JP2005002129A5 - - Google Patents
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- Publication number
- JP2005002129A5 JP2005002129A5 JP2004225107A JP2004225107A JP2005002129A5 JP 2005002129 A5 JP2005002129 A5 JP 2005002129A5 JP 2004225107 A JP2004225107 A JP 2004225107A JP 2004225107 A JP2004225107 A JP 2004225107A JP 2005002129 A5 JP2005002129 A5 JP 2005002129A5
- Authority
- JP
- Japan
- Prior art keywords
- treatment
- benzyloxycarbonyl
- amino
- use according
- tetrahydrothieno
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 208000002193 Pain Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 230000004224 protection Effects 0.000 claims 5
- 230000005961 cardioprotection Effects 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 210000000653 nervous system Anatomy 0.000 claims 3
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 2
- 208000003734 Supraventricular Tachycardia Diseases 0.000 claims 2
- 238000009098 adjuvant therapy Methods 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 238000002399 angioplasty Methods 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- GULCAVRIFKAGBA-UHFFFAOYSA-N benzyl 2-amino-3-(4-chlorobenzoyl)-5,7-dihydro-4h-thieno[2,3-c]pyridine-6-carboxylate Chemical compound NC=1SC=2CN(C(=O)OCC=3C=CC=CC=3)CCC=2C=1C(=O)C1=CC=C(Cl)C=C1 GULCAVRIFKAGBA-UHFFFAOYSA-N 0.000 claims 2
- FDOKFNOHDQGWHZ-UHFFFAOYSA-N benzyl 2-amino-3-(4-fluorobenzoyl)-5,7-dihydro-4h-thieno[2,3-c]pyridine-6-carboxylate Chemical compound NC=1SC=2CN(C(=O)OCC=3C=CC=CC=3)CCC=2C=1C(=O)C1=CC=C(F)C=C1 FDOKFNOHDQGWHZ-UHFFFAOYSA-N 0.000 claims 2
- GAOXTEDKYOARFC-UHFFFAOYSA-N benzyl 2-amino-3-(4-phenylbenzoyl)-5,7-dihydro-4h-thieno[2,3-c]pyridine-6-carboxylate Chemical compound NC=1SC=2CN(C(=O)OCC=3C=CC=CC=3)CCC=2C=1C(=O)C(C=C1)=CC=C1C1=CC=CC=C1 GAOXTEDKYOARFC-UHFFFAOYSA-N 0.000 claims 2
- SWMIKGPXARWYGZ-UHFFFAOYSA-N benzyl 2-amino-3-benzoyl-5,7-dihydro-4h-thieno[2,3-c]pyridine-6-carboxylate Chemical compound NC=1SC=2CN(C(=O)OCC=3C=CC=CC=3)CCC=2C=1C(=O)C1=CC=CC=C1 SWMIKGPXARWYGZ-UHFFFAOYSA-N 0.000 claims 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 2
- 125000001589 carboacyl group Chemical group 0.000 claims 2
- 230000000747 cardiac effect Effects 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 235000021588 free fatty acids Nutrition 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 125000005179 haloacetyl group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 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 claims 2
- 238000010253 intravenous injection Methods 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 230000005923 long-lasting effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 2
- 102000009346 Adenosine receptors Human genes 0.000 claims 1
- 108050000203 Adenosine receptors Proteins 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 238000001467 acupuncture Methods 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 238000007675 cardiac surgery Methods 0.000 claims 1
- 230000009137 competitive binding Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- GSYSFVSGPABNNL-UHFFFAOYSA-N methyl 2-dimethoxyphosphoryl-2-(phenylmethoxycarbonylamino)acetate Chemical group COC(=O)C(P(=O)(OC)OC)NC(=O)OCC1=CC=CC=C1 GSYSFVSGPABNNL-UHFFFAOYSA-N 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 1
- 230000029537 positive regulation of insulin secretion Effects 0.000 claims 1
- 230000035945 sensitivity Effects 0.000 claims 1
- 230000009861 stroke prevention Effects 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/959,758 US5939432A (en) | 1997-10-29 | 1997-10-29 | Thiophenes useful for modulating the adenosine receptor |
| US09/156,077 US6323214B1 (en) | 1997-10-29 | 1998-09-17 | Allosteric adenosine receptor modulators |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000517772A Division JP2003517429A (ja) | 1997-10-29 | 1998-09-30 | アロステリックアデノシン受容体修飾物質 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005002129A JP2005002129A (ja) | 2005-01-06 |
| JP2005002129A5 true JP2005002129A5 (enExample) | 2005-11-17 |
Family
ID=25502368
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000517772A Pending JP2003517429A (ja) | 1997-10-29 | 1998-09-30 | アロステリックアデノシン受容体修飾物質 |
| JP2004225107A Pending JP2005002129A (ja) | 1997-10-29 | 2004-08-02 | アロステリックアデノシン受容体修飾物質 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000517772A Pending JP2003517429A (ja) | 1997-10-29 | 1998-09-30 | アロステリックアデノシン受容体修飾物質 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US5939432A (enExample) |
| EP (1) | EP1025106B1 (enExample) |
| JP (2) | JP2003517429A (enExample) |
| AT (1) | ATE330959T1 (enExample) |
| AU (1) | AU9671798A (enExample) |
| CA (1) | CA2302396C (enExample) |
| WO (1) | WO1999021617A2 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6727258B2 (en) * | 1997-10-29 | 2004-04-27 | King Pharmaceutical Research & Development, Inc. | Allosteric adenosine receptor modulators |
| DE19947154A1 (de) * | 1999-10-01 | 2001-10-04 | Bayer Ag | Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung |
| JP4502435B2 (ja) * | 1999-11-30 | 2010-07-14 | 興和創薬株式会社 | ４，５，６，７−テトラヒドロチエノ〔２，３−ｃ〕ピリジン系化合物 |
| JP4548882B2 (ja) * | 1999-11-30 | 2010-09-22 | 興和創薬株式会社 | ４，５，６，７−テトラヒドロチエノ〔２，３−ｃ〕ピリジン化合物 |
| JP4548884B2 (ja) * | 1999-12-03 | 2010-09-22 | 興和創薬株式会社 | ４，５，６，７−テトラヒドロチエノ〔２，３−ｃ〕ピリジン誘導体 |
| CA2414623A1 (en) * | 2000-08-01 | 2002-02-07 | University Of Virginia Patent Foundation | Use of selective adenosine a1 receptor agonists, antagonists and allosteric enhancers to manipulate angiogenesis |
| US6489356B2 (en) * | 2000-09-05 | 2002-12-03 | Edward Leung | Method for treating pain in humans |
| US6248774B1 (en) * | 2000-09-05 | 2001-06-19 | King Pharmaceuticals Research & Development, Inc. | Method for treating hyper-excited sensory nerve functions in humans |
| GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
| GB0100620D0 (en) * | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical cokpounds V |
| GB0100624D0 (en) * | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| GB0100621D0 (en) * | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VI |
| US20020115635A1 (en) * | 2001-02-21 | 2002-08-22 | Pnina Fishman | Modulation of GSK-3beta activity and its different uses |
| JP4303474B2 (ja) | 2001-03-30 | 2009-07-29 | キング・ファーマシューティカルズ・インコーポレイティッド | 医薬活性のある化合物及び使用方法 |
| US6713638B2 (en) * | 2001-05-18 | 2004-03-30 | Joel M. Linden | 2-amino-3-aroyl-4,5 alkylthiophenes: agonist allosteric enhancers at human A1 adenosine receptors |
| CA2469872A1 (en) | 2001-12-12 | 2003-07-03 | F. Hoffmann-La Roche Ag | Benzothiophenes as adenosine receptor modulators |
| EP1583530A4 (en) * | 2002-01-16 | 2008-07-23 | Univ Virginia | 2-AMINOTHIAZOLE ALLOSTERIC AMPLIFIERS OF A1 ADENOSINE RECEPTORS |
| US20040121406A1 (en) * | 2002-05-23 | 2004-06-24 | Wilson Constance Neely | Methods and formulations for increasing the affinity of a1 adenosine receptor ligands for the a1 adenosine receptor |
| EP1633756B1 (en) | 2003-04-09 | 2008-12-24 | Biogen Idec MA Inc. | A2a adenosine receptor antagonists |
| US7285550B2 (en) | 2003-04-09 | 2007-10-23 | Biogen Idec Ma Inc. | Triazolotriazines and pyrazolotriazines and methods of making and using the same |
| WO2004092177A1 (en) | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | Triazolopyrazines and methods of making and using the same |
| US8062272B2 (en) * | 2004-05-21 | 2011-11-22 | Bluesky Medical Group Incorporated | Flexible reduced pressure treatment appliance |
| KR20090112627A (ko) * | 2006-11-13 | 2009-10-28 | 킹 파머슈티칼스 리서치 앤드 디벨로프먼트 아이엔씨 | 에이1 아데노신 수용체의 알로스테릭 조절제 |
| US7855209B2 (en) * | 2006-11-13 | 2010-12-21 | King Pharmaceuticals Research And Development, Inc. | Allosteric modulators of the A1 adenosine receptor |
| US7897596B2 (en) * | 2006-11-13 | 2011-03-01 | King Pharmaceuticals Research & Development, Inc. | Allosteric modulators of the A1 adenosine receptor |
| PA8801401A1 (es) * | 2007-10-25 | 2009-05-15 | Janssen Pharmaceutica Nv | Arilindenopirimidinas y su uso como adenosina a2a |
| GB0722340D0 (en) * | 2007-11-14 | 2007-12-27 | Univ Leiden | Sphingosine-1-phosphate (S1P) receptor compounds |
| US20090281145A1 (en) * | 2008-05-08 | 2009-11-12 | Pier Giovanni Baraldi | Allosteric enhancers of the a1 adenosine receptor |
| GB0906579D0 (en) | 2009-04-16 | 2009-05-20 | Vernalis R&D Ltd | Pharmaceuticals, compositions and methods of making and using the same |
| US20100093714A1 (en) * | 2008-10-13 | 2010-04-15 | Devraj Chakravarty | AMIDES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| US20100093702A1 (en) * | 2008-10-13 | 2010-04-15 | Barbay J Kent | METHYLENE AMINES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| US20100093763A1 (en) * | 2008-10-13 | 2010-04-15 | Barbay J Kent | PHENYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINES AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| WO2011010306A1 (en) | 2009-07-21 | 2011-01-27 | Ramot At Tel-Aviv University Ltd. | A3 adenosine receptor ligands for modulation of pigmentation |
| CN113874015B (zh) | 2018-12-21 | 2024-05-24 | 细胞基因公司 | Ripk2的噻吩并吡啶抑制剂 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH540247A (de) * | 1967-04-21 | 1973-09-28 | Ciba Geigy Ag | Verfahren zur Herstellung von heterocyclischen, Asthylendoppelbindungen enthaltenden Verbindungen |
| ES393101A1 (es) * | 1971-07-09 | 1974-05-16 | Made Labor Sa | Procedimiento para la preparacion de derivados de tieno- diazepina. |
| FI54312C (fi) * | 1972-05-09 | 1978-11-10 | Sumitomo Chemical Co | Foerfarande foer framstaellning av tieno-(2,3-d)pyrimidinderivat med avsoendring av urinsyra i urin utoekande |
| JPS5342400B2 (enExample) | 1973-05-30 | 1978-11-10 | ||
| PH30676A (en) | 1986-07-22 | 1997-09-16 | Boehringer Ingelhein Kg | Hetrazepine compounds which have useful pharmaceutical utility |
| CH677511A5 (enExample) * | 1988-10-12 | 1991-05-31 | Mefina Sa | |
| US5026698A (en) | 1988-11-02 | 1991-06-25 | Nissan Chemical Industries, Ltd. | Thienopyridine type mevalonolactones |
| CA2020806A1 (en) * | 1989-07-12 | 1991-01-13 | Karl-Heinz Weber | Thienodiazepine derivatives |
| KR100255493B1 (ko) * | 1991-10-11 | 2000-08-01 | 가마쿠라 아키오 | 골조송증 치료제 |
| JPH05345785A (ja) * | 1992-01-16 | 1993-12-27 | Yoshitomi Pharmaceut Ind Ltd | トリアゾロオキサゼピン化合物 |
| TW263498B (enExample) * | 1993-11-10 | 1995-11-21 | Takeda Pharm Industry Co Ltd | |
| JPH07304755A (ja) * | 1994-05-12 | 1995-11-21 | Yamanouchi Pharmaceut Co Ltd | 縮合ジアゼピン誘導体 |
| FI971974L (fi) * | 1994-11-08 | 1997-06-18 | Takeda Chemical Industries Ltd | Tienopyridiini- tai tienopyrimidiinijohdannaiset ja niiden käyttö |
| US5585538A (en) | 1995-03-08 | 1996-12-17 | Pioneer Hi-Bred International, Inc. | Hybrid maize plant & seed (3936) |
| JPH08337583A (ja) * | 1995-04-13 | 1996-12-24 | Takeda Chem Ind Ltd | 複素環化合物およびその製造法 |
| US5757486A (en) * | 1996-11-22 | 1998-05-26 | Eastman Kodak Company | Digital camera image sensor positioning apparatus including a non-coherent light interferometer |
-
1997
- 1997-10-29 US US08/959,758 patent/US5939432A/en not_active Expired - Lifetime
-
1998
- 1998-09-30 WO PCT/US1998/020333 patent/WO1999021617A2/en not_active Ceased
- 1998-09-30 AT AT98950745T patent/ATE330959T1/de not_active IP Right Cessation
- 1998-09-30 CA CA002302396A patent/CA2302396C/en not_active Expired - Fee Related
- 1998-09-30 EP EP98950745A patent/EP1025106B1/en not_active Expired - Lifetime
- 1998-09-30 AU AU96717/98A patent/AU9671798A/en not_active Abandoned
- 1998-09-30 JP JP2000517772A patent/JP2003517429A/ja active Pending
-
1999
- 1999-05-07 US US09/307,225 patent/US6177444B1/en not_active Expired - Fee Related
- 1999-05-07 US US09/307,286 patent/US6194449B1/en not_active Expired - Fee Related
-
2004
- 2004-08-02 JP JP2004225107A patent/JP2005002129A/ja active Pending
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