RU94019984A - ПИРИДАЗИНЫ КАК ИНГИБИТОРЫ ИНТЕРЛЕЙКИН-1 β ПРЕОБРАЗУЮЩЕГО ФЕРМЕНТА, ФАРМКОМПОЗИЦИЯ НА ИХ ОСНОВЕ И ИХ ПРИМЕНЕНИЕ - Google Patents
ПИРИДАЗИНЫ КАК ИНГИБИТОРЫ ИНТЕРЛЕЙКИН-1 β ПРЕОБРАЗУЮЩЕГО ФЕРМЕНТА, ФАРМКОМПОЗИЦИЯ НА ИХ ОСНОВЕ И ИХ ПРИМЕНЕНИЕInfo
- Publication number
- RU94019984A RU94019984A RU94019984/04A RU94019984A RU94019984A RU 94019984 A RU94019984 A RU 94019984A RU 94019984/04 A RU94019984/04 A RU 94019984/04A RU 94019984 A RU94019984 A RU 94019984A RU 94019984 A RU94019984 A RU 94019984A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- compounds
- aryl
- heteroaryl
- interleukin
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Предлагаются соединения формулы и их фармацевтически приемлемые соли:где R- галоген, связанная через кислород уходящая группа, включающая простой ароматический эфир, сложный ароматический эфир, алкил сульфонат, арил сульфонат, алкил фосфонат, арил фофонат, алкил фосфат или арил фосфат; Rявляется OR, NH (CHR)- COOR, NH (CHR)CON (R)R, N (R)Rили NH (CHR)OH; представляет H или алкил; представляет H, замещенный или незамещенный арил, гетероарил или алкил; Rи Rпредставляют независимо H, низший алкил, арил, гетероарил, аралкил, гетероаралкил или низший циклоалкил; m = 1 - 6; n = 2 - 6, фармацевтические композиции, содержащие соединения, и способ ингибирования активности интерлейкин-1β протеазы у млекопитающих, использующий соединения и композиции.
Claims (1)
- Предлагаются соединения формулы и их фармацевтически приемлемые соли: где R1 - галоген, связанная через кислород уходящая группа, включающая простой ароматический эфир, сложный ароматический эфир, алкил сульфонат, арил сульфонат, алкил фосфонат, арил фофонат, алкил фосфат или арил фосфат; R2 является OR5, NH (CHR5)m - COOR5, NH (CHR5)m CON (R5)R6, N (R5)R6 или NH (CHR5)nOH; представляет H или алкил; представляет H, замещенный или незамещенный арил, гетероарил или алкил; R5 и R6 представляют независимо H, низший алкил, арил, гетероарил, аралкил, гетероаралкил или низший циклоалкил; m = 1 - 6; n = 2 - 6, фармацевтические композиции, содержащие соединения, и способ ингибирования активности интерлейкин-1β протеазы у млекопитающих, использующий соединения и композиции.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US7391493A | 1993-06-08 | 1993-06-08 | |
US073914 | 1993-06-08 |
Publications (1)
Publication Number | Publication Date |
---|---|
RU94019984A true RU94019984A (ru) | 1997-04-10 |
Family
ID=22116553
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU94019984/04A RU94019984A (ru) | 1993-06-08 | 1994-06-07 | ПИРИДАЗИНЫ КАК ИНГИБИТОРЫ ИНТЕРЛЕЙКИН-1 β ПРЕОБРАЗУЮЩЕГО ФЕРМЕНТА, ФАРМКОМПОЗИЦИЯ НА ИХ ОСНОВЕ И ИХ ПРИМЕНЕНИЕ |
Country Status (18)
Country | Link |
---|---|
US (3) | US6121266A (ru) |
EP (1) | EP0628550B1 (ru) |
JP (1) | JPH0769894A (ru) |
KR (1) | KR950000673A (ru) |
AT (1) | ATE163412T1 (ru) |
AU (1) | AU693786B2 (ru) |
CA (1) | CA2125359A1 (ru) |
CZ (1) | CZ140194A3 (ru) |
DE (1) | DE69408598T2 (ru) |
DK (1) | DK0628550T3 (ru) |
ES (1) | ES2114654T3 (ru) |
FI (1) | FI942693A (ru) |
HU (1) | HUT67413A (ru) |
IL (1) | IL109918A0 (ru) |
NO (1) | NO306061B1 (ru) |
NZ (1) | NZ260698A (ru) |
RU (1) | RU94019984A (ru) |
SK (1) | SK69794A3 (ru) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5874424A (en) * | 1995-12-20 | 1999-02-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
US6204261B1 (en) | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
US6008217A (en) * | 1995-12-20 | 1999-12-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
DE69408598T2 (de) | 1993-06-08 | 1998-09-17 | Vertex Pharmaceuticals Inc Cam | Pyridazine als Interleukin-1-beta Verwandlungsenzym Inhibitoren |
US5756466A (en) * | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
US5716929A (en) * | 1994-06-17 | 1998-02-10 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
US5847135A (en) * | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
US6420522B1 (en) | 1995-06-05 | 2002-07-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
EP0820464A2 (en) * | 1995-03-31 | 1998-01-28 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
US5843904A (en) * | 1995-12-20 | 1998-12-01 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1βconverting enzyme |
GB9715640D0 (en) * | 1997-07-24 | 1997-10-01 | M J Highway Technology Limited | Road repair material |
TWI241295B (en) * | 1998-03-02 | 2005-10-11 | Kowa Co | Pyridazine derivative and medicine containing the same as effect component |
JP2000247959A (ja) * | 1999-02-26 | 2000-09-12 | Kowa Co | ピリダジン−3−オン誘導体及びこれを含有する医薬 |
EP2329842A3 (en) * | 2000-05-12 | 2011-07-27 | Immunex Corporation | Interleukin-1 inhibitors in the treatment of diseases |
US6664256B1 (en) | 2000-07-10 | 2003-12-16 | Kowa Co., Ltd. | Phenylpyridazine compounds and medicines containing the same |
EP1430033A4 (en) | 2001-08-31 | 2004-12-15 | Univ Northwestern | PROTEIN KINASE ANTI-INFLAMMATORY AND INHIBITOR COMPOSITION AND METHOD OF USE |
TWI314455B (en) * | 2002-12-10 | 2009-09-11 | Nippon Kayaku Kk | 3-phenyl-cinnoline derivatives and anti-tumor agent containing the same |
CN1759103A (zh) | 2003-03-18 | 2006-04-12 | 兴和株式会社 | 水溶性苯基哒嗪衍生物及含有该衍生物的医药品 |
PA8619901A1 (es) | 2003-12-12 | 2005-11-25 | Wyeth Corp | Quinolinas utiles en el tratamiento de enfermedades cardiovasculares |
EP1720893B1 (en) * | 2004-02-26 | 2014-08-13 | Baylor Research Institute | Compositions and methods for the systemic treatment of arthritis |
WO2005115362A1 (en) * | 2004-05-15 | 2005-12-08 | Vertex Pharmaceuticals Incorporated | Treating seizures using ice inhibitors |
GB0411056D0 (en) | 2004-05-18 | 2004-06-23 | Novartis Ag | Organic compounds |
EP1812007B1 (en) | 2004-11-02 | 2011-09-07 | Northwestern University | Pyridazine compounds and methods |
MX2007005247A (es) | 2004-11-02 | 2008-03-13 | Univ Northwestern | Compuestos de piridazina, composiciones y metodos. |
WO2007127475A2 (en) * | 2006-04-28 | 2007-11-08 | Northwestern University | Pyridazines for demyelinating diseases and neuropathic pain |
WO2007127375A2 (en) | 2006-04-28 | 2007-11-08 | Northwestern University | Formulations containing pyridazine compounds for treating neuroinflammatory diseases |
WO2007127474A2 (en) | 2006-04-28 | 2007-11-08 | Northwestern University | Compositions and treatments using pyridazine compounds and cholinesterase inhibitors |
WO2012075393A2 (en) * | 2010-12-02 | 2012-06-07 | President And Fellows Of Harvard College | Activators of proteasomal degradation and uses thereof |
US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
KR102419136B1 (ko) | 2017-06-15 | 2022-07-08 | 삼성전자주식회사 | 다채널 특징맵을 이용하는 영상 처리 장치 및 방법 |
AU2019302534A1 (en) * | 2018-07-09 | 2021-01-28 | Lieber Institute, Inc. | Pyridazine compounds for inhibiting NaV1.8 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1603244A (en) * | 1977-05-20 | 1981-11-18 | Max Planck Gesellschaft | Medicaments for the suppression of pathological processes |
FR2511366A1 (fr) * | 1981-08-11 | 1983-02-18 | Sanofi Sa | Nouveaux derives de la pyridazine, leur procede de preparation et les medicaments, actifs sur le systeme nerveux central, qui en contiennent |
US4590194A (en) * | 1981-10-05 | 1986-05-20 | Sterling Drug Inc. | 3-[methyl or dimethyl)amino]-6-(pyridinyl)pyridazines and their cardiotonic use |
GR860542B (en) * | 1985-03-01 | 1986-06-25 | Duphar Int Res | Benzoyl urea derivatives having antitumor activity |
US5055451A (en) * | 1986-12-22 | 1991-10-08 | Syntex Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
DE4134467A1 (de) * | 1991-10-18 | 1993-04-22 | Thomae Gmbh Dr K | Heterobiarylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
US5081145A (en) * | 1990-02-01 | 1992-01-14 | Merck Frosst Canada, Inc. | Indole-2-alkanoic acids compositions of and anti allergic use thereof |
AU7775991A (en) * | 1990-04-04 | 1991-10-30 | Immunex Corporation | Interleukin 1beta protease |
EP0519748B1 (en) * | 1991-06-21 | 1998-09-02 | Merck & Co. Inc. | Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme |
DE69408598T2 (de) | 1993-06-08 | 1998-09-17 | Vertex Pharmaceuticals Inc Cam | Pyridazine als Interleukin-1-beta Verwandlungsenzym Inhibitoren |
-
1994
- 1994-06-04 DE DE69408598T patent/DE69408598T2/de not_active Expired - Lifetime
- 1994-06-04 DK DK94201597T patent/DK0628550T3/da active
- 1994-06-04 ES ES94201597T patent/ES2114654T3/es not_active Expired - Lifetime
- 1994-06-04 EP EP94201597A patent/EP0628550B1/en not_active Expired - Lifetime
- 1994-06-04 AT AT94201597T patent/ATE163412T1/de not_active IP Right Cessation
- 1994-06-07 KR KR1019940012681A patent/KR950000673A/ko not_active Application Discontinuation
- 1994-06-07 IL IL10991894A patent/IL109918A0/xx unknown
- 1994-06-07 CA CA002125359A patent/CA2125359A1/en not_active Abandoned
- 1994-06-07 JP JP6125091A patent/JPH0769894A/ja active Pending
- 1994-06-07 AU AU64556/94A patent/AU693786B2/en not_active Ceased
- 1994-06-07 SK SK697-94A patent/SK69794A3/sk unknown
- 1994-06-07 NZ NZ260698A patent/NZ260698A/en unknown
- 1994-06-07 RU RU94019984/04A patent/RU94019984A/ru unknown
- 1994-06-08 NO NO942133A patent/NO306061B1/no not_active IP Right Cessation
- 1994-06-08 HU HU9401714A patent/HUT67413A/hu unknown
- 1994-06-08 CZ CZ941401A patent/CZ140194A3/cs unknown
- 1994-06-08 FI FI942693A patent/FI942693A/fi unknown
-
1995
- 1995-05-19 US US08/444,984 patent/US6121266A/en not_active Expired - Lifetime
-
1996
- 1996-04-03 US US08/625,680 patent/US6624166B1/en not_active Expired - Fee Related
-
2003
- 2003-09-22 US US10/668,475 patent/US6995261B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
ES2114654T3 (es) | 1998-06-01 |
FI942693A (fi) | 1994-12-09 |
US20040110725A1 (en) | 2004-06-10 |
NO942133L (no) | 1994-12-09 |
IL109918A0 (en) | 1994-10-07 |
SK69794A3 (en) | 1995-02-08 |
CZ140194A3 (en) | 1995-01-18 |
NZ260698A (en) | 1996-09-25 |
EP0628550A2 (en) | 1994-12-14 |
NO306061B1 (no) | 1999-09-13 |
US6995261B2 (en) | 2006-02-07 |
AU693786B2 (en) | 1998-07-09 |
EP0628550B1 (en) | 1998-02-25 |
DE69408598D1 (de) | 1998-04-02 |
EP0628550A3 (en) | 1995-01-18 |
HUT67413A (en) | 1995-04-28 |
ATE163412T1 (de) | 1998-03-15 |
DK0628550T3 (da) | 1998-09-28 |
AU6455694A (en) | 1994-12-15 |
DE69408598T2 (de) | 1998-09-17 |
US6624166B1 (en) | 2003-09-23 |
FI942693A0 (fi) | 1994-06-08 |
NO942133D0 (no) | 1994-06-08 |
US6121266A (en) | 2000-09-19 |
HU9401714D0 (en) | 1994-09-28 |
CA2125359A1 (en) | 1994-12-09 |
JPH0769894A (ja) | 1995-03-14 |
KR950000673A (ko) | 1995-01-03 |
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