AR009363A1 - Compuestos 3-mercaptoacetilamino-1,5-sustituido--oxo-azepan utiles como inhibidores de metaloproteinasas de la matriz, composicion farmaceutica y usos para la fabricacion de medicamentos para el tratamiento de enfermedades que responden a la inhibicion de metaloproteinasas de la matriz - Google Patents
Compuestos 3-mercaptoacetilamino-1,5-sustituido--oxo-azepan utiles como inhibidores de metaloproteinasas de la matriz, composicion farmaceutica y usos para la fabricacion de medicamentos para el tratamiento de enfermedades que responden a la inhibicion de metaloproteinasas de la matrizInfo
- Publication number
- AR009363A1 AR009363A1 ARP970104242A ARP970104242A AR009363A1 AR 009363 A1 AR009363 A1 AR 009363A1 AR P970104242 A ARP970104242 A AR P970104242A AR P970104242 A ARP970104242 A AR P970104242A AR 009363 A1 AR009363 A1 AR 009363A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- hydrogen
- alkyl
- inhibition
- manufacture
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000011159 matrix material Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 238000011282 treatment Methods 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- -1 morpholino, piperidino, pyrrolidino Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 102000010750 Metalloproteins Human genes 0.000 abstract 1
- 108010063312 Metalloproteins Proteins 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000005544 phthalimido group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Heart & Thoracic Surgery (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Cardiology (AREA)
- Biophysics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biochemistry (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se describen compuestos de formula (I), donde: R1 es alquilo C1-C6, un grupo W-(CH2)m-, o un grupo Q-Z-(CH2)m donde W es ftalimido; Z es un enlace oes oxi, NR6, C(O)NR6, NR6C(O), NHC(O)NR6, OC(O)NR6, HNC(O)O, o SO2NR6; Q es hidrogeno, o ung rupo Y-(CH2)n- donde Y es hidrogeno, arilo C6-C10, heteroariloC3-C9, -C(O)OR6, -N(R6)2, morfolino, piperidino, pirrolidino o isoindolilo; R2 es alquilo C1-C4, un grupo -(CH2)p-heteroarilo C3-C9, o un grupo (CH2)p-Ar1donde Ar1 es fenilo o naftiloopc ionalmente sustituido; R3 es hidrogeno, alquilo C1-C6, -CH2SCH2NHCOCH3, un grupo -(CH2)n-A, un grupo -(CH2)m-B oun grupo -CH2-D-R7 donde A es arilo C6-C10, heteroarilo C3-C9, o ciclohexilo; B es -N(R7)2, guanidino, nitroguanidino, -C(O)OR6 o - C(O)NR6; y D es oxi o tio;R4 es hidrogeno o un grupo -(CH2)m-S(O)X(R6)2; R5 es hidrogeno, alquilo C1-C6 o R4 y R5 tomados junto con el átomo de nitrogeno al que están ancladosforman piperidino, pirrolidino, o isoindolilo; R6 eshidrogeno o alq uilo C1-C6; R7 es hidrogeno, alquilo C1-C4, o un grupo -(CH2)p-Ar donde Ar es fenilo onaftilo opcionalmente sustituido; R8 es hidrogeno, -C(O)R7, un grupo C(O)-(CH2)q-K un grupo -S-G-, donde K se selecciona del grupoformado poramino, alq uilamino, fenilalquilamino, heterociclos y heterociclos substituidos; G se selecciona del grupo formado por formulas (II); R12 a R16 son entre otrosalquilo o -(CH2)pAr; V1 es O, S o NH; V2 es N o CH; V3 es un enlace o -C(O)-;V4 es -(CH2)w-, I, S, NR7, o NC(O)R11; X y X son cada uno independientementeCH o N; una sal, estereoisomero o hidrato farmacéuticamente aceptable del mismo. Los derivados se incluyen en una composicion farmacéutica y se usanen la fabricacionde medicamentos para tra tar enfermedades que responden a la inhibicion de las metaloproteínas de la matriz.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71929196A | 1996-09-19 | 1996-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR009363A1 true AR009363A1 (es) | 2000-04-12 |
Family
ID=24889504
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP970104242A AR009363A1 (es) | 1996-09-19 | 1997-09-17 | Compuestos 3-mercaptoacetilamino-1,5-sustituido--oxo-azepan utiles como inhibidores de metaloproteinasas de la matriz, composicion farmaceutica y usos para la fabricacion de medicamentos para el tratamiento de enfermedades que responden a la inhibicion de metaloproteinasas de la matriz |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP0928291B1 (es) |
| JP (1) | JP3962091B2 (es) |
| KR (1) | KR100545460B1 (es) |
| CN (1) | CN1150205C (es) |
| AR (1) | AR009363A1 (es) |
| AT (1) | ATE229034T1 (es) |
| AU (1) | AU718055B2 (es) |
| BR (1) | BR9713207A (es) |
| CA (1) | CA2266759C (es) |
| DE (1) | DE69717647T2 (es) |
| DK (1) | DK0928291T3 (es) |
| ES (1) | ES2184126T3 (es) |
| HU (1) | HUP9904165A3 (es) |
| IL (2) | IL129035A0 (es) |
| NO (1) | NO991316L (es) |
| NZ (1) | NZ334490A (es) |
| PT (1) | PT928291E (es) |
| TW (1) | TW445262B (es) |
| WO (1) | WO1998012211A1 (es) |
| ZA (1) | ZA978307B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000040577A1 (en) * | 1998-12-31 | 2000-07-13 | Aventis Pharmaceuticals Inc. | 1-carboxymethyl-2-oxo-azepan derivatives useful as selective inhibitors of mmp-12 |
| US6770640B1 (en) | 1998-12-31 | 2004-08-03 | Aventis Pharmaceuticals Inc. | 1-Carboxymethyl-2-oxo-azepan derivatives useful as selective inhibitors of MMP-12 |
| AU1926500A (en) * | 1998-12-31 | 2000-07-24 | Aventis Pharmaceuticals Inc. | 3-substituted pyrrolidines useful as inhibitors of matrix metallo-proteinases |
| US6486193B2 (en) | 1998-12-31 | 2002-11-26 | Aventis Pharmaceuticals Inc. | 3-substituted pyrrolidines useful as inhibitors of matrix metalloproteinases |
| AU760174B2 (en) | 1999-02-09 | 2003-05-08 | Bristol-Myers Squibb Company | Lactam inhibitors of FXa and method |
| US6344450B1 (en) | 1999-02-09 | 2002-02-05 | Bristol-Myers Squibb Company | Lactam compounds and their use as inhibitors of serine proteases and method |
| AU1588901A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| EP1229914A4 (en) | 1999-11-10 | 2004-06-23 | Smithkline Beecham Corp | PROTEASE INHIBITORS |
| JP2003513972A (ja) | 1999-11-10 | 2003-04-15 | スミスクライン・ビーチャム・コーポレイション | プロテアーゼ阻害剤 |
| US7141607B1 (en) | 2000-03-10 | 2006-11-28 | Insite Vision Incorporated | Methods and compositions for treating and inhibiting retinal neovascularization |
| KR20020082896A (ko) | 2000-03-21 | 2002-10-31 | 스미스클라인 비참 코포레이션 | 프로테아제 억제제 |
| US6511973B2 (en) | 2000-08-02 | 2003-01-28 | Bristol-Myers Squibb Co. | Lactam inhibitors of FXa and method |
| PE20030701A1 (es) | 2001-12-20 | 2003-08-21 | Schering Corp | Compuestos para el tratamiento de trastornos inflamatorios |
| US7704521B2 (en) | 2007-04-11 | 2010-04-27 | Zinpro Corporation | Rumen protected essential amino acids |
| US20080255234A1 (en) * | 2007-04-11 | 2008-10-16 | Zinpro Corporation | Rumen protected lysine |
| EP3630969B1 (en) | 2017-05-31 | 2023-06-07 | BRAIN Biotech AG | Optimization of the expression of serine proteases in host cells |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2586942B2 (ja) * | 1987-03-17 | 1997-03-05 | リサーチ コーポレーシヨン テクノロジーズ インコーポレーテツド | 哺乳動物コラゲナーゼの合成阻止剤 |
| JPH07304746A (ja) * | 1994-05-11 | 1995-11-21 | Kanebo Ltd | 新規ベンゾアゼピンカルボン酸誘導体 |
| JP3787605B2 (ja) * | 1994-10-05 | 2006-06-21 | ダーウィン・ディスカバリー・リミテッド | ペプチジル化合物および金属プロテアーゼのインヒビターとしてのその治療的使用 |
| US5672598A (en) * | 1995-03-21 | 1997-09-30 | The Procter & Gamble Company | Lactam-containing hydroxamic acids |
-
1997
- 1997-08-04 ES ES97935308T patent/ES2184126T3/es not_active Expired - Lifetime
- 1997-08-04 NZ NZ334490A patent/NZ334490A/xx not_active IP Right Cessation
- 1997-08-04 PT PT97935308T patent/PT928291E/pt unknown
- 1997-08-04 IL IL12903597A patent/IL129035A0/xx active IP Right Grant
- 1997-08-04 CA CA002266759A patent/CA2266759C/en not_active Expired - Fee Related
- 1997-08-04 DK DK97935308T patent/DK0928291T3/da active
- 1997-08-04 AT AT97935308T patent/ATE229034T1/de active
- 1997-08-04 CN CNB971990247A patent/CN1150205C/zh not_active Expired - Fee Related
- 1997-08-04 WO PCT/US1997/013738 patent/WO1998012211A1/en not_active Ceased
- 1997-08-04 KR KR1019997002336A patent/KR100545460B1/ko not_active Expired - Fee Related
- 1997-08-04 AU AU38278/97A patent/AU718055B2/en not_active Ceased
- 1997-08-04 EP EP97935308A patent/EP0928291B1/en not_active Expired - Lifetime
- 1997-08-04 DE DE69717647T patent/DE69717647T2/de not_active Expired - Lifetime
- 1997-08-04 BR BR9713207-1A patent/BR9713207A/pt not_active IP Right Cessation
- 1997-08-04 HU HU9904165A patent/HUP9904165A3/hu unknown
- 1997-08-04 JP JP51465898A patent/JP3962091B2/ja not_active Expired - Fee Related
- 1997-09-13 TW TW086113339A patent/TW445262B/zh not_active IP Right Cessation
- 1997-09-15 ZA ZA9708307A patent/ZA978307B/xx unknown
- 1997-09-17 AR ARP970104242A patent/AR009363A1/es active IP Right Grant
-
1999
- 1999-03-17 IL IL129035A patent/IL129035A/en not_active IP Right Cessation
- 1999-03-18 NO NO991316A patent/NO991316L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| DE69717647T2 (de) | 2003-09-25 |
| ZA978307B (en) | 1998-03-19 |
| CN1150205C (zh) | 2004-05-19 |
| DK0928291T3 (da) | 2003-03-17 |
| WO1998012211A1 (en) | 1998-03-26 |
| AU3827897A (en) | 1998-04-14 |
| HUP9904165A2 (hu) | 2000-03-28 |
| NO991316L (no) | 1999-05-18 |
| CA2266759C (en) | 2004-10-26 |
| IL129035A (en) | 2006-12-10 |
| EP0928291A1 (en) | 1999-07-14 |
| AU718055B2 (en) | 2000-04-06 |
| ATE229034T1 (de) | 2002-12-15 |
| PT928291E (pt) | 2003-03-31 |
| JP2001501926A (ja) | 2001-02-13 |
| CN1234039A (zh) | 1999-11-03 |
| EP0928291B1 (en) | 2002-12-04 |
| JP3962091B2 (ja) | 2007-08-22 |
| BR9713207A (pt) | 2000-04-04 |
| NZ334490A (en) | 2000-08-25 |
| HK1020741A1 (en) | 2000-05-19 |
| IL129035A0 (en) | 2000-02-17 |
| NO991316D0 (no) | 1999-03-18 |
| HUP9904165A3 (en) | 2002-01-28 |
| TW445262B (en) | 2001-07-11 |
| DE69717647D1 (de) | 2003-01-16 |
| KR20000036246A (ko) | 2000-06-26 |
| CA2266759A1 (en) | 1998-03-26 |
| ES2184126T3 (es) | 2003-04-01 |
| KR100545460B1 (ko) | 2006-01-24 |
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Legal Events
| Date | Code | Title | Description |
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| FG | Grant, registration |