MXPA03002788A - Moduladores de receptor c5a de molecula pequena de alta afinidad. - Google Patents
Moduladores de receptor c5a de molecula pequena de alta afinidad.Info
- Publication number
- MXPA03002788A MXPA03002788A MXPA03002788A MXPA03002788A MXPA03002788A MX PA03002788 A MXPA03002788 A MX PA03002788A MX PA03002788 A MXPA03002788 A MX PA03002788A MX PA03002788 A MXPA03002788 A MX PA03002788A MX PA03002788 A MXPA03002788 A MX PA03002788A
- Authority
- MX
- Mexico
- Prior art keywords
- alkyl
- amino
- mono
- alkoxy
- optionally substituted
- Prior art date
Links
- 102000005590 Anaphylatoxin C5a Receptor Human genes 0.000 title abstract 4
- 108010059426 Anaphylatoxin C5a Receptor Proteins 0.000 title abstract 2
- 150000003384 small molecules Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 114
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 50
- 230000000694 effects Effects 0.000 claims abstract 3
- 239000005557 antagonist Substances 0.000 claims abstract 2
- -1 carbocyclic aryl Chemical group 0.000 claims 957
- 125000000217 alkyl group Chemical group 0.000 claims 684
- 125000003545 alkoxy group Chemical group 0.000 claims 373
- 229910052736 halogen Inorganic materials 0.000 claims 361
- 150000002367 halogens Chemical group 0.000 claims 361
- 125000001188 haloalkyl group Chemical group 0.000 claims 360
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 327
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 324
- 125000004093 cyano group Chemical group *C#N 0.000 claims 321
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 268
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 264
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 204
- 125000003282 alkyl amino group Chemical group 0.000 claims 200
- 229910052739 hydrogen Inorganic materials 0.000 claims 199
- 239000001257 hydrogen Substances 0.000 claims 199
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 194
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 188
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 167
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 154
- 125000000753 cycloalkyl group Chemical group 0.000 claims 153
- 125000003342 alkenyl group Chemical group 0.000 claims 117
- 125000000304 alkynyl group Chemical group 0.000 claims 109
- 125000004076 pyridyl group Chemical group 0.000 claims 105
- 125000001544 thienyl group Chemical group 0.000 claims 94
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 88
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 88
- 125000003373 pyrazinyl group Chemical group 0.000 claims 83
- 125000004663 dialkyl amino group Chemical group 0.000 claims 81
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 78
- 125000001041 indolyl group Chemical group 0.000 claims 77
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 75
- 125000000928 benzodioxinyl group Chemical group O1C(=COC2=C1C=CC=C2)* 0.000 claims 71
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 71
- 125000001624 naphthyl group Chemical group 0.000 claims 69
- 125000001424 substituent group Chemical group 0.000 claims 69
- 229910052760 oxygen Inorganic materials 0.000 claims 67
- 239000001301 oxygen Substances 0.000 claims 67
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 66
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 66
- 125000002619 bicyclic group Chemical group 0.000 claims 64
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 64
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 59
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 55
- 150000002148 esters Chemical class 0.000 claims 55
- 125000003710 aryl alkyl group Chemical group 0.000 claims 46
- 150000001735 carboxylic acids Chemical class 0.000 claims 46
- 125000002541 furyl group Chemical group 0.000 claims 46
- 125000005842 heteroatom Chemical group 0.000 claims 45
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 44
- 125000002883 imidazolyl group Chemical group 0.000 claims 43
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 43
- 125000000168 pyrrolyl group Chemical group 0.000 claims 43
- 125000003226 pyrazolyl group Chemical group 0.000 claims 42
- 125000001786 isothiazolyl group Chemical group 0.000 claims 41
- 125000000842 isoxazolyl group Chemical group 0.000 claims 41
- 125000002971 oxazolyl group Chemical group 0.000 claims 41
- 125000003831 tetrazolyl group Chemical group 0.000 claims 41
- 125000000335 thiazolyl group Chemical group 0.000 claims 41
- 125000001425 triazolyl group Chemical group 0.000 claims 41
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 40
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 40
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 39
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 38
- 125000003884 phenylalkyl group Chemical group 0.000 claims 36
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 34
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 34
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 32
- 125000000723 dihydrobenzofuranyl group Chemical group O1C(CC2=C1C=CC=C2)* 0.000 claims 31
- 125000000547 substituted alkyl group Chemical group 0.000 claims 31
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 claims 30
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 28
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 28
- 125000001977 isobenzofuranyl group Chemical group C=1(OC=C2C=CC=CC12)* 0.000 claims 27
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 27
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 27
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 26
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 24
- 229910052799 carbon Inorganic materials 0.000 claims 23
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 22
- 239000000651 prodrug Substances 0.000 claims 20
- 229940002612 prodrug Drugs 0.000 claims 20
- 150000001721 carbon Chemical group 0.000 claims 18
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 16
- 125000004122 cyclic group Chemical group 0.000 claims 16
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 15
- 125000002431 aminoalkoxy group Chemical group 0.000 claims 13
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 13
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 229910014585 C2-Ce Inorganic materials 0.000 claims 11
- 125000005422 alkyl sulfonamido group Chemical group 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 10
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 claims 9
- RMVRSNDYEFQCLF-UHFFFAOYSA-N thiophenol Chemical compound SC1=CC=CC=C1 RMVRSNDYEFQCLF-UHFFFAOYSA-N 0.000 claims 9
- 238000003556 assay Methods 0.000 claims 8
- 230000035605 chemotaxis Effects 0.000 claims 8
- 230000001404 mediated effect Effects 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 230000027425 release of sequestered calcium ion into cytosol Effects 0.000 claims 8
- 125000002837 carbocyclic group Chemical group 0.000 claims 7
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 7
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 7
- 239000002253 acid Substances 0.000 claims 6
- 150000003973 alkyl amines Chemical class 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 5
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 3
- 241000271569 Rhea Species 0.000 claims 3
- 125000002393 azetidinyl group Chemical group 0.000 claims 3
- 125000005605 benzo group Chemical group 0.000 claims 3
- 239000011575 calcium Substances 0.000 claims 3
- 125000005945 imidazopyridyl group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006730 (C2-C5) alkynyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- HJMZMZRCABDKKV-UHFFFAOYSA-N carbonocyanidic acid Chemical compound OC(=O)C#N HJMZMZRCABDKKV-UHFFFAOYSA-N 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 239000000306 component Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims 1
- KTZQTRPPVKQPFO-UHFFFAOYSA-N 1,2-benzoxazole Chemical group C1=CC=C2C=NOC2=C1 KTZQTRPPVKQPFO-UHFFFAOYSA-N 0.000 claims 1
- QABCDCRBWNTCGD-UHFFFAOYSA-N 1,2-dihydroazete Chemical compound C1NC=C1 QABCDCRBWNTCGD-UHFFFAOYSA-N 0.000 claims 1
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N 1H-imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 1
- VMJNTFXCTXAXTC-UHFFFAOYSA-N 2,2-difluoro-1,3-benzodioxole-5-carbonitrile Chemical group C1=C(C#N)C=C2OC(F)(F)OC2=C1 VMJNTFXCTXAXTC-UHFFFAOYSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 241000790917 Dioxys <bee> Species 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- RAXXELZNTBOGNW-UHFFFAOYSA-O Imidazolium Chemical compound C1=C[NH+]=CN1 RAXXELZNTBOGNW-UHFFFAOYSA-O 0.000 claims 1
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical group [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical group OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims 1
- 239000003513 alkali Substances 0.000 claims 1
- 150000001345 alkine derivatives Chemical class 0.000 claims 1
- 125000000033 alkoxyamino group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- SMWDFEZZVXVKRB-UHFFFAOYSA-O hydron;quinoline Chemical group [NH+]1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-O 0.000 claims 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical group C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000816 peptidomimetic Substances 0.000 claims 1
- 238000000159 protein binding assay Methods 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 150000003335 secondary amines Chemical class 0.000 claims 1
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- UWYZHKAOTLEWKK-UHFFFAOYSA-N tetrahydro-isoquinoline Natural products C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical class C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 108010078546 Complement C5a Proteins 0.000 abstract 2
- 239000003446 ligand Substances 0.000 abstract 2
- 239000000556 agonist Substances 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000011268 leukocyte chemotaxis Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- C07D207/327—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82B—NANOSTRUCTURES FORMED BY MANIPULATION OF INDIVIDUAL ATOMS, MOLECULES, OR LIMITED COLLECTIONS OF ATOMS OR MOLECULES AS DISCRETE UNITS; MANUFACTURE OR TREATMENT THEREOF
- B82B3/00—Manufacture or treatment of nanostructures by manipulation of individual atoms or molecules, or limited collections of atoms or molecules as discrete units
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
- C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
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- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C—CHEMISTRY; METALLURGY
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- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- H—ELECTRICITY
- H01—ELECTRIC ELEMENTS
- H01J—ELECTRIC DISCHARGE TUBES OR DISCHARGE LAMPS
- H01J1/00—Details of electrodes, of magnetic control means, of screens, or of the mounting or spacing thereof, common to two or more basic types of discharge tubes or lamps
- H01J1/02—Main electrodes
- H01J1/30—Cold cathodes, e.g. field-emissive cathode
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Applications Claiming Priority (1)
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| PCT/US2000/026816 WO2002049993A2 (en) | 2000-09-29 | 2000-09-29 | High affinity small molecule c5a receptor modulators |
Publications (1)
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| MXPA03002788A true MXPA03002788A (es) | 2004-12-13 |
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Family Applications (1)
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| MXPA03002788A MXPA03002788A (es) | 2000-09-29 | 2000-09-29 | Moduladores de receptor c5a de molecula pequena de alta afinidad. |
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| PA8535601A1 (es) | 2000-12-21 | 2002-11-28 | Pfizer | Derivados benzimidazol y piridilimidazol como ligandos para gabaa |
| CA2479928A1 (en) * | 2002-03-28 | 2003-10-09 | Neurogen Corporation | Substituted biaryl amides as c5a receptor modulators |
| WO2003082828A1 (en) | 2002-03-28 | 2003-10-09 | Neurogen Corporation | Substituted tetrahydroisoquinolines as c5a receptor modulators |
| US6858637B2 (en) | 2002-03-28 | 2005-02-22 | Neurogen Corporation | Substituted biaryl amides as C5a receptor modulators |
| JP2005528368A (ja) * | 2002-03-29 | 2005-09-22 | ニューロジェン・コーポレーション | C5a受容体モジュレータである新規なアリールイミダゾール及び関連化合物。 |
| GB0214139D0 (en) * | 2002-06-19 | 2002-07-31 | Glaxo Group Ltd | Chemical compounds |
| US7169775B2 (en) | 2002-08-21 | 2007-01-30 | Neurogen Corporation | Amino methyl imidazoles as C5a receptor modulators |
| JP3714948B2 (ja) | 2002-09-11 | 2005-11-09 | 呉羽化学工業株式会社 | アミン化合物及びその用途 |
| ATE552253T1 (de) | 2002-11-08 | 2012-04-15 | Novartis Int Pharm Ltd | 3-substituierte-6-aryl- pyridin derivate als liganden für c5a-rezeptoren |
| US8329169B2 (en) | 2003-05-15 | 2012-12-11 | Genentech, Inc. | Methods and compositions for the prevention and treatment of sepsis |
| CA2558600C (en) | 2004-03-10 | 2013-07-09 | Kureha Corporation | A substituted-trialkyl amine compound with anti-viral activity based on antagonism against a chemokine receptor cxcr4 |
| EP1814576A2 (en) * | 2004-07-20 | 2007-08-08 | Critical Therapeutics, Inc. | Combination therapies of hmgb and complement inhibitors against inflammation |
| JP2007284352A (ja) * | 2004-08-05 | 2007-11-01 | Dai Ichi Seiyaku Co Ltd | ピラゾール誘導体 |
| EP1817030A2 (en) | 2004-12-01 | 2007-08-15 | Kalypsys, Inc. | Inducible nitric oxide synthase dimerization inhibitors |
| AR052674A1 (es) | 2005-02-17 | 2007-03-28 | Wyeth Corp | Derivados de indol, benzotiofeno, benzofurano e indeno cicloalquilcondensados |
| EP1739078A1 (de) | 2005-05-30 | 2007-01-03 | Jerini AG | C5a-Rezeptor-Antagonisten |
| RS54998B1 (sr) | 2008-12-22 | 2016-11-30 | Chemocentryx Inc | Antagonisti c5ar |
| HRP20171176T1 (hr) | 2010-06-24 | 2017-10-06 | Chemocentryx, Inc. | C5ar antagonisti |
| BR112015026847A2 (pt) * | 2013-04-22 | 2017-07-25 | Abbvie Inc | tiazóis e usos dos mesmos |
| CN106999481B (zh) | 2014-09-29 | 2021-04-16 | 凯莫森特里克斯股份有限公司 | 制备C5aR拮抗剂的方法和中间体 |
| EP3072891A1 (en) * | 2015-03-24 | 2016-09-28 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | New Toll-Like Receptor 9 Antagonists |
| TWI791423B (zh) | 2016-01-14 | 2023-02-11 | 美商卡默森屈有限公司 | C3腎絲球病變之治療方法 |
| MA44629A (fr) | 2016-04-04 | 2021-03-24 | Chemocentryx Inc | Antagonistes de c5ar solubles |
| MA48803A (fr) | 2017-05-31 | 2020-04-08 | Chemocentryx Inc | Cycles 6-5 fusionnés utilisés en tant qu'inhibiteurs de c5a |
| MA48800A (fr) | 2017-05-31 | 2020-04-08 | Chemocentryx Inc | Cycles 5-5 fusionnés utilisés en tant qu'inhibiteurs de c5a |
| EP3703687A4 (en) | 2017-10-30 | 2021-04-07 | ChemoCentryx, Inc. | DEUTERATED COMPOUNDS USED AS IMMUNOMODULATORS |
| CN111788185B (zh) | 2017-12-22 | 2024-12-13 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的二芳基取代的6,5稠合环化合物 |
| MA51327A (fr) | 2017-12-22 | 2021-05-26 | Chemocentryx Inc | Composés cycliques fusionnés en 5,5 à substitution diaryle, utilisés en tant qu'inhibiteurs du c5ar |
| MA52245A (fr) | 2018-04-02 | 2021-04-28 | Chemocentryx Inc | Promédicaments d'antagonistes de c5ar bicycliques fusionnés |
| CN114957165A (zh) * | 2021-02-26 | 2022-08-30 | 清华大学 | 一种抗病毒化合物及其制备方法和应用 |
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| JPS6157590A (ja) * | 1984-08-29 | 1986-03-24 | Asahi Shiyueebell Kk | シラン化合物およびその製造法 |
| US5159083A (en) * | 1990-12-28 | 1992-10-27 | Neurogen Corporation | Certain aminomethyl phenylimidazole derivatives; a class of dopamine receptor subtype specific ligands |
| US5681956A (en) * | 1990-12-28 | 1997-10-28 | Neurogen Corporation | 4-aryl substituted piperazinylmethyl phenylimidazole derivatives; a new class of dopamine receptor subtype specific ligands |
| MX9308025A (es) * | 1992-12-22 | 1994-08-31 | Lilly Co Eli | Compuestos inhibidores de la proteasa del virus dela inmunodeficiencia humana, procedimiento para supreparacion y formulacion farmaceutica que los contiene. |
| US5652237A (en) * | 1994-09-09 | 1997-07-29 | Warner-Lambert Company | 2-substituted-4H-3, 1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease for the treatment of inflammatory processes |
| BR9509760A (pt) * | 1994-11-23 | 1998-06-30 | Neurogen Corp | Composto |
| GB9426103D0 (en) * | 1994-12-23 | 1995-02-22 | Merck Sharp & Dohme | Therapeutic agents |
| WO1998002434A1 (en) * | 1996-07-13 | 1998-01-22 | Glaxo Group Limited | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| EP1017382B1 (en) * | 1997-05-29 | 2006-03-01 | Merck & Co., Inc. (a New Jersey corp.) | Biarylalkanoic acids as cell adhesion inhibitors |
| MY153569A (en) * | 1998-01-20 | 2015-02-27 | Mitsubishi Tanabe Pharma Corp | Inhibitors of ?4 mediated cell adhesion |
| CN1181817C (zh) * | 1998-03-20 | 2004-12-29 | 第一三得利制药株式会社 | 以苯基甲苯醌为有效成分的NF-kB抑制剂 |
| ES2258331T3 (es) * | 1998-05-22 | 2006-08-16 | Scios Inc. | Compuestos heterociclicos y procedimientos de tratamiento de insuficiencia cardiaca y otros trastornos. |
| EP1097137A1 (en) * | 1998-07-10 | 2001-05-09 | AstraZeneca AB | N-substituted naphthalene carboxamides as neurokinin-receptor antagonists |
| US6423519B1 (en) * | 1998-07-15 | 2002-07-23 | Gpc Biotech Inc. | Compositions and methods for inhibiting fungal growth |
| AU743411B2 (en) * | 1998-08-21 | 2002-01-24 | Viropharma Incorporated | Compounds, compositions and methods for treating or preventing viral infections and associated diseases |
| US6437146B1 (en) * | 1998-09-25 | 2002-08-20 | Fujisawa Pharmaceutical Co., Ltd. | Oxazole compounds as prostaglandin e2 agonists or antagonists |
| EP1126843A4 (en) * | 1998-10-29 | 2005-06-15 | Bristol Myers Squibb Co | AMINO-CELL DERIVATIVE COMPOUNDS INHIBITORS OF ENZYME IMPDH |
| US6503905B1 (en) * | 1998-12-29 | 2003-01-07 | Pfizer Inc | 3,3-biarylpiperidine and 2,2-biarylmorpholine derivatives |
| PL350998A1 (en) * | 1999-03-24 | 2003-02-24 | Anormed Inc | Chemokine recpetor binding heterocyclic compounds |
| US6369226B1 (en) * | 1999-06-21 | 2002-04-09 | Agouron Pharmaceuticals, Inc. | Substituted benzamide inhibitors of rhinovirus 3C protease |
| ATE339406T1 (de) * | 1999-09-23 | 2006-10-15 | Astrazeneca Ab | Chinazoline verbindungen als heilmittel |
| DE60143457D1 (de) * | 2000-09-15 | 2010-12-23 | Anormed Inc | Chemokin Rezeptor bindende heterozyklische Verbindungen |
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| NO20031370L (no) | 2003-05-30 |
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| EP1322309B1 (en) | 2008-08-13 |
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| WO2002049993A2 (en) | 2002-06-27 |
| BR0017338A (pt) | 2004-04-27 |
| EP1322309A4 (en) | 2004-10-13 |
| WO2002049993A3 (en) | 2003-02-20 |
| IL154993A0 (en) | 2003-10-31 |
| KR20030060887A (ko) | 2003-07-16 |
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