JP2005514332A5 - - Google Patents
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- Publication number
- JP2005514332A5 JP2005514332A5 JP2003532474A JP2003532474A JP2005514332A5 JP 2005514332 A5 JP2005514332 A5 JP 2005514332A5 JP 2003532474 A JP2003532474 A JP 2003532474A JP 2003532474 A JP2003532474 A JP 2003532474A JP 2005514332 A5 JP2005514332 A5 JP 2005514332A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- substituted
- carboxy
- hydroxy
- group
- 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
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 31
- 125000001424 substituent group Chemical group 0.000 claims 30
- -1 hydroxy, carboxy Chemical group 0.000 claims 25
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 18
- 239000011737 fluorine Substances 0.000 claims 17
- 229910052731 fluorine Inorganic materials 0.000 claims 17
- 229910052757 nitrogen Inorganic materials 0.000 claims 17
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 16
- 239000011593 sulfur Substances 0.000 claims 16
- 125000001544 thienyl group Chemical group 0.000 claims 14
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 239000001301 oxygen Substances 0.000 claims 13
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 10
- 125000006413 ring segment Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical group 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000002541 furyl group Chemical group 0.000 claims 7
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000000320 amidine group Chemical group 0.000 claims 6
- 150000001409 amidines Chemical class 0.000 claims 6
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 5
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 5
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical group [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 238000010276 construction Methods 0.000 claims 5
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052698 phosphorus Chemical group 0.000 claims 5
- 239000011574 phosphorus Chemical group 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 150000002829 nitrogen Chemical class 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 125000004744 butyloxycarbonyl group Chemical group 0.000 claims 1
- 150000003857 carboxamides Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000008030 elimination Effects 0.000 claims 1
- 238000003379 elimination reaction Methods 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000004995 haloalkylthio group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000005928 isopropyloxycarbonyl group Chemical group [H]C([H])([H])C([H])(OC(*)=O)C([H])([H])[H] 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- XUXJHBAJZQREDB-UHFFFAOYSA-N methylbutylamide Natural products CCC(C)C(N)=O XUXJHBAJZQREDB-UHFFFAOYSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 230000004962 physiological condition Effects 0.000 claims 1
- XUWVIABDWDTJRZ-UHFFFAOYSA-N propan-2-ylazanide Chemical compound CC(C)[NH-] XUWVIABDWDTJRZ-UHFFFAOYSA-N 0.000 claims 1
- 230000009467 reduction Effects 0.000 claims 1
- 238000006722 reduction reaction Methods 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- BHRZNVHARXXAHW-UHFFFAOYSA-N sec-butylamine Chemical compound CCC(C)N BHRZNVHARXXAHW-UHFFFAOYSA-N 0.000 claims 1
- MMNTZXRQPVRSSO-UHFFFAOYSA-N sulfamoylformic acid Chemical group NS(=O)(=O)C(O)=O MMNTZXRQPVRSSO-UHFFFAOYSA-N 0.000 claims 1
- 125000005864 sulfonamidyl group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 230000001732 thrombotic effect Effects 0.000 claims 1
- 0 Cc1c(*)c(*)c(C(N)=N)c(*)c1* Chemical compound Cc1c(*)c(*)c(C(N)=N)c(*)c1* 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32672101P | 2001-10-03 | 2001-10-03 | |
| US33862301P | 2001-10-24 | 2001-10-24 | |
| US33285701P | 2001-11-06 | 2001-11-06 | |
| US33329201P | 2001-11-14 | 2001-11-14 | |
| US33210701P | 2001-11-21 | 2001-11-21 | |
| US33201401P | 2001-11-21 | 2001-11-21 | |
| PCT/US2002/031784 WO2003029224A1 (en) | 2001-10-03 | 2002-10-03 | 6-membered unsaturated heterocyclic compounds useful for selective inhibition of the coagulation cascade |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005514332A JP2005514332A (ja) | 2005-05-19 |
| JP2005514332A5 true JP2005514332A5 (https=) | 2006-01-05 |
Family
ID=27559730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003532474A Pending JP2005514332A (ja) | 2001-10-03 | 2002-10-03 | 凝固カスケードの選択阻害に有用な６員不飽和複素環式化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20040106626A1 (https=) |
| EP (1) | EP1448534A1 (https=) |
| JP (1) | JP2005514332A (https=) |
| BR (1) | BR0213126A (https=) |
| CA (1) | CA2462647A1 (https=) |
| MX (1) | MXPA04003167A (https=) |
| WO (1) | WO2003029224A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005535710A (ja) * | 2002-08-09 | 2005-11-24 | トランス テック ファーマ，インコーポレイテッド | アリールおよびヘテロアリール化合物ならびに凝固を調節する方法 |
| US7208601B2 (en) * | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
| US7501538B2 (en) | 2003-08-08 | 2009-03-10 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
| WO2005014533A2 (en) * | 2003-08-08 | 2005-02-17 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions, and methods of use |
| AR047521A1 (es) * | 2004-02-06 | 2006-01-25 | Astrazeneca Ab | Compuestos piridin-2-ona utiles como inhibidores de trombina |
| CN101223167B (zh) * | 2005-07-15 | 2011-08-31 | 弗·哈夫曼-拉罗切有限公司 | 杂芳基稠合的环状胺 |
| MD20140044A2 (ro) | 2011-11-11 | 2014-08-31 | Pfizer Inc. | 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare |
| AU2016257179A1 (en) | 2015-05-05 | 2017-11-02 | Pfizer Inc. | 2-thiopyrimidinones |
| CN112867706B (zh) | 2018-05-29 | 2024-11-15 | 奥默罗斯公司 | Masp-2抑制剂和使用方法 |
| US11584714B2 (en) | 2018-05-29 | 2023-02-21 | Omeros Corporation | MASP-2 inhibitors and methods of use |
| BR112022010881A2 (pt) | 2019-12-04 | 2022-08-23 | Omeros Corp | Composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio associado a serina protease-2 associada à lectina de ligação ao manan |
| IL293550A (en) | 2019-12-04 | 2022-08-01 | Omeros Corp | 2-masp inhibitor compounds, preparations containing them and their uses |
| JP7699389B2 (ja) | 2019-12-04 | 2025-06-27 | オメロス コーポレーション | Ｍａｓｐ－２阻害剤および使用方法 |
| EP4069676A1 (en) | 2019-12-04 | 2022-10-12 | Omeros Corporation | Masp-2 inhibitors and methods of use |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5910541A (ja) * | 1982-07-09 | 1984-01-20 | Takeda Chem Ind Ltd | キノン化合物 |
| JPS60255749A (ja) * | 1984-05-31 | 1985-12-17 | Univ Nagoya | キノン誘導体 |
| US5304658A (en) * | 1984-08-01 | 1994-04-19 | Takeda Chemical Industries, Ltd. | Quinone derivatives, their production and use |
| IL81264A (en) * | 1986-01-30 | 1990-11-05 | Takeda Chemical Industries Ltd | Quinone derivatives,their production and pharmaceutical compositions containing them |
| US5441960A (en) * | 1992-04-16 | 1995-08-15 | Zeneca Limited | 1-pyrimidinylacetamide human leukocyte elastate inhibitors |
| US5618792A (en) * | 1994-11-21 | 1997-04-08 | Cortech, Inc. | Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase |
| US6011158A (en) * | 1994-12-13 | 2000-01-04 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| US5658930A (en) * | 1994-12-13 | 1997-08-19 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| US5656645A (en) * | 1994-12-13 | 1997-08-12 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| US5741819A (en) * | 1995-06-07 | 1998-04-21 | 3-Dimensional Pharmaceuticals, Inc. | Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors |
| US5668289A (en) * | 1996-06-24 | 1997-09-16 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
| US5872138A (en) * | 1996-09-13 | 1999-02-16 | Merck & Co., Inc. | Thrombin inhibitors |
| US5869487A (en) * | 1996-10-24 | 1999-02-09 | Merck & Co., Inc. | Pyrido 3,4-B!pyrazines for use as thrombin inhibitors |
| US5792779A (en) * | 1997-02-19 | 1998-08-11 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
| US5866573A (en) * | 1997-04-21 | 1999-02-02 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
| TWI222441B (en) * | 1997-11-26 | 2004-10-21 | Dimensional Pharm Inc | Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
| EP0997474B1 (en) * | 1998-08-14 | 2003-10-29 | Pfizer Inc. | Antithrombotic agents |
| US6664255B1 (en) * | 1999-05-19 | 2003-12-16 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade |
| IL146245A0 (en) * | 1999-05-19 | 2002-07-25 | Pharmacia Corp | Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade |
| EA004867B1 (ru) * | 1999-05-19 | 2004-08-26 | Фармация Корпорейшн | Замещенные пиримидиноновые соединения, композиция и способ лечения, ингибирования или предупреждения тромботических состояний у млекопитающих |
| AU2001255399A1 (en) * | 2000-04-14 | 2001-10-30 | Corvas International, Inc. | Pyridine and pyrazine derivatives as thrombin inhibitors |
| WO2001087842A1 (en) * | 2000-05-18 | 2001-11-22 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade |
| AU2001222501A1 (en) * | 2000-05-18 | 2001-11-26 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade |
-
2002
- 2002-10-03 EP EP02800488A patent/EP1448534A1/en not_active Withdrawn
- 2002-10-03 JP JP2003532474A patent/JP2005514332A/ja active Pending
- 2002-10-03 CA CA002462647A patent/CA2462647A1/en not_active Abandoned
- 2002-10-03 US US10/263,525 patent/US20040106626A1/en not_active Abandoned
- 2002-10-03 WO PCT/US2002/031784 patent/WO2003029224A1/en not_active Ceased
- 2002-10-03 BR BR0213126-9A patent/BR0213126A/pt not_active IP Right Cessation
- 2002-10-03 MX MXPA04003167A patent/MXPA04003167A/es not_active Application Discontinuation
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