RU2003104017A - Ингибиторы тромбина, содержащие аминоизохинолиновую группу - Google Patents
Ингибиторы тромбина, содержащие аминоизохинолиновую группу Download PDFInfo
- Publication number
- RU2003104017A RU2003104017A RU2003104017/04A RU2003104017A RU2003104017A RU 2003104017 A RU2003104017 A RU 2003104017A RU 2003104017/04 A RU2003104017/04 A RU 2003104017/04A RU 2003104017 A RU2003104017 A RU 2003104017A RU 2003104017 A RU2003104017 A RU 2003104017A
- Authority
- RU
- Russia
- Prior art keywords
- compound according
- cyclohexyl
- isochinoline
- group
- containing amino
- Prior art date
Links
- 229940122388 Thrombin inhibitor Drugs 0.000 title 1
- OSILBMSORKFRTB-UHFFFAOYSA-N isoquinolin-1-amine Chemical group C1=CC=C2C(N)=NC=CC2=C1 OSILBMSORKFRTB-UHFFFAOYSA-N 0.000 title 1
- 239000003868 thrombin inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 108090000190 Thrombin Proteins 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- 0 *CC(*N1C(*NCc2ccc3c(N)nc(*)cc3c2)CCCC1)N* Chemical compound *CC(*N1C(*NCc2ccc3c(N)nc(*)cc3c2)CCCC1)N* 0.000 description 1
Classifications
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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)
Claims (9)
1. Соединение, имеющее формулу (I)
где R1 представляет циклопентил, циклогексил или разветвленный (3-4С)алкил;
R2 представляет циклогексил или фенил;
R3 представляет Н или метил;
А представляет незамещенный насыщенный 4, 5 или 6-членный цикл;
или его фармацевтически приемлемая соль.
2. Соединение по п.1, где А представляет пятичленный цикл.
3. Соединение по п.1, где R2 представляет циклогексил.
4. Соединение по п.1, где R3 представляет Н.
5. Соединение по п.1, где R1 представляет циклогексил.
6. Соединение по п.5, где R1 представляет циклогексил, R2 представляет циклогексил, R3 представляет Н и А представляет пятичленный цикл.
7. Фармацевтическая композиция, включающая соединение по любому из пп.1-6 и фармацевтически приемлемые вспомогательные вещества.
8. Соединение по любому из пп.1-6 для применения в терапии.
9. Применение соединения по любому из пп.1-6 в производстве лекарственного препарата для лечения или профилактики заболеваний, связанных с тромбином.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00202491.7 | 2000-07-12 | ||
| EP00202491 | 2000-07-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2003104017A true RU2003104017A (ru) | 2004-08-20 |
Family
ID=8171793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2003104017/04A RU2003104017A (ru) | 2000-07-12 | 2001-07-09 | Ингибиторы тромбина, содержащие аминоизохинолиновую группу |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6642253B2 (ru) |
| EP (1) | EP1303491A1 (ru) |
| JP (1) | JP2004502759A (ru) |
| KR (1) | KR20030022270A (ru) |
| CN (1) | CN1441784A (ru) |
| AR (1) | AR029596A1 (ru) |
| AU (1) | AU2001278476A1 (ru) |
| BR (1) | BR0112338A (ru) |
| CA (1) | CA2413035A1 (ru) |
| CZ (1) | CZ200392A3 (ru) |
| EC (1) | ECSP034422A (ru) |
| HR (1) | HRP20030017A2 (ru) |
| HU (1) | HUP0301258A2 (ru) |
| IL (1) | IL153611A0 (ru) |
| MX (1) | MXPA03000337A (ru) |
| NO (1) | NO20030145L (ru) |
| NZ (1) | NZ523553A (ru) |
| PE (1) | PE20020209A1 (ru) |
| PL (1) | PL359787A1 (ru) |
| RU (1) | RU2003104017A (ru) |
| SK (1) | SK322003A3 (ru) |
| WO (1) | WO2002004423A1 (ru) |
| ZA (1) | ZA200300080B (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2468011C2 (ru) * | 2006-12-27 | 2012-11-27 | Санофи-Авентис | Замещенные циклоалкиламином производные изохинолина и изохинолинона |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6906192B2 (en) | 2000-11-07 | 2005-06-14 | Bristol Myers Squibb Company | Processes for the preparation of acid derivatives useful as serine protease inhibitors |
| HUP0400651A2 (hu) | 2000-11-07 | 2004-06-28 | Bristol-Myers Squibb Company | Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| TWI389899B (zh) * | 2006-08-08 | 2013-03-21 | Msd Oss Bv | 具口服活性之凝血酶抑制劑 |
| US7927378B2 (en) * | 2007-03-05 | 2011-04-19 | Scussel Sbj Systems, Llc | Vacuum assisted prosthetic sleeve and socket |
| CN109810174B (zh) * | 2017-11-21 | 2021-01-01 | 首都医科大学 | 异喹啉-3-甲酰-TARGD(aa)aa,其制备,抗静脉血栓活性和应用 |
| CN109810173B (zh) * | 2017-11-21 | 2020-11-27 | 首都医科大学 | 二氢异喹啉-3-甲酰-TARGD(aa)aa,其制备,抗静脉血栓活性和应用 |
| CN109810172B (zh) * | 2017-11-21 | 2021-01-01 | 首都医科大学 | 异喹啉-3-甲酰-PARGD(aa)aa,其制备,抗静脉血栓活性和应用 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL123986A (en) | 1997-04-24 | 2011-10-31 | Organon Nv | Medicinal compounds |
-
2001
- 2001-07-09 WO PCT/EP2001/007887 patent/WO2002004423A1/en not_active Ceased
- 2001-07-09 IL IL15361101A patent/IL153611A0/xx unknown
- 2001-07-09 US US10/332,792 patent/US6642253B2/en not_active Expired - Fee Related
- 2001-07-09 BR BR0112338-6A patent/BR0112338A/pt not_active IP Right Cessation
- 2001-07-09 CN CN01812607A patent/CN1441784A/zh active Pending
- 2001-07-09 RU RU2003104017/04A patent/RU2003104017A/ru not_active Application Discontinuation
- 2001-07-09 HU HU0301258A patent/HUP0301258A2/hu unknown
- 2001-07-09 HR HR20030017A patent/HRP20030017A2/hr not_active Application Discontinuation
- 2001-07-09 PL PL35978701A patent/PL359787A1/xx not_active Application Discontinuation
- 2001-07-09 NZ NZ523553A patent/NZ523553A/en unknown
- 2001-07-09 JP JP2002509290A patent/JP2004502759A/ja not_active Withdrawn
- 2001-07-09 MX MXPA03000337A patent/MXPA03000337A/es unknown
- 2001-07-09 CA CA002413035A patent/CA2413035A1/en not_active Abandoned
- 2001-07-09 AU AU2001278476A patent/AU2001278476A1/en not_active Abandoned
- 2001-07-09 EP EP01956519A patent/EP1303491A1/en not_active Withdrawn
- 2001-07-09 KR KR10-2003-7000363A patent/KR20030022270A/ko not_active Withdrawn
- 2001-07-09 CZ CZ200392A patent/CZ200392A3/cs unknown
- 2001-07-09 SK SK32-2003A patent/SK322003A3/sk not_active Application Discontinuation
- 2001-07-10 PE PE2001000684A patent/PE20020209A1/es not_active Application Discontinuation
- 2001-07-11 AR ARP010103283A patent/AR029596A1/es not_active Application Discontinuation
-
2003
- 2003-01-03 ZA ZA200300080A patent/ZA200300080B/en unknown
- 2003-01-10 EC EC2003004422A patent/ECSP034422A/es unknown
- 2003-01-10 NO NO20030145A patent/NO20030145L/no not_active Application Discontinuation
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2468011C2 (ru) * | 2006-12-27 | 2012-11-27 | Санофи-Авентис | Замещенные циклоалкиламином производные изохинолина и изохинолинона |
Also Published As
| Publication number | Publication date |
|---|---|
| NO20030145D0 (no) | 2003-01-10 |
| US6642253B2 (en) | 2003-11-04 |
| AR029596A1 (es) | 2003-07-02 |
| AU2001278476A1 (en) | 2002-01-21 |
| KR20030022270A (ko) | 2003-03-15 |
| NZ523553A (en) | 2004-04-30 |
| ECSP034422A (es) | 2003-03-10 |
| BR0112338A (pt) | 2003-07-22 |
| HRP20030017A2 (en) | 2003-04-30 |
| SK322003A3 (en) | 2003-06-03 |
| NO20030145L (no) | 2003-01-10 |
| MXPA03000337A (es) | 2004-04-05 |
| IL153611A0 (en) | 2003-07-06 |
| PL359787A1 (en) | 2004-09-06 |
| CZ200392A3 (cs) | 2003-05-14 |
| CA2413035A1 (en) | 2002-01-17 |
| JP2004502759A (ja) | 2004-01-29 |
| WO2002004423A9 (en) | 2003-05-15 |
| EP1303491A1 (en) | 2003-04-23 |
| WO2002004423A1 (en) | 2002-01-17 |
| HUP0301258A2 (hu) | 2003-08-28 |
| CN1441784A (zh) | 2003-09-10 |
| WO2002004423A8 (en) | 2003-03-06 |
| ZA200300080B (en) | 2004-04-05 |
| PE20020209A1 (es) | 2002-03-19 |
| US20030166579A1 (en) | 2003-09-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20050616 |