JP2002541257A5 - - Google Patents
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- Publication number
- JP2002541257A5 JP2002541257A5 JP2000610853A JP2000610853A JP2002541257A5 JP 2002541257 A5 JP2002541257 A5 JP 2002541257A5 JP 2000610853 A JP2000610853 A JP 2000610853A JP 2000610853 A JP2000610853 A JP 2000610853A JP 2002541257 A5 JP2002541257 A5 JP 2002541257A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- aryl
- compound according
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 description 28
- 150000001875 compounds Chemical class 0.000 description 28
- 230000000875 corresponding Effects 0.000 description 17
- 125000003118 aryl group Chemical group 0.000 description 16
- 125000001072 heteroaryl group Chemical group 0.000 description 15
- 150000001204 N-oxides Chemical class 0.000 description 14
- 229910005965 SO 2 Inorganic materials 0.000 description 14
- 125000000753 cycloalkyl group Chemical group 0.000 description 12
- 150000002148 esters Chemical class 0.000 description 12
- 229910052739 hydrogen Inorganic materials 0.000 description 12
- 239000001257 hydrogen Substances 0.000 description 12
- 239000000651 prodrug Substances 0.000 description 12
- 229940002612 prodrugs Drugs 0.000 description 12
- -1 cycloalkenylalkyl Chemical group 0.000 description 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 10
- 125000002947 alkylene group Chemical group 0.000 description 9
- 230000002378 acidificating Effects 0.000 description 8
- 125000000524 functional group Chemical group 0.000 description 7
- 150000002431 hydrogen Chemical class 0.000 description 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 7
- 229910052760 oxygen Inorganic materials 0.000 description 7
- 125000003710 aryl alkyl group Chemical group 0.000 description 6
- 150000003839 salts Chemical class 0.000 description 6
- 239000011780 sodium chloride Substances 0.000 description 6
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 5
- 239000012453 solvate Substances 0.000 description 5
- 229910052717 sulfur Inorganic materials 0.000 description 5
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 description 4
- 125000004450 alkenylene group Chemical group 0.000 description 3
- 125000000304 alkynyl group Chemical group 0.000 description 3
- 125000004419 alkynylene group Chemical group 0.000 description 3
- 230000001668 ameliorated Effects 0.000 description 3
- 125000000732 arylene group Chemical group 0.000 description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 3
- 230000021164 cell adhesion Effects 0.000 description 3
- 125000000392 cycloalkenyl group Chemical group 0.000 description 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 3
- 125000002993 cycloalkylene group Chemical group 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 230000001404 mediated Effects 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- KPHMACREDSGBEK-UHFFFAOYSA-N 3-[5-[[2-[2-(2-methylanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-2-yl]butanoic acid Chemical compound C1=NC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C(=CC=CC=2)C)O2)C2=C1 KPHMACREDSGBEK-UHFFFAOYSA-N 0.000 description 2
- 208000006673 Asthma Diseases 0.000 description 2
- 125000004414 alkyl thio group Chemical group 0.000 description 2
- 125000004093 cyano group Chemical group *C#N 0.000 description 2
- 125000005724 cycloalkenylene group Chemical group 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 description 2
- 125000006588 heterocycloalkylene group Chemical group 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 125000004043 oxo group Chemical group O=* 0.000 description 2
- 125000000547 substituted alkyl group Chemical group 0.000 description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 description 1
- HZKFOQAVQRXXIS-UHFFFAOYSA-N 3-[5-[[2-(2-anilino-1,3-benzoxazol-6-yl)acetyl]amino]pyridin-2-yl]butanoic acid Chemical compound C1=NC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C=CC=CC=2)O2)C2=C1 HZKFOQAVQRXXIS-UHFFFAOYSA-N 0.000 description 1
- FFIFGJCAAORBLY-UHFFFAOYSA-N 3-[5-[[2-[2-(2-chloroanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-2-yl]butanoic acid Chemical compound C1=NC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C(=CC=CC=2)Cl)O2)C2=C1 FFIFGJCAAORBLY-UHFFFAOYSA-N 0.000 description 1
- CLPSFMAETRLPJT-UHFFFAOYSA-N 3-[5-[[2-[2-(2-methoxyanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-2-yl]butanoic acid Chemical compound COC1=CC=CC=C1NC(OC1=C2)=NC1=CC=C2CC(=O)NC1=CC=C(C(C)CC(O)=O)N=C1 CLPSFMAETRLPJT-UHFFFAOYSA-N 0.000 description 1
- NRQLBNIMMGKSJE-UHFFFAOYSA-N 3-[5-[[2-[2-(2-methylanilino)-3H-benzimidazol-5-yl]acetyl]amino]pyridin-2-yl]butanoic acid;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1=NC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C(=CC=CC=2)C)N2)C2=C1 NRQLBNIMMGKSJE-UHFFFAOYSA-N 0.000 description 1
- QEBMPSSBGWOGFB-UHFFFAOYSA-N 3-[5-[[2-[4-methyl-2-(2-methylanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-2-yl]butanoic acid Chemical compound C1=NC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC(C)=C(N=C(NC=2C(=CC=CC=2)C)O2)C2=C1 QEBMPSSBGWOGFB-UHFFFAOYSA-N 0.000 description 1
- DDVHIBFDBPGRSV-UHFFFAOYSA-N 3-[6-[[2-(2-anilino-1,3-benzoxazol-6-yl)acetyl]amino]pyridin-3-yl]butanoic acid Chemical compound N1=CC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C=CC=CC=2)O2)C2=C1 DDVHIBFDBPGRSV-UHFFFAOYSA-N 0.000 description 1
- AOLBSYQVGHVHAG-UHFFFAOYSA-N 3-[6-[[2-[2-(2-chloroanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-3-yl]butanoic acid Chemical compound N1=CC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C(=CC=CC=2)Cl)O2)C2=C1 AOLBSYQVGHVHAG-UHFFFAOYSA-N 0.000 description 1
- HTFKAMFYXWBFIM-UHFFFAOYSA-N 3-[6-[[2-[2-(2-methoxyanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-3-yl]butanoic acid Chemical compound COC1=CC=CC=C1NC(OC1=C2)=NC1=CC=C2CC(=O)NC1=CC=C(C(C)CC(O)=O)C=N1 HTFKAMFYXWBFIM-UHFFFAOYSA-N 0.000 description 1
- OYHMQPKSWPLBLQ-UHFFFAOYSA-N 3-[6-[[2-[2-(2-methylanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-3-yl]butanoic acid Chemical compound N1=CC(C(CC(O)=O)C)=CC=C1NC(=O)CC1=CC=C(N=C(NC=2C(=CC=CC=2)C)O2)C2=C1 OYHMQPKSWPLBLQ-UHFFFAOYSA-N 0.000 description 1
- PEDWWPLZSFETTA-UHFFFAOYSA-N 3-[6-[[2-[2-(3-methoxyanilino)-1,3-benzoxazol-6-yl]acetyl]amino]pyridin-3-yl]butanoic acid Chemical compound COC1=CC=CC(NC=2OC3=CC(CC(=O)NC=4N=CC(=CC=4)C(C)CC(O)=O)=CC=C3N=2)=C1 PEDWWPLZSFETTA-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 125000004442 acylamino group Chemical group 0.000 description 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 description 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 125000005530 alkylenedioxy group Chemical group 0.000 description 1
- 125000003275 alpha amino acid group Chemical group 0.000 description 1
- 125000003435 aroyl group Chemical group 0.000 description 1
- 125000005239 aroylamino group Chemical group 0.000 description 1
- 125000005018 aryl alkenyl group Chemical group 0.000 description 1
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 description 1
- 125000004659 aryl alkyl thio group Chemical group 0.000 description 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 description 1
- 125000005015 aryl alkynyl group Chemical group 0.000 description 1
- 125000004350 aryl cycloalkyl group Chemical group 0.000 description 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 1
- 125000005135 aryl sulfinyl group Chemical group 0.000 description 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 description 1
- 125000005110 aryl thio group Chemical group 0.000 description 1
- 125000004104 aryloxy group Chemical group 0.000 description 1
- 125000004429 atoms Chemical group 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 description 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 description 1
- 125000005518 carboxamido group Chemical group 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 125000001475 halogen functional group Chemical group 0.000 description 1
- 125000004447 heteroarylalkenyl group Chemical group 0.000 description 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 description 1
- 125000005312 heteroarylalkynyl group Chemical group 0.000 description 1
- 125000005553 heteroaryloxy group Chemical group 0.000 description 1
- 200000000018 inflammatory disease Diseases 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
- 239000000546 pharmaceutic aid Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 125000005017 substituted alkenyl group Chemical group 0.000 description 1
- 125000004426 substituted alkynyl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 125000004434 sulfur atoms Chemical group 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9908355.2 | 1999-04-12 | ||
| GBGB9908355.2A GB9908355D0 (en) | 1999-04-12 | 1999-04-12 | Chemical compounds |
| US14147099P | 1999-06-29 | 1999-06-29 | |
| US9908355.2 | 1999-06-29 | ||
| US60/141,470 | 1999-06-29 | ||
| PCT/GB2000/001393 WO2000061580A1 (en) | 1999-04-12 | 2000-04-12 | Substituted bicyclic heteroaryl compounds as integrin antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002541257A JP2002541257A (ja) | 2002-12-03 |
| JP2002541257A5 true JP2002541257A5 (ru) | 2007-05-24 |
| JP4864206B2 JP4864206B2 (ja) | 2012-02-01 |
Family
ID=10851398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000610853A Expired - Lifetime JP4864206B2 (ja) | 1999-04-12 | 2000-04-12 | インテグリンアンタゴニストとしての置換された二環式ヘテロアリール化合物 |
Country Status (6)
| Country | Link |
|---|---|
| JP (1) | JP4864206B2 (ru) |
| CR (1) | CR6559A (ru) |
| EA (1) | EA200101067A1 (ru) |
| GB (1) | GB9908355D0 (ru) |
| YU (1) | YU71501A (ru) |
| ZA (1) | ZA200108302B (ru) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006056830A (ja) * | 2004-08-20 | 2006-03-02 | Dai Ichi Seiyaku Co Ltd | ２−アリールアミノベンゾオキサゾール誘導体 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU674553B2 (en) * | 1992-10-14 | 1997-01-02 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| AU675689B2 (en) * | 1992-12-01 | 1997-02-13 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| MX9801716A (es) * | 1995-08-30 | 1998-05-31 | Searle & Co | Derivados de meta-guanidina, urea, tiourea o acido aminobenzoico azaciclico, como antagonistas de integrina. |
| IL125033A0 (en) * | 1995-12-29 | 1999-01-26 | Smithkline Beecham Corp | Vitronectin receptor antagonists |
| JP4373497B2 (ja) * | 1996-06-19 | 2009-11-25 | ローン−プーラン・ロレ・リミテツド | 置換されたアザビシクロ化合物、ならびにｔｎｆおよびサイクリックａｍｐホスホジエステラーゼ産生の阻害剤としてのそれらの使用 |
| EP1007026A4 (en) * | 1997-01-17 | 2002-08-07 | Merck & Co Inc | INTEGRIN ANTAGONISTS |
| NZ507292A (en) * | 1998-04-10 | 2003-12-19 | G | Heterocyclic glycyl beta-alanine derivatives useful as vitronectin antagonists |
| DK1153017T3 (da) * | 1999-02-16 | 2006-07-17 | Aventis Pharma Ltd | Bicykliske forbindelser og deres anvendelse som integrinreceptorligander |
| GB9910394D0 (en) * | 1999-05-05 | 1999-07-07 | Rhone Poulenc Rorer Ltd | Chemical compounds |
-
1999
- 1999-04-12 GB GBGB9908355.2A patent/GB9908355D0/en not_active Ceased
-
2000
- 2000-04-12 YU YU71501A patent/YU71501A/sh unknown
- 2000-04-12 JP JP2000610853A patent/JP4864206B2/ja not_active Expired - Lifetime
- 2000-04-12 EA EA200101067A patent/EA200101067A1/ru unknown
-
2001
- 2001-10-09 ZA ZA200108302A patent/ZA200108302B/xx unknown
-
2002
- 2002-01-23 CR CR6559A patent/CR6559A/es not_active Application Discontinuation
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