyloxy-6-(2-decyloxy-phenyl)-. Bisidine-2-carbonyl]-amine 77 201245154 】}-3-o-tolyl-propionic acid (S)-3-[(5·decyloxy-6-m-tolyl-η-pyridyl·2_ Carbonyl)-amino]_3_ o-tolyl-propionic acid (S)-3-{[6-(2-chloro-phenyl)-5-methoxy-acridine_2·carbonyl]-aminopur 3_ o-tolyl-propionic acid (S)-3-{[6-(3,4-difluoro-phenyl)-5-methoxy-indenyl-2-amino]-amino}-3 -o-indole phenyl-propionic acid (S)-3_{[6-(2,5-difluoro-phenyl)-5.nonyloxyl ratio _2_yl]-amino}-3- o-Phenylphenyl-propionic acid (S)-3-{[6-(2,5-di-phenyl)-5-methoxylpyridinyl-2-yl]-amino}-3- -tolyl-propionic acid (S)-3-{[6-(3,5-dimethyl-iso-inden-4-yl)5-nonyloxy-oxime-2-_2carbonyl]-amino group }-3·o-p-phenyl-propionic acid (S)-3-{[6-(2,3-indolyl-phenyl)-5-decyloxy-π ratio π定_2_|| Base]_Amino}-3-o-tolyl-propionic acid (S)-3-{[6-(2,4-methyl-phenyl)-5-methoxy-oxime 2_Lhenyl]·Amino}-3-o-tolyl-propionic acid (S)-3-{[6-(4•fluoro-2-indolyl-phenyl)-5-decyloxy- ο than bite _2•carbonyl]-amino}-3-o-tolyl-propionic acid (S)-3-{[6-(2-chloro-5-methyl-phenyl)-5-methoxy Base-π ratio β fixed _2_carbyl]_amino group }-3-o-tolyl-propionic acid (S)-3-(2-a-phenyl)_3_[(6-methoxy-5-o-methyl-phenyl)-biter -amino]-propionic acid (S)-3-(2-chloro-phenyl)-3-{[5-methoxy-6-(2-decyloxy-phenyl) ratio 78 201245154 α定- 2-(yl)-aminopropionic acid (S)-3-(2-chloro-phenyl)-3-[(5-methoxy-6-m-m-phenyl-acridin-2-carbonyl) -amino]-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2-chloro-phenyl)-5-decyloxy-acridin-2-carbonyl] -Amino hydrazine-propionic acid (8)-3-(2-muro-phenyl)-3-{[6-(2-a-phenyl)-5-decyloxy-. Carbonyl]-aminopropionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,4-difluoro-phenyl)-5-methoxy-oxime 11 -2-yl]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,3-dichloro-phenyl)-5-methoxy (1)-(Carboxyl)-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,3-difluoro-phenyl) -5-decyloxyl ratio sigma-t-yl]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,5-difluoro -phenyl)-5-methoxyl ratio α-butyryl]-amino}-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(4- Fluor-2-mercapto-phenyl)-5-methoxy-0 butyl-2-yl]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3- {[6-(2,3-二曱) -phenyl)-5-decyloxy-0-bite-2-domain]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-[(3,2' -dimethoxy-[2,3']bipyridyl-6-carbonyl)-amino]-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(5 -fluoro-2-indolyl-phenyl)-5-decyloxy-α ratio α-di-2-chloro]-aminopropionic acid (S)-3-(2-chloro-phenyl)-3- {[6-(4-Fluoro-2-methoxy-phenyl)-5-anthracene 79 201245154 base-π ratio °-2-alkyl]-amino}•propionic acid (S)-3- {[6-(4-Ga-2-methoxy-phenyl)-5-methoxy^pyridin-2-carbonyl]-amino}-3-(2-a-phenyl)-propionic acid (S)-3-(2·Ga-phenyl)-3-{[6-(5-fluoro-2-indolyl-phenyl)-5-methoxy-β-pyridin-2-carbonyl] -amino}-propionic acid (S)-3-(2-carb-yl)-3-{[6-(2-a-5-dimethyl-phenyl)-5-methoxy- D is more than bite-2-rebase]-aminopropionic acid (S)-3_{[5-methoxy-6-(2·trifluoromethyl-phenyl)-° ratio bite ]-Amino}-3-o-indolephenyl-propionic acid (S)-3-{[6-(2,4-difluoro-phenyl)-5-methoxypyridin-2-carbonyl] -amino}-3-o-tolyl-propionic acid (S)-3-{[6-(4-fluoro-2-methyl-phenyl)-5.nonyloxybipyridine_2-carbonyl] -amino}-3-o-indolephenyl-propionic acid (S)-3-[(3,2'-dioxaoxy-[2,3']-bipyridyl-pyridyl- 6-carbonyl)-amino]_3_o-indolephenyl-propionic acid (8)-3-[(3'-fluoro-3-indolyl-[2,4']bipyridyl-6-carbonyl)-amine (3-)-p-phenyl-propionic acid (S)-3-{[5-decyloxy-6-(2-methyl-furan-3-yl)-acridin-2-carbonyl]- Amino}·3-o-indolephenyl-propionic acid (S)-3-{[6-(4-cyano-2-fluoro-phenyl)-5-decyloxy^ ratio. Benz-2-carbonyl]-amino}-3-o-, fluorenyl-propionic acid (s)-3-(2-a-phenyl)_3_{[6-(2-fluoro-5-decyloxy) -phenyl)·5_decyloxy-pyridine-2-carbonyl]-amino}-propionic acid (s)-3-(2-a-phenyl)_3-{[6-(2-fluoro-5 - mercapto-phenyl)-5-decyloxy_ 201245154. ratio. (2-)-aminopropionic acid (S)-3-{[6-(3-chloro-2-indolyl-phenyl)-5-decyloxy-acridin-2-carbonyl]-amine -3-}-3-(2-Ga-phenyl)-propionic acid (S)-3-(2-Ga-phenyl)_3_{[6_(3_Fluoro-2-indolyl-phenyl)_5_A Oxy-p-pyridinylcarbonyl]-amino}-propionic acid (8)-indole [6·(5-a-2-1.phenyl)-5-decyloxy-acridin-2-carbonyl]-amino group )-3-(2-chloro-phenyl)-propionic acid (8)! (2·gas-phenyl)_3_[(3|_fluoro_3_methoxy_[2,4,]-linked 0-pyridyl-6-carbonyl)-amino]-propionic acid (S)-3 -(2-Fluoro-phenyl)-3-[(5-decyloxy-6-吼α well-2-yl-indole ratio -2-mercapto)-amino]-propionic acid (S) -3- {[6-(3-Gas-2-fluoro-phenyl)-5-methoxy-η ratio n-but-2-yl]-amino}-3-(2- gas-phenyl )-propionic acid (S)-3-(2-a-phenyl)-3-{[5-decyloxy-6-(2-methyl-.f-*»--3-yl)-pyridine- 2-carbonyl]-aminopropionic acid (S)-3-{[6-(2-gas-3-fluoro-phenyl)-5-methoxy-η ratio _2-carbonyl]-amino group }-3-(2-Chloro-phenyl)-propionic acid (S)-3-{[6-(2-a-3-indolyl-phenyl)-5-methoxypyridin-2-ylcarbonyl ]-Amino}-3-(2-a-phenyl)-propionic acid 3-biben-4-yl-3-[(6-Gas-0 ratio sigma-2-yl)-amino] -propionic acid (S)_3-[(6-gas ratio. _2_yl)-amino]_3·o-nonylphenyl-propionic acid (S)-3_[(3,5-diamino) -6-chloro-indole _2·carbonyl)-amino]_3_o-tolyl-propionic acid 3-biphenyl-4-yl-3-[(3,5-diamino-6-gas -intD well-2-alkyl)-amine 81 201245154 】]-propionic acid (S)-3-{[6-(2- gas-phenyl)-° ratio β--2-16 carbon-]-amine (S)-3-(3-fluoro-phenyl)-3-{[6-(2-fluoro-phenyl)-°pyridin-2-carbonyl]- (-) propionic acid (S)-3-(2-fluoro-phenyl)-3-{[6-(2-fluoro-phenylpyridin-2-carbonyl)-amino}-propionic acid (S) 3-(4-fluoro-phenyl)-3-{[6-(2-fluoro-phenyl)-«pyridin-2-carbonyl]amino}-propionic acid 3-(2-chloro-phenyl -3-[(6-decyloxy-indole-2-carbonyl)-amino]-propionic acid (S)-3-[(6-methoxy-biphenyl-3-yl-yl)- Amino]-3-o-tolyl-propionic acid (S)-3-{[6-(2-chloro-phenyl)-~pyridin-2-carbonyl]-amino}-3-inter-indole Phenyl-propionic acid (S)-3-{[6-(2- gas-phenyl)-0 ratio. D-the-mute carbon-]-amino}·_3-(4-indole-benzene ()-propionic acid (S)-3-{[6-(2- gas-phenyl)-° ratio 0--2-yl]-amino]^-3-(2- gas-phenyl) -propionic acid (S)-3-{[6-(2- gas-phenyl)-amino}-3-(4-carb-phenyl)-propionic acid (S)-3-(3 - Chloro-phenyl)-3-{[6-(2-chaotic-local)-α ratio β-1,4-chloro]-amino}-propionic acid (S)-3-(4-gas-benzene Base)-3-{[6-(2-f-phenyl)-. Bisidine-2-carbonyl]-amino}-propionic acid 82 201245154 (S)-3-(4-chloro-phenyl)-3-{[6-(2-chloro-phenyl)-«pyridinium- 2-carbonyl]-amino}-propionic acid (S)-3-(3-nitro-phenyl)-3 -{[6-(2-chloro-phenyl)-°-but-2-yl] -amino}-propionic acid 3-(2- gas-phenyl)-3-{[6-(2-chloro-phenyl)-amino}-propionic acid (S)-3-{[6 -(2-fluoro-phenyl)-.0-0-2-reyl]-amino}-3-(3-trifluorodecyl-phenyl)-propionic acid (S)-3-{[6 -(2-nitro-phenyl)-ntba-but-2-weilyl]-amino}-3-(2,4-dichloro-benyl)-propionic acid (S)-3-{[6-( 2-Gas-Phenyl)-O-β ° 毅 毅 毅]-Amino}-3-(4-trimethylsulfonyl-phenyl)-propionic acid (S)-3-{[6-( 2-Chloro-phenyl)-° ratio °-2-Williyl]-amino}-3-(3-trimethylsulfonyl-phenyl)-propionic acid (8)-3-{[6-&gt Odor-5-(3,3-dimercapto-2-@同-butoxy)-pyridine-2-carbyl]-amino}-3-o-indolephenyl-propionic acid For example, also a subject of the invention is a compound of formula I which is selected from the group consisting of (S)-3-[(5-decyloxy-6-phenyl-acridin-2-carbonyl)-amino]-3-yl -Phenylphenyl-propionic acid (S)-3-{[6-(2,3-dimethyl-phenyl(-.bis-bito-ro-carbyl)-amino}-3-o-toluene -propionic acid (S)-3-{[6-(2- gas-phenyl)-π ratio 0--2-yl]- -3-}-3-o-indole phenyl-propionic acid (S)-3-{[6-(2-gas-phenyl)-Di:be-but-2-yl]-amino}-3-ortho -Toluene 83 201245154-propionic acid (S)-3-{[6-(5-fluoro-2-methyl-phenyl)-acridin-2-carbonyl]-amino}-3-o-indenylbenzene (-)-propionic acid (S)-3-o-indolephenyl-3-[(6-m-indolyl-n-bipyridyl-2-carbonyl)-amino]-propionic acid (S)-3-( {6-[3-(l-hydroxy-1-indolyl-ethyl)-phenyl]pyridin-2-carbonyl}-amino)_3_o-indolephenyl-propionic acid (S)-3- (2,4-Dichloro-phenyl)-3-[(5-decyloxy-6-phenyl-.pyridyl-2-carboyl)-amino]-propionic acid (S)-3 -[(2,6-didecyloxy-B-den-10-ding-4-yl)-amino]-3-o-tolyl-propionic acid (S)-3-[(5-phenyl-indole) (pyridine-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid (S)-3-{[3-(4,6-di-anthracene-sigmine-2-oxy) -πΛο定-2-毅基]_Amino}-3-o-indolephenyl-propionic acid (S)-3-{[4-(. Σσ定-2-ylthioalkyl)-π ratio β--2-yl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[5-(2, 3-Dichloro-phenyl)-. (β)-3-{[5-(2,3-dimercapto-phenyl)-α ratio 0--3 -monoyl]-amino}-3-o-indole phenyl-propionic acid (S)-3-{[5-(2-chloro-phenyl)-n-pyridyl-3-carbonyl]-amino} -3-o-indolyl-propionic acid (8)-3-{[6-(2,3-di-phenyl)-0- 17-but-2-yl]-amino}-3- o-Phenylphenyl-propionic acid 84 201245154 (8)-3-{[6-(2-Motor-5-decyloxy-phenyl)-° ratio <7-but-2-yl]-amino group }-3-o-tolyl-propionic acid (S)-3 - {[6-(2-fluoro-5-fluorenyl-phenyl)-D than sigma-2-yl]-amino}- 3-o-indolyl-propionic acid (S)-3-{[6-(2-decyloxy-4-trifluoromethyl-phenyl)-acridin-2-carbonyl]-amino}- 3-o-indolephenyl-propionic acid (S)-3-({5-decyloxy-6-[3-(5-fluorenyl-[1,3,4]oxadiazol-2-yl) -phenyl]-acridin-2-carbonyl}-amino)-3-o-indolephenyl-propionic acid (S)-3-(2-a-phenyl)-3-[(5-oxime) -6-n-2-yl-0-buty-2-carboyl)-amino]-propionic acid (S)-3-(2-chloro-phenyl)-3-[(5-oxime) (6-pyridin-2-yl-acridin-2-carbonyl)-amino]-propionic acid (S)-3-(2-chloro-phenyl)-3-[(6-decyloxy- 5-naphthalen-2-yl-acridin-3-carbonyl)-amino]-propionic acid (S)-3-(2-a-phenyl)-3-{[5-decyloxy-6-( 2-曱基- σ 喃 -3--3-yl)-pyridine-2-carbonyl]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,3-diindole) -phenyl)-5-methoxy-π ratio α-di-2-chloro]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6- (2-Chloro-phenyl)-5-methoxypyridin-2-carbonyl]-aminopropionic acid (S)-3-(2-fluoro-phenyl)-3-{[5-oxime Base-6-(1,3,5-tridecyl-1Η-mouth ratio 〇-4-yl)-π ratio σ定-2- > carbon-based]-aminopropionic acid (S)-3 -(2-murine-phenyl)-3-{[5-曱-milyl-6-(1-indolyl-ΙΗ-口引〇朵-5. 基)-^比咬-2-yl]- Amino}-propionic acid 85 201245154 (S)-3-[(5-methoxy-6-m-tolyl-acridin-2-carbonyl)-amino]-3-o-tolyl-propionic acid (S)-3-{[6-(2-Gas-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-o-tolyl-propionic acid (S)-3 -{[6-(3,5-diamidino-isoxazolyl)-5-methoxy-pyridine-2-carbonyl]-amino}-3-o-tolyl-propionic acid (8)- 3-{[6-(4-Gas-phenyl)-5-methoxy-0 to 17-but-2-yl]-amino}-3-o-indolephenyl-propionic acid (S)- 3-{[6-(4-chloro-phenyl)-5-methyllacyl-indenylpyridin-2-yl]-amino}-3_p-indolephenyl-propionic acid (S)-3 -{[6-(5-Ethyl-thiophen-2-yl)-5-decyloxy-acridin-2-carbonyl]- (_)3-(2-chloro-phenyl)-propionic acid (S)-3-{[6-(2-fluoro-phenyl)-5-methoxybipyridine-2-carbonyl]-amino} 3-o-indolyl-propionic acid or a compound thereof, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, wherein the compound of formula I is in any of its stereoisomers Mixtures of the form or stereoisomeric form in any ratio are the subject of the present invention, unless a specific stereoisomeric form is specified with respect to any carbon atom in each compound. Another subject of the invention is a process for the preparation of a compound of formula I, which is outlined below and which is obtained by this process. For example, the preparation of a compound of formula I can be carried out by reacting a compound of formula II with a compound of formula III to form a guanamine linkage. A variety of synthetic methods for forming indoleamine linkages are disclosed, for example, in C. A. G. N. Montalbetti et al., 86 201245154

Tetrahedron 61 (2005), 10827-10852. The compounds normally disclosed in this patent are synthesized according to the general scheme:

The formation of a guanamine bond between the carboxylic acid and the beta-amino acid can be carried out via the use of a coupling agent well known to those skilled in the art and disclosed, for example, in Tetrahedron (2005), 61(46), 10827-10852. Carboxylic acid can be used in place of the carboxylic acid, and a beta-amino acid ester, especially a methyl or ethyl ester, can be substituted for the free beta-amino acid. The beta-amino acids used in this work are either commercially available or prepared by methods such as those disclosed in JACS 1935, 1279 or by Rhodinow in Chem. Abstr. 1953, 1051. The Rhodionow schema is summarized as follows:

The p-isomerically pure beta-amino acid can be obtained commercially or from a racemic material by methods disclosed in Bioscience, Biotechnology and Biochemistry, 2006, 1941. A general procedure for the use of a heterocyclic carboxylic acid for the coupling process is described in 87 201245154. The carboxylic acid used was obtained from a commercial supply.

Method A A 0.25 mM molar carboxylic acid was weighed into a reaction vessel, and 〇245 mmol of N-ethyl fluorene in 1 ml of DMF was added followed by 1.25 mM T 在 in 0.5 ml of DMF. TU. The mixture was allowed to react at room temperature for 30 minutes. 0.275 mmol of m-amino acid suspended in 毫升 $ ml of dmf was added, and the vessel was sealed with a screw cap and shaken overnight at room temperature. 0.2 ml of TFA was added and the solution was filtered through a syringe filter and directly subjected to preparative HPLC. Product Yield: 5% and 80% The following shows another general procedure involving the synthesis of amino acid derivatives containing functional groups suitable for subsequent Suzuki reactions.

The synthesis procedure is illustrated in more detail as follows: Step 1: Esterification of β-amino acid 88 201245154 Synthesis of (S)-3-amino-3-(2-fluoro-phenyl)-propionic acid ethyl ester 5.0 g (27 (3 mmol) of (S)-3-amino-3-(2-fluorophenyl)-propionic acid was suspended in 27 ml of decyl-THF and 16 ml of ethanol and heated to 80 °C. 2.45 mL (4.02; 33.8 mmol; 1.24 eq.) of S0C12 was added and the obtained mixture was stirred at 80 ° C for 2.5 hr. The mixture was allowed to reach room temperature and stirred overnight. The solvent was evaporated in vacuo to give 9.2 g of crude material, which was washed several times with diisopropyl ether to afford 6.34 g of pure material (yield: 94%). According to this method, the following derivatives were prepared: (S)-3-Amino-3-(2-chloro-phenyl)-propionic acid ethyl ester (S)-3-amino-3-o-indolephenyl- Ethyl propionate (S)-3-Amino-3-p-tolyl-propionic acid ethyl ester Step 2: Coupling from the product of Step 1 to a heterocyclic carboxylic acid substituted with a chlorine or bromine atom: Synthesis (8) -3-[(6->Smelly-5-decyloxy-0 to α-di-2-carboyl)-amino]-3-(2-chloro-phenyl)-propionic acid ethyl ester will be 4.87 Grams (21 mmol) of 6-bromo-5-methoxy-pyridine-2-carboxylic acid and 4.17 g (25.2 mmol, 1,2 equivalents) of CDI suspended in 54 mL of Me-THF and heated to 50 °C. After stirring at this temperature for 3.5 hours, the mixture was cooled to 〇 ° C in an ice bath and 3.39 ml (24.2 mM, 1.15 eq.) of triethylamine was added. Then 6.1 g (23.1 mmol, 1,1 equivalent) of (S)-3-amino-3-(2-a-phenyl)-propionic acid ethyl ester was added over 20 minutes and the resulting mixture was allowed to reach the chamber. Stir and stir overnight. 50 ml of water was added, the layers were separated and the organic layer was washed several times with 50 mL of a s. The organic layer was evaporated in vacuo to give 8.43 g. Yield: 89%. According to this method, the following derivatives were prepared: (S)-3-[(6->odor-5-oxime-α ratio α-carboxyl-amino)-amino]-3-o-tolyl _ Ethyl propionate (S)-3-[(6-bromo-5-decyloxypyridin-2-carbonyl)-amino]-3-p-indolephenyl-propionic acid ethyl ester (S)- 3-[(6->Smell-5-曱乳-D vs. 0-2-pyryl)-amino]-3-(2-a-phenyl)-propionic acid ethyl ester (S)- 3-[(5-Ga-6-oxime-0-specific -3-yl)-amino]-3-o-tolyl-ethyl propionate (S)-3-[(5- Gas-6-曱乳--0 to ^-3-,Carbo)-amino]-3-(2-(phenyl-phenyl)-propionate ethyl ester (S)-3-[(5-> Smelly-β-β-α--3-yl)-amino]-3-o-indole-propionic acid B-(S)-3-[(2-chloro-6-decyloxy-α ratio) --4-Petyl)-Amino]-3-o-tolyl·ethyl propionate (S)-3-[(2-gas-° than bite-4-carbyl)-amino] -3-o-indolyl-propionic acid ethyl acetate (S)-3-[(6-chloro-π ratio α-butyryl)-amino]-3-o-indole phenyl-propionic acid Step 3: Hydrolysis of the product from step 2: Synthesis of (S)-3-[(5-gas-6-decyloxy-α ratio. 1,4--3-yl)-amino]-3-(2 - gas _ phenyl)-propionic acid will be 8.03 g (20,21 mmol) of (3)-3-[(5-gas-6-decyloxy-acridinylcarbonyl)-amino]-3- (2 - The gas-phenyl)-propionic acid ethyl acetate was dissolved in a 15.2 liter 201245154 (30.32 mmol, 1,5 equivalent) 2N NaOH solution and stirred at 50 ° C for 9 hours. The resulting mixture was stirred at room temperature overnight. Add 105 ml of water and 30 ml of isopropanol and adjust the pH to pH = 3.0 with 2N HCl. The precipitate was dried under vacuum to give 3.74 g of product (yield: 50%). According to this method, the following derivatives were prepared: (S)-3-[(6->odor-5-oxime-0-pyridin-2-#carbonyl)-amino]-3-(2- Gas-phenyl)-propionic acid (S)-3-[(6->odor-5-oxime-° ratio biting-2-weiry)-amino]-3-o-tolyl·c Acid (S)-3-[(6->Smelly-5-anthracene-oxime ratio sec-2-yl)-amino]-3-p-tolyl-propionic acid (S)-3 -[(6- > odor-5-曱乳-° ratio ̄-2-weiyl)-amino]-3-(2-fluoro-phenyl)-propionic acid (S)-3-[ (5-azino-6-decyloxy-3-yl)-amino]-3-o-indolephenyl-propionic acid carbon-)-amino]-3-o-indolephenyl-propionic acid (S)-3-[(2-chloro-6-decyloxy-0 to 0-1,4-deyl)-amino]-3-o-tolyl-propionic acid (S)-3-[( 2-gas-0-pyridyl-4-phospho)-amino]-3-o-indolephenyl-propionic acid (8)-3-[(6-rat-0 to 17-but-2-yl) Method of using -amino]-3-o-indole phenyl-propionic acid for Suzuki coupling:

General procedure B 91 201245154 Synthesis of (S)-3-(2-fluoro-phenyl)-3-[(5-decyloxy-6-phenylpyridin-2-carbonyl)-amino]-propionic acid ( Example 263) 50 mg (0.12 mmol) of (S)-3-[(6-bromo-5-decyloxypyridin-2-carbonyl)-amino]-3-(2-fluoro-phenyl) - Propionic acid was dissolved in 3 ml of DMF, 120 mg (0.16 mmol, 1,35 equivalents) of phenylboronic acid, 10 mg of bis(triphenylphosphine) palladium (II) as catalyst and 1 ml were added. 1N Na2C03 solution and the resulting mixture was heated to 100 ° C for 6 hours. The mixture was filtered through a pad of celite and subjected to preparative </ RTI> <RTIgt; </RTI> <RTIgt;

General Procedure C Synthesis of (S)-3-(2-chloro-phenyl)-3-[(6-decyloxy-5-phenylpyridin-3-carbonyl)-amino]-propionic acid (Example 353 ) in 50 mg (0.13 mmol) of (S)-3-[(5-Ga-6-methoxy-acridin-3-carbonyl)-amino]-3-(2-chloro-phenyl) - Propionic acid was added to a solution of 3 ml of DMF: 25 mg (0.21 mmol, 1.5 equivalents) of phenylboronic acid, 60 mg of Na2C03 (0.56 mmol, 4.2 equivalents) and 10 mg (0.13 equivalents) of di-micro- Chlorobis[2-[(didecylamino)indenyl]phenyl-C,N]DIPAL is used as a catalyst. After adding 1 ml of water, the resulting mixture was heated to 100 ° C for 6 hours, and the resulting mixture was filtered through a layer of celite and the obtained solution was subjected to preparative HPLC chromatography to give 16 mg of product (yield: 29%) . The groups A, D, E, L, G, R1g, R3Q, R4Q, R5G and R6G in the compounds of the formulae II and III are according to the definitions in the compounds of the formula I and the other functional groups may be present in protected form or The form of the precursor group is subsequently converted to the final group. The group J in the hydrazine compound may be 92 201245154 H〇-(hydroxyl), that is, the compound of the formula II may be a carboxylic acid, or another group in which the compound of the formula III may be substituted with an NH group in the substitution reaction, For example, an oxy group such as an optionally substituted phenoxy group or an alkoxy group such as (C1-C4)-alkyl-oxime-such as (crc3)-alkyl such as a decyloxy group or an ethoxy group, or a halogen group such as a gas. Or bromine, and the hydrazine compound may be a reactive ester of each carboxylic acid such as an aryl ester or an alkyl ester such as an oxime ester or an ethyl ester, or a fluorenyl halide such as a mercapto group or a mercapto bromine. The formula II and the hydrazine compound can also be used in the form of a salt, for example an acid addition salt of a compound of the formula III, for example a hydrohalide salt such as a hydrogen acid salt and/or an alkali metal salt, for example a sodium salt of a compound of the formula II wherein J is HO- , a compound of formula I is obtained. Similarly, in all other reactions for the preparation of the compounds of formula I, the preparation of the starting compounds, the compounds employed and/or the resulting products may also be in the form of a salt. If a compound of formula II is used wherein J is HO-, the carboxylic acid group HO-C(O)- is typically activated or converted to a reactive carboxylic acid derivative via a conventional indoleamine coupling agent which can be prepared or isolated on the spot. For example, a compound of formula II wherein 110 is - can be converted to a mercapto halide, such as a compound of formula II wherein J is gas or bromine, treated with sulphur sulphate, phosphorus pentoxide or phosphorus sulphate Alternatively, treatment with an alkyl chloroantimonate such as ethyl benzoate or isobutyl chloroformate affords a mixed anhydride. In an advantageous process for conversion to a ruthenium based gas, in a catalytic amount from about 〇 ° C to about 6 (at a temperature of TC, such as at room temperature, in an inert solvent such as a hydrocarbon or gasified hydrocarbon or hydrazine) The guanamine is treated with chloroquinone in the presence of a guanamine such as N,N-diindenylamine. The conventional guanamine coupling agent which can be used is propyl oxime anhydride, N,N'-carbonyldiazole such as hydrazine. , hydrazine, -carbonyldiimidazole (CDI), carbonized two 93 201245154 quinone imines such as 1,3-diisopropylcarbodiimide (DIC), 1,3-dicyclohexylcarbodiimide ( DCC) or 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), carbodiimide-based binding additive such as 1-hydroxy-benzotriazole (HOBT) or 1-hydroxy-7-azabenzotriazole (HOAT), urea matrix coupling agent such as 〇-(7-azabenzotriazol-1-yl)-N,N,N',N '-Tetramethylurea hexafluorophosphate (HATU), 〇-(benzotriazol-1-yl)-N,N,N',N,-tetramethylurea hexafluorophosphate (HBTU) or hydrazine -(cyano(ethoxycarbonyl)methyleneamino)-N,N,N,,N,-tetramethylurea tetrafluoroborate (TOTU) and squara Coupling agents such as (benzotriazole-!·oxy) ginseng (dimethylamino)sodium hexafluorophosphate (B〇p), (benzotriazolyl) tris-pyrrolidine hexafluorophosphate Salt (PyBOP) or bromine III. Birolidine hexafluorophosphate (PyBroP). The reaction conditions for the preparation of the compounds of formula I from the compounds of formula II and III depend on the particular situation, such as the meaning or use of the group j. Coupling agents, and those skilled in the art will understand from the general knowledge of the art. For example, if a compound of formula II wherein J is an alkyl group such as a decyloxy group or an ethoxy group, is reacted with a compound of formula m, usually the reaction is In an inert solvent such as a hydrocarbon or a gasified hydrocarbon such as benzene, toluene, xylene, chlorobenzene, chloroform or a gas, such as tetrahydrobite (thf), 2-methyltetrahydrofuran, dioxane, Dibutyl ether, diisopropyl ether or dimethoxy, in a hospital (DME), or solvent mixture, at elevated temperatures, for example, from about 4 〇C to a 'force 140 C temperature', especially at about 5 〇. To about 2 〇., for example, at about the boiling point of the solvent. If the formula j is a compound in which J is recorded, for example, money, is III compound reaction, usually 94 201245154 This reaction is also in an inert solvent such as the above hydrocarbon or chlorinated hydrocarbon or ether, ester such as ethyl acetate or butyl acetate, nitrile such as acetonitrile or water, or a mixture of solvents including water and water The mixture of mutually soluble or immiscible organic solvents is carried out at a temperature of from about -10 ° C to about 100 ° C, particularly from about 0 ° C to about 80 ° C, for example at room temperature. A compound wherein J is a reaction of a halo group with a compound of formula III, which is advantageous in bases such as tertiary amines such as triethylamine, N-ethyl-diisopropylamine (EDIA), N-mercapto oxime, N- Ethyl oxime or acridine or an inorganic base such as a metal hydroxide, an acid salt or a hydrogencarbonate such as sodium hydroxide, potassium hydroxide, sodium carbonate or sodium hydrogencarbonate is used. If a compound of formula II wherein J is HO-, is reacted with a compound of formula III and the carboxylic acid group is activated via a guanamine coupling agent such as carbodiimide or TOTU, the reaction is usually under anhydrous conditions in an inert solvent such as an ether such as THF. , dioxane or DME, decylamine such as N,N-dimercaptodecylamine (DMF) or -mercaptopyrrolidine (NMP), at temperatures from about -10 ° C to about 40 ° C, especially It is carried out at a temperature of from about 0 ° C to about 30 ° C, such as room temperature, in the presence of, for example, a tertiary amine such as triethylamine, EDIA, N-mercapto porphyrin or N-ethylfosfo. If a compound of formula III is reacted with a hydrazine compound in the form of an addition salt, a sufficient amount of a base is usually added to liberate the free compound of formula III. As noted above, during the formation of a guanamine bond between the compounds of Formula II and III, the functional groups in the compounds of Formulas II and III can exist in protected form or as precursor forms. Depending on the particular circumstances, it may be necessary or desirable to temporarily mask any functional groups via a protecting group to prevent unwanted or subsequent reactions and subsequent removal, or to have functional groups present as precursors and subsequently converted to The final group desired. This point applies correspondingly to all reactions in the synthesis of the compounds of formula I, including the synthesis of intermediates, starting compounds and building blocks, and various synthetic strategies are commonly used in the art. The details of the protecting group and its addition and removal are disclosed in, for example, PGM Wuts and T. W. Greene, Greene's Protective Groups in Organic Synthesis, 4. ed. (2007), John Wiley &amp; S ο ns ° An example of a group is a benzyl protecting group which can be present in the form of a benzyl ether of a hydroxy group and a benzyl ester of a carboxylic acid wherein the benzyl group can be removed by catalytic hydrogenation in the presence of a palladium catalyst, a t-butyl protecting group. It can occur in the form of a third butyl ester of a carboxylic acid in which the third butyl group can be removed by treatment with trifluoroacetic acid, which can be used to protect the hydroxyl group and the amine in the form of esters and guanamines. And it can be dissociated via acidic or basic hydrolysis, and the alkoxycarbonyl protecting group can occur in the form of a third butoxycarbonyl derivative of the amine group and it can be cleaved by treatment with trifluoroacetic acid. An unwanted reaction of a carboxylic acid group, such as a carboxylic acid group present in a compound of formula III, if G is a carboxylic acid group in the desired compound of formula I, it may also be used in alkyl esters such as methyl ester or The form of the ethyl ester is prevented by reaction with a hydrazine compound and it can be dissociated via hydrolysis, for example via an alkali metal hydroxide such as sodium hydroxide or lithium hydroxide. As an example of a precursor group, cyano (NC-, Νβ-) can be exemplified by conversion to a carboxylic acid group, a carboxylate group and a formamidine group under hydrolysis conditions or converted to an amine sulfhydryl group via reduction and The nitro group can be converted to an amine group via reduction, for example via catalytic hydrogenation or via reduction with, for example, disulfide 96 201245154 sodium sulfinate. Another example of a precursor group is a ketone group which may be initially present in the synthesis of a compound having a hydroxyl group, and which may be, for example, reduced with a complex hydride such as sodium hydride, or with an organometallic compound such as a Grignard compound. If any protecting group or precursor group is present in the compound of formula II and hydrazine and the direct product of the reaction is not the desired final compound, the protecting group can usually be removed or converted to the desired compound in situ. The starting compounds for the synthesis of the compounds of formula I can generally be prepared according to the methods disclosed in the literature or by analogous methods or from commercial sources. The β-amino acids and derivatives of formula III are commercially available or can be synthesized from readily available starting compounds by well-known standard methods or analogously to such methods. For example, the preparation of a ruthenium-based ruthenium acid and an alkyl ester thereof wherein R50 and R60 are hydrogen, a carbonyl compound of the formula r30_C(0)_r4〇, particularly an aldehyde of the formula R32-C(0)-H, Reaction with monoethyl malonate and ammonia in the presence of a base such as an alkali metal hydroxide such as potassium hydroxide in a solvent such as an alcohol such as ethanol', for example, disclosed in M. Rodionov et al., Izv. Akad. Nauk SSSR, Ser. Khim. (1952), 696-702 (Chem. Abstr. 47 (1953), abstr. no. 61888), or a gas addition to the condensation product of a carbonyl compound with malonic acid or diethyl malonate The bond and in the case of a condensation product with malonic acid diethyl acetonate, the reaction product is treated with an acid such as hydrochloric acid, for example, as disclosed in V. Scudi, J. Am.

Chem. Soc. 57 (1935), 1279; 4M.K.Tseetal., Chem.

Eur. J. 12 (2006), 1855-1874, and when the product is obtained, according to the requirements of 97 201245154 and the above summary, the ester group is hydrolyzed to a carboxylic acid, respectively, or the carboxylic acid group is esterified. The compound of the formula III which is pure to palm isomerism can be obtained, for example, from the crystallization of a racemic compound via a salt with an optically active acid such as tartaric acid, via stereoselective enzymes or microbial degradation, for example as disclosed in Μ. K. The literature from Tse et al. is available at j. Man〇et ai., Bioscience, Biotechnology and Biochemistry 70 (2006), 1941-1946. In another strategy for the synthesis of this compound, in particular compounds wherein R4G, R5Q and R60 are hydrogen and R30 is R32, each 3-substituted acrylic acid, which may be obtained from the corresponding aldehyde, is for example Conversion to mercapto chloride and conversion of mercapto chloride to an ester with an alcohol, such as conversion to a third butanol with a third butanol, and subsequent introduction of an amine group via reaction with a lithium salt of an optically active amine, such as (R)- a lithium salt of (+)-N-benzyl-N-(l-phenylethyl)amine, and is obtained as a 3-substituted 3-(N-benzyl-N-(l-phenylethyl) In the case of aminyl tert-butyl propionate, the benzyl and phenylethyl groups are dissociated via catalytic hydrogenation (see SG Davies et al., Tetrahedron: Asymmetry 2 (1991), 183-186); SG Davies et al. J. Chem. Soc. Perkin Trans. 1 (1994), 1129-1139) ° When a structural group of a compound of the formula I is introduced, the synthesis can also be carried out in a different order than the above. For example, in the case of a compound of formula I wherein R1G is a group other than a hydroxyl group, it is not a compound of formula II which contains R1G and which reacts with a compound of formula III, and a compound of formula lie which specifically contains a hydroxyl group instead of r1g, which may be combined with Compound III is reacted, and the resulting compound of formula la is subsequently changed to a hydroxy group by reaction with a compound of formula VIII to give a compound of formula I wherein R1G is not hydroxy', i.e., 98 201245154 lb compound. At the end, as in the preparation of the compound of formula I as described above, any protecting group in the compound of formula lb can still remove protection and/or convert the precursor group to the final group.

The groups A, D, E, L, G, R30, R40, R50 and R60 in the compounds of the formula la, lb and lie are according to the definitions in the compounds of the formula I and the other functional groups may be present in protected form or In the form of a precursor group it is subsequently converted to the final group. The group J in the compound of the formula lie is based on the definition in the compound of the formula II. The group R1Ga in the compound of the formula lb is based on the definitions in the compounds of the formulas lib and VIII. The above description of the reaction of the compounds of the formulae II and III and the reaction of the compounds of the formulae Ila and VIII is carried out correspondingly to the reaction of the compounds of the formulae lie and III and the reaction of the compounds of the formulae la and VIII, respectively. In order to obtain other compounds of the formula I, the intermediates of the compounds of the formula I or the compounds of the formula I or the functional groups of the starting compounds can be subjected to different conversions from 99 201245154. For example, a mesogenic group, including a hydroxyl group representing R10 in the compound of formula i, can be esterified according to the above, for example under the conditions of the Mitsunobu reaction described above, in an inert solvent such as a guanamine such as DMF or NMP or a ketone such as acetone or butyl-2. Alkylation of a ketone or an individual with a halogen compound such as bromine or iodine in the presence of, for example, an alkali metal carbonate such as potassium carbonate or cesium carbonate. The hydroxy group can be esterified to give a tickic acid ester or sulfonate ' or converted to a _ compound by treatment with a _ifying agent. It is also possible to introduce a functional atom via a suitable reagent to replace the hydrogen atom in the starting compound, for example via elemental bromine, thiopurine or chloromethyl-4-fluoro-1,4-diazonium bicyclic. [2.2.2] Octane bis(tetrafluoroborate) which introduces bromine, chlorine and fluorine substituents, respectively, for example at the 4-position in the compound of formula lib. In the substitution reaction, which may also be a transition metal catalyzed reaction, the halogen atom can be substituted with a plurality of groups. The nitro group can be reduced to an amine group, for example via catalytic hydrogenation. The amine group can be altered under standard conditions of alkylation, for example via reaction with a dentate compound or by reductive amination via a carbonyl compound, or thiolation or sulfonylation, for example via an activated carboxylic acid or carboxylic acid Derivatives such as sulfhydryl or anhydride or sulfonium are reacted. The carboxylic acid ester group can be hydrolyzed under acidic or basic conditions to give a carboxylic acid. The acid group can be activated or converted into a reactive derivative according to the above and reacted with an alcohol or an amine or ammonia to give an ester or a guanamine. The primary guanamine can be dehydrogenated to give the nitrile. The sulfur atom in the alkyl-S- or heterocyclic ring can be oxidized with a peroxide such as hydrogen peroxide or a peracid to give a sulfoxide group s(〇) or a sulfone group s(〇)2. The carboxylic acid group, the carboxylate group and the ketone group can be reduced to an alcohol, for example, by using a composite hydrogen compound such as an aluminum hydride clock, lithium borohydride or sodium borohydride, or reacting with an organic gold 100 201245154 compound or a Grignard compound to obtain an alcohol. The primary and secondary hydroxyl groups can also be oxidized to a keto group. All reactions in the preparation of the compounds of formula I are known per se and can be carried out in a well known manner, for example, by methods known to those skilled in the art, or similar to those disclosed in the standard literature, for example

Houben-Weyl, Methods of Organic Chemistry, Thieme ; or Organic Reactions, John Wiley &amp;Sons; or R· C. Larock,

Comprehensive Organic Transformations: A Guide to Functional Group Preparations, 2. ed. (1999), John Wiley &amp; Sons, and references cited therein. Another subject of the invention is novel starting compounds and intermediates which are present in the synthesis of compounds of formula I, including compounds of formula Ia, chemist, η, hc, III, Ilia, IV, V and VIII, wherein group A , D, E, L, G, J, T, R2, R10, R10a, r30, 尺40, r50 and R6〇 are according to the above definition, in any of its stereoisomeric forms or stereoisomers in any Mixtures of ratios, salts thereof, and any solvates thereof, and their use as intermediates or starting compounds for synthesis. The specific examples of the numbers and groups of the compounds of formula I are provided above, and all the general explanations and explanations of the definitions apply correspondingly to the middle: no starting compounds. One subject of the invention is in particular the specific starting compounds and intermediates disclosed herein. It is not related to the salt which is revealed to be free-formed. The form of the compound in the free state and in its == are the subject of the present invention, and if a specific salt is disclosed, it is additionally included in the form of the specific salt. The inhibition of cathepsin by a compound of formula I can be demonstrated in the test disclosed below and in other tests known to those skilled in the art. The compound of the formula and its physiologically acceptable salts and solvates thereof are valuable pharmaceutically active compounds. The compounds of the formula and their physiologically acceptable salts and solvates can be used for the treatment of, for example, cardiovascular diseases such as heart failure. Heart failure including contractile heart failure, diastolic heart failure, diabetic heart failure and normal contraction rate, cardiomyopathy, myocardial infarction, left ventricular dysfunction including left ventricular dysfunction after myocardial infarction, cardiac hypertrophy, ventricular remodeling Including post-infarction or cardiac surgery, cardiac to remodeling, valvular heart disease, vascular hypertrophy, vascular remodeling including arteriosclerosis, blood pressure including pulmonary hypertension, hepatic portal hypertension and systolic hypertension, atherosclerosis Peripheral arterial obstructive disease (pA〇D), restenosis, thrombosis and vascular permeability disease, ischemia and/or reperfusion injury including ischemia and/or reperfusion injury of the heart and ischemia of the retina and/or Reperfusion injury, inflammation, and inflammatory diseases such as rheumatoid arthritis and osteoarthritis, kidney disease such as renal papillary necrosis Failure includes renal failure after ischemia/reperfusion, lung disease such as cystic fibrosis, chronic bronchitis, chronic obstructive pulmonary disease (c〇PD), asthma, acute respiratory tract syndrome (ARDS), respiratory infections, and lung cancer, Immune diseases, diabetic complications including diabetic nephropathy and diabetic cardiomyopathy, fibrotic diseases such as pulmonary interstitial fibrosis including idiopathic pulmonary fibrosis, myocardial fibrosis, gray tube fibrosis, perivascular fibrosis, renal interstitial Fibrosis includes tubulointerstitial fibrosis, fibrotic skin conditions including the formation of keloid pain, collagen disease and scleroderma, and liver fibrosis, liver diseases such as cirrhosis, pain such as neuralgia, diabetic pain and inflammatory Pain, macular degeneration, neurodegenerative diseases or psychosis, or for cardioprotection including cardioprotection after myocardial infarction and after cardiac surgery, or for kidney protection. The treatment of the disease is the existing disease or organ dysfunction or existing symptoms of the private medicine and the goal is to eliminate, alleviate or cure, and to prevent the disease in humans or animals that are prone to and need prophylaxis or prevention (preventj〇n). Or organ dysfunction or symptoms, the goal is to prevent or inhibit its occurrence or attenuate its occurrence. For example, patients with a history of disease are prone to myocardial infarction, and preventive medical treatment can prevent the occurrence or recurrence of myocardial occlusion or reduce their stagnation and sequelae, or in patients who are prone to asthma attacks. Sexual medical treatment can prevent this episode or reduce its severity. Treatment of the disease can occur in both acute and chronic conditions. The efficacy of the compounds of formula I can be demonstrated in the pharmacological tests described below and in other tests by those skilled in the art. A compound of the formula I containing G selected from R - N(R )-C(0)- and physiologically acceptable salts and solvates thereof can also be used as a prodrug. The compounds of the formula I and their physiologically acceptable salts and solvates can thus be used in the form of pharmaceuticals, in particular in mammals and especially in humans, in themselves, in mixtures with others or in the form of pharmaceutical compositions. (pharmaceutica D or medicament. The subject of the invention is also the use of a compound of the formula I and its physiologically acceptable salts and solvates as a medicament] and pharmaceutical compositions and medicaments which comprise an effective amount of at least one compound of the formula I and / or a physiologically acceptable salt thereof and / or a pharmaceutically acceptable salt thereof as an active ingredient and a pharmaceutically acceptable agent, that is, - or more (d) academically non-toxic, or harmless (four) agent and / or 103 201245154 excipient And optionally one or more other pharmaceutically active compounds. The subject of the invention is also a formula of a guanidine compound and physiologically acceptable salts and solvates thereof for use in the treatment of a disease as mentioned above or below, including the treatment of any of the mentioned diseases First, for example, treating heart failure, myocardial infarction, cardiac hypertrophy, diabetic nephropathy, diabetic cardiomyopathy, myocardial fibrosis, or ischemia and/or Reperfusion injury, or for the use of a heart-protecting compound of the formula I and its physiologically acceptable salts and solvates for the manufacture of a medicament for the treatment of a disease as mentioned above or below, includes the treatment of any of the mentioned diseases For example, treating heart sorrow, myocardial infarction, cardiac hypertrophy, diabetic nephropathy, diabetic cardiomyopathy, myocardial fibrosis, or ischemia and/or reperfusion injury, or for cardioprotection, wherein the treatment of the disease includes the above Medical and prophylactic, and its use for the production of a medicament for inhibiting cathepsin A. The subject of the invention is also a method for the treatment of a disease as mentioned above or below, comprising the treatment of one of any of the mentioned diseases, for example for the treatment of heart failure , myocardial infarction, cardiac hypertrophy, diabetic nephropathy, diabetic cardiomyopathy, myocardial fibrosis, or ischemia and/or reperfusion injury, or for cardioprotection, comprising administering an effective amount of at least one compound of formula I and/or The physiologically acceptable salt and/or its solvate is administered to a human or animal in need thereof. Compound of formula 1 and pharmaceutical group The preparations and medicaments therewith may be administered enterally, for example, by oral, sublingual or rectal administration, parenteral administration, for example via intravenous, intramuscular, subcutaneous or intraperitoneal injection or infusion, or via other types of administration such as topical administration. , transdermal, transdermal, intra-articular or intraocular administration. The compound of formula I and its physiologically acceptable salts and solvates are also used in combination with other pharmaceutically active compounds, wherein, in combination, Formula I The compound and/or its physiologically acceptable salt and/or solvate thereof and one or more other pharmaceutically active compounds may be present in one and the same pharmaceutical composition or in two or more pharmaceutical compositions for separation, simultaneous or in accordance with Examples of such other pharmaceutically active compounds are agents, drainage diuretics, angiotensin converting enzyme (ACE) inhibitors, vasopressin receptor blockers, renin inhibitors, P blockers, Foxglove, aldosterone antagonist, N〇 donor, nitrate, hydralazines, 〇notr〇pes, vasopressin receptor antagonist, soluble Birds for acid cyclase activators, statins, peroxisome proliferator-activated receptor_α (ppAR_a) activators, peroxisome proliferator-activated recipients _γ (ρρΑΙι_γ) Activator, rosiglitazone (r〇SiglitaZ〇ne), glitazone (pi〇gmaz〇ne), metformin, sulfonylurea, glucagon peptide 1 (GLP-1) agonist, dipeptide Peptidase IV = PPIV) inhibitor, temsin, antiarrhythmia, endothelin receptor temple. Anti-state dance antagonist, acid diesterase inhibitor, acid-lower diesterase type 5 (PDE5) inhibitor, factor II/factor Ila inhibitor, factor Ix/factor IXa inhibitor, factor χ/factor inhibitor 'Factor Km / ^ sub XIIIa inhibitor, heparin, glycoprotein Ilb / IIIa antagonist, Ρ2γι 2 ^ body antagonist, chlorine to thunder (4). Pidogrel), coumarin, epoxidase / d-ethyl salicylic acid, RAF kinase inhibitor and p38 mitotically activated protein _ sylphysin. The subject matter of the invention is also the use of any two or more of the compounds of formula 1 disclosed herein, and physiologically acceptable salts and solvates thereof, in any combination with any one or more, for example, or other pharmaceutically active compounds. The pharmaceutical compositions and pharmaceutical products according to the present invention generally comprise from about 0.5 to about 90% by weight of a compound of formula I and/or a physiologically acceptable salt thereof and/or a solvate thereof, and per unit dose of the active ingredient of formula I and Or the amount of the physiologically acceptable salt and/or solvate thereof is usually from about 2 mg to about 1.5 g, especially from about 0.2 mg to about 1 g, more particularly from about 0.5 mg to about 〇. 5 grams, for example from about 1 milligram to about 3 grams. Depending on the type of pharmaceutical composition and other details of the particular situation, the amount may deviate from the specified amount. The production of pharmaceutical compositions and pharmaceuticals can be carried out in a manner known per se. In this regard, the compound of the formula I and/or its physiologically achievable salt and/or its solvate are admixed with one or more solid or liquid vehicles and/or excipients, if desired in combination with one or more other pharmaceuticals. The active compound is, for example, as mentioned above, and is administered in a suitable form for administration and administration, which can be subsequently used in human or animal medicine. As the vehicle, it can also be regarded as a diluent or a swelling agent, and a suitable organic and inorganic substance which does not react with the compound of the formula I in an undesired manner can be used. Examples of excipients or additions that can be included in pharmaceutical compositions and pharmaceuticals, such as lake slipper preservatives, thickeners, stabilizers, decomposers, humidifiers, Effect agents, emulsifiers, salts, for example, are used to affect penetration [, substances, dyes, flavors, and aromas. Examples of 4 agents and excipients are water, vegetable oil, soil, alcohols such as ethanol, isopropanol, 1,2-propylene glycol, alcohol, glycerin, polyol, polyethylene glycol or polypropylene glycol, diacetin cool , polyvinylpyrrolidone, gelatin, cellulose, 106 201245154 Carbohydrates such as lactose or powders such as corn powder, gasified sodium, stearic acid and its salts such as magnesium stearate, talc, lanolin, petrolatum or A mixture thereof such as brine or a mixture of water and one or more organic solvents such as a mixture of water and an alcohol. For oral and rectal use, the pharmaceutical forms which can be used are, for example, lozenges, capsules, sugar-coating agents, granules, hard and soft gelatin capsules, suppositories, solutions including oily, alcoholic or aqueous solutions, syrups. , fruit juices or drops, as well as suspensions or lotions. For parenteral use, e.g., via injection or infusion, a pharmaceutical form that can be used is, for example, a solution such as an aqueous solution. For topical use, pharmaceutical forms which can be used are, for example, ointments, creams, pastes, lotions, gels, sprays, foams, aerosols, solutions or powders. Other suitable forms of medicine are, for example, implants and patches and in a form suitable for inhalation. The compound of formula I and its physiologically acceptable salts can also be lyophilized and used to produce, for example, injectable compositions. Particularly for topical applications, liposome compositions are also suitable. The pharmaceutical compositions and medicaments may also contain one or more other active ingredients and/or, for example, one or more vitamins. As usual, the dosage of the compound of formula I will depend on the particular circumstances and will be adjusted by the clinician according to conventional rules and methods. It depends, for example, on the efficacy and duration of the administration of the compound of formula I and its effects, the nature and severity of the individual symptoms, the sex, age, weight and individual response of the human or animal being treated, the treatment being acute or chronic or prophylactic, Whether other pharmaceutically active compounds are administered in addition to the compound of formula I. Typically, in the case of administration to an adult having a body weight of about 75 kg, the amount of the agent 107 201245154 is from about 0.1 mg to about 100 mg per day per kg, especially from about 1 mg to about 20 mg per day per kg, for example from about 1 mg to about 10 mg per kg per day, (in each case in milligrams per kilogram of body weight). Each dose can be administered in the form of a single dose or divided into individual doses, such as two, three or four individual doses. Administration can be carried out continuously, for example via continuous injection or infusion. Depending on the individual manifestations of a particular situation, it may be necessary to deviate upward or downward from the specified dose. In addition to being a pharmaceutically active compound in human medicine and animal medicine, the compounds of the formula I can also be used as adjuvants in biochemical research or as scientific tools or for diagnostic purposes, for example in vitro in biological samples, if intent Inhibition of cathepsin A. The compounds of the formula I and their salts can also be used as intermediates, for example for the preparation of other pharmaceutically active substances. [Embodiment] The following examples illustrate the invention. Abbreviation ACN Acetonitrile DCM Dioxane DMF N,N-Dimercaptoamine DMSO Diterpenoid EA Ethyl Acetate EDIA N-Ethyl-Diisopropylamine FA Tannic Acid MOH Sterol 108 201245154 NEM N-B Base - 福福. TFA Trifluoroacetic acid THF Tetrahydrofuran τοτυ 〇-(Cyano(ethoxycarbonyl) fluorenylene)-Ν, Ν, Ν', Ν'-tetradecyl gland PTFE pentasate Exemplary compounds of the group are purified on a reverse phase (RP) column material via preparative high pressure liquid chromatography (HPLC), and as is customary, the eluent is a gradient mixture of water and acetonitrile containing trifluoroacetic acid. Part of this is obtained as an acid addition salt with trifluoroacetic acid, depending on the details of the treatment such as evaporation or freeze drying conditions. In the nomenclature and structural formulae of the example compounds, 'trifluoroacetic acid is not indicated. Similarly, other acid components of the exemplified compounds obtained in the form of acid addition salts are generally not indicated in the nomenclature and structural formula. The prepared compounds are generally identified via spectral data and chromatographic data, in particular mass spectrometry (MS) and HPLC retention time (Rt; minutes) which are identified by combined analytical HPLC/MS (LC/MS) and/or nuclear magnetics. Obtained by resonance (NMR) spectroscopy. Unless otherwise indicated, the iH_NMR spectrum was recorded at 5 〇〇 MHz Z at 298 K in D6_DMS as a solvent. In the NMR identification, the chemical shift δ (ppm), the number of hydrogen atoms (η), and the multi-cracking property of the peak (s: single peak, d. double crack peak, dd: double crack peak, t: three-split peak, q: four-cracked bee, m• multi-cracked peak). In MS identification, molecular ions [M] such as [M+] or related ions [M+1] such as [(M+1)+] are usually provided, that is, protonated molecules are separated from 109 201245154 [(M+H) +], or ion [Μ-l] such as [(Ml)-], that is, deprotonated molecular ion [(mass of Μ-ΗΠ peak (m/z), depending on the ionization method used) Usually, the ionization method is the electron spray free method (ES). The details of the LC/MS method used are as follows. Method LC1 Column: YMC-Pack Jsphere H80, 33 X 2·1 mm, 4 μm; : 1.3 ml / min; room temperature; eluent A: water + 0.05 % TFA; eluent B: ACN + 0.05 % TFA; gradient: from 95 % A + 5 % B to 5% A + 95 % B MS free method: ES+ method LC2 column: Waters XBridge C18, 50 x 4.6 mm, 2.5 microns; flow rate: 1.3 ml/min; room temperature; eluent A: water + 0.1% FA; eluent B : ACN + 0.08 % FA ; Gradient: from 97 % A + 3 % B to 40 % A + 60 % B in 3.5 minutes, then to 2 % A + 98 % B in 0.5 minutes, then 2 % A + 98% B over 1.0 minutes, then to 97% A + 3 % B in 0.2 minutes, 97 % A + 3 % B over 1.3 minutes; MS free method: ES - method LC3 column: YMC-Pack Jsphere H80, 33 x 2.1 mm, 4 microns; flow rate: 1.0 ml/min; room temperature; eluent A : water + 0.05 % TFA; eluent B: ACN + 0.05 % TFA; gradient: 98 % A + 2 % B over 1.0 min, then to 5% A + 95 % B in 4.0 min, then 110 201245154 after 5 % A+ 95 %B over 1.25 minutes; MS free method: ES+ method LC4 column: Waters XBridge C18, 50 x 4.6 mm, 2.5 microns; flow rate: 1.3 ml/min; 40 °C; eluent A: water + 〇. 1 % FA ; Eluent B : ACN + 0.1 % FA ; Gradient: from 97 % A + 3 % B to 40 % A + 60 % B in 3 · 5 minutes, then to 2 % A + 98 % B in Within 0.5 min, then 2 ° / 〇A + 98 % B over 1.0 min, then to 97 % A + 3 % B in 0.2 min, then 97 % A + 3 % B over 1.3 min; MS free method: ES- Method LC5 column: Waters XBridge C18, 50 X 4.6 mm, 2.5 microns; flow rate: 1.7 ml/min; 40 °C; eluent A: water + 〇.〇5 % TFA; eluent B: ACN + 0.05 % TFA ; Gradient: from 95 % A + 5 % B to 5% A + 95 % B at 3. Within 3 minutes, then 5% A + 95 % B over 0.55 minutes, then to 95 % A + 5 % B in 0.15 minutes; MS free method: ES+ method LC6 column: Waters XBridge C18, 50 X 4.6 mm, 2.5 Micron; flow rate: 1.7 ml/min; 50. (:; Eluent A: water + 0.05% TFA; eluent B: ACN + 〇.〇5 % TFA; gradient: 95 % A + 5 % B over 0.2 minutes 'and then to 5% A +95 % B Within 2.2 minutes, then 5% A + 95 % B over 1.1 minutes, then to 95 % A + 5 % B in 0.1 minutes, then 95% A + 5 % B over 0.9 minutes; MS free method: ES+ 111 201245154 Method LC7 column: Waters XBridge C18, 50 x 4.6 mm, 2.5 microns; flow rate: 1.7 ml/min; 40 °C; eluent A: water + 0.05% TFA; eluent B: ACN + 0.05% TFA; gradient : 95 % A + 5 ° / 〇 B over 0.2 minutes, then to 5% A + 95 % B in 2.2 minutes, then 5% A + 95 % B over 0.8 minutes, then to 95 % A + 5 % B at Within 0.1 min, then 95% A + 5 % B over 0.7 min; MS free method: ES+ method LC8 column: Waters XBridge C18, 50 X 4.6 mm, 2.5 microns; flow rate: 1.7 ml/min; 40 °C; Extract A: water + 0.05% TFA; eluent B: ACN + 0.05% TFA; gradient: 95% A + 5 % B over 0.3 minutes, then to 5% A + 95 % B in 3.2 minutes, then 5 % A + 95 % B over 0.5 minutes; MS free method: ES+ method LC9 tube : Merck Chromolith FastGrad RP-18e, 50 X 2 mm; flow rate: 2.0 ml/min; room temperature; eluent A: water + 0.05% TFA; eluent B: ACN + 0.05 % TFA; gradient: 98% A + 2 % B over 0.2 minutes, then to 2 % A + 98 % B in 2.2 minutes, then 2 % A + 98 % B over 0.8 minutes, then to 98 % A + 2 % B in 0.1 minutes, then 98 % A + 2 % B over 0.7 min; MS free method: ES+ method LC10 column: Waters XBridge C18, 50 X 4·6 mm, 2.5 μm; stream 112 201245154 speed: 1.3 ml/min; 45 °C; eluent A : water + 0.1 % FA; eluent B: ACN + 0.1 % FA; gradient: from 97 % A + 3 % B to 40 % A + 60 % B in 3.5 minutes, then 2 % A + 98 % B in Within 0.5 min, then 2% A + 98 % B over 1.0 min, then to 97 % A + 3 % B in 0.2 min, then 97 % A + 3 % B over 1.3 min; MS free method: ES+ method LC11 tube Column: Waters UPLCBEHC18, 50 x 2.1 mm, 1.7 μm; flow rate · ··························· : from 95 % A + 5 % B to 5% A + 95 % B in 1.1 minutes Inside, then 5% A + 95 % B over 0.6 min, then to 95 % A + 5 % B in 0.1 min, then 95 % A + 5 % B over 0.2 min; MS free method: ES+ method LC11_2 column: Waters UPLC BEH C18, 50 X 2.1 mm, 1.7 μm; flow rate: 0.9 ml/min; 55 °C; eluent A: water + 0.05% FA; eluent B: ACN + 0.035 % FA; gradient: from 95 % A + 5 % B to 5% A + 95 % B in 1_1 minutes, then 5% A + 95 % B over 0.6 minutes, then to 95 % A + 5 % B in 0.1 minutes, then 95 % A + 5 % B over 0.2 min; MS free method: ES+ method LC113 column: Waters UPLCBEHC18, 50 x 2.1 mm, 1.7 μm; flow rate: 0.9 ml/min; 55 ° C; eluent A: water + 〇.〇5 % FA ; Eluent B : ACN + 0.035 % FA ; Gradient: from 95 % A + 5 % 113 201245154 B to 5% A + 95 %B in 1.1 minutes, then 5% A + 95 %B over 0.6 minutes , then to 95% A + 5B in 0.2 minutes, then 95% A + 5 % B over 0.1 minutes; MS free method: ES+

Method LC11_X column. Waters UPLC BEH C18, 50 X 2.1 mm, 1.7 μm; /force l speed. 0.9 ml/min; 55 °C; eluent A: water + 〇.〇 5 % TFA;

Eluent B: ACN + 0.035 % TFA; Gradient: from 98 % A + 2. /〇B to 5% A + 95 % B in 2.0 minutes, then 5 〇 / 〇A + 95 〇 / 〇 B after 0.6 minutes 'and then to 95 % A + 5 % B in 0.1 minutes, then 95 % A + 5 % B over 0.3 minutes; MS free method: ES+

Method LC X column: Waters XBridgeC18, 50x4. 6 mm, 2. 5 microns; flow rate. 1. 7 liters per minute; 40 ° C; eluent A: water + 〇. 〇5 % TFA ; Eluent B : ACN + 0. 05 % TFA ; Gradient: from 95 % A + 5 % B to 95 ° / 〇 A + 5 % B at 0. Within 2 minutes, then to 5% A + 95 % B at 2. Within 2 minutes, then 5% A + 95 % B is 0. 8 minutes, then to 95 0 / 〇 A + 5 % B at 0. Within 1 minute, then 95% A + 5 % B passes 0. 7 min; MS free method: ES+ method LC12 column: YMC-Pack Jsphere H80, 33x2. 1 mm, 4 μm; Flow rate: 1. 0 ml / min; room temperature; eluent A: water + 〇 〇 5 % Tfa; eluent B : MOH + 0. 05 % TFA ; Gradient: 98 % A + 2 % B by 1. 0 minutes, then to 5% A +95 % B at 4. Within 0 minutes, then 5% A + 95 % B was 1. 25 minutes; MS free method: ES+ 114 201245154 Method LC13 Column: Waters XBridge C18, 50 x 4. 6, 2. 5 microns; flow rate: 1.3 ml/min; room temperature; eluent A: water + 0. 1% FA; eluent Β : ACN + 0. 08 % FA; Gradient: from 97 % Ά + 3 % B to 2 % A + 98 % 8 at 18. Within 0 minutes, then 2% Α+98 % Β1. 0 minutes, then to 97 % Α + 3 % Β at 0. Within 5 minutes, then 97% Α + 3 % Β via 0. 5 min; MS free method: ES+ method LC14 column: Waters XBridge C18 4. 6*50 mm; 2,5 μm, flow rate: 1. 3 ml / min; eluent A: H2O + 0. 1% FA; eluent B: ACN + 0. 08% FA; Gradient: from 97% A + 3% B to 2% A + 98% B in 18 minutes, then 2% A + 98% B over 1 minute, then to 97% A + 3% B at 0 . Within 5 minutes, then to 97:3 via 0. 5 minutes. The compounds of the formula I listed in Table 1 were prepared analogously to the methods illustrated in the synthesis examples. Table 1. Example compound of formula I Example number Compound name m/z (1) Rt (minutes) LC/MS method activity [μΜ] 1 (S)-3-[(5-decyloxy-6-phenyl-0 ratio bite -2-domain group)-amino]-3-o-indolephenyl-propionic acid 391. 19 1. 27 LC11 0. 1231 2 (S)-3-(2,4-Dichloro-phenyl)-3-[(5-decyloxy-6-phenyl) 445. 1 1. 33 LC11 0. 547 115 201245154 -0-pyridin-2-carbonyl)-amino]-propionic acid 3 (S)-3-[(6-Ga-5-decyloxy-0-pyridine-2-carbonyl)-amino] -3-o-indole phenyl-propionic acid 349. 09 1. 06 LC11 0. 274 4 (S)-3-{[3-(4,6-Dioxaoxylyl-2-yloxy)-β ratio -2-carbonyl]-amino}-3-o-indolephenyl -propionic acid 439. 17 1. 19 LC11 0. 353 5 (S)-3-[(.bipyridyl-2-carbonyl)-amino]-3-o-tolyl-propionic acid 285. 14 1. 13 LC11 3. 98 6 (S)-3-[(°tb ϋ定-4·绿基)-amine]-3-o-indole phenyl-propionic acid 285. 16 0. 97 LC11 7 (S)-3-[(5-Bromo-pyridine-3-carbonyl)-amino]-3-o-indolephenyl-propionic acid 363. 04 1. 14 LC11 &gt;10. 0 8 (8)-3-[(° ratio 11--3-amino)-amino]-3-o-indolephenyl-propionic acid 285. 16 0. 99 LC11 10. 4 9 (S)-3-[(3-decyloxypyridin-2-yl)-amino]-3-o-indole phenyl-propionic acid 315. 18 1. 04 LC11 7. 25 10 (S)-3-[(6-fluorenyl-«» bis-2-carbonyl)-amino]-3-o-phenylene-propionic acid 299. 17 1. 18 LC11 1. 24 116 201245154 11 (S)-3-[(4,6-Didecyl ratio. -3-yl)-amino]-3-o-indole phenyl-propionic acid 313. 2 0. 92 LC11 &gt;10. 0 12 (S)-3-[(6-decylamino-pyridin-2-yl)-amino]-3-o-indole phenyl-propionic acid 315. 17 1. 08 LC11 7. 32 13 (S)-3-[(2,6-bis-dimethylamino-pyrimidine-4-carbonyl)-amino]-3-o-indole-propionic acid 372. 24 3. 25 LC2 10. 1 14 (S)-3-[(4-indolyl-pyridine -2-carbonyl)-amino]-3-o-tolyl-propionic acid 299. 17 1. 18 LC11 4. 35 15 carbonyl)-amino]-3-o-tolyl-propionic acid 361. 32 3. 85 LC2 2. 16 16 (S)-3-[(2,6-Dimethoxy-indolyl-4-carbonyl)-amino]-3-o-tolyl-propionic acid 346. 15 1. 2 LC11 1. 05 17 (S)-3-[([l,6]Naphthyridin-2-carbonyl)-amino] o--p-phenyl-propionic acid 336. 16 1. 09 LC11 3. 09 18 (S)-3-[(4-Ethyl-pyridin-2-carboyl)-amino]-3-o-indole-propionic acid 313. twenty one. 22 LC11 3. 06 117 201245154 19 (S)-3-[(2-Ethylamino- to sigma-4-yl)-amino]-3-o-tolyl-propionic acid 342. 17 1. 03 LC11 &gt;10. 0 20 (S)-3-[(3,4,5,6-tetrahydro-2H-[1,2']bipyridyl-4'-carbonyl)-amino]-3-o-tolyl- Propionic acid 368. 22 1. 04 LC11 21 (S)-3-[(2-decylbipyridin-4-yl)-amino]-3-o-indole phenyl-propionic acid 315. 17 1. 12 LC11 22 (S)-3-{[2-(2,2-Dimercapto-propionylamino)-pyridine-4-carbonyl]-amino}-3-o-tolyl-propionic acid 384 . twenty one. 17 LC11 23 (S)-3-[(6-bromo-5-methoxy-° ratio sigma-2-yl)-amino]-3· o-phenylphenyl-propionic acid 393. 05 1. 21 LC11 0. 564 24 (S)-3-[(6-Methoxypyridin-3-ylidene)-amino]-3-o-indole phenyl-propionic acid 315. 17 1. 11 LC11 25 (S)-3-[(6-?-of-ollin-4-yl_0-0--2-yl)-amino]-3-o-tolyl-propionic acid 370. 19 1. 17 LC11 118 201245154 26 27 (S)-3-[(2-°Byrrolidin-1-yl-0 to 0-1,4-methyl)-amino]-3-o-indole phenyl-propionic acid 354. 22 0. 97 LC11 (S)-3-[(l-ethyl-3,6-dimercapto-1H-pyrido[3,4-b]0-pyridin-4-carbonyl)-amino]-3- O-nonylphenyl-propionic acid 381. 23 1. 15 LC11 28 (S)-3-[(6-Cyclopropyl-1,3-dioxo-1H-pyrazolo[3,4-b]pyridine-4-carbonyl)-amino]-3- O-nonylphenyl-propionic acid 393. 21 1. 2 LC11 29 (S)-3-[(2-N-B-B-phenyl-4-yl-O-O-1,4-decyl)-amino]-3-o-indole-propionic acid 370. 21 1. 03 LC11 30 31 (S)-3-[(4,6-Dioxalyl 4 α-den-2-yl)-amino]-3-o-indolephenyl-propionic acid 344. 27 1. 15 LC11 4. 21 (S)-3-[(6-decylpyridinyl-2-hydroxy)-amino]-3-o-phenyl-propionic acid 315. 17 1. 19 LC11 4. 77 32 (S)-3-{[6-(Tetrahydro-indolyl-4-yloxy)-α-pyridin-3-carbonyl]-amino}·_3-o-indolephenyl-propionic acid 385 . 18 1. 14 LC11 119 201245154 33 (S)-3-[(3-Fluorobipyridine-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid 301. 26 1. 1 LC11 3. 42 34 (S)-3-[(3H-Imidazo[4,5-b]pyridine-5-carbonyl)-amino]-3-o-indolephenyl-propionic acid, the compound containing trifluoroacetic acid 325. 16 1 LC11 5. 07 35 (S)-3-{[4-(pyrimidin-2-ylthioalkyl)-° ratio sigma-2-yl]-amino}-3-o-indolephenyl-propionic acid 395. 13 1. 19 LC11 0. 844 36 (S)-3-[(2-indolyl-4-carboyl)-amino]-3-o-phenylene-propionic acid 299. 18 0. 94 LC11 37 (S)-3-[(6-Phenylpyridin-2-yl)-amino]-3-o-indolyl-propionic acid 361. twenty one. 14 LC11_2 0. 1302 38 (S)-3-[(3-Phenylpyridin-2-carbonyl)-amino]-3-o-indolyl-propionic acid 361. 17 1. 19 LC11 39 (S)-3-[(4-phenylpyridin-2-carbonyl)-amino]-3-o-phenylene-propionic acid 361. 19 1. 28 LC11 1. 08 40 (S)-3-[(5-Phenylpyridin-2-carbonyl)-amino]-3-o-indenylbenzene 361. 18 1. 28 LC11 0. 45 120 201245154 BASE-propionic acid 41 (S)-3-[(5-fluorenyl-1-yl-σ ratio α--3-yl)-amino]-3-o-tolyl-propionic acid The compound contains trifluoroacetic acid 354. twenty one. 01 LC11 42 (S)-3-[(5-fluorenyl tillin-2-carboyl)-amino]-3-o-tolyl-propionic acid 298. 26 1. 1 LC11 43 (S)-3-{[6-(3-decyloxy-phenyl)-° ratio 0-but-2-yl]-amino}-3-o-indolephenyl-propionic acid 391 . 19 1. 14 LC11_2 2. 27 44 (S)-3-{[6-(2-decyloxy-phenyl)-° ratio σ定-2-)]-amino}-3-o-indolephenyl-propionic acid 391. 23 1. 14 LC11_2 1. 192 45 (S)-3-{[6-(4-decyloxy-phenyl)-. σ -2 · · · ] ] ] - - 391 391 391 391 391 391 391 391 391 391 391 18 1. 26 LC11 3. 09 46 (S)-3-[(6-Phenoxy-acridin-3-yl-yl)-amino]-3-o-phenyl-propionic acid 377. 16 1. 23 LC11 9. 94 47 (S)-3-[(4-Hydroxypyridin-2-carbonyl)-amino]-3-o-phenylene-propionic acid 301. 14 0. 97 LC11 121 201245154 48 (S)-3-[(6-Fluoro-acridin-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid 301. 28 1. 15 LC11 1. 67 49 (S)-3-[(6-°Byrrolidin-1-yl-.pyridin-3-carbonyl)-amino]-3-o-indolephenyl-propionic acid 354. 21 0. 95 LC11 50 (S)-3-[(4-Isofosin-4-yl-° ratio σ定-2-Prison)-Amino]-3· o-Phenylphenylpropionic acid 370. 2 0. 93 LC11 7. 73 51 (S)-3-[(4,6-Dimercapto-pyridine-2-carbonyl)-amino]&gt; 3-o-indole phenyl-propionic acid 313. 19 1. 2 LC11 1. 81 52 (S)-3-[(2-Amino-6-isobutyl-pyrimidine-4-carbonyl)-amino]-3-o-tolyl-propionic acid; compound containing trifluoroacetic acid 357. 03 1. 18 LC11 3. 68 53 54 ------ (S)-3-[(3,6-Difluoropyridin-2-carbonyl)-amino]-3-o-tolyl-propionic acid 319. 24 1. 12 LC11 2. 83(S)-3-[(3,4,5,6-Tetraoxy-2H-[1,2,]bipyridyl-6,-yl)-amino]-3-o-indolephenyl - Propionic acid 368. 22 1. 3 LC11 8. 93 122 . 201245154 55 (S)-3-[(2,6-Dimethyl-β-Bite-4-yl)-amino]-3-o-phenyl-propionic acid ’ 314. 19 1. 11 LC11 5. 26 56 (S)-3-[(6-p-Sodium-1-ylylidene-2-yl)-amino]-3-o-tolyl-propionic acid 351. 16 0. 95 LC11 11. 1 57 (S)-3-{[5-(4-decyloxy-phenyl)-pyridine-3-carbonyl]-amine]'-3-o-tolyl-propionic acid 391. 23 1. 17 LC11 11. 46 58 (S)-3-[(6-decyloxy-[2,4,]bipyridyl-4-carbonyl)-amino]-3-o-indolephenyl-propionic acid; Acetic acid 392. 24 0. 91 LC11_2 &gt;30. 0 59 (S)-3-[(6-Methoxy-[2,3']bipyridyl-4-carbonyl)-amino]-3-o-indolephenyl-propionic acid; Acetic acid 392. 33 0. 96 LC11-2 &gt;30. 0 60 (S)-3-o-indolyl-3-{[5-(3-trifluoromethyl-phenyl)- 0-succinyl-3-yl]-amino}•propionic acid 429 . 41 4. 36 LC2 61 (S)-3-{[5-(2,4-dioxa-phenyl p-pyridin-3-carbonyl)•amine}-3·o-methylphenyl-propionic acid 429. 17 1. 14 LC11_2 5. 14 123 201245154 62 (S)-3-{[5-(4-Fluoro-phenyl)-° ratio. Benz-3-yl]-amino}-3_ o-tolyl-propionic acid 377. 23 1. 06 LC11_2 63 (S)-3-o-indolyl-3-[(5-p-tolyl-pyridine-3-carbonyl)-amino]-propionic acid 375. 39 4. 09 LC2 64 (S)-3-o-tolyl-3-{[5-(4-trifluorodecyl-phenyl)-. Than σ -3 -3 - alkyl] amide propyl propyl 429. 41 4. 4 LC2 65 (S)-3-{[5-(3-decyloxy-phenyl)-π ratio -3--3-yl]-amino}-3-o-indolephenyl-propionic acid 391. 41 3. 91 LC2 66 (S)-3-o-indolyl-3-{[5-(2-trifluoromethyl-phenyl)-° ratio -3-amino]-amino}-propionic acid 429. 34 4. 21 LC2 4. 29 67 (S)-3-{[5-(2-decyloxy-phenyl)-° ratio sigma-3-carbonyl]-amino}-3-o-indolephenyl-propionic acid 391. 41 3. 83 LC2 4. 97 68 (S)-3-o-indolyl-3-[(5-m-methyl-carbyl-° ratio sigma-3-carbo]-amino]propionic acid 375. 39 4. 1 LC2 69 (S)-3-{[5-(2-Fluoro-phenyl)-. 0-0-3-weiki]-amino}^-3-379. 38 3. 92 LC2 1. 4 124 201245154 o-Phenylphenyl-propionic acid 70 (S)-3-{[5-(3-Cyano-phenyl)-π ratio α--3-yl]-amino}-3-ortho -曱Phenyl-propionic acid 386. 38 3. 78 LC2 71 (S)-3 - {[5-(4-Alkyl-phenyl)-° ratio σ定-3-carbyl]-amine]·_3-o-indolephenyl-propionic acid 386. 26 1. 03 LC11_2 72 (S)-3-{[5-(3,4-Dimethoxy-phenyl)_°°°-3-base]-Amino}-3-o-tolyl-C Acid 421. 44 3. 59 LC2 73 (S)-3-{[5-(2,4-Difluoro-phenyl)-. Pyridin-3-carbonyl]-amino}-3-o-indolephenyl-propionic acid 395. 21 1. 07 LC11_2 3. 25 74 (S)-3-{[5-(3,4-Difluoro-phenyl)-° ratio sigma-3-phenyl]-amino}-3-o-indolephenyl-propionic acid 395 . 19 1. 08 LC11_2 75 (S)-3-{[5-(2,6-Difluoro-phenyl)-ntb σ--3-yl]-amino}-3-o-indole-propionic acid 395. 17 1. 07 LC11_2 76 (S)-3-[(5-Benzo[1,3]dioxa scorpion fine-5-ylpyr sigma-3 _ aryl)_amino]-3-o-tolyl - propionic acid 405. 34 3. 78 LC2 8. 04 125 201245154 77 (S)-3-{[5-(3,4-Dimethyl-phenyl)-pyridinium-3-carbonyl]-amino}-3-o-indolephenyl-propionic acid 389. 39 4. 29 LC2 78 (S)-3-o-tolyl-3-{[5-(3,4,5-trimethoxy-phenyl)-pyridin-3-carbonyl]-amino}-prop Acid 451. 31 1. 03 LC11_2 79 (S)-3-{[5-(2,3-Difluoro-phenyl)-ηpyridin-3-carbonyl]-amine}}-o-indolephenyl-propionic acid 395. 17 1. 07 LC11_2 5. 01 80 (S)-3-{[5-(2-Cyano-phenyl)-pyridin-3-carbonyl]-amino}-3-o-tolyl-propionic acid 386. 23 1. 02 LC11_2 81 (S)-3-{[5-(3,5-Dimercapto-isoxazol-4-yl)-oxaridin-3-carbonyl]-amino}-3-o-tolyl- Propionic acid 380. 26 0. 98 LC11_2 82 (S)-3-{[5-(4-fluoro-2-methyl·indolyl)-π ratio α定_3 -mercapto]-amino}-3-o--p-phenyl- Propionic acid 393. 37 4. 13 LC2 3. 08 83 (S)-3-[(5-Pyrimidine-5-ylpyridin-3-carbonyl)-amino]-3-o-tolyl-propionic acid; the compound contains trifluoroacetic acid 363. 22 0. 88 LC11_2 126 201245154 84 (S)-3-{[5-(2-Didecylamino)-phenyl-phenyl)-ntlja-1,3--3-yl]-amino}-3-o-indene Base _ propionic acid 432. 42 3. 34 LC2 85 (S)-3-{[5-(4-fluoro-2-indolyl-phenyl)-n ratio a--3-yl]-amino}·_3-o-indolephenyl - propionic acid 409. 4 3. 96 LC2 7. 83 86 (S)-3-{[5-(2-decyloxy-4-difluoro] decyl-phenyl)-. Ratio _3_ Rotamyl]-amino}·_3-o-indolyl-propionic acid 459. 37 4. 42 LC2 87 (S)-3-{[5-(Bubenzyl-1H-indol-4-yl)-° ratio sigma-3-indenyl]-amino}-3-o-indolephenyl- Propionic acid 441. 45 3. 78 LC2 88 (S)-3-{[5-(2-Fluoro-5-decyloxy-phenyl)-atbσ-3-phenyl]-amino}-3-o-indolephenyl-propene Acid 407. 26 1. 07 LC11_2 8. 51 89 (S)-3-{[5-(2-Didecylamino) σ σ σ -5 -5 -yl)-° ratio a--3 domain]-amino}-3-o-曱Phenyl-propionic acid; the compound contains trifluoroacetic acid 406. 32 0. 99 LC11_2 127 201245154 Acid 90 (S)-3-[(2'_Morfosolin-4-yl-[3,4]. Ratio. Stationary-5-domain)-Amino]-3-o-曱Phenyl-propionic acid 447. 34 0. 88 LC11_2 91 (S)-3-[(5'-Fluoro-[3,3'] hydrazine σ-decyl-5-yl)-amino]-3_-o-phenyl-propionic acid 380. 22 0. 97 LC11_2 92 (S)-3-{[2-(4-曱-oxy-phenyl)-° ratio σ定-4- 基基]-amino}-3-o-indole phenyl-propionic acid 391 . twenty one. 16 LC11 93 (S)-3-o-tolyl-3-{[2-(4-trifluoromethyl-phenyl)-acridin-4-yl]-amino}-propionic acid 429. 19 1. 27 LC11 94 (S)-3-{[2-(3-decyloxy-phenyl)-° ratio. 1,4--4-yl]-amino}-3-o-tolyl-propionic acid 391. 23 1. 18 LC11 95 (S)-3-{[2-(2-decyloxy-phenyl)-° ratio. 1,4--4-yl]-amino]--3-o-indolephenyl-propionic acid 391. 22 1. 13 LC11 96 (S)-3-o-indolyl-3-[(2-m-indole-anthracene-diethyl-4-carbo)-amino]-propionic acid 375. 23 1. 22 LC11 128 201245154 97 (S)-3-{[2-(2-Fluoro-phenyl)-° ratio 0--4-domain group]-amino} -3_-o-phenylene-propionic acid 379. twenty one. 17 LC11 2. 71 98 (S)-3-{[2-(3,4-Dimethoxy-phenyl)_°°°-4-terminal]-amino}-3-o-tolyl-propionic acid 421. 23 1. 13 LC11 99 (S)-3-{[2-(3,5-Difluoro-phenyl)-° ratio sigma-4-yl]-amino}-3-o-indolephenyl-propionic acid 397. 18 1. 24 LC11 100 (S)-3-{[2-(3,4-difluoro-phenyl)-° ratio bit-4-domain]-amine}_3_o-indolephenyl-propionic acid 397. twenty one. 23 LC11 101 (S)-3-[(2-Benzo[1,3]dioxanthracene-5'-carbonyl)-amino]-3-o-phenylene-propionic acid 405. 21 1. 16 LC11 102 (S)-3-o-indolyl-3-{[2-(3,4,5-trimethoxy-phenyl)-° ratio sigma-4-domain]-amino group }-propionic acid 451. 26 1. 16 LC11 103 (S)-3-[([2,3']biacridinyl-4-phenyl)-amino]-3-o-indole phenyl-propionic acid 362. 19 0. 98 LC11 129 201245154 104 (S)-3-{[2-(2,5-Dichloro-phenyl)-° ratio -4-yl]-amino}-3-o-indole phenyl-propene Acid 429. 16 1. 24 LC11 105 (S)-3-{[2-(3,5-Dimercapto-isoxazol-4-yl)-pyridine-4-carbonyl]-amino}-3-o-tolyl-propenyl Acid 380. twenty one. 11 LC11 106 (S)-3-[(2'_ fluorenyl-[2,4']-linked 0-s-butyryl-4-yl)-amino]-3-o-tolyl-propionic acid 376. 21 0. 94 LC11 107 (S)-3-{[2-(4-|l-2-decyloxy-phenyl)-σ ratio sigma-4-yl]-amino}-3-o-tolyl - propionic acid 409. 21 1. 16 LC11 108 (S)-3-{[2-(l-benzyl-1Η-° ratio σ sit-4-yl)-° ratio ^-4-$carbyl]_amino}-3-o- Tolyl-propionic acid; the compound contains trifluoroacetic acid 441. 27 1. 16 LC11 109 (S)-3-{[2-(2-Fluoro-5-decyloxy-phenyl)-° ratio β--4-yl]-amino}_3_o-indolephenyl- Propionic acid 409. 21 1. 18 LC11 110 (S)-3-{[2-(3-Cyclopropylphosphonio-phenyl)-acridin-4-carbonyl]- 431. 27 1. 25 LC11 130 201245154 Amino}-3-o-indolephenyl-propionic acid 111 (S)-3-{[5-(3-chloro-4-fluoro-phenyl)-° than bite-3) -amino}-3-o-indole-propionic acid 413. 23 1. 11 LC11_2 112 (S)-3 - {[5-(2-Gas-phenyl)_. Pyridin-3-carbonyl]-amino}-3-o-tolyl-propionic acid 395. 33 4. 09 LC2 0. 826 113 (S)-3-{[5-(4-Tertibutyl-phenyl)-b-pyridine-3-carbonyl]-amine}-3-o-tolyl-propionic acid 417. 45 4. 66 LC2 114 (S)-3-{[5-(2,3-Dichloro-phenylpyridin-3-carbonyl)-amino}-3-o-indolephenyl-propionic acid 429. 21 1. 13 LC11_2 0. 95 115 (S)-3-[([3,4']biacridinyl-5-carbonyl)-amino]-3-o-indole styryl-propionic acid 362. 21 0. 8 LC11_2 116 (S)-3-{[5-(2,3-dimethyl-phenyl)-oxaridin-3-carbonyl]-amine}}-o-indole phenyl-propionic acid 389. 39 4. 24 LC2 1. 01 117 (S)-3-{[5-(2,4-Didecyl-benyl)-° ratio sigma-3-thiol]-amino}-3-o-tolyl-propionic acid 389 . 39 4. 29 LC2 5. 27 131 201245154 118 (S)-3-[(2·-Methyl-[3,4,]bipyridyl-5-carbonyl)-amino]-3-o-tolyl-propionic acid 376. 26 0. 79 LC11_2 119 (S)-3-{[5-(4-Ga-2-methoxy-phenyl)-n-pyridylcarbonyl]-amino}-3-o-tolyl-propionic acid 425. 24 1. 11 LC112 120 (S)-3-({5-[3-(5-Methyl-[1,3,4]oxadiazol-2-yl)-phenyl]-pyridine-3-carbonyl}-amine Base)-3-o-tolyl-propionic acid 443. 3 1 LC11_2 121 (S)-3-{[5-(3-Gas-4-didecylaminoindenyl-phenyl). Pyridine-3-carbonyl]-amino}-3-o-tolyl-propionic acid 466. 27 0. 99 LC112 122 (S)-3-[(2·Biphenyl-3-yl-indolepyridin-4-carbonyl)-amino]_3_o-tolyl-propionic acid 437. 27 1. 29 LC11 123 (8)-3-{[2_(2,3-dioxa-phenyl)-pyridin-4-carbonyl]-amine}-3-o-indole-propionic acid 429. 12 1. 23 LC11 3. 7 124 (S)-3-{[2-(3,4-Dimercapto-phenyl)-pyridin-4-carbonyl]-amine}-3-o-indole-propionic acid 389. 23 1. 24 LC11 132 201245154 125 (S)-3-{[2-(2,3-Difluoro-phenyl)-° ratio σ -4-amino]-amino}-3-o-indole phenyl- Propionic acid 397. 18 1. 19 LC11 126 (S)-3-{[2-(2-Cyano-phenyl sigma-4-terminal]-amino}-3-o-indolephenyl-propionic acid 386. 18 1. 14 LC11 127 (S)-3-{[2-(4-fluoro-2-methyl-phenyl)-° ratio σ定-4-carbyl]-amino}-3-o-indolephenyl- Propionic acid 393. twenty one. 2 LC11 128 (S)-3-{[2-(2-oxime-4-trifluoromethyl-phenyl)-pyridin-4-carboyl]-amino}-3-o- Phenyl phenyl-propionic acid 459. 22 1. 25 LC11 129 (S)-3-{[2-(4-Ga-2-methoxy-phenyl)-. Pyridin-4-carbonyl]-amino}-3-o-indolephenyl-propionic acid 425. 17 1. 21 LC11 130 (S)-3-[(2'_Morfosolin-4-yl-[2,4']bipyridyl-4-carbonyl)-amino]-3-o-indolephenyl-propenyl Acid 447. 27 1 LC11 131 (S)-3-[(5,-Fluoro-[2,3'] hydrazine σ -4--4-yl)-amino]-3-o-indolephenyl-propionic acid 380. 18 1. 12 LC11 133 201245154 132 (S)-3-({2-[3-(l-Hydroxy-1-indolyl-ethyl)-phenyl]-n-pyridin-4-yl}}-amino)- 3-o-tolyl-propionic acid 419. 25 1. 13 LC11 133 (S)-3-o-tolyl-3-{[6-(3-trifluoromethyl-phenyl)-. Bipyridine-2-carbonyl]-amino}-propionic acid 429. 18 1. 19 LC11_2 5. 76 134 (S)-3-{[6-(3-Gas-4-say-phenyl ratio °-2-yl)-amino}-3-o-indole-propionic acid 413. 14 1. 19 LC11_2 3. 62 135 (S)-3-{[6-(4-Fluoro-phenyl)-. ratio. -2--2-Methoxy]amino} -3· o-tolyl-propionic acid 379. 17 1. 15 LC11_2 1. 18 136 (S)-3-{[6-(4-Chloro-phenyl)-° ratio σ定-2-yl]-amino} - 3· o--phenyl-propionic acid 395. 13 1. 19 LC112 4. 85 137 (S)-3-o-indolyl-3-[(6-p-tolylcarbyl)-amino]-propionic acid 375. 21 1. 18 LC11_2 1. 24 138 (S)-3-o-indolyl-3-{[6-(4-trifluoromethyl-phenylpyridin-2-yl)-amino}-propionic acid 429. 19 1. 2 LC112 6. 83 139 (S)-3-o-indolyl-3-{[6-(2-trifluoromethyl-phenylpyridinium 429. 19 1. 16 LC11_2 1. 09 134 201245154 -24 Carbon-]-amino}-propionic acid 140 (S)-3-{[6-(3-chloro-phenyl)- 0 ratio sigma-2-yl]-amino} 3· o-Phenylphenyl-propionic acid 395. 18 1. 18 LC11_2 1. 57 141 (S)-3-o-tolyl-3-[(6-m- fluorenyl-2-pyridin-2-yl)-amino]-propionic acid 375. 21 1. 18 LC11_2 0. 1608 142 (S)-3-{[6-(2-Chloro-phenyl)-^ ratio σ定-2 -纟carbyl]-amino} - 3 · o--phenyl-propionic acid 395. 14 1. 16 LC11_2 0. 05 143 (S)-3-{[6-(2-Fluoro-phenyl)-0 butyl-2-yl]-amino}-3-o-tolyl-propionic acid 379. 16 1. 15 LC11_2 0. 0733 144 (S)-3-{[6-(4-Terbutyl-phenyl)-° ratio. Ding-2 -luki]-amino}-3-o-indolephenyl-propionic acid 417. 29 1. 26 LC11_2 145 (S)-3-{[6-(3-Cyano-phenyl)-Dtb sigma-2-carboxy]-amino}-3-o-indolephenyl-propionic acid 386. 21 1. 11 LC11_2 7. 46 146 (S)-3-{[6-(4-Cyano-phenyl)-° ratio sigma-2-mercapto]-amino}-3-o-indolephenyl-propionic acid 386. 17 1. 11 LC11_2 2. 16 147 (S)-3-[(6-biphenyl-3-yl ratio 437. 26 1. 24 LC11_2 3. 16 135 201245154 sigma-2-yl)-amino]-3-o-phenylphenyl-propionic acid 148 (S)-3-{[6-(3,4-dimethoxy-phenyl) -^ ratio °-2-amino]-amino}-3-o-tolyl-propionic acid 421. 22 1. 1 LC11_2 149 (S)-3-{[6-(2,4-di-n-phenyl)-π ratio -2-yl]-amino}-3-o-tolyl-propionic acid 397. 16 1. 16 LC11_2 4. 4 150 (S)-3-{[6-(3,5-Difluoro-phenyl)-t•Bis-2-yl]-amino}-3-o-indole-propionic acid 397 . 15 1. 16 LC11_2 1. 02 151 (S)-3-{[6-(3,4-Difluoro-phenyl)-D ratio sigma-t-yl]-amino}-3-o-indolephenyl-propionic acid 397 . 18 1. 16 LC11_2 1. 18 152 (S)-3-[(6-Benzo[1,3]dioxa sulphate-5-yl-11-bito-2-carbonyl)-amino]-3-o-tolyl- Propionic acid 405. 19 1. 12 LC11_2 1. 55 153 (S)-3-{[6-(3,4-Dimercapto-phenyl)-. ratio. -2--2-Methoxy]•amine}-3-o-indolephenyl-propionic acid 389. 23 1. 21 LC11_2 1. 19 154 (S)-3-o-indolyl-3-{[6-(3,4,5-trimethoxy-phenyl)-° ratio sigma-2-weiryl]-amino} - C. 451. 24 1. 12 LC11_2 136 201245154 Acid 155 (S)-3-[([2,3']biacridinylcarbonyl)-amino]-3-o-indole phenyl-propionic acid 362. 17 0. 93 LC11_2 156 (S)-3-{[6-(2,3-difluoro-phenyl)-° ratio. -2--2-Mercapto]-amino}-3-o-tolyl-propionic acid 397. 18 1. 16 LC11_2 0. 272 157 (S)-3 - {[6·(2 -Gasyl-phenyl)-° ratio σ定-2-mercapto]-amino}-3-o-tolyl-propionic acid 386. 14 1. 1 LC11_2 2. 46 158 (S)-3-{[6-(2,5-Difluoro-phenyl)-° ratio ̄-2-yl]-amino}-3-o-indolephenyl-propionic acid 397 . 15 1. 27 LC11 0. 126 159 (S)-3-{[6-(3,5-dimercapto-iso-supplement σ-s-yl)-° ratio °-2-mercapto]-amino}-3- o-Phenylphenyl-propionic acid 380. 15 1. 18 LC11 14. 4 160 (S)-3-{[6-(4-fluoro-2-indolyl-phenyl)_° ratio -2- yl]-amino}_3_o-tolyl-propionic acid 393. 16 1. 29 LC11 0. 472 161 (S)-3-{[6-(2,3-Dimercapto-phenyl)-° ratio °-2-alkyl]-amino}-3-o-indolephenyl-propionic acid 389. 19 1. 31 LC11 0. 0294 137 201245154 162 (S)-3-{[6-(2,4-Dimethyl-phenyl)-° ratio. Determining -2-yl]-amino}-3-o-indolephenyl-propionic acid 389. 17 1. 32 LC11 1. 43 163 (S)-3-[(2,-Mercapto-[2,4,]-linked 0-α-based-6-yl)-amino]-3-o-tolyl-propionic acid 376. 17 0. 96 LC11 164 (8)-3-[(6-0 crypto-5-yl-to-mouth ratio: -2-pyryl)-amino]-3-o-indole phenyl-propionic acid; Trifluoroacetic acid 363. 15 1. 09 LC11 165 (S)-3-{[6-(5-fluoro-2-methyl-phenyl)-° ratio σ定·2 -alkyl]-amino}-3-o-tolyl-propyl Acid 393. 16 1. 29 LC11 0. 0944 166 (S)-3-{[6-(4-Fluoro-2-methoxy-phenyl)-σ ratio biting-2-_carbonyl]_amino}_3_o-tolyl-propionic acid 409. 16 1. 27 LC11 167 (S)_3-{[6-(2-Methoxy-4-trifluoromethyl-phenyl)-»bipyridine-2-carbonyl]-amino}-3-o-indolephenyl - Propionic acid 459. 18 1. 32 LC11 0. 963 168 (S)-3-{[6-(4-Ga-2-indolyl-phenyl)-° ratio σ-defined-2-domain group]·Amino 丨-3-o-indole phenyl- C. 425. 13 1. 31 LC11 0. 425 138 201245154 Acid 169 (S)-3-{[6-(l-Benzyl-1H-mouthbisazol-4-yl)-pyridine-2-carbonyl]-amino}-3-o-indolephenyl _ propionic acid; the compound contains trifluoroacetic acid 441. 19 1. 23 LC11 170 (S)-3-{[6-(2-Fluoro-5-decyloxy-phenyl)-° ratio σ定-2 -基基]_Amino-o-phenyl-propionic acid 409 . 16 1. 28 LC11 0,815 171 (S)-3-{[6-(3-cyclopropylmethoxy-phenyl)-. °°-2-carbyl]_amino-o-gastric phenyl-propionic acid 431. 22 1. 33 LC11 6. 98 172 (S)-3-{[6-(3-Fluoro-2-indolyl-phenyl)-° ratio bit-2-yl]-amino}_3_o-methyl-propionic acid 393 . 17 1. 29 LC11 3. 21 173 (S)-3-{[6-(2-Dimethylamino _ 〇岔α定-5-yl)-. The ratio of _ 2 - _ carbon-]-amino}_3-o-indole phenyl-propionic acid; the compound contains trifluoroacetic acid 406. 21 1. 2 LC11 174 (S)-3-{[6-(3-chloro-4-didecylaminodecyl-phenyl)-11 ratio 464. 31 1. 18 LC11 1. 59 139 201245154 α定-2-Weiyl]-Amino}-3-o-p-phenyl-propionic acid 175 (S)-3-{[6-(5-Gas-2-fluoro-4-fluorenyl) -Phenyl)-pyridine-2-carbonyl]•Amino}_3_o-indolephenyl-propionic acid 427. 13 1. 34 LC11 2. 36 176 (S)-3-({6-[3-(l-Hydroxy-1-indolyl-ethyl)-phenyl]-0) 定-2-demethylamino)-3-o- Phenyl phenyl-propionic acid 419. twenty one. 2 LC11 3. 32 177 (S)-3-{[2-(2-Didecylamino)-. ratio. -4-amino]-amino}'-3-o-indolephenyl-propionic acid; the compound contains trifluoroacetic acid 406. 25 1. 12 LC11 178 (S)-3-{[6-(2-Fluoro-phenyl)-5-decyloxy-° ratio. -2--2-Methoxy]-amino}-3-o-indolephenyl-propionic acid 409. 1 1. 12 LC11_2 0. 0683 179 (S)-3-{[2-(3-Gas-phenyl)-° ratio σ定-4-拔基]-Amino} -3_ O-Phenylphenyl-propionic acid 395. 23 4. 51 LC2 180 (S)-3-{[6-(2-Fluoro-5-fluorenyl-phenyl)-. Pyridin-2-carbonyl]-amino}·3-o-indole-propionic acid 393. 16 1. 3 LC11 0. 289 140 201245154 181 (S)-3-{[5-decyloxydimethyl-phenyl)-n ratio 11 _2 _ carbonyl]-amino}-3-p-indole phenyl-propionic acid 459 . 28 1. 19 LC11_2 5 182 (S)-3-[(5-Methoxy-6-phenyl-indolyl-2-carbonyl)-amino]_3_ p-nonylphenyl-propionic acid 389. 28 1. 14 LC11_2 0. 232 183 (S)-3-{[6-(2,4-dioxa-phenyl)-5-decyloxy-n ratio. Ding-2-carbonyl]-amino}-3-p-tolyl-propionic acid 459. 21 1. 2 LC11_2 1. 009 184 (S)-3-{[6-(3-Chloro-4-fluoro-phenyl)-5-decyloxy-pyridine-2-carbonyl]-amino}-3-p-tolyl-propyl Acid 443. 23 1. 19 LC11_2 &gt;10. 0 185 (S)-3-{[6-(4•Gas-phenyl)-5-decyloxy-pyridine-2-carbonyl]-amino}-3-p-tolyl-propionic acid 409. 23 1. 15 LC11_2 1. 289 186 (S)-3-{[6-(4-Gas-phenyl)-5-decyloxy-pyridine-2-carbonyl]-amine}-3-p-phenylene-propionic acid 425. 25 1. 18 LC11_2 3. 56 187 (S)-3-{[5-Methoxy-6-(4-decyloxy-phenyl)-. Bipyridine-2-carbonyl]-amino}-3-p-tolyl- 419. 32 1. 13 LC11_2 4. 85 141 201245154 Propionic acid 188 (S)-3-[(5-decyloxy-6-p-tolyl-σ ratio sigma-2-yl)-amino]-3-p-phenylene- Propionic acid 403. 31 1. 17 LC11_2 4. 45 189 (S)-3-{[5-methoxy-6-(4-dioxamethyl-phenyl)_° ratio. -2--2-Mercapto]-amino}-3-p-tolyl-propionic acid 457. 35 1. 2 LC112 &gt;10. 0 190 (S)-3-[(5-decyloxy-6-o-indolephenyl-° ratio sec-2-yl)-amino]-3-p-indolephenyl-propionic acid 403 . 33 1. 14 LC11_2 0. 0813 191 (S)-3-{[5-decyloxy-6-(3-decyloxy-benyl)_° ratio °-2-carboyl]-amino}-3-pair-oxime Phenyl-propionic acid 419. 34 1. 14 LC11_2 4. 57 192 (S)-3-{[5-decyloxy-6-(2-trifluoromethyl-phenyl)-acridin-2-yl]-amino}_3_p-indolephenyl- Propionic acid 457. 33 1. 15 LC112 0. 1457 193(S)-3 - {[6-(3-Chloro-phenyl)-5_ oxime-° ratio °-2-alkyl]-amino}·-3-p-tolyl-propenyl Acid 425. 17 1. 18 LC11_2 2. 74 194 (S)-3 - {[6-(3 - defeat-phenyl)-5- 407. 29 1. 15 LC11_2 0. 725 142 201245154 曱乳-° ratio bite_2-green base]-amino}-3-p-indole phenyl-propionic acid 195 (S)-3-[(5-decyloxy-6-naphthalene* 2-Base-° ratio biting 2-carbyl)-amino]-3-p-indolephenyl-propionic acid 441 1. 2 LC11_2 8. 83 196 (S)-3-{[5-decyloxy-6-(2-methoxy-phenyl)-fluorene ratio.定-2-裁基]-Amino}_3-p-tolyl-propionic acid 419. 33 1. 11 LC11_2 0. 1191 197 (S)-3-[(5-decyloxy-6-m-tolyl-indole ratio. dec-2-yl)-amino]-3-p-tolyl-propionic acid 404. 68 1. 17 LC11_2 1. 71 198 (S)-3-{[6-(2-Chloro-phenyl)-5-methoxy-π ratio sigma-2-yl]-amino}-3-p-phenylene- Propionic acid 423. 24 1. 14 LC11_2 0. 159 199 (S)-3-{[6-(2-Gas-phenyl)-5-decyloxy-0 ratio. -2--2-Mercapto]-amino}-3-p-indolephenyl-propionic acid 407. 28 1. 12 LC11_2 0. 228 200 (S)-3-{[6-(4-Terti-butyl-phenyl)-5-decyloxypyridin-2-yl-yl]-amino}-3-p-indolephenyl - Propionic acid 445. 39 1. 25 LC11_2 &gt;10. 0 201 (S)-3-{[6-(3-Cyano-phenyl)-5-decyloxy-0 σ 定 -2- carb 415. 81 1. 12 LC11_2 &gt;10. 0 143 201245154 ]]-amino}_3_p-nonylphenyl-propionic acid 202 (S)-3 - {[6-(4-ranyl-phenyl)-5-hydrazinyl-. Specific bite-]-number base]-amino}_3_p-nonylphenyl-propionic acid 416. 24 1. 11 LC11_2 &gt;10. 0 203 (S)-3-{[6-(3-Ethyl-phenyl)-5-decyloxy-. σ定定-2-罗炭基]-Amino}_3_p-indole phenyl-propionic acid 433. 31 1. 1 LC11_2 8. 35 204 (S)-3-[(6-Biphenyl-3-yl-5-oximeoxy-0 to 0-but-2-yl)-amino]-3-p-tolyl-propionic acid 465 . 32 1. 22 LC11_2 1. 402 205 (S)-3-{[6-(4-Ethyl-phenyl)-5-methoxy ratio. Ding-2-carboyl]-amino}-3-p-tolyl-propionic acid 431. 43 1. 1 LC11_2 &gt;10. 0 206 (S)-3-{[6-(2,4-Difluoro-phenyl)-5-methoxy-anthracene--mineral]-amino}_3_p-nonylphenyl_ Propionic acid 425. 26 1. 14 LC11_2 0. 1556 207 (S)-3-{[6-(3,5-dioxa-phenyl)-5-decyloxy-° ratio 0-but-2-carboyl]-amino}}_3_p-曱Phenyl - 425. 28 1. 16 LC11_2 2. 65 144 201245154 Propionic acid 208 (S)-3-{[6-(3,4-Difluoro-phenyl)-5-decyloxy-° ratio -2--2-梦炭基]-amino}- 3-p-tolyl-propionic acid 425. 31 1. 16 LC11_2 7. 42 209 (S)-3-{[6-(2,3-Dichloro-phenyl)-5-decyloxy-0-pyridin-2-carboyl]amino]-_3-p-toluene Base-propionic acid 457. 27 1. 18 LC11_2 0. 0696 210 (S)-3-{[6-(5-Ethyl-thiophen-2-yl)-5-methoxypyridin-2-yl]-amino}-3-p-quinone Base-propionic acid 437. 3 1. 1 LC11_2 7. 52 211 (S)-3-{[6-(2-Chloro-5-trifluoromethyl-phenyl)-5-methoxy-indole-2_domain]-amino} -3-pair _ phenyl phenyl-propionic acid 493. 24 1. 19 LC11_2 0. 421 212 (S)-3-{[6-(3-Fluoro-2-indolyl-phenyl)-5-decyloxy-acridin-2-carboyl]-amino}_3-(2- Fluoro-phenyl)-propionic acid 427. 27 1. 13 LC11_2 0. 1497 213 (S)-3-{[6-(2-Chloro-5-trifluorodecyl-phenyl)-5-decyloxy-α ratio 497. twenty one. 17 LC11_2 0. 887 145 201245154. Benz-2-yl]-amino}-3-(2-fluoro-phenyl)-propionic acid 214 (S)-3-(2-a-phenyl)-3-{[6-(2- Gas-4-trifluoromethyl-phenyl)-5-decyloxypyridin-2-carbonyl]-aminoindole-propionic acid 497. 21 1. 19 LC11_2 7. 02 215 (S)-3-[(3-decyloxy-[2,4|] hydrazide-6-carbyl)-amino]-3·p-phenylene-propionic acid 390. 2 0. 88 LC11_2 9. 66 216 (S)-3-[(3-Methoxy-[2,3]bipyridyl-6-carbonyl)amino]-3-p-phenylene-propionic acid 390. 25 0. 93 LC11_2 &gt;10. 0 217 (S)-3-{[6-(2,3-Difluoro-phenyl)-5-methoxyl-butyl-2-carbonyl]-amino}-3-p-phenylene-propyl Acid 425. 32 1. 13 LC11_2 0. 0902 218 (S)-3-{[6-(2,5-Difluoro-phenyl)-5-foxy-pyridine-2-carbonyl]-amino}-3-p-tolyl-propionic acid 425. 31 1. 13 LC11—2 0. 0998 219 (S)-3-{[6-(2,5-Dichloro-phenyl)-5-methoxyl-butyl-2-yl]-amino}-3-p-tolyl-propenyl Acid 457. 25 1. 18 LC11_2 0. 91 146 201245154 220 (S)-3-{[6-(3,5-Dimercapto-isoxazol-4-yl)-5-decyloxy-. Σσ定-2-戴基]-amino}-3-tero-p-phenyl-propionic acid 408. 28 1. 07 LC11_2 0. 143 221 (S)-3-{[6-(4-Fluoro-2-methyl-phenyl)-5-methoxypyridin-2-yl]-amino}-3-p-tolyl - Propionic acid 421. 35 1. 15 LC11_2 0. 239 222 (S)-3-{[6-(2,3-Dimercapto-phenyl)-5-decyloxy-pyridine-2-carbonyl]-amino}-3-p-tolyl-propyl Acid 417. 34 1. 17 LC11_2 0. 037 223 (S)-3-{[6-(3-Fluoro-4-methyl-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-p-indolephenyl -propionic acid 423. 27 1. 18 LC11_2 1. 294 224 (S)-3-{[6-(2,4-Dimercapto-phenyl)-5-methoxy-acridin-2-carbonyl]-amino}-3-p-indolephenyl ·•Protein 417. 36 1. 18 LC11_2 3. 39 225 (S)-3-{[6-(4-Fluoro-3-methyl-phenyl)-5-methoxy-p-pyridin-2-yl]-amino]-_3-pair- Phenyl phenyl-propionic acid 421. 33 1. 18 LC11_2 3. 26 147 201245154 226 (S)-3-[(5-Methoxy-6-pyrimidin-5-ylpyridin-2-carbonyl)-amine]-3-p-phenylene-propionic acid 391. 29 1 LC11_2 &gt;10. 0 227 (S)-3-[(6'-Fluoro-3-indolyl•[2,3']-bipyridyl-6-carbonyl)-amino]-3-p-tolyl-propane Acid 408. 28 1. 09 LC11_2 7. 63 228 (S)-3-{[6-(2-Didecylaminomethylindenyl-phenyl)-5-decyloxy-pyridine-2-carbonyl]-amino}_3_ p-phenylene - Propionic acid 462. 31 1. 06 LC11_2 3. 96 229 (S)-3-[(3,2'-Dioxalyl-[2,3'] linked ratio. Stationary-6-Rotyl)-amino]-3-p-phenylene _ Propionic acid 422. 29 1. 07 LC11_2 0. 609 230 (S)-3-{[6-(5-fluoro-2-methyl-phenyl)-5-methoxy-indole ratio 2-carbonyl]-aminophenyl 3-p-tolyl -propionic acid 423. 27 1. 15 LC11_2 0. 1113 231 (S)-3-{[6-(4-fluoro-2-indolyl-phenyl)-5-decyloxy-acridin-2-carbonyl]-amino}-3-p-toluene Base-propionic acid 439. 27 1. 12 LC112 0. 305 148 201245154 232 (S)-3-{[6-(4-Chloro-2-indolyl-phenyl)-5-decyloxy-° ratio 咬-2-yl]-amino}-3 -p-Phenylphenyl-propionic acid 455. 26 1. 16 LC11_2 2. 33 233 (S)-3-{[6-(5-Chloro-2-indolyl-phenyl)-5-methoxypyridin-2-ylcarbonyl]-amino}-3-pair- Phenyl phenyl-propionic acid 455. 25 1. 15 LC11_2 2. 24 234 (3)-3-{[6-(5-1-2-曱-oxy-phenyl)-5-decyloxypyridin-2-yl]-amino}}_3-pair-曱Phenyl-propionic acid 439. 28 1. 12 LC11_2 0. 51 235 (S)-3-{[6-(2,5-Dimethoxy-phenyl)-5-decyloxy-. Bisidine-2-Isyl]-amino}_3_p-phenylphenyl-propionic acid 451. 3 1. 1 LC11_2 &gt;10. 0 236 (S)-3-{[6-(2-|l-5-trifluorodecyl-phenyl)-5-methyllacyl-0-bite----------------------- Tolyl-propionic acid 477. 27 1. 18 LC11_2 3. 57 237 (S)-3-{[5-decyloxy-6-(5-fluorenyl-amino-2-yl)-α ratio sigma-2-carbonyl]-amino}-3-pair- Phenyl phenyl-propionic acid 395. 25 1. 11 LC11_2 3. 54 149 201245154 238 (S)-3-{[5-decyloxy-6-(1-indolyl-1H-pyrazol-4-yl)-pyridyl. -2--2-绿基]-amino} -3-p-phenylphenyl-propionic acid 395. 26 1. 02 LC11_2 &gt;10. 0 239 θ)-3-{[6-(2-1-5-decyloxy-phenyl)-5-decyloxypyridin-2-carbyl]-amino}-3-p-quinone Base-propionic acid 439. 28 1. 12 LC11_2 1. 16 240 (S)-3-{[6-(5-Tertibutyl-2-decyloxy-phenyl)-5-methoxyl-° 〇 -2 -2 -1 -yl]-amino} -3-p-tolyl-propionic acid 477. 37 1. 22 LC11_2 &gt;10. 0 241 (S)-3-{[6-(2-Fluoro-4-trifluoromethyl-phenyl)-5-decyloxy-. Ratio π ̄ ̄ ̄ ̄ ̄ 几 ] ] ] - 3 3 3 3 477 477 477 477 477 477 477 27 1. 19 LC11_2 &gt;10. 0 242 (S)-3-{[6-(2-Fluoro-5-fluorenyl-phenyl)-5-decyloxy-acridin-2-phenyl]-amine}_3_p-phenylene Base-propionic acid 423. 29 1. 15 LC11_2 0. 278 243 (S)-3-{[6-(3-Gas-2-indolyl-phenyl)-5-decyloxy-0 ratio. Ding-2-carboyl]-aminoindole-3-p-phenylene-propionic acid 439. 27 1. 19 LC11_2 0. 2027 150 201245154 244 (S)-3-{[6-(3-Fluoro-2-methyl-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-pair -曱Phenyl-propionic acid 423. 29 1. 15 LC11_2 0. 0901 245 (S)-3-{[6-(5-Chloro-2-fluoro-phenyl)-5-decyloxy-° ratio 0-but-2-carboyl]-amino}_3_pair- Tolyl_propionic acid 443. 24 1. 17 LC11_2 0. 44 246 (S)-3-{[6-(4-Gas-3-gas-phenyl)-5-decyloxy-0-precipitate-2-carboyl]amino}-3-p-toluene Base _ propionic acid 443. 22 1. 2 LC11_2 4. 48 247 (S)-3-[(2\Chloro-3-indolyl-5'-indolyl-[2,3"bipyridyl-6-carbonyl)-amino]-3-p-indenebenzene Base-propionic acid 440. 27 1. 09 LC11_2 8. 43 248 (S)-3-{[6-(3-Chloro-5-methyl-phenyl)-5-decyloxypyridin-2-yl-yl]-amino}-3-p-toluene Base-propionic acid 439. 25 1. 21 LC11_2 &gt;10. 0 249 (S)-3-({5-decyloxy-6-[3-(5-fluorenyl-[1,3,4]oxadiazol-2-yl)-phenyl]pyridin-2 -carbonylamino)-3-p-phenylene- 473. 29 1. 08 LC11_2 8. 71 151 201245154 Propionic acid 250 (S)-3-{[5-methoxy-6-(1,3,5-trimethyl-1H-pyrazol-4-yl)-吼σ定-2-rebel ]]-amino}-3-p-tolyl-propionic acid 423. 32 1. 02 LC11_2 &gt;10. 0 251 (S)-3-{[5-decyloxy-6-(1-indolyl-1H-hydroxyl-6-yl)-°pyridine-2-weiki]-amino} - 3 - p- 曱 phenyl-propionic acid 444. 31 1. 16 LC11_2 8. 94 252 (S)-3-{[6-(4-Chloro-3-indolyl-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-pair-oxime Phenyl-propionic acid 455. 26 1. 18 LC11_2 &gt;10. 0 253 (S)-3-(2-|l-phenyl)-3-{[5-decyloxy-6-(3-trifluorodecyl-phenylindole-吼σ定-2-carbyl) ]-Amino}-propionic acid 461. 3 1. 17 LC11_2 4. 06 254 (S)-3-(2-Fluoro-phenyl)-3-[(5-decyloxy-6-phenyl-acridin-2-carbonyl)-amino]-propionic acid 395. 25 1. 11 LC11_2 0. 1818 255 (S)-3-{[6-(2,4-dioxa-phenyl)-5-methyllacyl-0 to 0-but-2-carboyl]-aminopyr-3-(2- |t-benzene 463. 18 1. 18 LC11_2 0. 879 152 201245154 base)-propionic acid 256 (S)-3-{[6-(3-chloro-4-vapor-phenyl)-5-decyloxy-. Specific bite-2-amine]••amino}-3-(2- gas-phenyl)-propionic acid 447. 21 1. 17 LC11_2 &gt;10. 0 257 (S)-3-(2-Any-phenyl)-3-{[6-(4-f-phenyl)-5-methyllacyl-0 ratio.定-2 - _Carbo]-amino}-propionic acid 413. 21 1. 12 LC11_2 1. 263 258 (S)-3-{[6-(4-Gas-phenyl)-5-methoxy-n-pyridin-2-carbonyl]-amino}-3-(2-mur-phenyl) - propionic acid 429. 24 1. 17 LC11_2 5. 27 259 (S)-3-(2-Gas-phenyl)-3 - {[5-decyloxy-6-(4-methoxy-phenyl)-σ ratio sigma-2 -carbyl] -amino}-propionic acid 425. 27 1. 11 LC11_2 5. 01 260 (S)-3-(2-Fluoro-phenyl)-3-[(5-decyloxy-6-p-anthracenylphenyl)-amino]-propionic acid 409. 27 1. 15 LC11_2 5. 18 261 (S)-3-(2_fluoro-phenyl)-3 - {[5-decyloxy-6-(4-trifluoromethyl-phenyl)-° ratio σ定-2-绿基] -amino}-propionic acid 463. 27 1. 18 LC11_2 &gt;10. 0 153 201245154 262 (S)-3-(2-Fluoro-phenyl)-3-[(5-methoxy-6-o-tolylpyridin-2-carbonyl)-amino]-propionic acid 407. 26 1. 12 LC11_2 0. 0819 263 (S)-3-(2-Gas-phenyl)-3-{[5-decyloxy-6-(3-decyloxy-phenyl)-α ratio. Ding-2-yl]-amino}-propionic acid 425. 27 1. 11 LC11_2 5. 06 264 (S)-3-(2-Fluoro-phenyl)-3-{[5-decyloxy-6-(2-trifluoromethyl-phenyl)-. Than deg-2-reyl]-amino}-propionic acid 463. 25 1. 12 LC11_2 0. 179 265 (S)-3-{[6-(3-Chloro-phenyl)-5-methoxy-° ratio ̄-2-yl]-amino}-3-(2-gas-benzene Base)-propionic acid 429. 23 1. 16 LC11_2 1. 719 266 (S)-3-(2-|l-phenyl)-3-{[6-(3-fluoro-phenyl)-5-methoxyl-° ratio σ定-2-yl]- Amino}-propionic acid 413. 23 1. 13 LC11_2 1. 26 267 (S)-3-(2-Fluoro-phenyl)-3-[(5-decyloxy-6-n-2-yl-π ratio α-decyl)-amino]- Propionic acid 445. 3 1. 18 LC11_2 &gt;10. 0 268 (S)-3-(2-Fluoro-phenyl)-3-{[5-decyloxy-6-(2-decyloxy-phenyl)-° ratio. Ding-2-yl]-amine 425. 25 1. 08 LC11_2 0. 102 154 201245154 base}-propionic acid 269 (S)-3-(2-fluoro-phenyl)-3-[(5-decyloxy-6-m-tolyl ratio α-t-yl)- Amino]-propionic acid 409. 26 1. 15 LC11_2 1. 015 270 (8)-3-{[6-(2-Chloro-phenyl)-5_ 曱 基 -^^^^^^^^^^^^^^^^^^^^^^^^^ Base)-propionic acid 429. 23 1. 11 LC11_2 0. 9178 271 (S)-3-(2-Fluoro-phenyl)-3-{[6-(2-fluoro-phenyl)-5_ 曱 基 基 -2- ; ; ; ; ; ; ; ; ; ; }-propionic acid 413. 23 1. 1 LC11_2 0. 0418 272 (S)-3-{[6-(4-Tertibutyl-phenyl)-5-methoxypyridin-2-yl]amino}-3-(2- gas-benzene Base)-propionic acid 451. 34 1. 23 LC11_2 &gt;10. 0 273 (S)-3-{[6-(3-N-Mercapto-phenyl)-5-decyloxypyridin-2-carbonyl]-aminoindole-3-(2-fluoro-phenyl)- Propionic acid 420. 25 1. 09 LC11_2 9. 57 274 (S)-3-{[6-(4-Cyano-phenyl)-5-decyloxy-0 ～β-2-yl]••Amino}-3-(2-Fluorine -Phenyl)-propionic acid 420. 23 1. 09 LC11_2 &gt;10. 0 155 201245154 275 (S)-3-{[6-(3-Ethyl-phenyl)-5-methoxy-α ratio 0--2-yl]-amino} -3-(2 - gas-phenyl)-propionic acid 437. 25 1. 08 LC11_2 8. 54 276 (S)-3-[(6-biphenyl-3-yl-5-decyloxyl~~_2-yl)-amino]-3-(2-a-phenyl)-prop Acid 471. 33 1. 21 LC11_2 2. 16 277 (S)-3-{[6-(4-Ethyl-phenyl)-5-methoxyl ratio 0-but-2-yl]-amino}-3-(2-fluoro-benzene Base)-propionic acid 437. 27 1. 07 LC11_2 &gt;10. 0 278 (S)-3-{[6-(2,4-Difluoro-phenyl)-5-methoxyl-° ratio -2-amino]-amino}-3-(2 - rat -Phenyl)-propionic acid 431. 24 1. 12 LC11_2 0. 1201 279 (S)-3-{[6-(3,5-Difluoro-phenyl)-5-decyloxy-° ratio. Ding-2-cutting base]-amino}-3-(2-fluoro-phenyl)-propionic acid 431. 21 1. 15 LC11_2 3. 85 280 (S)-3-{[6-(3,4-Diphenyl)-5-decyloxy-. ratio. -2--2-裁基]-Amino}-3-(2-disorgano-phenyl)-propionic acid 431. 23 1. 14 LC11_2 3. 12 156 201245154 281 (S)-3-{[6-(2,3-Dichloro-phenyl)-5-methoxy-0 to 0-but-2-yl]-amino}-3-( 2-chaotic-local V-propionic acid 463. 16 1. 15 LC11_2 0. 114 282 (S)-3-(2-Fluoro-phenyl)-3-[(3-decyloxy-[2,4']bipyridyl-6-carbonyl)-amino]-propionic acid 396. 21 0. 84 LC11_2 &gt;10. 0 283 (S)-3-{[6-(5-Cyano-thiophen-2-yl)-5-methoxypyridin-2-carboyl]-amino}-gas-propenyl)- Propionic acid 426. 15 1. 1 LC11_2 5. 4 284 (S)-3-(2-Fluorophenyl)-3-[(3-decyloxy-[2,3·]bipyridyl-6-yl)-amino]-diacid 396 . 22 0. 88 LC11_2 &gt;10. 0 285 (S)-3-{[6-(2,3-Difluoro-phenyl)-5-decyloxy-0 to 0-but-2-yl]-amino}-3-(2- Gas-phenyl)-propionic acid 431. 25 1. 11 LC11__2 0. 234 286 (S)-3-{[6-(2,5-Difluoro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-(2-fluoro-phenyl )-propionic acid 431. 23 1. 11 LC11_2 0. 171 287 (S)-3-{[6-(3,5-Dimercapto-isoxazol-4-yl)-5-methoxy- 414. 25 1. 04 LC11_2 0. 645 157 201245154 ° ratio σ -2--2-yl]-amino}-3-(2- gas-phenyl)-propionic acid 288 (S)-3-{[6-(4-fluoro-2-methyl Benzyl-phenyl)-5-decyloxypyridin-2-carboyl]-amino}-3-(2-fluoro-phenyl)-propionic acid 427. 27 1. 13 LC11_2 0. 394 289 (S)-3-{[6-(2,3-Dimercapto-phenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-(2-fluoro-benzene Base)-propionic acid 423. 29 1. 14 LC11_2 0. 0528 290 (S)-3-{[6-(3-Fluoro-4-indolyl-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-(2-fluoro -Phenyl)-propionic acid 427. 26 1. 16 LC11_2 3. 81 291 (S)-3-{[6-(2,4-Dimercaptophenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-(2-fluoro-benzene Base)-propionic acid 423. 29 1. 15 LC11_2 4. 02 292 (S)-3-{[6-(4-Fluoro-3-indolyl-phenyl)-5-decyloxypyridin-2-carboyl]-amino}-3-(2- Fluoro-phenyl)-propionic acid 427. 25 1. 16 LC11_2 4. 13 293 (S)-3-(2-Fluoro-phenyl)-3-[(5-decyloxy-6-°-0--5-yl--0 ratio 397. 2 0. 96 LC11_2 &gt;10. 0 158 201245154 bite-2-domain)-amino]-propionic acid 294 (S)-3-[(6'-fluoro-3-methoxy-[2,31]linked σ ratio σ定基-6- Rotamyl)-amino]-3-(2-fluoro-phenyl)-propionic acid 414. 22 1. 06 LC11_2 &gt;10. 0 295 (S)-3-{[6-(2-Didecylaminoindenyl-phenyl)-5-methoxy-indolyl-2-yl]-amino}-3- (2-murine-phenyl)-propionic acid 464. 38 1. 02 LC11_2 4. 51 296 (S)-3-[(3,2'-Dimethoxy-[2,3']bipyridyl-6-carbonyl)-amino]-3-(2·fluoro-phenyl)- Propionic acid 426. 26 1. 04 LC11_2 0. 756 297 (S)-3-{[6-(5-Gas-2-indolyl-phenyl)-5-methoxypyridin-2-yl]-amino}-3-(2-fluoro -Phenyl)-propionic acid 427. 25 1. 13 LC11_2 0. 475 298 (S)-3-{[6-(4-Fluoro-2-decyloxy-phenyl)-5-methoxypyridin-2-phenyl]-amino}-3-(2- Fluorine-phenyl)-propionic acid 443. 26 1. 1 LC11_2 0. 389 299 (S)-3-{[6-(4-Chloro-2-methoxy-phenyl)-5-decyloxy-n-bipyridine 459. 24 1. 14 LC11_2 1. 83 159 201245154 • 2-carbonyl]-aminopyr-3-(2-fluoro-phenyl)-propionic acid 300 (S)-3-{[6-(5·Ga-2-decyloxy-phenyl) -5-decyloxy-n-pyridin-2-yl-amino]-amino} _3-(2· defeat-phenyl)·propionic acid 459. 25 1. 13 LC11_2 4. 11 301 (S)-3-{[6-(5-Gas-2-methoxy-phenyl)-5-methoxy-η ratio -2-carbonyl]-amino}-3-(2 -Fluoro-phenyl)-propionic acid 443. 26 1. 1 LC11_2 0. 0737 302 (S)-3-(2-Fluoro-phenyl)-3-{[5-decyloxy-6-(1-indolyl-1H-indole-5-yl)-pyridine-2-carbonyl ]-Aminopropionic acid 448. 3 1. 12 LC11_2 &gt;10. 0 303 (S)-3-{[6-(2,5-Dimethoxy-indenyl)-5-methoxy ratio. Ding-2-carbonyl]-amino}-3-(2-fluoro-phenyl). )-propionic acid 455. 29 1. 08 LC11-2 &gt;10. 0 304 (S)-3-(2-phenyl)-3 - {[6_(2·fluoro-5-trifluoromethyl-phenyl)-5-decyloxyl-bito-2-carboyl] -amino}-propionic acid 481. 23 1. 16 LC11_2 3. 99 305 (S)-3-(2-|1-phenyl)-3-{[5-decyloxy-6-(5-fluorenyl-furan 399. 23 1. 09 LC11_2 &gt;10. 0 160 201245154 -2-base)-σ ratio. Benz-2-carbo]-amino}-propionic acid 306 (S)-3-(2-fluoro-phenyl)-3-{[5_ methoxy-6-(1-mercapto-1H-pyridyl) Azole-4-yl)-. Bipyridine-2-carbonyl]-amino}-propionic acid 399. 22 0. 99 LC11_2 &gt;10. 0 307 (S)-3-{[6-(2-Fluoro-5-methoxy-phenyl)-5-decyloxy-° ratio.定-2-征基]-Amino}-3-(2-disorgano-phenyl)-propionic acid 443. 26 1. 1 LC11_2 2. 92 308 (S)-3-{[6-(5-Tertibutyl-2-methoxy-phenyl)-5-decyloxy-° ratio α定-2 -Iryyl]-amino} -3-(2-fluoro-phenyl)-propionic acid 481. 44 1. 2 LC11_2 &gt;10. 0 309 (S)-3-(2-Gas-phenyl)-3_ {[6-(2-fluoro-4-trifluoromethyl-phenyl)-5-methoxypyridin-2-carboxol Base]_amino group}_propionic acid 481. 25 1. 17 LC11_2 &gt;10. 0 310 (S)-3-{[6-(2-Fluoro-5-methyl-phenyl)-5-decyloxypyridin-2-carboyl]t-aminopurin 3-(2-fluoro -Phenyl)-propionic acid 427. 26 1. 13 LC11_2 0. 262 311 (S)-3-{[6-(3-Chloro-2-methyl-phenyl)-5-decyloxy-acridine-2- 443. 25 1. 16 LC11_2 0. 2019 161 201245154 benzyl]-amino}-3-(2-f-phenyl)-propionic acid 312 (S)-3-{[6-(5-Ga-2-donyl-phenyl)-5-曱oxy-σ ratio 0-but-2-yl]-amino}-3-(2-fluoro-phenyl)-propionic acid 447. 19 1. 14 LC11_2 0. 481 313 (S)-3-{[6-(4-Ga-3-don-phenyl)-5-methoxy-° ratio -2--2-yl]-amino}'-3-( 2-fluoro-phenyl)-propionic acid 447. 21 1. 18 LC11_2 3. 55 314 (S)-3-[(2'-Chloro-3-indolyl-5-indolyl-[2,3']bipyridyl-6-decyl)-amino]-3-( 2 - gas _ phenyl) - propionic acid 444. 23 1. 06 LC11_2 &gt;10. 0 315 (S)-3-{[6-(3-Gas-5-fluorenyl-phenyl)-5-decyloxypyridin-2-carboyl]-amino}-3-(2- Deficient-phenyl)-propionic acid 443. 25 1. 19 LC11_2 &gt;10. 0 316 (S)-3-(2-Fluoro-phenyl)-3-( {5-decyloxy-6-[3-(5-fluorenyl-[1,3,4] oxadiazole-2 -yl)-phenyl]-° ratio. -2 -alkyl}-amino)-propionic acid 477. 31 1. 06 LC11_2 &gt;10. 0 162 201245154 317 (S)-3-(2-Fluoro-phenyl)-3-{[5-decyloxy-6-(l,3,5-tridecyl-1H-吼0坐-4- Base) - 0 to 0 - -2- carbene - amino} _ propionic acid 427. 27 0. 99 LC11_2 &gt;10. 0 318 (S)-3-(2-phenyl)-3 - {[5-methoxy-6-(1-indolyl-1H-indolyl-6-yl)-ntbα--24-carbon ]_ Amino}-propionic acid 448. 3 1. 13 LC11_2 &gt;10. 0 319 (S)-3-{[6-(4-Chloro-3-indolyl-phenyl)-5-methoxy-σ ratio 0--2-yl]-amino}-3- (2 - gas _ phenyl) - propionic acid 459. 22 1. 16 LC11_2 &gt;10. 0 320 (S)-3-{[6-(3-chloro-2-fluoro-phenyl)-5-methoxy-0-buty-2-yl]-amino}-3-(2- Gas-phenyl)-propionic acid 447. 22 1. 14 LC11_2 0. 0484 321 (S)-3-(2-|l-phenyl)-3-[(3-indotyl-2'-isofolin-4-yl-4-yl-[2,4·]bipyridyl- 6-carbonyl)-amino]-propionic acid 481. 33 0. 91 LC11_2 &gt;10. 0 322 (S)-3-(2_l-phenyl)-3-{[5-decyloxy-6-(2-indolyl-furan-3-yl)-pyrene-Bite-2-indole carbon-based] _Amino}-propionic acid 399. 21 1. 11 LC11_2 0. 0813 163 201245154 323 (S)-3-{[6-(2-Chloro-5-methyl-benyl)-5-decyloxy ratio. -2_carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid 443. 18 1. 14 LC11_2 2. 31 324 (S)-3-{[6-(2-Gas-3-1-phenyl)-5-methoxy-0 ratio. Ding-2-carboyl]-amino}^-3-(2- gas-phenyl)-propionic acid 447. twenty one. 12 LC11_2 1. 266 325 (S)-3-{[6-(4-Cyano-2-fluoro-phenyl)-5-methoxypyridin-2-yl]-amino}-3-(2-dun -Phenyl)-propionic acid 438. 23 1. 08 LC112 3. 58 326 (S)-3-(2-Fluoro-phenyl)-3-({6-[3-(3-hydroxy-oxetan-3-yl)-phenyl]-5-oxime The basal-β ratio is β-restricted to 2-remediate}-amino)-propionic acid 467. 29 1 LC11_2 8. 46 327 (S)-3-(2-|l·Phenyl)-3-({6-[3-(1-hydroxy-1-indolyl-ethyl)-phenyl]-5-methoxy _ 0 than ^-2-^ carbon-based oxime-amino)-propionic acid 453. 32 1. 07 LC11_2 7. 32 328 (S)-3-{[6-(2-Ga-3-indolyl-phenyl)-5-decyloxy^pyridin-2- 443. 24 1. 14 LC11_2 0. 1192 164 201245154 benzyl]-amino}-3-(2-murine-benyl)-propionic acid 329 (S)-3 &lt;2-Chloro-phenyl)-3-{[5-indole-based-6-(3-dioxamethyl-phenyl)_α ratio α-di-2-chloro]-amino}-propionic acid 479. 11 1. 21 LC11_3 3. 74 330 (S)-3-(2-Chloro-phenyl)-3-[(5-methoxy-6-phenylpyridin-2-carbonyl)-amino]-propionic acid 411. 12 1. 14 LC11_3 0. 0751 331 (S)-3-(2-gastriphenyl)-3_ {[6-(2,4-di-phenyl)-5-anthracene-° ratio bite-2-green base]- Amino}-propionic acid 479. 05 1. 21 LC11_3 0. 589 332 (S)-3-{[6-(3-Chloro-4-fluoro-phenyl)-5-decyloxy-0 ratio. Ding-2-carboyl]-amino}'-3-(2-a-phenyl)-propionic acid 463. 07 1. 2 LC11_3 5. 24 333 (S)-3-(2-Gas-phenyl)-3. {[6-(4-Fluoro-phenyl)-5-fluorenyl--. Ratio of 11 to 2-isyl]-amino}_propionic acid 429. 12 1. 16 LC11_3 0. 909 334 (8)-3-(2-Gas-phenyl)-3· {[6-(4-Gas-phenyl)-5-decyloxy-α ratio sigma-2-indenyl]-amine Base}- 445. 09 1. 2 LC11_3 1. 81 165 201245154 Propionic acid 335 (S)-3-(2-chloro-phenyl)-3-{[5-methoxy-6-(4-methoxy-phenyl)-** ratio. Ding-2-yl]-amino}-propionic acid 441. 13 1. 14 LC11_3 2. 25 336 (S)-3-(2-Gas-phenyl)-3-[(5-decyloxy-6-p-tolylpyridyl-2-yl)-amino]-propionic acid 425. 14 1. 18 LC11_3 3. 13 337 (S)-3-(2-Gas-phenyl)-3-{[5-methoxy-6-(4-trifluoromethyl-phenyl)-° ratio bite - 2 prison base]- Amino}-propionic acid 479. 11 1. 21 LC11_3 9. 5 338 (S)-3-(2-Gas-phenyl)-3-[(5-decyloxy-6-o-indoleylpyrene-β-but-2-yl)-amino]-propionic acid 425. 14 1. 15 LC11_3 &gt;10. 0 339 (8)-3-(2-Gas-phenyl)-3-{[5_ 曱oxy-6-(3-methoxy-phenyl)-° ratio °-2-enyl]- Amino}-propionic acid 441. 13 1. 14 LC11_3 2. 78 340 (S)-3-(2-Gas-phenyl)-3-{[6-(3-chloro-phenyl)-5-methoxyl-°°°-2-chloro]-amine Base} _ propionic acid 445. 09 1. 19 LC11_3 1. 51 166 201245154 341 (S)-3-(2-Gas-phenyl)-3-{[5-(3-fluoro-phenyl)-6-methoxy-° ratio σ-3-yl] -amino} _ propionic acid 429. 22 1. 13 LC11_2 9. 86 342 (S)-3-{[6-Methoxy-5-(4-trifluoromethyl-phenyl)-pyridin-3-carbonyl]-amino}-3-o-tolyl- Propionic acid 459. 27 1. 18 LC11_2 &gt;10. 0 343 (S)-3-(2-Gas-phenyl)-3-{[6-decyloxy-5-(3-difluoroindolyl-yl)-° ratio β--3-green Amino}-propionic acid 479. 22 1. 18 LC11_2 &gt;10. 0 344 (S)-3-(2-Chloro-phenyl)-3-[(6-indole-5-phenyl-° than 唆-3 _ Rotamyl)-amino]-propionic acid 411 . 23 1. 12 LC11_2 3. 49 345 (S)-3-{[5-(3-Chloro-4-fluoro-phenyl)-6-decyloxy-π ratio sigma-3-carboyl]-amino}_3-(2 -Chloro-phenyl)-propionic acid 463. 16 1. 17 LC11_2 &gt;10. 0 346 (S)-3-(2-Chloro-phenyl)-3_ {[5-(4-1-phenyl)-6-fluorenyl-° ratio. Ding-3 -monoyl]-amino}_propionic acid 429. twenty one. 13 LC11_2 8. 26 167 201245154 347 (S)-3-{[5-decyloxy-6-(3-trifluorodecyl-phenyl)_. Bipyridin-2-carboyl]-amino}-3-o-indolyl-propionic acid 459. 08 1. 19 LC11_2 0. 981 348 (S)-3-{[6-(2,4-Di-(yl)phenyl)-5-decyloxy-0-pyrene-2-yl]-amino}_3_o-indene Base _ propionic acid 459. 01 1. 19 LC11_2 0. 161 349 (S)-3-{[6-(3-Chloro-4-octyl-phenyl)-5-methoxy-0 to 0-but-2-carboyl]-amino}}_3- -曱Phenyl _ propionic acid 443. 03 1. 19 LC11_2 1. 458 350 (S)-3-{[6-(4-Fluoro-phenyl)-5-decyloxy-° ratio _2--yl]-amino}-3-o-indolephenyl- Propionic acid 409. 08 1. 14 LC11_2 0. 267 351 (S)-3-{[6-(4-Gas-phenyl)-5-methoxyl-° ratio _2--yl]-amino}-3-o-tolyl-propyl Acid 425. 04 1. 18 LC11_2 0. 501 352 (S)-3-[(5-decyloxy-6-p-nonylphenyl-acridin-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid 405. 12 1. 17 LC11_2 0. 586 353 (S)-3-{[5-decyloxy-6-(4-trifluoromethyl-phenyl)-pyridin-2-carboyl]-amino}-3-o-indole Benzene 459. 08 1. 19 LC11_2 &gt;10. 0 201245154 BASE-propionic acid 354 (S)_3 - {[6-(3-chloro-phenyl)-5_ decyloxy-0 butyl-2-yl]-amino}-3-o- fluorene Base-propionic acid 425. 05 1. 18 LC11_2 0. 53 355 (S)-3-{[5-decyloxy-6-(2-decyloxy-phenyl)-σ ratio 0-but-2-yl]-amino}-3-o-indenylbenzene Base-propionic acid 421. 13 1. 1 LC11_2 0. 0833 356 (S)-3-[(5-decyloxy-6-m-p-phenylene-° ratio -2 domain)-amino]_3_o-indolephenyl-propionic acid 405. 09 1. 16 LC11_2 0. 152 357 (S)-3 - {[6-(2-Chloro-styl)-5_ decyloxy ratio. -2--2-Mercapto]-amino}-3-o-indolephenyl-propionic acid 425. 06 1. 13 LC11_2 0. 223 358 (S)-3-{[6-(4-Tertibutyl-phenyl)-5-decyloxypyridin-2-yl]-amino}_3_o-indolephenyl-propane Acid 447. 19 1. 25 LC11_2 &gt;10. 0 359 (S)-3-{[6-(3-Cyano-phenyl)-5-indole--π ratio °-2-carboyl]-amino}-3-o-indene benzene Base-propionic acid 416. 1 1. 11 LC11_2 4. 49 360 (S)-3-{[6-(3-Ethyl-Benzene 433. 13 1. 1 LC11_2 2. 42 169 201245154 base)-5-decyloxy-.约定定-2-罗炭基]•Amino}_3_o-tolyl_propionic acid 361 (S)-3-{[6-(4-Ethyl-phenyl)-5-methoxy -0 ratio.定-2-裁基]-Amino}-3-o-indolephenyl-propionic acid 433. 12 1. 09 LC11_2 9. 24 362 (S)-3-{[6-(3,5-Difluoro-phenyl)-5-decyloxy ratio. -2--2-Methoxy]-amino}-3-o-tolyl-propionic acid 427. 08 1. 16 LC11_2 1. 43 363 (S)-3-{[6-(3,4-Difluoro-phenyl)-5-decyloxyl 0-but-2-carboyl]-amino}-3-o-tolyl _ Propionic acid 427. 11 1. 16 LC11_2 0. 258 364 (S)-3-{[6-(5-Ethyl-thiophen-2-yl)-5.methoxy-. Than -2-yl]-amino}-3-o-indole benzyl-propionic acid 439. 09 1. 1 LC11_2 9. 25 365 (S)-3-[(3-decyloxy _[2,4']. σ 定 -6-6-yl)-amino]-3-o-indole phenyl-propionic acid 392. 13 0. 87 LC11_2 5. 45 366 (3)-3-{[6-(2,5-Bismo-phenyl)-5-methoxy-0 ratio.定-2- Several 427. 09 1. 13 LC11_2 0. 121 170 201245154 】]amino}}-3_o-indole phenyl-propionic acid 367 (S)-3-{[6-(2,5-dichloro-phenyl)-5-decyloxy- π is 0 爹-2-爹 carbon-based]-amino}·_3-o-tolyl-propionic acid 459. 01 1. 18 LC11_2 0. 385 368 (S)-3-{[6-(3,5-Dimercapto-isoxazol-4-yl)-5-decyloxy- ° ratio σ定-2-yl]-amino} -3_ o-tolyl-propionic acid 410. 24 4 LC2 0. 1873 369 (S)-3-{[6-(2,3-Dimercapto-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-o-indolephenyl - Propionic acid 419. 14 1. 16 LC11_2 0. 1318 370 (S)-3-{[6-(3-|i-4-indolyl-phenyl)-5-decyloxypyridin-2-yl-yl]-amino}-3-o- Phenyl phenyl-propionic acid 423. 11 1. 18 LC11_2 1. 585 371 (S)-3-{[6-(2,4-Dimercapto-phenyl)-5-methoxy-. Ratio ° -2 carbonyl]-amino}-3-o-phenylene-propionic acid 419. 16 1. 17 LC11_2 0. 457 372 (S)-3-[(5-decyloxy-6-pyrimidin-5-yl-atb °--2-yl)-amine 393. 11 0. 98 LC11_2 8. 88 171 201245154 yl]-3-o-tolyl-propionic acid 373 (S)-3-[(6'-fluoro-3-indolyl-[2,3']-linked.pyridyl-6-carbonyl )-Amino]-3-o-indolephenyl-propionic acid 410. 1 1. 08 LC11_2 1. 6 374 (S)-3-{[6-(2-Didecylaminoindenyl-phenyl)-5-methoxy-0-sigma-2-yl]-amino} - 3 · o-Phenylphenyl-propionic acid 460. 12 1. 04 LC112 2. 48 . 375 (S)-3-{[6-(4-Fluoro-2-decyloxy-phenyl)-5-decyloxypyridin-2-reyl]-amino}-3-o-indenylbenzene Base-propionic acid 439. 13 1. 12 LC11_2 0. 216 376 (S)-3-{[5-methoxy-6-(5-methyl-αα-pentan-2-yl)-0 ratio. -2--2-Mercapto]-amino}-3-o-indole phenyl-propionic acid 395. 11 1. 11 LC11_2 6. 1 377 (S)-3-{[5-decyloxy-6-(diphenyl-1H-.bizozol-4-yl)-pyridin-2-reyl]-amino} -3 -ortho- 曱Phenyl-propionic acid 395. 13 1. 01 LC11_2 &gt;10. 0 378 (S)-3-{[6-(3-Chloro-5-fluorenyl-phenyl)-5-decyloxypyridin-2- 439. 1 1. 21 LC11_2 7. 49 172 201245154 Rotamyl]-amino}-3-o-tolyl-propionic acid 379 (S)-3-{[5-decyloxy-6-(1,3,5-tridecyl-lH -η-pyrazol-4-yl)-α ratio α-di-2-yl]-amino}-3-o-tolyl-propionic acid 421. 13 1 LC11_2 &gt;10. 0 380 (S)-3_{[5-methoxy-6-(1-indolyl-1H-indol-6-yl)-pyridin-2-yl]-amino}-3-o- Phenyl phenyl-propionic acid 444. 15 1. 15 LC11_2 5. 33 381 (S)-3-[(3-Methoxy-2'-, phenanthrene. lin-4-yl-[2,4']. Ratio. Defen-6-yl)-amino]- 3-o-tolyl-propionic acid 477. 16 0. 93 LC11_2 &gt;10. 0 382 (S)-3-{[6-(2-chloro-5-methyl-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-o-indolephenyl -propionic acid 439. 13 1. 16 LC11_2 0. 497 383 (S)-3-{[6-(2-Chloro-3-fluoro-phenyl)-5-decyloxy-D is 0-but-2-yl]-amino}-3-o- Phenyl phenyl-propionic acid 443. 06 1. 14 LC11_2 1. 635 384 (S)-3-({6-[3-(3-Pytyl-oxo-dip-3-yl)-phenyl]-5- 463. 15 1. 02 LC11_2 2. 39 173 201245154 methoxy-pyridine-2-carbonyl}-amino)-3-o-tolyl-propionic acid 385 (S)-3-({6-[3-(l-hydroxy-1-methyl) -Ethyl)-phenyl]-5-decyloxy _ ° than bite-2 - prison base}-amino)-3-o-tolyl-propionic acid 449. 17 1. 08 LC11_2 1. 15 386 (S)-3-(2-Chloro-phenyl)-3-{[5-(4-Gas-phenyl)-6-methoxy-π ratio 11-decyl]-indenyl]-amine Base} _ propionic acid 445. 17 1. 17 LC11_2 10. 4 387 (S)-3-(2-Gas-phenyl)-3-{[6-methoxy-5-(4-methoxy-phenyl)-° ratio ° -1 -yl] -amino}-propionic acid 441. 24 1. 11 LC11_2 9. 43 388 (S)-3-(2-Chloro-phenyl)-3·[(6· 曱oxy-5-p-fluorenylphenyl to 17--3-yl)-amino]-propionic acid 425. 24 1. 15 LC11_2 7. 12 389 (S)-3-(2-Gas-phenyl)-3-{[6-decyloxy-5-(4-trifluoromethyl-phenyl)- ta-dec-3-yl] -amino}-propionic acid 479. 21 1. 18 LC11_2 &gt;10. 0 390 (S)-3-(2-Gas-phenyl)-3-[(6-decyloxy-5·•o-indolephenyl-indole. Ding·^-:^carbyl)-amino group ]-propionic acid 425. 25 1. 13 LC11_2 0. 702 174 201245154 391 (S)-3-(2-Chloro-phenyl)-3-{[6-decyloxy-5-(3-methoxy-phenyl)-° ratio -3-carbon group ]-Amino}-propionic acid 441. 24 1. 12 LC11_2 10. 6 392 (S)-3-(2-Chloro-phenyl-p-phenyl)-6_ 曱 基-〇 σ σ -3- -3- wei wei]-amine --propionic acid 445. twenty one. 16 LC11_2 10. 3 393 (S)-3-(2-Chloro-phenyl)·3-[(6·曱乳-5-Qin-2-yl-° ratio. Carbon-based)-Amino]-propionic acid 461 . 25 1. 18 LC11_2 &gt;10. 0 394 (S)-3-(2-Chloro-phenyl)-3-{[6-decyloxy-5-(2-decyloxy-phenyl)-α ratio bite-3-indole carbon base] -amino}-propionic acid 441. 25 1. 1 LC11_2 3. 76 395 (S)-3-(2-Chloro-phenyl)-3-[(6-曱-lactyl-5-m-decyl-based-sigma ratio)-amino]-propyl Acid 425. 24 1. 15 LC11_2 6. 57 396 (S)-3-{[5-(4-Terbutyl-phenyl)-6-decyloxypyridin-3-carboyl]-amino]-3-(2- gas· -Phenyl)-propionic acid 467. 31 1. 24 LC11_2 &gt;10. 0 397 (S)-3-(2-Chloro-phenyl)-3-{[5-(3-cyano-phenyl)-6-decyloxy 436. 23 1. 09 LC11_2 &gt;10. 0 175 201245154 • ° ° ° -3 -Werki]-amino}-propionic acid 398 (S)-3-(2-chloro-phenyl)-3-{[5-(4-ranyl-benzene Base)-6-decyloxy-° ratio.定-3 - prison base]-amino hydrazine-propionic acid 436. 23 1. 09 LC11_2 &gt;10. 0 399 (S)-3-{[5-(3-Ethyl-phenyl)-6-fluorenyloxy-° ratio -3--3-梦炭基]-amino}_3-(2 -虱-Phenyl)-propionic acid 453. 25 1. 08 LC11_2 &gt;10. 0 400 (S)-3-[(5-biphenyl-3-yl-6-oxime-° ratio)-amino]-3-(2- gas-phenyl) - Propionic acid 487. 27 1. 21 LC11_2 &gt;10. 0 401 (S)-3-{[5-(4-Ethyl-phenyl)-6-fluorenyloxy-^ is a bit of ^-mute carbon-]-amino}_3-(2-chloro-benzene Base)-propionic acid 453. 25 1. 08 LC11_2 &gt;10. 0 402 (S)-3-(2-chloro-phenyl)-3_ {[5-(3,5-difluoro-phenyl)-6-decyloxyl sigma-3-reyl]-amine Base}-propionic acid 447. twenty one. 15 LC11_2 &gt;10. 0 403 (S)-3-(2-Gas-phenyl)-3-{[5-(3,4-difluoro-phenyl)-6-fluorenyl--. ratio.定-3-戴基]-amine 447. twenty one. 14 LC11_2 &gt;10. 0 176 201245154 base}-propionic acid 404 (S)-3-(2_chloro-phenyl)-3_ {[5-(4-fluoro-2-methyl-phenyl)-6-decyloxy-° ratio °定-3-爹Carbonyl]-amino}-propionic acid 443. 26 1. 14 LC11_2 7. 14 405 (S)-3-[(6-decyloxy-5-phenyl-fluorenyl-3-amino)-amino]-3-o-indole-propionic acid 391. 28 1. 12 LC11_2 3. 9 406 (S)-3-{[5-(3-Chloro-4-fluoro-phenyl)-6-decyloxy-0 to 0--3-yl]-amino}_3_---anthracene Phenyl-propionic acid 443. 22 1. 17 LC11_2 10 407 (S)-3-{[5-(4-|l-phenyl)-6-decyloxy&quot;.唆-]-Methoxy]-amino}-3-o-tolyl-propionic acid 409. 24 1. 13 LC11_2 4. 39 408 (S)-3-{[5-(4-Chloro-phenyl)-6-fluorenyl-α ratio 0--3-carbyl]-amino}-3-o-indole - Propionic acid 425. 22 1. 17 LC11_2 5. 73 409 (S)-3-{[6-decyloxy-5-(4-indole-phenyl)-π ratio -3-carbonyl]-amino}_3_o-indole phenyl Propionic acid 421. 3 1. 11 LC11_2 9. 04 410 (S)-3-[(6-decyloxy-5-p-405. 26 1. 15 LC11_2 5. 38 177 201245154 Tolyl-° ratio. Benz-3-yl)-amino]-3-o-indolephenyl-propionic acid 411 (S)-3-[(6-decyloxy-5-o-indolephenyl-pyridine-3-carbonyl) )-Amino]-3-o-indolephenyl-propionic acid 405. 27 1. 13 LC11_2 1,186 412 (S)-3-{[6-methoxy-5-(3-decyloxy-phenyl)_° ratio °-3-carboyl]-amino}-3- -tolyl-propionic acid 421. 27 1. 12 LC11_2 8. 36 413 (S)-3-{[5-(3-Gas-phenyl)-6-methoxy-α than sigma-3-yl]-amino}-3-o-indolephenyl- Propionic acid 425. 21 1. 16 LC112 6. 24 414 (S)-3-{[5-(3-Fluoro-phenyl)-6-methoxyl-butyl-3-amino]-amino}-3-o-indole-propionic acid 409 . 22 1. 13 LC11_2 8. 07 415 (S)-3-[(6-decyloxy-5-naphthalen-2-yl-indole-3-yl)-amino]-3-o-tolyl-propionic acid 441. 33 1. 18 LC11_2 &gt;10. 0 416 (S)-3-{[6-decyloxy-5-(2-methoxy-phenyl)-pyridinium-3-carbonyl]amino}-3-o-indolephenyl- propyl Acid 421. 31 1. 1 LC11_2 3. 42 417 (S)-3-[(6-decyloxy-5-m-tolyl-n ratio. -3-yl)-amine 405. 28 1. 15 LC11_2 4. 86 178 201245154 yl]-3-o-indole phenyl-propionic acid 418 (S)-3-{[5-(2-fluoro-phenyl)-6-decyloxy-pyridine-3-carbonyl]-amino }-3-o-indole phenyl-propionic acid 409. 23 1. 11 LC11_2 1. 083 419 (S)-3-{[5-(4-Terbutyl-phenyl)-6-methoxypyridin-3-carbonyl]-amino}-3-o-indolephenyl-propane Acid 447. 38 1. 24 LC11_2 &gt;10. 0 420 (S)-3-{[5-(3-Cyano-phenyl)-6-fluorenyl]-amino}-3-o-tolyl-propionic acid 416. 25 1. 09 LC11_2 &gt;10. 0 421 (S)-3-{[5-(4-Cyano-phenyl)-6-fluorenyl-indenyl 17--3-carboyl]-amino}·-3-o-indolylbenzene Base _ propionic acid 416. 29 1. 09 LC11_2 10. 4 422 (S)-3-{[5-(3-Ethyl-phenyl)-6-indole-based-bite-carbo]-amino}-3-o-tolyl-propionic acid 433. 28 1. 08 LC11_2 &gt;10. 0 423 (S)-3-[(5-Biphenyl-3-yl-6-decyloxy-pyridine-3-carbonyl)-amino]-3-o-indolephenyl-propionic acid 467. 34 1. 21 LC11_2 &gt;10. 0 179 201245154 424 (S)-3-{[5-(4-Ethyl-phenyl)-6-methoxyl-° ratio -3-yl]-amino}-3-o-曱Phenyl _ propionic acid 433. 28 1. 08 LC11_2 &gt;10. 0 425 (S)-3-{[5-(3,4-Difluoro-phenyl)-6-decyloxy ratio. -3-amino]-amino}-3-o-indolephenyl-propionic acid 427. 25 1. 15 LC11_2 8. 84 426 (S)-3-(2-Gas-phenyl)-3-{[6-(3-1-phenyl)-5-fluorenyl-° ratio. Ding-2 -monoyl]-amino}-propionic acid 429. 12 1. 16 LC11_3 1. 54 427 (S)-3-(2-Chloro-phenyl)-3-[(5-decyloxy-6-tea-2-yl-. 约定-2--phenyl)-amino]- Propionic acid 461. 14 1. 21 LC11_3 7. 11 428 (S)-3-(2-Gas-phenyl)-3-{[5-decyloxy-6-(2-methoxy-phenyl)-σ ratio α定-2- 基基] -Aminopropionic acid 441. 14 1. 11 LC11_3 0. 1161 429 (S)-3-(2-Gas-phenyl)-3-[(5-decyloxy-6-m-p-phenyl ratio: determin-2-domain)-amino]-propionic acid 425. 14 1. 18 LC11_3 0. 335 430 (S)-3-(2-Gas-phenyl)-3-{[6-(2-Gas-phenyl)-5-decyloxy- 445. 09 1. 14 LC11_3 0. 147 180 201245154 ° ratio σ··2 -yl]-amino]•-propionic acid 431 (S)-3-(2-nitro-phenyl)-3-{[6_(2-fluoro-phenyl) -5-decyloxy _ 0 ratio. Ding-2-chloro]-amino}-propionic acid 429. 11 1. 13 LC11_3 0. 132 432 (S)-3-{[6-(4-Tertibutyl-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-(2- gas-benzene Base)-propionic acid 467. 18 1. 26 LC11_3 &gt;10. 0 433 (S)-3-(2- gas-phenyl)-3-{[6_(3-cyano-phenyl)-5-methoxy-° ratio 11--2-yl]-amine Base}-propionic acid 436. 12 1. 12 LC11_3 8. 26 434 (S)-3-(2-Gas-phenyl)-3-{[6_(4-cyano-phenyl)-5-decyloxyl sigma-2-yl]-amino} - Propionic acid 436. 12 1. 12 LC11_3 &gt;10. 0 435 (S)-3-{[6-(3-Ethyl-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}_3-(2-a-phenyl)- Propionic acid 453. 13 1. 11 LC11_3 4. 2 436 (S)-3-[(6-Biphenyl-3-yl-5-decyloxy-.-Bite----yl)-amine 487. 16 1. 24 LC11_3 2. 97 181 201245154 ρ-^---yl]-3-(2-Ga-phenyl)-propionic acid _ 437 (S)-3-{[6-(4-Ethyl-phenyl)-5- Methoxy- acridine-2-carbonyl]-amino}-3-(2-chloro-phenyl)-propionic acid 453. 13 1. 1 LC11_3 &gt;10. 0 438 (3)-3-(2-Gas-phenyl)-3_ {[6-(2,4-di-phenyl)-5-decyloxy-pyridine-2-carbonyl]-amino} • Propionic acid 447. 19 1. 13 LC11_2 0. 0491 439 (S)-3-(2-Gas-phenyl)-3-{[6-(3,5-difluorophenyl)-5-decyloxy-pyridine-2-carbonyl]-amino} - Propionic acid 447. 11 1. 18 LC11_3 2. 39 440 (S)-3-(2-Gas-phenyl)_3_ {[6-(3,4-difluoro-phenyl)_5_decyloxypyridine-2-carbonyl]-amino}•propionic acid 447. 11 1. 17 LC11_3 1. 96 441 (S)-3-(2-Gas-phenyl)_3· {[6-(2,3-Dichloro-phenyl)_5-decyloxy·pyridine-2-carbonyl]•Amino}- Propionic acid 479. 05 1. 18 LC11_3 0. 2352 442 (S)-3-{[6-(5-Ethyl-thiophene-2-yl)-5-oxime-base. Contains 459. 09 --- 1. 11 LC11_3 &gt;10. 0 ------1 182 201245154 -2-Rebel]-Amino}^-3-(2-^-phenyl)-propionic acid 443 (S)-3-(2-Chloro-phenyl) -3-[(3-decyloxy-[2,4']biacridinyl-6-yl)-amino]-propionic acid 412. 12 0. 86 LC11_3 8. 04 444 (S)-3-(2-Chloro-phenyl)-3-[(3·methoxy-[2,3′]-bipyridyl 6-yl)-amino]-propionic acid 412. 12 0. 91 LC11_3 10. 1 445 (S)-3-(2-Chloro-phenyl)-3 - {[6-(2,3-di-phenyl)-5-indole--ntb β-dec-2-" ]-Amino} _ Propionic acid 447. 11 1. 14 LC11_3 0. 1505 446 (S)-3-(2-Chloro-phenyl)-3-{[6-(2,5-difluoro-phenyl)-5-indolyl-. Than bite 2 - luki]-amino} _ propionic acid 447. 1 1. 14 LC11_3 0. 0571 447 (S)-3-(2-murine-phenyl)-3_ {[6_(4-fluoro-2-indolyl-phenyl)-5-indoleyl-ntb °定-2 - Yiji] -amino}-propionic acid 443. 13 1. 16 LC11_3 0. 1106 448 (8)-3-(2_Gas-phenyl)-3-{[6·(2,3-Dimercapto-phenyl)-5-hydrazyl-° ratio bite-2-yl ]-Amino}-propionic acid 439. 15 1. 17 LC11_3 0. 1393 183 201245154 449 (S)-3-(2-Chloro-phenyl)-3-{[6-(3-fluoro-4-methyl-phenyl)-5-methoxy-. Ratio π -2 -monoyl]-amino}-propionic acid 443. 13 1. 2 LC11_3 2. 016 450 (S)-3-(2-Gas-phenyl)-3-{[6-(2,4-dimethyl-phenyl)-5-methoxy-° ratio Base]-aminopropionic acid 439. 15 1. 18 LC11_3 1. 6 451 (S)-3-(2-Chloro-phenyl)-3-{[6-(4-fluoro-3-indolyl-phenyl)-5-methoxyl_° ratio °-2 Rebel]-amino}-propionic acid 443. 13 1. 19 LC11_3 3. 79 452 (S)-3-(2-Chloro-phenyl)-3-[(5-methoxy-6-0 crypt-5-yl-0 σ σ-2-yl)-amino group ]-propionic acid 413. 11 0. 99 LC113 &gt;10. 0 453 (S)-3-(2-Gas-phenyl)-3-[(6'-fluoro-3-indolyl_[2,3'] linked &quot;specific σ-based-6-yl) -amino]-propionic acid 430. 11 1. 09 LC11_3 6. 49 454 (S)-3-(2-Gas-phenyl)-3-{[6-(2-didecylaminoindenyl-phenyl)-5-methoxy-. Bipyridine-2-carbonyl]-aminopropionic acid 482. 3 1. 04 LC112 2. 5 184 201245154 455 (S)-3-(2-Chloro-phenyl)-3-[(3,2·-didecyloxy-[2,3]linked ratio σ定基·6-Lu-ji)- Amino]_propionic acid 442. 13 1. 07 LC11_3 0. 185 456 (S)-3-(2-Chloro-phenylfluoro-2-methyl-phenyl)-5-indole milyl-° ratio. -2-2 -Methoxy]-amino}-propionic acid 443. 13 1. 16 LC11_3 0. 1193 457 (S)-3-(2-Chloro-phenyl)-3-{[6-(4-fluoro-2-methoxy-phenyl)-5-indole-based-π ratio sigma-2 - Yiji]-amino}-propionic acid 459. 13 1. 13 LC11_3 0. 1072 458 (S)-3-{[6-(4-Chloro-2-methoxy-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-(2- Gas-phenyl)-propionic acid 475. 1 1. 17 LC11_3 0. 415 459 (S)-3-{[6-(5-Chloro-2-indolyl-phenyl)-5-decyloxypyridin-2-yl]-amino}-3-(2- Gas-phenyl)-propionic acid 475. 1 1. 16 LC11_3 1. 147 460 (S)-3-(2-Chloro-phenyl)-3 - {[6-(5-fluoro-2-indolyl-phenyl)-5-hydrazinyl-. Ratio of 17 to 2-alkyl]-amino}-propionic acid 459. 12 1. 12 LC11_3 0. 1073 ΰ 185 201245154 461 (S)-3-(2-Chloro-phenyl)-3-{[6-(2,5-dimethoxy-phenyl)-5-decyloxy-° ratio 0 -2-Rebel]-amino}·-propionic acid 471. 14 1. 11 LC11_3 8. 31 462 (S)-3-(2-Gas-phenyl)-3-{[6-(2-fluoro-5-trifluoromethyl-phenyl)-5-decyloxy-° ratio- 2-rebase]-amino} propionic acid 497. twenty one. 18 LC11_2 0. 597 463 (S)-3-(2-Gas-phenyl)-3-{[5-decyloxy-6-(5-fluorenyl-furan-2-yl)-° ratio ]-Aminopropionic acid 415. 15 1. 11 LC11_2 &gt;10. 0 464 (S)-3-{[5-methoxy-6-(2-disindolyl-phenyl)-° ratio. -2-2_ carbonyl]-amino}-3-o-tolyl-propionic acid 459. 1 1. 14 LC11_2 0. 0993 465 (S)-3-{[6-(4-Cyano-phenyl)-5-methyllacyl-0 ratio. Ding-2-carboyl]-amino}_3_o-indolephenyl-propionic acid 416. 1 1. 1 LC11_2 6. 8 466 (S)-3-{[6-(2,4-dioxa-phenyl)-5-decyloxy-0 ratio. Ding-2-carboyl]-amino}_3_o-indolephenyl-propionic acid 427. 09 1. 13 LC11_2 0. 0463 186 201245154 467 (S)-3-{[6-(4-Fluoro-2-indolyl-phenyl)-5-indole--------------------------------------- -曱Phenyl-propionic acid 423. 09 1. 14 LC11_2 0. 1768 468 (S)-3-[(3,2'-Dimethoxy-[2,3']biacridinyl-6-carbonyl)-amino]-3-o-indolephenyl-propionic acid 422. 12 1. 06 LC11_2 0. 347 469 (S)-3-[(2'_ chloro-3-indolyl-5'-indolyl-[2,3']-linked.pyridinyl-6-yl)-amino]-3 -o-tolyl-propionic acid 440. 1 1. 08 LC11_2 5. 63 470 (S)-3-[(3'_Fluoro-3-indolyl-[2,4'] Linkage Ordodyl-6-Rotyl)-Amino]-3-o-indolylbenzene Base _ propionic acid 410. 06 1. 06 LC11_2 0. 1182 471 (S)-3-({5-decyloxy-6-[3-(5-fluorenyl-[1,3,4]oxadiazol-2-yl)-phenyl]-° ratio bite -2 - _Carbonyl}-amino)-3-o-indolephenyl-propionic acid 473. 13 1. 07 LC11_2 4. 23 472 (S)-3-{[5-decyloxy-6-(2-indolyl-σf-amyl-3-ylbu)-amino-2-yl]-amino}-3-o- A 395. 04 1. 13 LC11_2 0. 096 187 201245154 Phenyl-propionic acid 473 (S)-3-{[6-(4-Cyano-2-fluoro-phenyl)-5-methoxy-acridin-2-yl]-amine }-3-o-indole phenyl-propionic acid 434. 13 1. 1 LC11_2 0. 288 474 (S)-3-(2- gas-phenyl)_3_ {[6-(2-fluoro-5-decyloxy-phenyl)-5-decyloxy-° ratio bite-2-green base ]-Amino} Propionic acid 459. 12 1. 13 LC113 0. 58 475 (S)-3-{[6-(5-Tert-butyl-2-methoxy-phenyl)-5-indolyl-. ratio. Ding-2 -anthracene]-amino}-3-(2-a-phenyl)-propionic acid 497. twenty one. 23 LC11_3 &gt;10. 0 476 (S)-3-(2-Gas-phenyl)-3-{[6-(2-Amino-5-methyl-phenyl)-5-methoxy_° than bite _2 - Base]-amino}-propionic acid 443. 13 1. 16 LC11_3 0. 3695 477 (S)-3-{[6-(3-Gas-2-indolyl-phenyl)-5-methoxy-acridin-2-carboyl]-amino}_3-(2- Nitro-phenyl)-propionic acid 459. 1 1. 19 LC11_3 0. 11 478 (S)-3-(2-Gas-phenyl)-3-{[6-(3-fluoro-2-indolyl-phenyl)-5-oxime 443. 13 1. 16 LC113 0. 192 201245154 oxy-indole-2-yl]-amino}-propionic acid 479 (S)-3-{[6-(5-chloro-2- gas-phenyl)-5-decyloxy -° ratio 歹-2-歹 carbon-]-amino}-3-(2- gas-phenyl)-propionic acid 463. 08 1. 17 LC11_3 0. 262 480 (S)-3-{[6-(4-Chloro-3-fluoro-phenyl)-5-hydrazinyl-0-pyridin-2-yl]-amino}-3-(2 - gas-phenyl)-propionic acid 463. 07 1. 21 LC11_3 4. 37 481 (S)-3-[(2'-Chloro-3-methoxy-5-methyl-[2,3']-linked.pyridinyl-6--carbyl)-amino]-3 -(2 - gas _ phenyl)-propionic acid 460. 1 1. 09 LC11_3 8. 77 482 (S)-3-(2-Gas-phenyl)-3-[(3'-fluoro-3-indolyl-[2,4] linked. σ-based-6-yl)-amine Base]-propionic acid 430. twenty one. 03 LC11_2 0. 1153 483 (S)-3-{[6-(3-Chloro-5-fluorenyl-phenyl)-5-decyloxy-.比 -2- -2- carbyl]-amino}-3-(2- gas-phenyl)-propionic acid 459. 1 1. 22 LC11_3 9. 49 484 (S)-3-(2-Gas-phenyl)-3-({5_ 曱oxy-6-[3-(5-methyl 493. 14 1. 09 LC11_3 6. 69 189 201245154 -[1,3,4]oxadiazol-2-yl)-phenyl]-° ratio α定-2-戴基}-amino)-propionic acid 485 (S)-3-(2 -Chloro-phenyl)-3-[(5-decyloxy-6-indole ratio 0 well-2-yl-° ratio bit-2-initial)-amino]-propionic acid 413 1. 07 LC11_3 0. 1588 486 (S)-3-(2-Gas-phenyl)-3-{[5-methoxy-6-(l,3,5-trimethyl-111-0 ratio. Sodium-4-yl )-0 ratio. Ding-2-carbonyl]-amino}-propionic acid 443. 16 1. 02 LC11_3 4. 95 487 (S)-3-(2-Gas-phenyl)-3-{[5-decyloxy-6-(1-indolyl-1H-indole -6-yl)-° ratio.定_2_嫉基]·Amino}-propionic acid 464. 15 1. 17 LC11_3 &gt;10. 0 488 (S)-3-{[6-(4-Chloro-3-methoxy-phenyl)-5-decyloxypyridin-2-yl]-amino} -3-(2- Gas _ phenyl)-propionic acid 475. 09 1. 19 LC11_3 &gt;10. 0 489 (S)-3-{[6-(3-Gas-2-H-phenyl)-5-decyloxy-. Ratio ° -2 -chloro]amino}-3-(2- gas-phenyl)-propionic acid 463. 08 1. 17 LC11_3 0. 1314 490 (S)-3-(2-Chloro-phenyl)-3-[(3-indotyl-2'- morphine. lin-4-yl 497. 17 0. 92 LC11_3 9. 08 190 201245154 _[2,4']bipyridyl-6-carbonyl)-amino]-propionic acid 491 (S)-3-(2-chloro-phenyl)-3-{[5-decyloxy -6-(2-indolyl-furan-3-yl)-° ratio sigma-2-chloro]-amino}-propionic acid 415. 12 1. 14 LC11_3 0. 199 492 (S)-3-{[6-(2-chloro-5-methyl-phenyl)-5-methoxy-pyridin-2-carboyl]-amino}_3-(2- gas -Phenyl)-propionic acid 459. 1 1. 17 LC11_3 1. 053 493 (S)-3-{[6-(2-Chloro-3-fluoro-phenyl)-5-methoxy-0-pyridin-2-yl]-amino}_3-(2 - Gas-phenyl)-propionic acid 463. 07 1. 15 LC11_3 0. 05065 494 (S)-3-(2-Gas-phenyl)-3 - {[6-(4-cyano-2-fluoro-phenyl)-5-decyloxy-α ratio bite-2 - terminal group ]-Aminopropionic acid 454. 11 1. 11 LC11_3 11. 4 495 (S)-3-(2-oxo-phenyl)-3-({6-[3-(3-hydroxy-oxetan-3-yl)-phenyl]-5-decyloxy Specific ratio of 2-carbyl}-amino)-propionic acid 483. 14 1. 04 LC113 3. 89 5 191 201245154 496 (S)-3-(2chloro-phenyl)-3-({6-[3-(l-hydroxy-1-indolyl-ethyl)-phenyl]-5-anthracene Base-0 to bite-2-hexyl}-amino)-propionic acid 469. 16 1. 1 LC11_3 2. 86 497 (S)-3-{[6-(2-Ga-3-methyl-phenyl)-5-methoxy-0 ratio. -2-2_ carbonyl]-amino}-3-(2·gas-phenyl)-propionic acid 459. 1 1. 17 LC11_3 0. 0678 498 3-Biphenyl-4-yl-3-[(3,6-dipyridyl-2-carbonyl)-amino]-propionic acid 413. 24 1. 13 LC11_2 8. 55 499 3-biphenyl-4-yl-3-[(4-gas-3-methoxybipyridine-2-carbonyl)-amino]-propionic acid 409. 23 1. 11 LC11_2 &gt;10. 0 500 3-biphenyl-4-yl-3-[(2-gas-6. fluorenyl-°bendidine-4-yl)-amine]•propionic acid 395. 22 1. 12 LC11_2 &gt;10. 0 501 3·biphenyl-4-yl-3-[(6-gas-°pyridin-2-carbonyl)-amino]-propionic acid 381. 18 1. 13 LC11_2 0. 463 502 3-biphenyl-4-yl-3-[(5-gas-6_ fenyl-° ratio ̄-3-Weiyl)-amino]-propionic acid 397. 18 1. 01 LC11_2 &gt;10. 0 192 201245154 503 3-biphenyl-4-yl-3-[(2-chloro-indolyl-4-indyl)-amino]-propionic acid 381. 18 1. 09 LC11_2 &gt;10. 0 504 3-biphenyl-4-yl-3-[(5·chloro-σ ratio 咬-3-Isyl)-amino]-propionic acid 381. 45 1. 09 LC11_2 &gt;10. 0 505 3-biphenyl-4-yl-3-[(5-gas-6-methyllacyl-° ratio -3-carbyl)-amino]-propionic acid 411. twenty one. 14 LC11_2 &gt;10. 0 506 (S)-3-[(3,6-Dichloro-pyridin-2-yl)-amino]-3-o-indolyl-propionic acid 353. 11 1. 03 LC11_2 8. 48 507 (S)-3-[(2-Chloro-6-indenyl ratio -4--4-diyl)-amino]-3-o-indole-propionic acid 331. 17 1. 02 LC11_2 &gt;10. 0 508 (S)-3-[(2-Ga-6-decyloxy_ 0 ate-4-domain)-amino]-3_-o-phenylene-propionic acid 349. 18 1. 07 LC11_2 &gt;10. 0 509 (S)-3-[(2,6-Dichloro-acridin-4-carbonyl)-amino]-3-o-phenylene-propionic acid 353. 12 1. 08 LC11_2 &gt;10. 0 510 (S)-3-[(6-gas ratio. 定-2-domain group)_amino]-3-o-indolephenyl-propionic acid 319. 16 1. 05 LC11_2 0. 2049 511 (S)-3-[(5-chloro-6-trans-base-to-mouth ratio -3-yl)-amino]-3-o--333. 14 0. 88 LC11_2 &gt;10. 0 193 201245154 Tolyl-propionic acid 512 (S)-3-[(2-Gas-pyridine-4-carbonyl)-amino]-3-o-tolyl-propionic acid 317. 16 0. 99 LC11_2 &gt;10. 0 513 (S)-3-[(5-Gabypyridin-3-carbonyl)-amino]-3-o-indolyl-propionic acid 319. 17 0. 98 LC11-2 &gt;10. 0 514 (S)-3-[(6-chloropyrene π well-2-carboyl)-amino]-3-o-indolyl-propionic acid 320. 03 3. 67 LC2 1. 21 515 (S)-3-[(3,5-Diamino-6-gas-pyroxy-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid 350. 16 0. 97 LC11_2 0. 0871 516 3-biphenyl-4-yl-3 - {[5-gas-6·(2-carbyl-ethylamino)·pyridine-3-carbonyl]-amino}•propionic acid 438. 29 1. 04 LC11_2 &gt;10. 0 517 (S)-3-[(5-Ga-6-methoxy-~pyridin-3-carbonyl)-amino]-3-o-indolephenyl-propionic acid 347. 15 1. 05 LC11_2 &gt;10. 0 518 (S)-3-[(2,5-Dichloro-11 pyridine-3-carbonyl)-amino]-3-o-tolyl-propionic acid 351. 11 1. 01 LC11_2 &gt;10. 0 194 201245154 519 3-biphenyl-4-yl-3-[(3,5-diamino-6-chloro-pyridine-2-carbonyl)-amino]-propionic acid 412. 19 1. 07 LC11_2 0. 563 520 (S)-3-[(4-Chloro-3-indolyl-° ratio sigma-2-yl)-amino]-3-o-tolyl-propionic acid 347. 16 1. 01 LC11_2 &gt;10. 0 521 3-(2-Chloro-phenyl)-3-[(indole-2-yl)-amino]-propionic acid 304. 19 1. 05 LC11_2 12. 8 522 3-(2-Chloro-phenyl)-3-[(pyridylpyridyl)-amino]-propionic acid 305. 07 0. 98 LC11_2 523 3-(2-Gas-phenyl)-3_[(° ratio 定-2-yl)-amino]-propionic acid 305. 08 1. 12 LC11_2 524 3-(2-Gas-phenyl)-3-[(acridin-4-yl)-amino]•propionic acid 305. 08 0. 97 LC11_2 10. 2 525 3-(2-Gas-phenyl)-3-[(5-fluorenyl-° ratio. Well-2-yl)-amino]_propionic acid 318. 17 1. 09 LC11_2 526 3-(2-Chloro-phenyl)-3-[(2-indolyl-° ratio. 1,4--4-yl)-amino]-propionic acid 319. 09 0. 94 LC11_2 527 3-(2-Chloro-phenyl)-3-[(6-fluorenyl-° ratio: -2-terminal)-amino]-propionic acid 319. 1 1. 16 LC11_2 4. 96 195 201245154 528 3-0 gas-phenyl)-3-[(4-indolyl-pyridin-2-carbonyl)-amino]-propionic acid 319. 1 1. 16 LC11_2 5. 81 529 3-(2-Gas-phenyl)-3-[(4-hydroxypyridin-2-carbonyl)-amino]-propionic acid 321. 06 0. 97 LC11_2 5. 12 530 3·(2-Gas·Phenyl)_3·[(3·Fluoro~°bipyridine·2-carbonyl)·Amino]-propionic acid 321. 14 1. 09 LC11_2 5. 27 531 3-(2-Gas-phenyl)_3_[(6-Fluoro-pyridin-2-carbonyl)-amino]•propionic acid 323. 06 1. 15 LC11_2 7. 65 532 3-(2-Gas-phenyl)_3_[(4-ethylpyridin-2-carbonyl)-amino]-propionic acid 331. 22 1. 21 LC11_2 10. 2 533 3-(2-Gas-phenyl)-3-[(4,6-dimethyl-acridine-2-carbonyl)-amino]-propionic acid 331. 22 1. 2 LC11_2 6. 29 534 3-(2-Gas-phenyl)-3-[(4,6-diamidinopyridine-3-carbonyl)-amino]-propionic acid 333. 11 0. 92 LC11_2 535 3-(2-Gas-phenyl)-3-[(6-fluorenylamino-pyrifos-2-decyl)-amino]-propionic acid 335. 08 1. 07 LC11_2 196 201245154 536 3-(2-Chloro-phenyl)-3-[(2-methoxyindoles-4-yl)-amino]-propionic acid 335. 08 1. 11 LC11_2 5. 08 537 3-(2-Chloro-phenyl)-3-[(6 gastric 曱 基 - - π 比 -3- -3- yl)-amino]-propionic acid 335. 08 1. 1 LC11_2 538 3-(2-chloro-phenyl)-3-[(6-曱 乳-° ratio °-2-domain)-amino]-propionic acid 335. 08 1. 18 LC11_2 539 3-(2-Chloro-phenyl)-3-[(3-indole-based-0-pyrene-2-yl)-amino]-propionic acid 335. 09 1. 03 LC11_2 &gt;10. 0 540 3-(2-Chloro-phenyl)-3-[(6-chloro-n ratio 0-but-2-yl)-amino]propionic acid 339. 02 1. 18 LC11_2 1. 6 541 3-(2-Chloro-phenyl)-3-[(3,6-di-gas-° ratio -2-yl)-amino]_propionic acid 339. 14 1. 12 LC11_2 542 3-(2-Chloro-phenyl)-3-[(3H-imidinary[4,5-b]° than 5-amino)-amino]-propionic acid; Trifluoroacetic acid 345. 06 1. 0 LC11_2 10,8 543 3-(2-Chloro-phenyl)-3-[([1,8]Nytidine-2-yl)-amino]-propene 356. 07 1. 09 LC11_2 197 201245154 Acid 544 3-(2-Chloro-phenyl)-3-[([1,6]N-butyl-2-yl)-amino]-propionic acid 356. 07 1. 08 LC11_2 11. 1 545 3-[(2-Ethylaminopyridin-4-yl)-amino]-3-(2-chloro-phenyl)-propionic acid 362. 08 1. 02 LC11_2 546 3-[(2-Amino-6-isopropyl-. dimethyl-4-denyl)-amino]-3-(2-a-phenyl)-propionic acid; Fluoroacetic acid 363. 12 1. 15 LC11_2 547 (S)-3-{[6-(2-D-phenyl)- 0 ratio sigma-2-reyl]-amino} - 3_phenyl-propionic acid 365. 29 1. 75 LC X 0. 345 548 3-(2-Gas-phenyl)-3-[(4,6-dioxaoxy-11-denyl-2-yl)-amino]-propionic acid 366. 07 1. 24 LC X 549 3-(2-Gas-phenyl)-3-[(2,6-didecyloxy-)-amino-]-propionic acid 366. 08 1. 19 LC X 550 3-[(6-chloro-5-decyloxy-pyridin-2-yl)-amino]-3-(2- gas-phenyl)-propionic acid 369. 03 1. 19 LC X 1. 08 201245154 551 3-(2-Gas-phenyl)-3-(^(6-17moxa-1-yl-acridin-2-carbonyl)-amino]-propionic acid 371. 08 0. 96 LC X 552 3-(2-Chloro-phenyl)-3-[(3,6-diox-.pyr.diethyl-2-carbyl)-amino]-propionic acid 371. 1 1. 18 LC X 553 3-(2-Chloro-phenyl)-3-[(2-吼洛.定-1 ·基-σ ratio -4-amino-amino)-amino]-propionic acid; Fluoroacetic acid 374. 11 0. 96 LC X 11. 1 554 3-(2-Gas-phenyl)-3-[(6_ 口比洛 bit-1 -yl-^ ratio bit-3-carbyl)-amino]-propionic acid; compound containing trifluoroacetate 374 . 11 0. 95 LC X 555 3-(2-Chloro-phenyl)-3-[(5-exoprozol- 0-l-yl-[rho]-pyridyl-3-monmoyl)-amino]-propionic acid; The compound contains trifluoroacetic acid 374. 13 1. 01 LC11_2 &gt;10. 0 556 (S)-3-{[5-chloro-6-(2-hydroxy-ethylamino)_° ratio]]]amino}-3-o-indolephenyl-propionic acid 376. 22 0. 92 LC11_2 &gt;10. 0 557 3-[(2-Amino-6-isobutyl. 1,4--4-yl)-amino]-3-(2- 377. 12 1. 19 LC11_2 14 199 201245154 gas-phenyl)-propionic acid 558 (S)-3-{[6-(2- gas·phenyl)-. Σσ-2-amino]-amino}-3-phenyl-butyric acid 379. 33 1. 8 LC X 559 (S)-3-{[6-(2-Fluoro-phenyl)-° ratio sigma-2-yl]-amino}-3-p-tolyl-propionic acid 379. 33 1. 81 LC X 4. 38 560 (S)-3-{[6-(2fluoro-phenyl)-0 σ σ-2-yl]-amino} ·3· m-methyl-propionic acid 379. 33 1. 81 LC X 12. 9 561 (R)-3 - {[6-(2-Fail-Phenyl)-0 ratio. -2--2-Methoxy]-amino}-4-phenyl-butyric acid 379,34 • One.  1. 79 LC X 5. 33 562 3-[(6-&gt; odor-^ ratio. -2--rebase)_amino]-3-(2- gas-phenyl)-propionic acid 381. 04 1. 2 LC11_2 2. 1 563 3-(2-Chloro-phenyl)-3-[(6-phenyl-° ratio: sec-2-yl)-amino]-propionic acid 381. 1 1. 27 LC11_2 3. 09 564 3-(2-Chloro-phenyl)-3-[(3-phenyl-.~0-but-2-yl)-amino]-propionic acid 381. 1 1. 18 LC11_2 565 3-(2-chloro-phenyl)-3-[(4-benzene 381. 1 1. 27 LC11_2 4. 07 200 201245154 base-° ratio 11--2-indole-based)-amino]_propionic acid 566 3-(2-chloro-phenyl)-3-[(5-phenyl-. Alkyl)-amino]_propionic acid 381. 11 1. 18 LC11_2 11. 7 567 (S)-3-{[6-(2-Chloro-phenyl)-. °°定-2--]]]]]]]]] 27 1. 77 LC X 2. 18 568 3-[(5-Bromo-acridin-3-carbonyl)-amino]-3-(2- gas-phenyl)-propionic acid 382. 97 1. 13 LC11_2 569 (S)-3-(3-fluoro-phenyl)-3_ {[6-(2-fluoro-phenyl)"pyridin-2-carbonyl]-aminopropionic acid- 383. 29 1. 77 LC11_ X 0. 429 570 (S)-3-(2-Fluoro-phenyl)-3_ {[6-(2-fluoro-phenyl)-acridin-2-carbonyl]-amino}-propionic acid 383. 3 1. 76 LC11_ X 0. 195 571 (S)-3-(4-Fluoro-phenyl)-3-{[6-(2-fluoro-phenyl)-. Bipyridine-2-carbonyl]-aminopropionic acid 383. 3 1. 77 LC11_ X 0. 514 572 3-(2- gas-phenyl)-3_ [(3,4,5,6-tetrahydro-2H-[1,2'] 吼 吼 定 - -41-lu-)-amino]- Propionic acid; the compound contains trifluoroethylene 388. 15 1. 03 LC11_2 &gt;10. 0 201 201245154 Acetic acid 573 3-(2-chloro-phenyl)-3 _ [(3,4,5,6-tetrahydro-2H-[1,2,] conjugate. σ 定------ )-amino]-propionic acid; the compound contains trifluoroacetic acid 388. 16 1. 29 LC11_2 574 3-(2-Chloro-phenyl)-3-[(6-morphine-4-yl-° ratio π-but-2-polycarbon)-amino]-propionic acid; Trifluoroacetic acid 390. 12 1. 16 LC11_2 575 3-(2-Gas-phenyl)-3-[(4-indolyllin-4-yl-)-amino-2-yl)-amino]-propionic acid; Acetic acid 390. 12 0. 93 LC11_2 576 3-(2 gas-stupyl)_3_[(2-isofolin-4-yl-° ratio. 1,4--4-yl)-amino]-propionic acid; the compound contains trifluoroacetic acid 390 . 13 1. 03 LC11_2 577 (S)-3-[(6-decyloxy-biphenyl-3-indolyl)-amino]-3-o-indole phenyl-propionic acid 390. twenty one. 26 LC11_ 0. 414 578 (S)-3-[(3-Methoxy _[2,3'] π π π-based-6-phenyl)-amine 392. 08 0. 91 LC11_ 7. 54 202 201245154 yl]-3-o-indole phenyl-propionic acid 579 3-[(2,6-bis-dimethylamino-. s-amino-4-yl)-amino]-3- Ρ-Chloro-stupyl)-propionic acid; the compound contains trifluoroacetic acid 392. 14 1. 01 LC11_2 580 (S)-3-{[6-(2-Gas-phenyl)-° ratio α-1,4-indole]-amino}-3-p-tolyl-propionic acid 393. 19 1. 95 LC 11_X 15. 6 581 (S)-3-{[6-(2-Chloro-phenyl)- 0 ratio sigma-2-yl]-amino}-3-phenyl-butyric acid 395. 17 1. 94 LC 11—X 5. 76 582 (S)-3-{[6-(2-Phenylphenyl)- ° ratio sigma -2 -yl]-amino} - 3 · m-phenylene-propionic acid 395. 18 1. 96 LC 11_X 0. 16 583 (R)-3 - {[6-(2-Chloro-phenyl)_ 0 is 0-but-2-indoleyl]-amino} -4 _phenyl-butyric acid 395. 29 1. 81 LC 11_X &gt;30. 0 584 (S)_3 - {[6-(2-Fluoro-phenyl)_ 0 is a bit of a 2-amino]-amino}-3-(4-indole-phenyl)-propionic acid 395 . 31 1. 74 LC X 0. 54 585 3-(2-Chloro-phenyl)-3-[(6-phenoxy-hydrazin-3-yl)-amine 397. 08 1. 21 LC 11 8. 67 203 201245154 】]propionic acid 586 (S)-3- {[6-(2-chloro-phenyl)_ 0 than sigma-2-yl]-amino}-3-(2-dung stomach Phenyl)-propionic acid 399. 13 1. 92 LC 11—X 0. 339 587 (S)-3-{[6-(2-Gas-phenyl)-. Σσ-2_ 叛基]-amino}-3-(3- gas-phenyl)-propionic acid 399. 15 1. 92 LC 11_X 7. 35 588 (S)-3-{[6-(2-Chloro-phenyl)-0 ratio. Ding-2-mercapto]-amino}-3-(4-mur-phenyl)-propionic acid 399. 23 4. 49 LC 11_X 0. 107 589 3-(2-Chloro-phenyl)-3-{[6-(2-say-phenyl)-° ratio -2-yl]-amino}-propionic acid 399. 26 1. 8 LC X 4. 89 590 (S)-3-(3-Chloro-phenyl)-3-{[6-(2-fluoro-phenyl)-pyridin-2-carbonyl]-aminoindole-propionic acid 399. 26 1. 83 LC ll—X 0. 339 591 (S)-3-(4-Gas-phenyl)-3-{[6-(2-fluoro-phenyl)-acridin-2-carbonyl]-aminopropionic acid 399. 27 1. 83 LC ll—X 0. 322 592 3-(2-Chloro-phenyl)-3-[(1-ethyl-3,6-dimercapto-1H-indazolo[3,4-b]acridin-4-carbonyl)- Amino]-propionic acid 401. 13 1. 14 LC 11—2 204 201245154 593 3-(2-Chloro-phenyl)-3 -{[2_(2,2-dimercapto-propionylamino)-α ratio °-4-Wiki] -amino}-propionic acid 404. 14 1. 17 LC 11_2 594 3-(2-Chloro-phenyl)-3-{[6-(four-rat-σ-pyran-4-milyl)-° ratio σ-fixed carbon]-amino}-propionic acid 405 . 1 1. 14 LC 11_2 595 3-(2-Chloro-phenyl)-3-{[6-(4-decyloxy-phenyl)-° ratio °-2-carboyl]-aminopropionic acid 409. 3 1. 27 LC 11_2 1. 42 596 3-(2-Gas-phenyl)-3-{[6-(3-indoleyl-phenyl)-° ratio -2-amino]amino}-propionic acid 411. 1 1. 27 LC 11-2 5. 77 597 3-(2-Chloro-phenyl)-3-{[6-(2-methoxy-phenyl)_° ratio _2·Rotamyl]-amino}_propionic acid 411. 1 1. 27 LC 11-2 1. 45 598 3-[(6-&gt;odor-5-oxime-0-bito-2-yl)-amino]-3-(2-chloro-phenyl)-propionic acid 411. 18 1. 2 LC 11_2 1. 46 599 (S)-3-{[6-(2-Chloro-phenyl)-0 ratio 0-but-2-yl]-amino}-3-(4-methyl-based-phenyl)-propyl Acid 411. 29 1. 77 LC 11_X 2. 83 205 201245154 600 3-(2-Gas-phenyl)-3-[(6-cyclopropyl-1,3-dimercapto-1H-indole. Sit and [3,4-13]° ratio. -4-amino)-amino]-propionic acid 413. 14 1. 19 LC 11_2 601 3-(2-Gas-phenyl)-3-{[4-(pyridin-2-ylthioalkyl)-° ratio -2 _ _ group]-aminopropionic acid 415. 05 1. 18 LC 11_2 3. 85 602 (S)-3-(4-Chloro-phenyl)-3_ {[6-(2-Gas-phenyl)-° ratio β-2-1-carbonyl]-aminopropionic acid 415. 09 1. 94 LC 11_X 0. 0623 603 (S)-3-(3-Chloro-phenyl)-3_ {[6-(2-chloro-phenyl)-. Bipyridine-2-carbonyl]-amino}-propionic acid 415. 12 1. 98 LC 11_2 0. 0803 604 3-(2-Gas-phenyl)-3-{[6-(2-gas-phenyl)-° ratio β定-2 -yl]]-aminopropionic acid 415. 25 1. 83 LC_X 0. 345 605 (S)-3-(2,4-Dichloro-phenyl)-3-{[6-(2- gas-phenyl)-. Ratio ° - 2 - carbonyl] - amino} - propionic acid 433. 24 1. 9 LC 11_X 2. 28 606 (S)-3-(2,3-Dichloro-phenyl)-3-{[6·(2-Gas-phenyl)-° ratio -2 - benzyl]-amino}*&quot ; propionic acid 433. 25 1. 87 LC 11_X 3. 93 607 (S)-3-{[6-(2-|i-phenyl)-° ratio °-2-alkyl]-amino} -3 - 433. 31 1. 83 LC_X 0. 88 206 201245154 (2-Trifluorodecyl-phenyl)-propionic acid 608 (S)-3-{[6-(2-Fluoro-phenyl)-. Ratio σ--2 - rimyl]-amino} - 3 _ (4-trifluoromethyl-phenyl)-propionic acid 433. 31 1. 87 LC_X 6. 27 609 (S)-3-{[6-(2-Fluoro-phenyl)-° ratio. Benz-2-yl]-amino} -3_(3-dimethylhydrazine-phenyl)-propionic acid 433. 32 1. 85 LC_X 0. 902 610 (S)_3- {[6-(2-chloro-phenyl)_ 0 ratio.搂-2-mercapto]•amino} -3· (2,3-di-phenyl)-propionic acid 449. 07 2. 01 LC ll-X 2. 32 611 (S)-3-{[6-(2-Chloro-phenyl)- ° ratio σ定-2- 基基]-amino} - 3-(2,4-diphenyl)-propyl Acid 449. 09 2. 05 LC 11_X 0. 27 612 (S)-3-{[6-(2-Chloro-phenyl)- ° ratio σ定-2-yl]-amino}-3-(2-dipyryl-phenyl)- Propionic acid 449. 13 1. 98 LC 11_X 1. 66 613 (S)-3-{[6-(2-Chloro-phenyl)-indole bite-2-carbyl]-amino}·3_(4-difluoroindolyl-phenyl)-propane Acid 449. 16 2. 02 LC 11_X 0. 406 614 (S)-3_ {[6-(2-Gasylphenyl)_° ratio σ定-2-绿基]-Amino}-3-(3-dimethylhydrazine-phenyl)-propyl Acid 449. 16 2. 0 LC ll—X 0. 315 207 201245154 615 3-(2-Chloro-phenyl)-3-{[3-(4,6-dioxaoxy-pyrimidin-2-yl)_α ratio π定-2- prison]]- Amino}-propionic acid 459. 13 1. 06 LC 11_2 3. 58 616 3-(2-Gas-phenyl)-3-[(6-phenyl-2-hexafluoropyrene-1-ytyl)-amino]-propionic acid; The compound contains trifluoroacetic acid 465. 21 5. 02 LC 11-2. 10. 4 617 (3)-3-{[6-Bromo-5-(3,3-dimercapto-2-indolyl-butyl-butyrydin-2-yl)-amino}-3-o-toluene Base-propionic acid 477. 03 1. 25 LC 11 0. 1568 618 (S)-3-{[5-(3,3-Dimethyl-2-indolyl-butoxy)-6-benyl-0 to 0-but-2-phenyl]-amino} -3- o- 曱 phenyl-propionic acid 1. 19 LC 11-2 (1) Mass spectrometry identification; ionic lipid mass number [(M+H)+] was observed unless otherwise specified. (2) Cathepsin A inhibitory activity was measured in the pharmacological test π cathepsin A inhibitory activity described below. Pharmacological Test a) Cathepsin A Inhibitory Activity Recombinant Human Cathepsin A (residues 29-480, containing C-terminal ΙΟ-His tag; R&amp;D Systems, #1049-SE) with recombined 208 201245154 Human Cathepsin L (R&amp;D Systems, #952-CY) protein breakdown activation. Briefly, put 1 μg/ml cathepsin A with 10 μg/ml cathepsin L in activation buffer (25 mmol concentration 2-(ifosin-4-yl)-ethyl tartaric acid (MES) , pH 6. 0, containing 5 mM concentration of dithiothreitol (DTT)) at 37. (: culture for 15 minutes. Then via the addition of the cysteine protease inhibitor E-64 (N-(trans-epoxysuccinyl)-L-free amine-4-mercaptoamine; sigma-Aldrich, # E3132 ; dissolved in activation buffer / DMSO) to a final concentration of 10 micromoles &gt; Chen 'stops cathepsin L activity. Activated cathepsin A in test buffer (25 millimolar MES, pH 5 . 5' diluted in 5' molar concentration DTT) and mixed with test compound (dissolved in test buffer containing (v/v) 3 % DMSO) in multiple test plates, or in control experiments with vehicle mixing. After incubation for 15 minutes at room temperature as a substrate, then with [[4®Bodipy FL (4,4-dioxa-5,7-dimercapto-4-bora-3a, 4a-di-H-) The s-dicyclopentadienylbenzo-3-propenyl)-labeled bradykinin (JPT Peptide Technologies GmbH; dissolved in assay buffer) was added to the mixture. The final concentration of cathepsin A was 833 ng/ml and the final concentration of the labeled bradykinin was 2 micromolar. After incubation for 15 minutes at room temperature, stop buffer (130 mg molar concentration of 2-(4-(2-hydroxy-ethyl)-hexahydroindole-1-yl)-ethanesulfonic acid, pH 7. 4, containing (v/v) 0. 013 % ® Triton X-100, 0. 13 % Coating Reagent 3 (Caliper Life Sciences), 6.5 % DMSO and 20 micromolar ibene lactone B (sigma, # E0886) stopped the reaction. 209 201245154 The undissociated substrate and product were then separated by microfluidic capillary electrophoresis on a LabChip® 3® Drug Discovery System (12-Sipper-Chip; Caliper Life Sciences) and quantified by measuring the respective peak areas. The turnover of the product was divided by the sum of the area of the substrate and the product, and the turnover of the substrate was calculated, and the enzyme activity and the inhibitory effect of the test compound were quantified accordingly. The inhibitory concentration ICso was calculated from the percentage inhibition of tissue protease A activity observed at several concentrations of the test compound, i.e., the enzyme activity was 5 〇〇/. The concentration of inhibition. The IC5 enthalpy of several example compounds at micromolar concentrations is provided in Table j. B) In vivo antihypertensive cardiac hypertrophy and renal protective activity The in vivo pharmacological activity of the compounds of the present invention can be studied, for example, in the mode of unilateral nephrectomized DOCA-salt-sensitive rats. Simply put 'in this model' in a 150- to 200-gram-weight Sprague Dawley rat for left unilateral nephrectomy (UNX)^ surgery and at the beginning of subsequent weeks, 3 mg via subcutaneous injection /kg body weight of DOCA (deoxycorticosterone acetate was administered to rats. Dendritic rats treated with DOCA supplied water containing 1% of gasified sodium (UNX/DOCA rats). UNX/DOCA rats produced hypertension Endothelial cell dysfunction, cardiac hypertrophy and fibrosis, and renal dysfunction. In the test group (UNX/DOCA test) and placebo group (UNX/DOCA placebo), it consisted of random UNX/DOCA rats. The rats were orally administered with a daily dose of the test compound (for example, 10 mg/kg body weight dissolved in the vehicle) or vehicle only at 6 am and 6 pm in two administrations. In the control group, it consisted of animals that were administered UNX and DOCA without 210 201245154. The animals were treated with regular drinking water and treated with vehicle only. After five weeks of treatment, the systolic blood pressure was measured non-invasively via the cuffs. (SBP) and heartbeat (HR). For protein Urine and creatinine were measured and 24-hour urine was collected in a metabolic cage. As previously disclosed (W.  Linz et al. Jraas (journal 〇f the renin-angiotensin-aldosterone system) 7 (2006), 155-161), assessed endothelial function in the thoracic aortic resection ring. For myocardial hypertrophy and fibrosis measurements, cardiac weight, left ventricular weight, and hydroxyproline were correlated with proline at the excised heart. [Simple diagram description] None [Main component symbol description] None 211

Claims (1)

201245154 VII. Scope of Application: 1. A compound of formula I in any stereoisomeric form or in a mixture of stereoisomeric forms in any proportion, or a physiologically acceptable salt thereof, or any physiologically acceptable Accepted solvate, A is a series selected from the group consisting of qR1) and N; D is a series selected from the group consisting of C(R2) and N; E is a series selected from C(R3) and N; L is selected from C(R4) and N a series consisting of: at least one and at most two A, D, E or L are N; G is selected from the group consisting of R7丨-OC(O)-, R72-N(R73)-C(0)· and tetrazole_ a series of 5_groups; R1 is selected from the group consisting of hydrogen, i group, (CrC6)-alkyl, HO-, (CrC6)-hospital-0-, (qC:6)-alkyl-S(0)m - and NC-composed series; R2 is selected from hydrogen, _ group, (CrC7)-alkyl, (CrQ)-alkyl-〇-, (Ci-C6)-hospital-CO-, (CrC6)· a series of alkyl-C0-HN-, NR12R13, Het2, (C3-C7)-cycloalkyl-CsH2s- and Ar-CsH2s-, wherein s is an integer selected from the group consisting of 0, 1, 2, and 3 R3 is selected from the group consisting of hydrogen, i group, (CrC6)-hospital, (CrC6)-hospital-S(0)m-, Het4-(0)t- &gt; -NR12R13 ^ Het2 &gt; Rn-〇- , R12-N(R13)-C(0)-〇- and Het2-C(0)-0- and NC-composition series, wherein s is selected from the group consisting of 〇, 1, 212 201245154 2 and 3 An integer and wherein t is an integer selected from the group consisting of 0 and 1; R4 is selected from hydrogen, aryl, (CVQ)-alkyl, crC6)-alkyl-〇-, H〇-, NRi2R13, Het2 composed of a series; R 疋 selected from hydrogen, _ group, ((: 丨-〇: 6)-alkyl, (c丨-c6)-burning a series consisting of 〇,, (CVC6)-alkyl-S(〇)m-, HO-, -NR12R13, Het2, phenyl-CsH2s-(0)r, wherein s is selected from 〇, 1, 2 And an integer of the series consisting of 3 and wherein t is an integer selected from the group consisting of 〇 and 1; or R1 and R2 or R2 and R3 form a pyridyl group; or R1 and R2 are -C((CrC3)-alkyl)= NN((CrC3)-alkyl)-; or R2 and R3 are -NH-CH=N-; a prerequisite is that one of R1, R2, R3, R4 or Ri〇 is a cyclic substituent; R11 is selected from hydrogen a series consisting of R14, (C3-C7)-cycloalkyl, Ar and Het3; R12 and R13 are each independently selected from the group consisting of hydrogen and r15; τ» 14 β R 疋(CrCio)-alkyl group, Optionally, one or more of the same or different selected from the group consisting of halo, HO-, R16-〇-, keto, (CrC7)-cycloalkyl, Ar, Het1, Het3, NC-, H2N-C(0)- , (CVQ)-alkyl-NH-C(0)_, bis((CrC4)-alkyl)NC(O)-, Ηβ-αΟ)- '(Cl-C4)-alkyl-C(0) a substituent of a series consisting of -NH- and (C1-C4)-alkyl-S(0)m- Substituting; Rl5 is (crc6)-alkyl, optionally substituted by one or more substituents of the same or different series selected from the group consisting of halo, HO- and (Ci-C6)-alkyl; 213 201245154 generation;疋(CVC6)-alkyl, optionally substituted by one or more substituents of the same or different series selected from the group consisting of HO·, (CrC4)-alkyl 〇 及 and sheng; R 30 is selected from R 31 , ( CVC7)-cycloalkyl, R32-CuH2u• and Het3-CuH2u- a series consisting of 'where u is an integer selected from the group consisting of 0, 2 and 3; R is (CrCio)-alkyl, which is optionally One or more of the same or different series selected from the group consisting of halo, (Crc7)-cycloalkyl, HO_, (Ci_C6)alkyl-〇·, (CrC6)-alkyl-S(〇)m_&amp; NC_ a substituent substituted; R32 is a series consisting of a phenyl group and an aromatic 5-membered 6-membered monocyclic heterocyclic group, which comprises one, two or three of the same or different series selected from the group consisting of nitrogen, oxygen and sulfur. A ring heteroatom is bonded via a ring carbon atom, wherein the phenyl and heterocyclic groups are all optionally substituted with one or more substituents of the same or different series selected from the group consisting of: i-based, (crc6)-alkyl (c3_C7)_cycloalkyl, R33, HO·, (crC6)-alkyl-〇-, R33-0-, R33-(crC4)·alkyl-Ο-,-0-CH2-〇-,-0 -CF2-0-, (CrC6)-alkyl_s(〇)m-, H2N-s(o)2-, (c丨-c4)-alkyl-NH-s(o)2-, two ( (CrC4)-alkyl)NS(0)2-, H2N-, (C"c6)-alkyl-NH-, bis((CrC6)-alkyl)N-, Het1, (CVCj)-alkyl- C(〇)-NH-, Ar-C(0)-NH-, (CrC4)-alkyl-S(〇)2-NH- and NC-; R33 is selected from phenyl and aromatic 5-members or a monocyclic heterocyclic group containing one, two or three ring heteroatoms of the same or different series selected from the group consisting of nitrogen, oxygen and sulfur and linked via a ring carbon atom, wherein the phenyl and heterocyclic groups are all 214 201245154 are optionally substituted by one or more substituents of the same or different series selected from the group consisting of halo, (Cl_C6)-alkyl, (〇3-匚7)-bad danic, HO-, (Ci-C6)-alkyl--0-, (Ci-C6)-alkyl-S(0)m-, H2N-S(〇)2-, (Ci-C4)-alkyl-nh-s( o) 2-, di((crc4)-alkyl)NS(0)2- and NC-; R40 is a series selected from the group consisting of hydrogen and (Q-C4)-alkyl; or R30 and R4G are ( CH2)X 'freely passes one or more phases Or a different (CrQ)-alkyl substituent substituted 'wherein X is an integer selected from the group consisting of 2, 3, 4 and 5; R50 is selected from the group consisting of hydrogen, (CrC6)-alkyl, HO- and (CVC6) a series of -alkyl-0-constitutes; R6Q is a series selected from the group consisting of hydrogen and (CrCe)-alkyl; or R5G and R6Q together with (CH2)y, optionally via one or more of the same or different (CrCO-alkyl substituent substituted, wherein y is an integer selected from the group consisting of 2, 3, 4 and 5; R71 is a series selected from the group consisting of hydrogen and (Ci-Cg)-alkyl, optionally passed through a Or a plurality of substituents of the same or different series selected from the group consisting of (CrC6)-alkyl-0- and (CrC6)-alkyl-C(0)-0-; R72 is selected from hydrogen, (crc6)- a series of alkyl, (rcc6)-cycloalkyl, -CH2-(CH2)b-(C3-C6)-cycloalkyl, Het4 and -(CH2)b-Het4, wherein alkyl or cycloalkyl is Optionally, one or more of the same or different selected from halo, HO-, HOOC-, (CrC6)-alkyl-0- and (CrC6)-alkyl-C(0)-〇-, NC-, N Substituted by a substituent of the ((CrC4)-alkyl)2 composition and b is 0, 1 or 2; 215 201245154 73 R is a compound selected from the group consisting of hydrogen and (Ci-C6)-alkyl ; Or R and. R together with the nitrogen atom to which it is bonded form a saturated 4- to 1-membered monocyclic heterocyclic group optionally containing a ring heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, optionally passing through Or a plurality of substituents of the same or different substituents selected from the group consisting of halo, (C1-C), HO· and (crc4)-alkyl--0-; Ar', other Ar-groups are independent of each other, a series consisting of a phenyl group and an aromatic 5 member or a 6: membered monocyclic heterocyclic group, which contains one, two or three ring heteroatoms of the same or different series selected from the group consisting of nitrogen, oxygen and sulfur and via a ring-nuclear linkage wherein the phenyl and heterocyclic groups are each optionally substituted with one or more substituents of the same or different series selected from the group consisting of halo, (C"c6)-alkyl, H0-( Crc6)_alkyl, Het4, _(CH2)xj, (CrC6)-hospital _〇·, (CrC7)_cycloalkyl _(CH2)x 〇_, π], -c〇-(c" C6)-alkyl, _NRi2Rl3, Het2, _c〇_nr12r13, CO-Het2, (CrC6)-alkyl-S(〇)m-, h2N-S(0)2- and NC-; By -CH=CH-CH=CH-,-0-CH2-0-, -o-ch2-ch2-o-, -〇_CF2-0_4_n((Ci_C3)_alkane CH=CH substituted; Het1 'is independent of each other, and is a saturated or unsaturated 4 to 8 membered monocyclic heterocyclic group containing a ring nitrogen atom and bonded thereto and optionally Two other ring heteroatoms of the same or different series selected from the group consisting of nitrogen, oxygen and sulfur, optionally at one or more of the same or different selected from the group consisting of i, (crc4)-alkyl, H0-, (cvc4) -Alkyl-0-, 216 201245154 Substituted by a substituent of the keto group and the NC-composition series; Het2 is a saturated 4-membered to 7-membered monocyclic heterocyclic group containing a ring nitrogen atom and Het2 is passed through it Linked and optionally - another ring heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, optionally at one or more of the same or different selected from halo, (CrC4)-alkyl, HO- and crC4)-alkyl-CM and substituted with a series of substituents; Het, independently of the other Het groups, is a saturated 4 member-membered monocyclic heterocyclic group containing one or two identical or different selected from Other ring heteroatoms of the series consisting of nitrogen, oxygen and sulfur and linked via a ring carbon atom, optionally randomly selected from one or more of the same or different Substituted by a series of (Ci_C4)-alkyl and keto groups; Het, independently of the other Het4 groups, is a saturated or unsaturated 4- to 8-membered monocyclic heterocyclic group containing one to four Other ring heteroatoms of the same or different series selected from the group consisting of nitrogen, oxygen and sulfur, optionally randomly selected from one or more of the same or different selected from the group consisting of halo, (CrC4)-alkyl, HO-, (CrC4)- Substituted by a substituent of a series of ketone groups, ketone groups and NC-; m' is independent of other numbers, and is an integer selected from the group consisting of ruthenium, 1 and 2; wherein all cycloalkyl groups are independently of each other Substituting one or more substituents of the same or different series selected from the group consisting of fluorine and (CrC4)-alkyl; wherein all alkyl groups, CsH2s, CuH2u, (CH2)X and (CH2)y are independent of each other and independent Any other substituent is optionally substituted with one or more fluorine substituents. 217 201245154 2. According to the application (4), the formula u Γ == what proportion of stereoisomers '_= two; b; t salt' or any of its physiologically acceptable G is selected from R7I-0 -C(0)- and r72 73 V. Is R'Cuh2u-, wherein u is selected from R2 is an integer selected from the group consisting of phenyl and aromatic 6Τ:Λ; w(tetra)cyclo group, which contains - or two 蚰 = 夕衣杂原子' where the phenyl and heterocyclic ring The bases are all random or the same or different from the base _ base cjrC7) - sulfhydryl, r33, Ηα, (CrC6) silk · 〇, R33 〇, R - (CVC nucleobase _ 〇 _, _ 〇 〇 〇 〇CF2 〇n 基-S(0)m_,:((CrC4)·alkyl)N s(〇)2, off, two ((Ci-CA alkyl)N_, Heti, (Ci C4) alkane Substituted by a substituent of the series consisting of -NH, 'i-CW-NH- and NC_; R is selected from the group consisting of a stupid group and an aromatic 6-membered monocyclic ring group containing one or two nitrogen atoms as a ring The hetero atom, the substrate and the heterocyclic group are all optionally subjected to - or a plurality of the same or different selected from the group, (Ci_c6) alkyl, (C3-C7)-cyclofil, H0-, (CrC6)- Substituent substitution of a series consisting of a group consisting of ke ke s(0)m H2N-S(0)2_, J^((cr(:4)-alkyl)-like (〇)2_ and NC_; R4() is hydrogen. 3. A compound according to any one or more of claims 1 and 2 of the patent application, in any stereoisomeric form or in any ratio a mixture of stereoisomeric forms, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, wherein 218 201245154, wherein G is R71-〇-C(0)-; R30 is R32-CuH2u - wherein U is 0; R32 is a series selected from the group consisting of phenyl wherein the phenyl group is optionally one or more of the same or different selected from halo, (CrC6)-alkyl, (CrC7)-environmental groups , R33, HO-, (C丨-C6)-alkyl-0-, R33-〇-, alkyl-Ο-, _〇CH2-〇-,-0-CF2-0-, (CrQ)-alkane s-S(0)m-, bis((CVC4)-alkyl)NS(0)2-, H2N-, bis((CrC6)-alkyl)N-, Hetl, (CrC4)-alkyl-C (0) a substituent substituted by a series of -NH-, Ar-C(0)-NH- and NC-; R33 is a series selected from the group consisting of phenyl, wherein the phenyl is optionally one or more identical or Differently selected from halo, (CrC6)-alkyl, (C3-C7)-ring, elemental, H〇_, (Ci-Cg)-alkyl--0-, (Ci_C6)-alkyl-S(0 a substituent substituted by a series of m-, H2N-S(〇)2-, bis((crc4)-alkyl)NS(0)2- and NC-; k4() is hydrogen. 4. Patent pending Any one or more of the scopes 1 to 3 j compound 'in any stereoisomeric form or a mixture of stereoisomeric forms in any proportion, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, wherein r5Q is hydrogen; R6 () is hydrogen. 5. ^ According to any one or more of the formulae 1 to 4 of the patent application, the compound of formula j is in any stereoisomeric form or in any proportion of a mixture of stereoisomers 219 201245154 isomeric forms, or physiologically Accepted, its physiologically acceptable solvate, where: Formula: Yes: two = to 1-7 6: According to the application: the compound of formula η of the fifth patent range, which is a compound: IT: formula or a stereoisomeric form in any ratio, "Do not, or a physiologically acceptable solvate thereof, wherein ^ 220 201245154 R10 R2 is Ar-CsH2s-, wherein S is an integer selected from 0; R3 is selected from the group consisting of hydrogen, il, Rn-〇-, HO-, (CrC6)-alkyl and (CrC6)-alkyl-oxime- a series; preferably HO- and (CrC6)-alkyl; R4 is hydrogen; R1() is hydrogen. 7. A compound of formula I according to claim 5 or 6 of the patent application, in any stereoisomeric form or in a mixture of stereoisomeric forms in any proportion, or a physiologically acceptable salt thereof, or any physiological An acceptable solvate wherein R3 is Ru-0-, wherein R11 is hydrogen or (CrC10)-alkyl. 8. A compound of formula I according to any one or more of claims 5 to 7 of the invention, in any stereoisomeric form or in a mixture of stereoisomeric forms in any proportion, or a physiologically acceptable salt thereof Or any physiologically acceptable solvate thereof wherein R3 is -0-CH3. 9. A compound of formula I, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, according to any one or more of claims 1 to 8, which is selected from (S)-3 -[(5-decyloxy-6-phenyl-.pyridylpyridin-2-weiry)-amino]-3-o-indole-propionic acid-(8)-3-(2,4- Dioxo-phenyl)_3-[(5-decyloxy-6-phenyl-11-pyridin-2-carbocarbon 221 201245154-)-amino]-propionic acid (S)-3-[(6 -gas-5-decyloxy-0-pyridin-2-# charcoal)-amino]-3-o-indolephenyl-propionic acid (S)-3-{[3-(4,6- Dimethoxy-pyrimidin-2-yloxy)-pyridyl-2-carbonyl]-amino}-3-o-tolyl-propionic acid (8)-3-[(6-&gt;odor _5 - 曱 〇 〇 -2- -2- -2- -2- ) ) ) ) ) -2- -2- -2- -2- -2- -2- -2- -2- { { { { { { { 基 基 基 基 基 基 基 基 基 基 基))-β ratio σ -2- 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 绿 [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ (3)-o-tolyl-propionic acid (S)-3-[(5-phenylpyridin-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid (S)- 3-{[5-(2-Gas-phenyl)-0-pyridin-3-yl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[5- (2,3-diqi-phenyl)-° ratio. -3--3-reradyl]-amino}-3-o-tolyl-propionic acid (S)-3-{[5-(2,3-dimethyl-phenyl)-° ratio 0--3 -domain base]-amino}·_3-o-nonylphenyl-propionic acid (S)-3-o-tolyl-3-[(6-m-m-phenylphenylpyridin-2-carbonyl)-amine (-)propionic acid (S)-3-{[6-(2-carbo-phenyl)-n-pyridin-2-yl]-amino}-3-o-indolephenyl-propionic acid ( S)-3-{[6-(2-Fluoro-phenyl)-. (bi)-2-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[6-(2,3-digas-phenyl)-° ratio bite-2- Wei Ke]-Amino}-3-o--A-22 201245154 Phenyl-propionic acid (S)-3-{[6-(2,5-difluoro-phenyl)-acridin-2-carbonyl]- Amino}-3-o-tolyl-propionic acid (S)-3-{[6-(4-fluoro-2-indolyl-phenyl)-° ratio 0--2-yl]-amino group }·_3-o-p-phenyl-propionic acid (S)-3-{[6-(2,3-dimercapto-phenyl)-0 to 0-but-2-yl]-amino} _3-o-tolyl-propionic acid (8)-3-{[6-(5-fluoro-2-methyl-phenyl)-11 than dec-2-yl]-amino}-3- o-Tolyl-propionic acid (S)-3-{[6-(2-decyloxy-4-trifluoromethyl-phenyl)-acridin-2-carbonyl]-amino}-3-ortho -Phenylphenyl-propionic acid (8)-3-{[6-(4-chloro-2-methoxy-phenyl)-° than sec-2-yl]-amino}-3-o- Phenylphenyl-propionic acid (8)-3-{[6-(2-fluoro-5-methoxy-phenyl)-°bendidine-2-|£carbyl]-amino}-3- o-Phenylphenyl-propionic acid (S)-3-{[6-(2-a-phenyl)-5-methoxy-. Specific bite ·^-alkyl]-amino}-3_ o-nonylphenyl-propionic acid (S)-3-{[6-(2- gas-5-methyl-phenyl)-° ratio bite- 2-(yl)-amino}-3-o-indolephenyl-propionic acid (S)-3-[(5-decyloxy-6-phenylpyridin-2-carbonyl)-amino]- 3-p-indole phenyl-propionic acid (S)-3-[(5-methoxy-6-o-tolyl-π ratio sigma-2-yl)-amino]-3-pair- Phenylphenyl-propionic acid (S)-3-{[5-decyloxy-6-(2-trifluoromethyl-phenyl)"pyridin-2-carbonyl]-223 201245154 Amino} -3 - p-Phenylphenyl-propionic acid (S)-3-{[6-(3-fluoro-phenyl)-5-methoxy-π-bipyridine-2-carbonyl]-amino}-3-pair- (曱)·propionic acid (S)-3-{〇methoxy-6-(2-methoxy-phenyl)pyridin-2-carbonyl]-amino}·3-p-tolyl·propyl Acid (S)-3-{[6-(2-Gas-phenyl)-5-decyloxypyridylcarbonyl]-amino}-3-p-indoleyl-propionic acid (S)-3- {[6-(2-Fluoro-phenyl)-5-indolyl-n ratio _2-mono)-amino}_3· p-nonylphenyl-propionic acid (S)-3-{[ 6-(2,4-Difluoro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-p-tolyl-propionic acid (S)-3-{[6- (2,3-dioxa-phenyl)-5-decyloxy acridine-2-carbonyl]-amino}-3-p-tolyl-propionic acid (S)-3-{[6_(2 -gas_5_trifluoromethyl phenyl )_5_曱oxy-0 ratio 0 _2 _ _ group] · amino}-3-p-tolyl-propionic acid (S)-3-{[6-(3-fluoro-2-indenyl) -phenyl)-5-decyloxy-acridin-2-carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid (S)-3-{[6-(2-虱-5-Tris-indenyl-phenyl)_5_decyloxy-«» ratio. (2)-amino]-amino}·3-(2-fluoro-phenyl)-propionic acid (S)-3-{[6-(2,3-fluoro-phenyl)-5-anthracene Oxy-d ratio. _2_2_ 叛基]-amino}-3-p-phenylene-propionic acid (S)-3-{[6-(2,5-monofluoro-phenyl)-5·nonyloxy-η ratio. _2 _ _ _ _ _ _ _ _ _ _ _ _ 对 曱 · · 丙 丙 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比Acridine_2_carbonyl]-amine 224 201245154 】}-3-p-Phenyl-propionic acid (S)-3-{[6-(3,5-dimercapto-isoxazol-4-yl) -5-decyloxypyridinium-2_ benzyl]-amino}-3-p-indolephenyl-propionic acid (S)-3-{[6-(4-fluoro-2-methyl-phenyl )-5-decyloxy-ηpyridinyl-2-carbonyl]-amino}-3-p-indolephenyl-propionic acid (S)-3-{[6-(2,3-didecyl- Phenyl)-5-decyloxy acridine-2-carbonyl]-amino}-3-p-tolyl-propionic acid (5)-3-[(3,2'-dimethoxy-[2, 3'] Dipyridinyl-6-carbonyl)-amino]-3-p-tolyl-propionic acid (S&gt;3-{[6-(5-fluoro-2-indolyl-phenyl)-5 -decyloxy-acridin-2-carbonyl]-amino}-3-p-indolyl-propionic acid β)·3·{[6-(4-fluoro-2-methoxy-phenyl) -5-methoxypyridin-2-carbonyl]-amino}-3-p-tolyl-propionic acid (S&gt;3_{[6-(5-fluoro-2-decyloxy-phenyl)- 5-decyloxy-n-pyridinyl-2-carbonyl]-aminopyr-3-3-p-phenyl-propionic acid (s&gt;3_{[6-(2·fluoro-5-fluorenyl-phenyl)- 5-decyloxy-acridin-2-carbonyl]-aminopyr-3-3-p-tolyl-propionic acid (S)_3-{[6-(3-chloro-2-indolyl-phenyl)·5 -曱oxy^ ratio Pyridin-2-carbonyl]-aminopyr-3-3-p-tolyl-propionic acid (S)_3-{[6-(3-fluoro-2-indolyl-phenyl)·5-decyloxy-pyridine- 2-carbonyl]-amino}-3-p-nonylphenyl-propionic acid·(S)_3_{[6-(5-Gas-2-fluoro-phenyl)-5-decyloxy^biidine _ 2_carbonyl]-amino}-3-p-indoleyl-propionic acid (S)-3-(2-fluoro-phenyl) winter [(5-decyloxy-6-phenylindolepyrimidine) 2_carbonyl)_ 225 201245154 Amino]-propionic acid (S)-3-{[6-(2,4-dichloro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino }-3-(2-Fluoro-phenyl)-propionic acid (S)-3-(2-fluoro-phenyl)-3-[(5-decyloxy-6-o-indolephenyl)pyridinium (-2-carbonyl)-amino]-propionic acid (S)-3-(2-fluoro-phenyl)-3-{[5-decyloxy-6-(2-trifluoromethyl-phenyl) -° ratio σ定-2-carbyl]-aminopropionic acid (S)-3-(2-fluoro-phenyl)-3-{[5-methoxy-6-(2-decyloxy) -phenyl)-.pyridin-2-carbonyl]-amino}-propionic acid (S)-3-{[6-(2-a-phenyl)-5-methoxypyridin-2-carbonyl ]-Amino}'-3-(2-Ga-phenyl)-propionic acid (S)-3-(2-^-phenyl)-3-{[6-(2-N-phenyl-phenyl)- 5 -decyloxy-0 to 0 -2 - carbonyl]-amino}-propionic acid (S)-3-{[6-(2,4-di-phenyl)-5-decyloxypyridinium -2-carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid (S)-3-{[6-(2 ,3-diazo-phenyl)-5-methoxyl ratio 0-but-2-reyl]-amino}'-3-(2-a-phenyl)-propionic acid (S)-3-{ [6-(2,3-Bismo-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-(2-a-phenyl)-propionic acid (S)-3 -{[6-(2,5-Difluoro-phenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-(2-a-phenyl)-propionic acid (S) -3-{[6-(4-fluoro-2-indolyl-phenyl)-5-methoxypyridin-2-carbonyl]-amino}_3-(2-murine-phenyl)-propionic acid (S)-3-{[6-(3,5-dimercapto-isoxazol-4-yl)-5-methoxypyridin-2- 226 201245154 succinyl]-amino}-3 -(2-disorganized-phenyl)-propionic acid (S)-3-{[6-(2,3-dimethyl-phenyl)-5-methyllacyl-0-pyridin-2-yl ]_Amino}-3-(2-mur-phenyl)-propionic acid (S)-3-[(3,2'-dimethoxy-[2,3']bipyridyl-6-carbonyl )-amino]-3-(2-fluoro-phenyl)-propionic acid (S)-3-{[6-(5-murine-2-methyl-phenyl)-5-indole-based-π ratio. Ding-2-domain group]-amino]^-3-(2-mur-phenyl)-propionic acid (S)-3-{[6-(4-fluoro-2-indolyl-phenyl) -5-decyloxypyridinium-2-carbonyl]amine S}-3-(2-^-phenyl)-propionic acid (S)-3-{[6-(5-fluoro-2-decyloxy) -phenyl)-5-decyloxy-0 to 11-but-2-ylidene]-amino}-3-(2-a-phenyl)-propionic acid (S)-3-{[6-( 2-fluoro-5-methyl-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-(2-mur-phenyl)-propionic acid (8)-3-{ [6-(3-Gas-2-indolyl-phenyl)-5-methoxy-0-βσ-2-yl]-amino}-3-(2-mur-phenyl)-propyl Acid (S)-3 - {[6-(5.Chloro-2-y-phenyl)-5-decyloxy-° ratio. (2-amino)-amino)^-3-(2-a-phenyl)-propionic acid (S)-3-{[6-(3-chloro-2-fluoro-phenyl)-5 -decyloxypyridin-2-carbonyl]-amino}-3-(2-mur-phenyl)-propionic acid (S)-3-(2-fluoro-phenyl)-3-{[5- Methoxy-6-(2-methyl-furan-3-yl)-0 σ sigma-2-&gt;Carbo]-amino}-propionic acid (S)-3-{[6-(2 -ox-3-mercapto-phenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid (S)-3-(2 -Chloro-phenyl)-3-[(5-decyloxy-6-phenylpyridin-2-carbonyl)-227 201245154 Amino]-propionic acid (S)-3-(2-chloro-phenyl )-3-{[6-(2,4-Di-phenyl)-5-methoxy-. Than. (2)-(Carbonyl)-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(4-fluoro-phenyl)-5-decyloxy - acridine-2-monanyl]-amino}_propionic acid (S)-3-{[5-decyloxy-6-(3-trifluorodecyl-phenyl)-acridin-2- Carbonyl]-aminopyr-3-o-indolephenyl-propionic acid (S)-3-{[6-(2,4-dichloro-phenyl)-5-decyloxypyridin-2-carbonyl] -amino}-3-o-indolephenyl-propionic acid (S)-3-{[6-(4-gas-phenyl)-5-methoxy-0 to 0--2-yl] -amino}- 3_o-nonylphenyl-propionic acid (S)-3-{[6-(4-chloro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}- 3-o-indolyl-propionic acid (S)-3-[(5-methoxy-6-p-tolylpyridin-2-carbonyl)-amino]-3-o-tolyl-propanyl Acid (S)-3-{[6-(3-chloro-phenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S) -3-{[5-decyloxy-6-(2-decyloxy-phenyl)-acridin-2-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)- 3-[(5-Methoxy-6-m- phenylphenylpyridin-2-carbonyl)-amino]-3-o-indolephenyl-propionic acid (S)-3-{[6-( 2-Chloro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3-o-tolyl-propionic acid (S)-3-{[6-(3,4-di Fluoro-phenyl)-5-decyloxypyridin-2-carbonyl]-amine 228 201245154 }-3-o-indolephenyl-propionic acid (S)-3-{[6-(2,5-difluoro-phenyl)-5-methoxypyridinylcarbonyl]-amino}-3- o-Tolyl-propionic acid (S)-3-{[6-(2,5-di-phenyl)-5-methoxy-η-pyridyl J.carbonyl]amino}-3-o- Phenylphenyl-propionic acid (S)-3-{[6-(3,5-dimercapto-iso-4-oxazol-4-yl)-5-decyloxy-D-bitocarbonyl]-amino}- 3-o-tolyl-propionic acid (S)-3-{[6-(2,3-dimercapto-phenyl)-5-methoxy-n-pyridinyl-2-amino group}- 3-o-indolyl-propionic acid (S)-3-{[6-(2,4-dimercapto-phenyl)-5-decyloxybipyridine-2 —Carboaminoamine}-3 o-Phenylphenyl-propionic acid (S)-3-{[6-(4-|^2-decyloxy-phenyl)-5-decyloxy-u ratio. _2_2_罗炭基]-Amino}-3-o-tolyl-propionic acid (S)-3-{[6-(2-a-5-methyl-phenyl)-5-methoxy --η ratio α定_2-alkyl]_amino}-3-o-indolephenyl-propionic acid (S)-3-(2-a-phenyl)-3-[(6-oxime) Base-5-o-tolyl ratio carbonyl group)-amino]•propionic acid (S)-3-(2-a-phenyl)-3-{[5_曱oxy-6-(2_曱Oxy-phenyl)-n-pyridin-2-carbonyl]-amino}-propionic acid (S)-3-(2-a-phenyl)-3-[(5-decyloxy-6-m-曱Phenyl·.Bis _2_ carbonyl)-amino]-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(2-gas-phenyl)-5- Methoxy-bite_2_ benzyl]-amino}-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(2-fluoro-phenyl)-5- Methoxy·π|:|;^·2 229 201245154 carbonyl]-aminopropionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,4-dft) -phenyl)-5-decyloxy-吼α定-2-yl-)-amino}-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(2 , 3-diqi-phenyl)-5-decyloxyl ratio 17-butyryl]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[ 6-(2,3-Difluoro-phenyl)-5-methoxyl-mouth ratio-2-reactive]-amino}-propionic acid (S)-3-(2-chloro-phenyl) -3-{[6-(2,5-Difluoro-phenyl)-5-methoxyl ratio α-di-yl-amino]-amino}-propionic acid (S)-3-(2-Gas-phenyl)-3-{[6-(4-fluoro-2-indolyl-phenyl)-5-methoxy-0 ratio. (2-)-amino]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2,3-dimercapto-phenyl)-5 - 曱oxy-° ratio. (2)-reactive group-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-[(3,2'-dimethoxy-[2,3'] (pyridyl-6-carbonyl)-amino]-propionic acid (S)-3-(2-a-phenyl)-3-{[6-(5-Ga-2-methyl-phenyl)-5 -曱oxy_pyridine-2-carbonyl]-amino}-propionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(4-fluoro-2-decyloxy- Phenyl)-5-decyloxy-° ratio. (2)-Werki]-amino}-propionic acid (S)-3-{[6-(4-Ga-2-oxalyl-phenyl)-5-methoxy-acridine-2_ Carbonyl]•Amino}-3-(2-Gas-Benzyl)-propionic acid (S)-3-(2-Chloro-phenyl)-3-{[6-(5-fluoro-2-oxime (-phenyl)-5-methoxy-α-biti-2-chloro]-aminopropionic acid (S)-3-(2-chloro-phenyl)-3-{[6-(2- Fluoro-5-trifluoromethyl-phenyl)-5-indole 230 201245154 Oxy-p-pyridine-2-carbonyl]-amino}-propionic acid (S)-3-{[5-decyloxy-6 -(2-trifluoromethyl-phenyl)-0-pyridyl-2-ylcarbonyl]-aminobu-3-o-indolephenyl-propionic acid (S)-3-{[6-(2,4-di Fluoro-phenyl)-5-methoxy·°pyridin-2-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[6-(4-fluoro- 2-methyl-phenyl)-5-methoxypyridin-2-carbonyl]-amino}-3-o-tolyl-propionic acid (S)-3-[(3,2'-dimethyl Oxy-[2,3·]bipyridyl-6-carbonyl)-amino]-3-o-indolyl-propionic acid (S)-3-[(3·-fluoro-3-methoxy) _[2,4']bipyridyl-6-carbonyl)-amino]-3-o-indolephenyl-propionic acid (S)-3-{[5-methoxy-6-(2-oxime Base-0 Fu 0 South-3-base)-«» ratio. Benz-2-yl]_ 私}} o-tolyl-propionic acid (S)-3-{[6-(4-cyano-2-fluoro-phenyl)-5-decyloxy -η ratio pyridine_2·carbonyl]·amino}-3-o-tolyl-propionic acid (s)-3-(2-a-phenyl)_3-{[6-(2-fluoro-5- Methoxy-phenyl)_5·decyloxy-° ratio nitr-2-yl]-aminopropionic acid (S)-3-(2-gas-stupyl)_3-{[6-(2 -Fluoro-5-fluorenyl-phenyl)_5_methoxy- _ ° ratio _2·carbonyl]-amino}-propionic acid gas-2-methyl-phenyl)_5-methoxypyridinium _2_carbonyl]·Aminobu 3-(2·Ga-phenyl)·propionic acid (S)_3-(2·Ga·Phenyl)-3-{[6-(3-Fluoro-2-A Base-phenyl)_5_methoxyoxine ° than the heart_county]-aminopropionic acid thief · ) 3 {[6-(5-chloro-2-fluoro-phenyl)_5_methoxy^ ratio. _2_2·数基]-amine 231 201245154 】}-3-(2-gas·phenyl)-propionic acid (S)_3_(2_gas-phenyl)_3-[(3'_fluoro-3_曱oxy-[2,4']-linked σ ratio fl-based _6-|^ ano)-amino]-propionic acid (S)-3-(2-a-phenyl)-3-[(5 -曱oxy-6-pyridin-2·ylpyridin-2-carbonyl)-amino]•propionic acid (S)-3-{[6-(3-chloro-2-fluoro-phenyl) -5-decyloxypyridin-2-carbonyl]-amino}-3-(2- gas·phenyl)-propionic acid (S)-3-(2- gas-phenyl)_3·{[5 -Methoxy-6-(2-indolyl.f-amyl-3-yl)-pyridine-2-carbonyl]-aminopropionic acid (S)-3-{[6-(2-gas-3 - gas-phenyl)-5-methoxy-acridine_2-carbonyl]-amino}-3-(2-a-phenyl)-propionic acid (S)-3-{[6-(2 -ox-3-mercapto-phenyl)-5-decyloxypyridinyl-2-carbonyl]-amino}-3-(2-chloro-phenyl)-propionic acid 3-biphenyl-4-yl -3-[(6-gas ratio -2-yl)-amino]-propionic acid (S)-3_[(6-a-pyridine-2-carbonyl)-amino]_3_o-tolyl Propionic acid (S)-H (3,5-:amino group_6_gas-indole 2·carbonyl)_amino]_3 o-tolyl-propionic acid 3_biphenylyl yl-_[ (3,5-diamino _6_gas_吼耕_2•carbonyl)_amino]-propionic acid (S)-3-{[6-(2-fluoro-phenyl)-吼 bite_2 _ sylamino}}phenylpropionic acid (S)-3-(3-fluoro-phenyl fluoride ·Phenyl) 吼口定_2_基基]_Amino}-propionic acid 232 201245154 】}-propionic acid (S)-3-(4-fluoro-phenyl)-3 - {[6-(2 -fluoro-phenyl)-α ratio α-but-2-yl]-amino}-propionic acid 3-(2-chloro-phenyl)-3-[(6-decyloxy-indole-2- (carbonyl)-amino]-propionic acid (S)-3-[(6-methoxy-biphenyl-3-(carboyl)-amino]-3-o-indolephenyl-propionic acid (S) -3-{[6-(2-chloro-phenyl)-»bipyridine-2-carbonyl]-amino}-3-m-indolephenyl-propionic acid (S)-3-{[6-( 2-fluoro-phenyl)-. (bi)-2-carbonyl]-amino}-3-(4-decyloxy-phenyl)-propionic acid (S)-3-{[6-(2-chloro-phenyl)-acridine-2 -carbonyl]-amino}-3-(2-fluoro-phenyl)-propionic acid (S)-3 -{[6-(2- gas-phenyl)-° ratio -2- _ base] -amino}-3-(4-carb-phenyl)-propionic acid (S)-3-(3-a-phenyl)-3-{[6-(2"fluoro-phenyl)-acridine -2-carbonyl]-amino}-propionic acid (S)-3-(4-a-phenyl)-3 - {[6-(2-mur-phenyl)-n ratio °--2-# Carbon-]-amino}-propionic acid (S)-3-(4-a-phenyl)-3 - {[6-(2-chloro-phenyl)-° ratio α_^-2-yl] -Aminopropionic acid (S)-3-(3-a-phenyl)-3-{[6-(2-chloro-phenyl)-. Bis-pyridine-2-carbonyl]-aminopropionic acid 3-(2-indolyl)-3-{[6-(2- gas-phenyl)-amino}-propionic acid 233 201245154 ( S)-3 -{[6-(2- gas-phenyl)-0 ratio sigma-2-nonyl]-amino}-3-(3-disorder methyl-phenyl)-propionic acid ( S)-3 - {[6-(2-chloro-phenyl)-π ratio π-but-2-yl]-amino}-3-(2,4-di-phenyl)-propionic acid ( S)-3-{[6-(2-chloro-phenyl)-.~0-but-2-yl]-amino}-3-(4-dimethylhydrazine-phenyl)-propionic acid ( S)-3-{[6-(2-Gas-phenyl)-0 σ σ-2-phenyl]-amino}-3-(3-dimethylhydrazine-phenyl)-propionic acid ( S)-3-{[6-&gt;Smelly-5-(3,3-dimethyl-2-indolyl-butoxy^.Bit-to-prison-]-amino}-3-ortho -tolyl-propionic acid. 10. A compound of formula I, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, according to any one or more of claims 1 to 8 Selected from (S)-3-[(5-methoxy-6-phenyl"pyridin-2-carbonyl)-amino]-3-o-indole phenyl-propionic acid (S)-3- {[6-(2,3-Dimethyl-phenyl)-acridin-2-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[6-( 2-chloro-phenyl)-°pyridine-2-deradyl]-amino}-3-o-indolephenyl-propion (S)-3-{[6-(2- gas-phenyl)-°tba-but-2-yl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{ [6-(5-Gas-2-methyl-phenyl)-° ratio. D-B-Carbo]-amino}-3-o-indolephenyl-propionic acid (S)-3-ortho -tolyl-3-[(6-m-tolyl-fluorenylpyridin-2-yl)-amino] 234 201245154 Propionic acid (S)-3-({6-[3-(l-曱-1-fluorenyl-ethyl)-phenyl]-. than bite-to-domain}-amino)-3-o-tolyl-propionic acid (8)-3-(2,4-di Gas-phenyl)-3-[(5-methoxy-6-phenyl than sigma-2-ylamino)-propionic acid (S)-3-[(2,6-dimethoxy) 。-4-decyl)-amino]-3-o-indolephenyl-propionic acid (S)-3-[(5-phenyl-acridin-2-carbonyl)-amino]-3 -o-tolyl-propionic acid (S)-3-{[3-(4,6-dimethoxy-indenyl-2-yl)-. -3-}-3-o-indole phenyl-propionic acid (S)-3 - {[4-(β密11定-2-ylthioalkyl)-° ratio β定-2-几_基]-amine -3---3-o-tolyl-propionic acid (8)-3-{[5-(2,3-dichloro-phenyl)-° ratio 11--3-amino]-amino}-3 - o-Phenylphenyl-propionic acid (S)-3-{[5-(2,3-dimercapto-phenyl)-. (bi)-3-carbonyl]-amino}-3-o-indolephenyl-propionic acid (S)-3-{[5-(2- gas-yl)--0 ratio -3-yl-yl ]-Amino}·_3-o-tolyl-propionic acid (S)-3-{[6-(2,3-dimur-phenylindole-^~11--2-yl)-amino group }-3-o-indole-propionic acid (8)-3-{[6-(2-fluoro-5-methoxy-phenyl)-° ratio 11--2-carboyl]-month Anki}-3-o-indolephenyl-propionic acid (S)-3-{[6-(2-fluoro-5-methyl-phenyl)-0 ratio. Anki}-3-o-indole phenyl-propionic acid 235 201245154 (S)-3-{[6-(2-decyloxy-t-difluorodecyl-phenyl)-° ratio σ定-2_ (amino) 3-amino-p-phenyl-propionic acid (S)-3-({5-decyloxy-6-[3-(5-methyl-[1,3,4]. (2)-2-phenyl)-phenyl]pyridin-2-carbonyl}-amino)-3-o-indolephenyl-propionic acid (S)-3-(2-chloro-phenyl)-3 -[(5-methoxy-6-naphthalen-2-ylpyridin-2-carbonyl)-amino]-propionic acid (S)-3-(2-carbyl)-3-[(5-曱乳--6-σ ratio 〇井-2-基比咬-2-罗炭基)-amino]-propionic acid (8)-3-(2-chloro-phenyl)-3-[(6 -methoxy-5-n-2-yl-0-pyridin-3-yl)-amino]-propionic acid (S)-3-(2-chloro-phenyl)-3-{[5 -decyloxy-6-(2-indolyl-furan-3-yl)-indenyl-2-pyridyl]-amino}-propionic acid (S) -3-(2-chloro-phenyl)-3-{[6-(2,3-dimethyl-phenyl)-5-decyloxy.pyridine-2-carbonyl]-aminopropionic acid ( S)-3-(2-Gas-phenyl)-3-{[6-(2-Ga-phenyl)-5-methoxy-n-pyridin-2-yl]-amino}-propyl Acid (S)-3-(2-fluoro-phenyl)·3-{[5-decyloxy-6-(1,3,5-tridecyl-1Η-pyrazol-4-yl)-pyridine -2-carbonyl]-aminopropionic acid (S)-3-(2-fluoro-phenyl)-3-{[5-decyloxy-6-(1-indolyl-1Η-吲哚-5 -yl)-pyridyl-2-carbonyl]-amino}-propionic acid (S)-3-[(5-decyloxy-6-m-nonylphenylpyridin-2-carbonyl)-amino group ]-3-O-Phenylphenyl-propionic acid (S)-3-{[6-(2-chloro-phenyl)-5-decyloxypyridin-2-carbonyl]-amino}-3- O--p-styl-propionic acid 236 201245154 (S)-3-{[6-(3,5-dimercapto-isoxazol-4-yl)_5_decyloxy_D ratio bite_2·carbonyl ]-Amino}-3-o-tolyl-propionic acid (S)-3-{[6-(4-a-phenyl)-5-decyloxy group bite · 2 carbonyl] 3· o-Phenylphenyl-propionic acid (S)-3-{[6-(4-chloro-phenyl)-5-decyloxybipyridine-2·carbonylaminobub3_p-tolyl-propyl Acid (S)-3-{[6-(5-ethinylthiophen-2-yl)-5-methoxy-11 ratio. _2_2_几基]月女基}-3-(2-Ga-phenyl)-propionic acid (S)-3-{[6-(2-fluoro-phenyl)-5·decyloxy ratio Acridine·2—carbonyl]•Aminodi 3_o-indolephenyl-propionic acid. A method for the preparation of a compound of the formula I, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, according to any one or more of the scope of claims 1 to 3, which comprises a compound of the formula π and Compound of formula III, one , D, E, L, G, The arsenic of the arsenic can be protected or in the form of a precursor group in the compound of the formula; it is a muscle-〇- or a halogen group. Where are the groups A, D, Ε R 10. n40_ T.50 in the compounds of the formulae II and III « ^60 = ... 237 201245154 12. According to the scope of the patent application! To a compound of the compound or a physiologically acceptable salt thereof or any phytate thereof which is physiologically used as a pharmaceutical. And L3 first, which comprises at least one compound of formula I according to any one or more of the patent applications, or a physiologically acceptable salt thereof, or any physiologically acceptable solvate thereof, and pharmaceutically acceptable Carrier. 14. A compound according to any one or more of claims 1 to 10, a compound I or a physiologically acceptable salt thereof or any physiologically pharmaceutically acceptable agent thereof for the treatment of heart failure, congestive depletion, myocardial infarction, Left ventricular dysfunction, cardiac hypertrophy, persistent disease, hypertension, atherosclerosis, peripheral arterial occlusive disease: restenosis, vascular permeability disease, treatment of edema, thrombosis, type of wet arthritis, f arthritis, renal function 2, cystic fibrosis, chronic bronchitis, chronic obstructive pulmonary disease, n and immune diseases, diabetic complications, fibrotic diseases, pain, blood or reperfusion injury or neurodegenerative diseases, Or heart protection or kidney protection or as a diuretic (either alone or in combination with existing agents). 238 201245154 IV. Designated representative map: (1) The representative representative of the case is: (No). (2) A brief description of the symbol of the representative figure: Benefits 5. If there is a chemical formula in this case, please disclose the chemical formula that best shows the characteristics of the invention = R10 3