RU93004666A - Сульфонамидокарбоксимиды - Google Patents
СульфонамидокарбоксимидыInfo
- Publication number
- RU93004666A RU93004666A RU93004666/04A RU93004666A RU93004666A RU 93004666 A RU93004666 A RU 93004666A RU 93004666/04 A RU93004666/04 A RU 93004666/04A RU 93004666 A RU93004666 A RU 93004666A RU 93004666 A RU93004666 A RU 93004666A
- Authority
- RU
- Russia
- Prior art keywords
- sulphonamidokarboximides
- sulfonamidocarboxamides
- amidation
- fibrinogen
- thrombin
- Prior art date
Links
- NKCXQMYPWXSLIZ-PSRDDEIFSA-N (2S)-2-[[(2S)-1-[(2S)-5-amino-2-[[2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-m Chemical compound O=C([C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)N1CCC[C@H]1C(=O)N[C@@H](CO)C(O)=O NKCXQMYPWXSLIZ-PSRDDEIFSA-N 0.000 claims 1
- 210000001772 Blood Platelets Anatomy 0.000 claims 1
- 108010049003 Fibrinogen Proteins 0.000 claims 1
- 229940012952 Fibrinogen Drugs 0.000 claims 1
- 102000008946 Fibrinogen Human genes 0.000 claims 1
- 229940019698 Fibrinogen containing hemostatics Drugs 0.000 claims 1
- 210000002381 Plasma Anatomy 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 238000007112 amidation reaction Methods 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000015271 coagulation Effects 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 150000003948 formamides Chemical class 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
Claims (1)
- Предложены новые сульфонамидокарбоксамиды формулы
где A, M, Q, X и Y имеют значения, указанные в описании, а также их гидраты или сольваты, подавляющие вызванное тромбинами скопление тромбоцитов и свертывание фибриногенов в плазме. Их получают путем амидирования циклической аминогруппы, служащей для образования группы X или образования амидов через C(O)N(Q).
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH728/92 | 1992-03-04 | ||
CH72892 | 1992-03-06 | ||
CH18093 | 1993-01-21 | ||
CH180/93 | 1993-01-21 |
Publications (2)
Publication Number | Publication Date |
---|---|
RU93004666A true RU93004666A (ru) | 1996-04-27 |
RU2133739C1 RU2133739C1 (ru) | 1999-07-27 |
Family
ID=25683792
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU93004666A RU2133739C1 (ru) | 1992-03-06 | 1993-03-04 | Сульфонамидокарбоксамиды, их гидраты и физиологически приемлемые соли, фармацевтическая композиция на их основе |
Country Status (24)
Country | Link |
---|---|
US (4) | US5405854A (ru) |
EP (1) | EP0559046B1 (ru) |
JP (1) | JPH0780848B2 (ru) |
CN (1) | CN1076690A (ru) |
AT (1) | ATE203013T1 (ru) |
AU (1) | AU665230B2 (ru) |
BG (1) | BG61506B1 (ru) |
CA (1) | CA2089972C (ru) |
CZ (1) | CZ286926B6 (ru) |
DE (1) | DE59310186D1 (ru) |
DK (1) | DK0559046T3 (ru) |
ES (1) | ES2161217T3 (ru) |
FI (1) | FI103880B1 (ru) |
GR (1) | GR3036870T3 (ru) |
HU (2) | HUT70156A (ru) |
IL (3) | IL104893A0 (ru) |
IS (1) | IS3983A (ru) |
MY (1) | MY131303A (ru) |
NO (1) | NO302818B1 (ru) |
NZ (1) | NZ247014A (ru) |
PT (1) | PT559046E (ru) |
RO (1) | RO112863B1 (ru) |
RU (1) | RU2133739C1 (ru) |
TW (1) | TW223629B (ru) |
Families Citing this family (71)
Publication number | Priority date | Publication date | Assignee | Title |
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TW201303B (ru) * | 1990-07-05 | 1993-03-01 | Hoffmann La Roche | |
TW223629B (ru) * | 1992-03-06 | 1994-05-11 | Hoffmann La Roche | |
US6534536B1 (en) * | 1994-03-16 | 2003-03-18 | Bristol-Myers Squibb Company | Alkylsulfonamido heterocyclic thrombin inhibitors |
JPH06340619A (ja) * | 1993-05-03 | 1994-12-13 | Bristol Myers Squibb Co | グアニジニルまたはアミジニル置換メチルアミノ複素環トロンビン抑制剤 |
US6984627B1 (en) | 1993-06-03 | 2006-01-10 | Astrazeneca Ab | Peptide derivatives |
TW394760B (en) * | 1993-09-07 | 2000-06-21 | Hoffmann La Roche | Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same |
US5536867A (en) * | 1994-04-27 | 1996-07-16 | Hoffmann-La Roche Inc. | Process for the manufacture of dicarboxamides |
EP0684238A3 (en) * | 1994-04-27 | 1997-01-15 | Hoffmann La Roche | Process for the preparation of dicarboxamides. |
US5731439A (en) * | 1995-03-24 | 1998-03-24 | The Dupont Merck Pharmaceutical Company | Piperidine containing aminobornic acids |
US5610308A (en) * | 1995-05-18 | 1997-03-11 | Bristol-Myers Squibb Company | Process for preparing intermediates for thrombin inhibitors |
WO1997001338A1 (en) * | 1995-06-27 | 1997-01-16 | Merck & Co., Inc. | Pyridinone-thrombin inhibitors |
SA96170106A (ar) | 1995-07-06 | 2005-12-03 | أسترا أكتيبولاج | مشتقات حامض أميني جديدة |
WO1997005108A1 (fr) | 1995-07-26 | 1997-02-13 | Mitsubishi Chemical Corporation | Derives de penicillinamine amide |
US5792769A (en) * | 1995-09-29 | 1998-08-11 | 3-Dimensional Pharmaceuticals, Inc. | Guanidino protease inhibitors |
CA2238175A1 (en) * | 1995-11-28 | 1997-06-19 | Cephalon, Inc. | D-amino acid derived inhibitors of cysteine and serine proteases |
TW541316B (en) | 1995-12-21 | 2003-07-11 | Astrazeneca Ab | Prodrugs of thrombin inhibitors |
JP2000503010A (ja) | 1995-12-29 | 2000-03-14 | スリー―ダイメンショナル・ファーマスーティカルス・インコーポレーテッド | アミジノプロテアーゼ阻害剤 |
ZA9756B (en) * | 1996-01-16 | 1997-07-17 | Warner Lambert Co | Process for preparing 4,6-disubstituted pyrido[3,4-d]-pyrimidines |
US5780480A (en) * | 1996-02-28 | 1998-07-14 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
SE9602263D0 (sv) | 1996-06-07 | 1996-06-07 | Astra Ab | New amino acid derivatives |
US5668289A (en) * | 1996-06-24 | 1997-09-16 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
US5840733A (en) * | 1996-07-01 | 1998-11-24 | Redcell, Canada, Inc. | Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes |
SE9602646D0 (sv) | 1996-07-04 | 1996-07-04 | Astra Ab | Pharmaceutically-useful compounds |
US6756389B2 (en) * | 1996-08-09 | 2004-06-29 | Cambridge Neuroscience, Inc. | Pharmaceutically active compounds and methods of use |
EP0922039A1 (en) * | 1996-08-15 | 1999-06-16 | Du Pont Pharmaceuticals Company | Cyclic carbamates and isoxazolidines as iib/iiia antagonists |
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 |
US6017934A (en) * | 1997-01-22 | 2000-01-25 | Merck & Co., Inc. | Thrombin inhibitors |
US5792779A (en) * | 1997-02-19 | 1998-08-11 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
US5932606A (en) * | 1997-03-24 | 1999-08-03 | Merck & Co., Inc. | Pyrazinone, pyridinone, piperidine and pyrrolidine thrombin inhibitors |
DE69833654T2 (de) * | 1997-05-29 | 2006-12-14 | Merck & Co., Inc. (A New Jersey Corp.) | Biarylalkansäuren in der verwendung als zelladhäsionsinhibitoren |
US6291511B1 (en) | 1997-05-29 | 2001-09-18 | Merck & Co., Inc. | Biarylalkanoic acids as cell adhesion inhibitors |
AR013084A1 (es) | 1997-06-19 | 2000-12-13 | Astrazeneca Ab | Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados |
US6011038A (en) * | 1997-09-05 | 2000-01-04 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
US6087373A (en) * | 1997-09-23 | 2000-07-11 | Merck & Co., Inc. | Thrombin inhibitors |
US6133297A (en) * | 1997-09-30 | 2000-10-17 | Merck & Co., Inc. | Thrombin inhibitors |
SE9704543D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Ab | New compounds |
US6623981B2 (en) * | 1998-01-27 | 2003-09-23 | Bristol-Myers Squibb Company | Detection of patients at risk for developing integrin antagonist/agonist mediated disease states |
US6147078A (en) * | 1998-05-19 | 2000-11-14 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
JP2002516326A (ja) * | 1998-05-26 | 2002-06-04 | メルク エンド カムパニー インコーポレーテッド | イミダゾピリジン系トロンビン阻害薬 |
EP1117660A4 (en) * | 1998-09-28 | 2002-01-09 | Merck & Co Inc | THROMBIN INHIBITORS |
EP1124822A4 (en) | 1998-10-30 | 2002-04-03 | Merck & Co Inc | THROMBIN INHIBITORS |
AU752186B2 (en) | 1998-10-30 | 2002-09-12 | Merck & Co., Inc. | Thrombin inhibitors |
SE9804313D0 (sv) | 1998-12-14 | 1998-12-14 | Astra Ab | New compounds |
CA2355792A1 (en) | 1999-01-13 | 2000-07-20 | Astrazeneca Ab | New amidinobenzylamine derivatives and their use as thrombin inhibitors |
US6239132B1 (en) | 1999-04-23 | 2001-05-29 | Merck & Co., Inc. | Thrombin inhibitors |
UA58636C2 (ru) | 1999-06-04 | 2003-08-15 | Мерк Енд Ко., Інк. | Пиразиноновые ингибиторы тромбина, фармацевтическая композиция, способ ингибирования образования тромбов в крови, способ лечения состояний, связанных с тромбообразованием |
WO2000074682A1 (en) | 1999-06-04 | 2000-12-14 | Merck & Co., Inc. | Thrombin inhibitors |
AU2044401A (en) | 1999-11-23 | 2001-06-04 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
SE0000382D0 (sv) | 2000-02-07 | 2000-02-07 | Astrazeneca Ab | New process |
EP1267876A1 (en) | 2000-03-23 | 2003-01-02 | Merck & Co., Inc. | Thrombin inhibitors |
SE0001803D0 (sv) | 2000-05-16 | 2000-05-16 | Astrazeneca Ab | New compounds i |
US6433186B1 (en) | 2000-08-16 | 2002-08-13 | Astrazeneca Ab | Amidino derivatives and their use as thormbin inhibitors |
AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
US7129233B2 (en) | 2000-12-01 | 2006-10-31 | Astrazeneca Ab | Mandelic acid derivatives and their use as thrombin inhibitors |
AR034517A1 (es) | 2001-06-21 | 2004-02-25 | Astrazeneca Ab | Formulacion farmaceutica |
GB0207449D0 (en) * | 2002-03-28 | 2002-05-08 | Glaxo Group Ltd | Novel compounds |
SE0201659D0 (sv) | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Modified release pharmaceutical formulation |
SE0201661D0 (sv) | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | New salts |
US7781424B2 (en) | 2003-05-27 | 2010-08-24 | Astrazeneca Ab | Modified release pharmaceutical formulation |
US7250415B2 (en) * | 2003-06-04 | 2007-07-31 | Bristol-Myers Squibb Company | 1,1-Disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, β-aminoacids, α-aminoacids and derivatives thereof as factor Xa inhibitors |
US7795205B2 (en) * | 2004-04-12 | 2010-09-14 | Canyon Pharmaceuticals, Inc. | Methods for effecting regression of tumor mass and size in a metastasized pancreatic tumor |
GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
JP2006298785A (ja) * | 2005-04-18 | 2006-11-02 | Mitsui Chemicals Inc | ジアミン誘導体、その製造方法およびそれらを有効成分とする殺菌剤 |
TW200827336A (en) | 2006-12-06 | 2008-07-01 | Astrazeneca Ab | New crystalline forms |
AU2014306883B2 (en) * | 2013-08-16 | 2017-09-14 | Los Alamos National Security, Llc | Compounds and methods for improving plant performance |
KR102116107B1 (ko) | 2013-12-30 | 2020-05-28 | 삼성디스플레이 주식회사 | 표시 장치 |
US9988421B2 (en) | 2014-01-10 | 2018-06-05 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
CN107073069B (zh) * | 2014-08-18 | 2022-03-08 | 康奈尔大学 | 作为人免疫蛋白酶体的抑制剂的二肽模拟物 |
EP3362754B1 (en) | 2015-10-15 | 2021-12-22 | Cornell University | Proteasome inhibitors and uses thereof |
US11203613B2 (en) | 2017-10-11 | 2021-12-21 | Cornell University | Peptidomimetic proteasome inhibitors |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
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SE420919B (sv) * | 1973-08-13 | 1981-11-09 | Mitsubishi Chem Ind | Forfarande for framstellning av n?722-dansyl-l-argininderivat och farmaceutiskt godtagbara syradditionssalter derav |
US4258192A (en) * | 1977-12-16 | 1981-03-24 | Mitsubishi Chemical Industries Limited | N2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof |
US4433152A (en) * | 1981-05-25 | 1984-02-21 | Nippon Chemiphar Co., Ltd. | Amidinopiperidine derivatives |
SE8203887D0 (sv) * | 1982-06-23 | 1982-06-23 | Kabivitrum Ab | Nya trombininhiberande foreningar |
US5053393A (en) * | 1988-07-20 | 1991-10-01 | Monsanto Company | Novel platelet-aggregation inhibitor |
US5037808A (en) * | 1988-07-20 | 1991-08-06 | Monsanto Co. | Indolyl platelet-aggregation inhibitors |
US4879313A (en) * | 1988-07-20 | 1989-11-07 | Mosanto Company | Novel platelet-aggregation inhibitors |
US5084466A (en) * | 1989-01-31 | 1992-01-28 | Hoffmann-La Roche Inc. | Novel carboxamide pyridine compounds which have useful pharmaceutical utility |
TW201303B (ru) * | 1990-07-05 | 1993-03-01 | Hoffmann La Roche | |
WO1992015607A2 (en) * | 1991-03-06 | 1992-09-17 | G.D. Searle & Co. | Phenyl amidines derivatives useful as platelet aggregation inhibitors |
TW223629B (ru) * | 1992-03-06 | 1994-05-11 | Hoffmann La Roche |
-
1993
- 1993-02-12 TW TW082100976A patent/TW223629B/zh active
- 1993-02-19 CA CA002089972A patent/CA2089972C/en not_active Expired - Fee Related
- 1993-02-22 EP EP93102767A patent/EP0559046B1/de not_active Expired - Lifetime
- 1993-02-22 PT PT93102767T patent/PT559046E/pt unknown
- 1993-02-22 DE DE59310186T patent/DE59310186D1/de not_active Expired - Fee Related
- 1993-02-22 ES ES93102767T patent/ES2161217T3/es not_active Expired - Lifetime
- 1993-02-22 DK DK93102767T patent/DK0559046T3/da not_active Application Discontinuation
- 1993-02-22 AT AT93102767T patent/ATE203013T1/de not_active IP Right Cessation
- 1993-02-24 US US08/021,919 patent/US5405854A/en not_active Expired - Fee Related
- 1993-02-26 NZ NZ247014A patent/NZ247014A/en unknown
- 1993-03-01 AU AU33916/93A patent/AU665230B2/en not_active Ceased
- 1993-03-01 IL IL104893A patent/IL104893A0/xx not_active IP Right Cessation
- 1993-03-01 IL IL12072793A patent/IL120727A/en not_active IP Right Cessation
- 1993-03-02 HU HU9300572A patent/HUT70156A/hu unknown
- 1993-03-03 RO RO93-00294A patent/RO112863B1/ro unknown
- 1993-03-03 MY MYPI93000383A patent/MY131303A/en unknown
- 1993-03-04 BG BG97493A patent/BG61506B1/bg unknown
- 1993-03-04 RU RU93004666A patent/RU2133739C1/ru active
- 1993-03-05 CZ CZ1993346A patent/CZ286926B6/cs not_active IP Right Cessation
- 1993-03-05 CN CN93101908A patent/CN1076690A/zh active Pending
- 1993-03-05 IS IS3983A patent/IS3983A/is unknown
- 1993-03-05 JP JP5069080A patent/JPH0780848B2/ja not_active Expired - Fee Related
- 1993-03-05 FI FI930990A patent/FI103880B1/fi active
- 1993-03-05 NO NO930819A patent/NO302818B1/no not_active IP Right Cessation
-
1994
- 1994-12-21 US US08/361,274 patent/US5578594A/en not_active Expired - Fee Related
-
1995
- 1995-06-19 HU HU95P/P00254P patent/HU211252A9/hu unknown
-
1996
- 1996-08-13 US US08/689,743 patent/US5677448A/en not_active Expired - Fee Related
-
1997
- 1997-04-25 IL IL12072797A patent/IL120727A0/xx unknown
- 1997-06-04 US US08/869,558 patent/US5763604A/en not_active Expired - Fee Related
-
2001
- 2001-10-11 GR GR20010401733T patent/GR3036870T3/el not_active IP Right Cessation
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