JP2006527708A5 - - Google Patents
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- Publication number
- JP2006527708A5 JP2006527708A5 JP2006515798A JP2006515798A JP2006527708A5 JP 2006527708 A5 JP2006527708 A5 JP 2006527708A5 JP 2006515798 A JP2006515798 A JP 2006515798A JP 2006515798 A JP2006515798 A JP 2006515798A JP 2006527708 A5 JP2006527708 A5 JP 2006527708A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- ethynylphenyl
- oxo
- dicarboxamide
- oxomorpholin
- 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
- -1 COOA Chemical group 0.000 claims description 212
- 150000001875 compounds Chemical class 0.000 claims description 28
- 239000012453 solvate Substances 0.000 claims description 24
- 150000003839 salts Chemical class 0.000 claims description 23
- 239000000203 mixture Substances 0.000 claims description 21
- 125000004432 carbon atom Chemical group C* 0.000 claims description 13
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 13
- 229910052801 chlorine Inorganic materials 0.000 claims description 10
- 239000000460 chlorine Substances 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 8
- 239000004480 active ingredient Substances 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 5
- 206010002383 Angina Pectoris Diseases 0.000 claims description 3
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 3
- 206010061218 Inflammation Diseases 0.000 claims description 3
- 206010022562 Intermittent claudication Diseases 0.000 claims description 3
- 206010027476 Metastases Diseases 0.000 claims description 3
- 208000019695 Migraine disease Diseases 0.000 claims description 3
- 208000006011 Stroke Diseases 0.000 claims description 3
- 208000007536 Thrombosis Diseases 0.000 claims description 3
- 208000009205 Tinnitus Diseases 0.000 claims description 3
- 238000002399 angioplasty Methods 0.000 claims description 3
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 3
- 230000004054 inflammatory process Effects 0.000 claims description 3
- 208000021156 intermittent vascular claudication Diseases 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 206010027599 migraine Diseases 0.000 claims description 3
- 208000010125 myocardial infarction Diseases 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 231100000886 tinnitus Toxicity 0.000 claims description 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 54
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 150000003857 carboxamides Chemical class 0.000 claims 7
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 6
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 6
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 5
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000004430 oxygen atom Chemical group O* 0.000 claims 5
- 229920006395 saturated elastomer Polymers 0.000 claims 5
- 125000004434 sulfur atom Chemical group 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 235000010290 biphenyl Nutrition 0.000 claims 3
- 239000004305 biphenyl Substances 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000001786 isothiazolyl group Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000002098 pyridazinyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 125000003831 tetrazolyl group Chemical group 0.000 claims 3
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 108010054265 Factor VIIa Proteins 0.000 claims 1
- 108010074860 Factor Xa Proteins 0.000 claims 1
- AKZWRTCWNXHHFR-PDIZUQLASA-N [(3S)-oxolan-3-yl] N-[(2S,3S)-4-[(5S)-5-benzyl-3-[(2R)-2-carbamoyloxy-2,3-dihydro-1H-inden-1-yl]-4-oxo-3H-pyrrol-5-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate Chemical compound NC(=O)O[C@@H]1Cc2ccccc2C1C1C=N[C@](C[C@H](O)[C@H](Cc2ccccc2)NC(=O)O[C@H]2CCOC2)(Cc2ccccc2)C1=O AKZWRTCWNXHHFR-PDIZUQLASA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- AOGYCOYQMAVAFD-UHFFFAOYSA-N chlorocarbonic acid Chemical class OC(Cl)=O AOGYCOYQMAVAFD-UHFFFAOYSA-N 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 0 CC1(*)CC(C(N/C2=C/C(C)(*)/C=C/C(C)(*)/C=C2)=O)NCC1 Chemical compound CC1(*)CC(C(N/C2=C/C(C)(*)/C=C/C(C)(*)/C=C2)=O)NCC1 0.000 description 2
- 229940079593 drug Drugs 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10327428.6 | 2003-06-18 | ||
| DE10327428A DE10327428A1 (de) | 2003-06-18 | 2003-06-18 | Ethinylprolinderivate |
| DE10329457.0 | 2003-07-01 | ||
| DE10329457A DE10329457A1 (de) | 2003-04-03 | 2003-07-01 | Ethinylprolinderivate |
| PCT/EP2004/005717 WO2004110433A1 (de) | 2003-06-18 | 2004-05-27 | Pyrrolidin-1, 2- dicarbonsäure- 1- [(4- ethinyl- phenyl) - amid]- 2- [(phenyl)- amid] derivative als inhibitoren der koagulationsfaktoren xa und viia zur behandlung von thrombosen |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006527708A JP2006527708A (ja) | 2006-12-07 |
| JP2006527708A5 true JP2006527708A5 (enExample) | 2007-07-12 |
| JP5015593B2 JP5015593B2 (ja) | 2012-08-29 |
Family
ID=33553467
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006515798A Expired - Fee Related JP5015593B2 (ja) | 2003-06-18 | 2004-05-27 | 血栓症の治療のための凝固因子ＸａおよびＶＩＩａの阻害剤としての１−［（４−エチニルフェニル）］−２−［（フェニル）］−ピロリジン−１，２−ジカルボキサミド誘導体 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7557222B2 (enExample) |
| EP (1) | EP1633346B1 (enExample) |
| JP (1) | JP5015593B2 (enExample) |
| KR (1) | KR20060023154A (enExample) |
| CN (1) | CN1809346A (enExample) |
| AR (1) | AR044818A1 (enExample) |
| AT (1) | ATE337000T1 (enExample) |
| AU (1) | AU2004246766B2 (enExample) |
| BR (1) | BRPI0411466A (enExample) |
| CA (1) | CA2529453C (enExample) |
| DE (1) | DE502004001289D1 (enExample) |
| ES (1) | ES2271894T3 (enExample) |
| MX (1) | MXPA05013536A (enExample) |
| PE (1) | PE20050229A1 (enExample) |
| TW (1) | TW200504012A (enExample) |
| WO (1) | WO2004110433A1 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004004731A1 (de) * | 2004-01-30 | 2005-08-18 | Merck Patent Gmbh | Harnstoffderivate |
| DE102004016605A1 (de) * | 2004-04-03 | 2005-10-20 | Merck Patent Gmbh | Thiocarbamoylproline |
| BRPI0618610A2 (pt) | 2005-11-16 | 2011-09-06 | Hoffmann La Roche | derivados de pirrolidina como inibidores de fator xa de coagulação |
| EP1818330A1 (de) | 2006-02-14 | 2007-08-15 | Boehringer Ingelheim Pharma GmbH & Co.KG | Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel |
| CA2653753C (en) * | 2006-05-16 | 2013-09-24 | Boehringer Ingelheim International Gmbh | Substituted prolinamides, production thereof and their use as medicaments |
| CA2691849A1 (en) * | 2007-06-28 | 2008-12-31 | Novartis Ag | Kallikrein 7 modulators |
| US8673920B2 (en) * | 2009-05-06 | 2014-03-18 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2012058116A1 (en) | 2010-10-27 | 2012-05-03 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9056859B2 (en) | 2010-10-29 | 2015-06-16 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| KR20140052034A (ko) | 2011-08-19 | 2014-05-02 | 머크 샤프 앤드 돔 코포레이션 | 신장 외수질 칼륨 채널의 억제제 |
| EP2755656B1 (en) | 2011-09-16 | 2016-09-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013062892A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013062900A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9493474B2 (en) | 2011-10-31 | 2016-11-15 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| EP2773206B1 (en) | 2011-10-31 | 2018-02-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013066714A1 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9206199B2 (en) | 2011-12-16 | 2015-12-08 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| GB201209138D0 (en) * | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
| AR092031A1 (es) | 2012-07-26 | 2015-03-18 | Merck Sharp & Dohme | Inhibidores del canal de potasio medular externo renal |
| US9777002B2 (en) | 2012-11-29 | 2017-10-03 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9573961B2 (en) | 2012-12-19 | 2017-02-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9604998B2 (en) | 2013-02-18 | 2017-03-28 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2014150132A1 (en) | 2013-03-15 | 2014-09-25 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| EP3027625B1 (en) | 2013-07-31 | 2018-05-30 | Merck Sharp & Dohme Corp. | Spiro-fused derivatives of piperidine useful for the treatment of inter alia hypertension and acute or chronic heart failure |
| WO2015065866A1 (en) | 2013-10-31 | 2015-05-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| JP6337750B2 (ja) * | 2013-11-22 | 2018-06-06 | 小野薬品工業株式会社 | 化合物 |
| WO2015107724A1 (ja) * | 2014-01-14 | 2015-07-23 | 大日本住友製薬株式会社 | 縮合５－オキサゾリジノン誘導体 |
| WO2016127358A1 (en) | 2015-02-12 | 2016-08-18 | Merck Sharp & Dohme Corp. | Inhibitors of renal outer medullary potassium channel |
| CN109796439B (zh) * | 2019-01-18 | 2020-05-19 | 西安交通大学 | 一种羟脯氨酸类肽衍生物及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU776053B2 (en) * | 2000-03-31 | 2004-08-26 | Astellas Pharma Inc. | Diazepan derivatives or salts thereof |
| US7312235B2 (en) * | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| DE60221505D1 (de) | 2001-03-30 | 2007-09-13 | Millennium Pharm Inc | FAKTOR Xa BENZAMIDIN INHIBITOREN |
| US7030141B2 (en) | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| DE102004014945A1 (de) * | 2004-03-26 | 2005-10-13 | Merck Patent Gmbh | Prolinylderivate |
-
2004
- 2004-05-27 AU AU2004246766A patent/AU2004246766B2/en not_active Ceased
- 2004-05-27 MX MXPA05013536A patent/MXPA05013536A/es not_active Application Discontinuation
- 2004-05-27 DE DE502004001289T patent/DE502004001289D1/de not_active Expired - Lifetime
- 2004-05-27 KR KR1020057024102A patent/KR20060023154A/ko not_active Withdrawn
- 2004-05-27 AT AT04735007T patent/ATE337000T1/de not_active IP Right Cessation
- 2004-05-27 CA CA2529453A patent/CA2529453C/en not_active Expired - Fee Related
- 2004-05-27 EP EP04735007A patent/EP1633346B1/de not_active Expired - Lifetime
- 2004-05-27 WO PCT/EP2004/005717 patent/WO2004110433A1/de not_active Ceased
- 2004-05-27 JP JP2006515798A patent/JP5015593B2/ja not_active Expired - Fee Related
- 2004-05-27 ES ES04735007T patent/ES2271894T3/es not_active Expired - Lifetime
- 2004-05-27 BR BRPI0411466-3A patent/BRPI0411466A/pt not_active Application Discontinuation
- 2004-05-27 US US10/561,227 patent/US7557222B2/en not_active Expired - Fee Related
- 2004-05-27 CN CNA2004800169550A patent/CN1809346A/zh active Pending
- 2004-06-14 PE PE2004000589A patent/PE20050229A1/es not_active Application Discontinuation
- 2004-06-16 TW TW093117389A patent/TW200504012A/zh unknown
- 2004-06-18 AR ARP040102129A patent/AR044818A1/es unknown
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