ZA200509634B - Heterocycle substituted carboxylic acids - Google Patents
Heterocycle substituted carboxylic acids Download PDFInfo
- Publication number
- ZA200509634B ZA200509634B ZA200509634A ZA200509634A ZA200509634B ZA 200509634 B ZA200509634 B ZA 200509634B ZA 200509634 A ZA200509634 A ZA 200509634A ZA 200509634 A ZA200509634 A ZA 200509634A ZA 200509634 B ZA200509634 B ZA 200509634B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- phenyl
- alkoxy
- groups
- halogen
- Prior art date
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- 125000000623 heterocyclic group Chemical group 0.000 title description 4
- 150000001735 carboxylic acids Chemical class 0.000 title description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 454
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 206
- 125000003545 alkoxy group Chemical group 0.000 claims description 150
- -1 arylalkanoyl Chemical group 0.000 claims description 126
- 229910052736 halogen Inorganic materials 0.000 claims description 125
- 150000002367 halogens Chemical class 0.000 claims description 124
- 150000001875 compounds Chemical class 0.000 claims description 114
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 72
- 125000001188 haloalkyl group Chemical group 0.000 claims description 61
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 56
- 125000001589 carboacyl group Chemical group 0.000 claims description 30
- 125000005037 alkyl phenyl group Chemical group 0.000 claims description 27
- 125000004122 cyclic group Chemical group 0.000 claims description 27
- 125000001041 indolyl group Chemical group 0.000 claims description 25
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 21
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 19
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 18
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 18
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 18
- 125000003386 piperidinyl group Chemical group 0.000 claims description 16
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims description 14
- 125000001624 naphthyl group Chemical group 0.000 claims description 13
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 13
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 11
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 11
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 10
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 10
- 125000002757 morpholinyl group Chemical group 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000000335 thiazolyl group Chemical group 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 7
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 7
- 125000001984 thiazolidinyl group Chemical group 0.000 claims description 7
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 6
- 125000005400 pyridylcarbonyl group Chemical group N1=C(C=CC=C1)C(=O)* 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 229920000728 polyester Polymers 0.000 claims description 5
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 4
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 4
- 125000004193 piperazinyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 3
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 3
- 229910014585 C2-Ce Inorganic materials 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000004988 dibenzothienyl group Chemical group C1(=CC=CC=2SC3=C(C21)C=CC=C3)* 0.000 claims description 2
- 125000005045 dihydroisoquinolinyl group Chemical group C1(NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 125000004627 thianthrenyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3SC12)* 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 29
- 239000002253 acid Substances 0.000 claims 5
- 229960002429 proline Drugs 0.000 claims 5
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 4
- 235000019260 propionic acid Nutrition 0.000 claims 4
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000000593 indol-1-yl group Chemical group [H]C1=C([H])C([H])=C2N([*])C([H])=C([H])C2=C1[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 3
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- WKFQZPSGKSPAAJ-SLXAZOFISA-N (2s)-1-[4-[4-(2-benzyl-1-benzofuran-3-yl)phenyl]benzoyl]-3-phenylpyrrolidine-2-carboxylic acid Chemical compound C=1C=CC=CC=1C([C@H]1C(=O)O)CCN1C(=O)C(C=C1)=CC=C1C(C=C1)=CC=C1C(C1=CC=CC=C1O1)=C1CC1=CC=CC=C1 WKFQZPSGKSPAAJ-SLXAZOFISA-N 0.000 claims 1
- QILVTHVZKUECAE-DEOSSOPVSA-N (2s)-1-[4-[[4-(4-chlorophenyl)-5-(4-ethylphenyl)-1,3-thiazol-2-yl]carbamoyl]phenyl]sulfonylpyrrolidine-2-carboxylic acid Chemical compound C1=CC(CC)=CC=C1C1=C(C=2C=CC(Cl)=CC=2)N=C(NC(=O)C=2C=CC(=CC=2)S(=O)(=O)N2[C@@H](CCC2)C(O)=O)S1 QILVTHVZKUECAE-DEOSSOPVSA-N 0.000 claims 1
- SHZGCJCMOBCMKK-GASJEMHNSA-N (3r,4s,5s,6r)-6-methyloxane-2,3,4,5-tetrol Chemical compound C[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O SHZGCJCMOBCMKK-GASJEMHNSA-N 0.000 claims 1
- DSPHFASHOJAOKN-UHFFFAOYSA-N 1-[(7-oxobenzo[a]phenalen-2-yl)amino]anthracene-9,10-dione Chemical compound C1=CC2=CC(NC3=C4C(=O)C5=CC=CC=C5C(C4=CC=C3)=O)=CC(C=3C(=CC=CC=3)C3=O)=C2C3=C1 DSPHFASHOJAOKN-UHFFFAOYSA-N 0.000 claims 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 1
- XNPJAGIPNLESFM-UHFFFAOYSA-N 2-[2-[4-[4-(2-benzyl-1-benzofuran-3-yl)phenyl]benzoyl]-3,4-dihydro-1h-isoquinolin-1-yl]acetic acid Chemical compound C1CC2=CC=CC=C2C(CC(=O)O)N1C(=O)C(C=C1)=CC=C1C(C=C1)=CC=C1C(C1=CC=CC=C1O1)=C1CC1=CC=CC=C1 XNPJAGIPNLESFM-UHFFFAOYSA-N 0.000 claims 1
- JTDNNFYHEKEZMS-UHFFFAOYSA-N 2-[3-(4-dibenzofuran-4-ylphenyl)-5-(4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]acetic acid Chemical compound C1=CC(OC)=CC=C1C1=NN(CC(O)=O)C(C=2C=CC(=CC=2)C=2C=3OC4=CC=CC=C4C=3C=CC=2)C1 JTDNNFYHEKEZMS-UHFFFAOYSA-N 0.000 claims 1
- RCWORNKLVJZNNF-UHFFFAOYSA-N 2-[4-[4-(2-benzyl-1-benzofuran-3-yl)phenyl]benzoyl]-3,4-dihydro-1h-isoquinoline-3-carboxylic acid Chemical compound OC(=O)C1CC2=CC=CC=C2CN1C(=O)C(C=C1)=CC=C1C(C=C1)=CC=C1C(C1=CC=CC=C1O1)=C1CC1=CC=CC=C1 RCWORNKLVJZNNF-UHFFFAOYSA-N 0.000 claims 1
- SGVVBUQPJQYTJG-UHFFFAOYSA-N 2-[5-(4-dibenzofuran-4-ylphenyl)-3-(4-methoxyphenyl)pyrazol-1-yl]acetic acid Chemical compound C1=CC(OC)=CC=C1C1=NN(CC(O)=O)C(C=2C=CC(=CC=2)C=2C=3OC4=CC=CC=C4C=3C=CC=2)=C1 SGVVBUQPJQYTJG-UHFFFAOYSA-N 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000006201 3-phenylpropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- ICBZSKCTKKUQSY-YUWZRIFDSA-N 4-[(1r,2s)-1-hydroxy-2-(methylamino)propyl]phenol;hydrochloride Chemical compound Cl.CN[C@@H](C)[C@H](O)C1=CC=C(O)C=C1 ICBZSKCTKKUQSY-YUWZRIFDSA-N 0.000 claims 1
- 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- UWDQVEPXORTQFO-UHFFFAOYSA-N 5-chloro-3-methyl-1-benzothiophene Chemical compound C1=C(Cl)C=C2C(C)=CSC2=C1 UWDQVEPXORTQFO-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 101100247323 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) ras-2 gene Proteins 0.000 claims 1
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- HHLFWLYXYJOTON-UHFFFAOYSA-N glyoxylic acid Chemical compound OC(=O)C=O HHLFWLYXYJOTON-UHFFFAOYSA-N 0.000 claims 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229960002591 hydroxyproline Drugs 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 1
- HXEACLLIILLPRG-RXMQYKEDSA-N l-pipecolic acid Natural products OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 claims 1
- 125000003506 n-propoxy group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 16
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- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 description 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 description 1
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- BSFODEXXVBBYOC-UHFFFAOYSA-N 8-[4-(dimethylamino)butan-2-ylamino]quinolin-6-ol Chemical compound C1=CN=C2C(NC(CCN(C)C)C)=CC(O)=CC2=C1 BSFODEXXVBBYOC-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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MX (1) | MXPA05011539A (fr) |
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DE4221583A1 (de) * | 1991-11-12 | 1993-05-13 | Bayer Ag | Substituierte biphenylpyridone |
DE4407488A1 (de) * | 1994-03-07 | 1995-09-14 | Bayer Ag | Verwendung von Biphenyl- und Pyridylmethylpyridonen |
US6310081B1 (en) * | 1999-05-10 | 2001-10-30 | American Home Products Corporation | Biphenyl sulfonyl aryl carboxylic acids useful in the treatment of insulin resistance and hyperglycemia |
JP2004502775A (ja) | 2000-07-07 | 2004-01-29 | ノボ ノルディスク アクティーゼルスカブ | 非ヌクレオシド逆転写阻害剤抗レトロウイルス療法をモニターするための手段および方法 |
AU2001268951A1 (en) | 2000-07-07 | 2002-01-21 | Novo-Nordisk A/S | Modulators of protein tyrosine phosphatases (ptpases) |
MXPA01013326A (es) * | 2001-02-14 | 2002-08-26 | Warner Lambert Co | Bifenil sulfonamidas utiles como inhibisdores de metaloproteinasa de matriz. |
CA2523743A1 (fr) | 2003-04-30 | 2004-11-18 | The Institutes For Pharmaceutical Discovery, Llc | Acides carboxyliques substitues par des heterocycles |
-
2004
- 2004-04-30 CA CA002523743A patent/CA2523743A1/fr not_active Abandoned
- 2004-04-30 AU AU2004236249A patent/AU2004236249A1/en not_active Abandoned
- 2004-04-30 MX MXPA05011539A patent/MXPA05011539A/es not_active Application Discontinuation
- 2004-04-30 EP EP04751194A patent/EP1628970A2/fr not_active Withdrawn
- 2004-04-30 US US10/835,818 patent/US7329680B2/en not_active Expired - Fee Related
- 2004-04-30 JP JP2006514245A patent/JP2006525366A/ja active Pending
- 2004-04-30 WO PCT/US2004/013702 patent/WO2004099192A2/fr active Application Filing
-
2005
- 2005-11-29 ZA ZA200509634A patent/ZA200509634B/en unknown
-
2008
- 2008-02-12 US US12/029,708 patent/US20080146574A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
EP1628970A2 (fr) | 2006-03-01 |
MXPA05011539A (es) | 2006-01-23 |
US20080146574A1 (en) | 2008-06-19 |
WO2004099192A3 (fr) | 2005-01-13 |
US20050004114A1 (en) | 2005-01-06 |
JP2006525366A (ja) | 2006-11-09 |
CA2523743A1 (fr) | 2004-11-18 |
WO2004099192A2 (fr) | 2004-11-18 |
US7329680B2 (en) | 2008-02-12 |
AU2004236249A1 (en) | 2004-11-18 |
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