FI113763B - Nipekotinsyraderivat som antitrombiska ämnen - Google Patents
Nipekotinsyraderivat som antitrombiska ämnen Download PDFInfo
- Publication number
- FI113763B FI113763B FI955498A FI955498A FI113763B FI 113763 B FI113763 B FI 113763B FI 955498 A FI955498 A FI 955498A FI 955498 A FI955498 A FI 955498A FI 113763 B FI113763 B FI 113763B
- Authority
- FI
- Finland
- Prior art keywords
- compound
- lys
- boc
- nip
- ala
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (13)
1. Förening med den allmänna formeln (I): X1 C02R6 v * λ c X2 Y-A 5 där X1 och X2 är lika eller olika och de har valts frän antingen H2 eller 0; där Y har valts frän följande: (CH2)m,
10 CH (NHCOR3) (CH2) m eller CH(NH2) (CH2)m; A har valts frän följande: NHR1, C(NH)NH2 eller en cykloalkylring med en kväveatom och vilken ring har valts frän följande: piperidin-2-yl, piperidin-3-yl, piperidin- 4-yl, pyrrolidin-2-yl och pyrrolidin-3-yl; 15 där Z har valts frän följande: (CH2)n eller CH(C02R4) (CH2) n; < · · .'.!t där R1 har valts frän följande H, Ci_8-alkyl eller CH(NH)NH2; *; där R2 har valts frän H eller Ci-8-alkyl; '· * 20 där R har valts frän Ci_8-alkoxi eller Ci_8-alkyl; ; : där R har valts frän Ci-8-alkyl eller fenyl-Ci-8- ,; · alkyl eller naftyl-Ci-8-alkyl ; där R6 har valts frän följande: H eller Ci_8-alkyl ,’· eller fenyl-Ci_8-alkyl eller naftyl-Ci-e-alkyl; 25 där m är ett heltal 0, 1, 2 eller 3; där n är ett heltal 0, 1 eller 2; eller dess enantiomer eller farmaceutiskt godtag-·.' bara salt. : 2. Förening enligt patentkrav 1, kännetecknad . 3 0 av att Z är (CH2)2- 113763
3. Förening enligt patentkrav 1, känneteck-nad av att R1 är H.
4. Förening enligt patentkrav 1, känneteck-n a d av att R2 är H. 5 5. Förening enligt patentkrav 1, känneteck- nad av att R3 är t-butoxi.
6. Förening enligt patentkrav 1, känneteck-nad av att R4 är metyl.
7. Förening enligt patentkrav 1, känneteck-10 nad av att Z är CH(C02R4) (CH2) .
8. Förening enligt patentkrav 1, kännetecknad av att den har valts frän följande: Na-Boc-L-Lys(Cbz)-Νϊρ-β-Ala-OBn (förening nr 1); Na-Boc-L-Lys-Nip-p-Ala-OH (förening nr 2) ;
15 Na-Boc-D-Lys-Nip-p-Ala-OH (förening nr 3); H-L-Lys-Nip-p-Ala-OH (förening nr 4); N- (Ne-aminokaproyl)-Νϊρ-β-Ala-OH (förening nr 5); Na-Ac-L-Lys-Nip-Gly-OH (förening nr 6) ; Nα-Ac-L-Lys-Nip-β-Ala-OH (förening nr 7);
20 Nα-Boc-L-Arg-Nip-β-Ala-OH (förening nr 8); Na-Boc-L-Lys-Nip-Y-aminosmörsyra (förening nr 9); H-D-Lys-Nip-β-Ala-OH (förening nr 10) ; Na-Boc-d-Lys-Nip-y-aminosmörsyra (förening nr 11) ; ·· Na-Boc-D-Lys-Nip-Gly-OH (förening nr 12); : ,·. 25 Na-Ac-D-Lys-Nip^-Ala-OH (förening nr 13) ; ; ,·, Na-Boc-D-Lys-S-( + )-Νίρ-β-Ala-OH (förening nr 14); Na-Boc-L-Lys-( + i-Pr)-Νίρ-β-Ala-OH (förening nr » » * 15); Na-Boc-D-Lys-R-(-)-Νίρ-β-Ala-OH (förening nr 16); ··; 30 N- [3-(4-piperidinpropionyl) ] -Νίρ-β-Ala-OH (före- , .· ning nr 17 ) ; Na-Boc-D-Lys-Nip-L-Asp-OMe (förening nr 18); eller N- (NE-aminokaproyl)-3-piperidinmetylaminopropion-syra (förening nr 19).
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21377294A | 1994-03-16 | 1994-03-16 | |
| US21377294 | 1994-03-16 | ||
| US36489694A | 1994-12-27 | 1994-12-27 | |
| US36489694 | 1994-12-27 | ||
| US9503145 | 1995-03-14 | ||
| PCT/US1995/003145 WO1995025091A2 (en) | 1994-03-16 | 1995-03-14 | Nipecotic acid derivatives as antithrombic compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI955498A0 FI955498A0 (sv) | 1995-11-15 |
| FI955498A FI955498A (sv) | 1996-01-15 |
| FI113763B true FI113763B (sv) | 2004-06-15 |
Family
ID=26908383
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI955498A FI113763B (sv) | 1994-03-16 | 1995-11-15 | Nipekotinsyraderivat som antitrombiska ämnen |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US5770575A (sv) |
| EP (1) | EP0746545B1 (sv) |
| JP (1) | JPH09510453A (sv) |
| KR (1) | KR100328287B1 (sv) |
| CN (1) | CN1083834C (sv) |
| AT (1) | ATE180470T1 (sv) |
| AU (1) | AU703397B2 (sv) |
| CA (1) | CA2163027A1 (sv) |
| DE (1) | DE69509875T2 (sv) |
| DK (1) | DK0746545T3 (sv) |
| ES (1) | ES2131313T3 (sv) |
| FI (1) | FI113763B (sv) |
| GR (1) | GR3030566T3 (sv) |
| HU (1) | HUT74871A (sv) |
| MX (1) | MX9504800A (sv) |
| NO (1) | NO304885B1 (sv) |
| NZ (1) | NZ283209A (sv) |
| RU (1) | RU2135470C1 (sv) |
| TW (1) | TW318179B (sv) |
| WO (1) | WO1995025091A2 (sv) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995008536A1 (en) * | 1993-09-22 | 1995-03-30 | Fujisawa Pharmaceutical Co., Ltd. | N-(3-piperidinylcarbonyl)-beta-alanine derivatives as paf antagonists |
| IL117495A (en) * | 1995-03-17 | 2002-05-23 | Fujisawa Pharmaceutical Co | History of b-alanine, the process for their preparation and the pharmaceutical preparations containing them |
| KR19990087694A (ko) * | 1996-03-13 | 1999-12-27 | 후지야마 아키라 | 피브리노겐 수용체 길항제로서의 N-[(R)-１-{３-(４-피페리딜)프로피오닐-３-피페리딜카보닐]-２(S)-아세틸아미노-β-알라닌 |
| DK0923555T3 (da) * | 1996-05-01 | 2005-08-15 | Ortho Mcneil Pharm Inc | pyrrolidin, piperidin og hexahydroazepin til behandling af trombotiske lidelser |
| EP1184374B1 (en) * | 1996-05-01 | 2009-01-28 | Ortho-McNeil Pharmaceutical, Inc. | Carboxamide derivatives of pyrrolidine, piperidine and hexahydroazepine for the treatment of thrombosis disorders |
| DE19741235A1 (de) * | 1997-09-18 | 1999-03-25 | Hoechst Marion Roussel De Gmbh | Neue Imidazolidinderivate, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| US6066651A (en) * | 1997-10-29 | 2000-05-23 | Ortho-Mcneil Pharmaceutical, Inc. | Orally-active nipecotamide glycolamide esters for the treatment of thrombosis disorders |
| AU1415099A (en) * | 1997-11-18 | 1999-06-07 | Merck & Co., Inc. | 4-substituted-4-piperidine carboxamide derivatives |
| US6020347A (en) * | 1997-11-18 | 2000-02-01 | Merck & Co., Inc. | 4-substituted-4-piperidine carboxamide derivatives |
| ES2199805T3 (es) * | 1999-03-22 | 2004-03-01 | Ortho-Mcneil Pharmaceutical, Inc. | Procedimiento para la preparacion de acido (s-(r*s*))-beta-(((1-(1-oxo-3-4-piperidinil)propil)-3-piperidinil)carbonil)amino)-3-piridinoproanoico y derivados. |
| AUPQ570100A0 (en) * | 2000-02-17 | 2000-03-09 | Fujisawa Pharmaceutical Co., Ltd. | Beta-alanine derivatives and their use as receptor antagonists |
| EP2404899A1 (en) | 2004-02-25 | 2012-01-11 | Astellas Pharma Inc. | Contrast medium for thrombus detection |
| EP3184149A1 (en) * | 2015-12-23 | 2017-06-28 | Julius-Maximilians-Universität Würzburg | Soluble glycoprotein v for treating thrombotic diseases |
| CN109734655B (zh) * | 2019-03-11 | 2020-06-02 | 都创(上海)医药科技有限公司 | 一种fkbp配体的同型二聚体合成工艺 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4857508A (en) * | 1987-12-03 | 1989-08-15 | Monsanto Company | Novel platelet-aggregation inhibitor peptide derivatives |
| US5318899A (en) * | 1989-06-16 | 1994-06-07 | Cor Therapeutics, Inc. | Platelet aggregation inhibitors |
| TW201303B (sv) * | 1990-07-05 | 1993-03-01 | Hoffmann La Roche | |
| IE912760A1 (en) * | 1990-08-06 | 1992-02-12 | Smith Kline French Lab | Compounds |
| ATE158589T1 (de) * | 1991-11-22 | 1997-10-15 | Yeda Res & Dev | Nicht-peptidische surrogate der arg-gly-asp sequenz und entsprechende pharmazeutische zusammensetzungen |
| US5219867A (en) * | 1991-12-16 | 1993-06-15 | Research Corporation Technologies, Inc. | Platelet aggregation inhibitory agents |
| WO1994013698A1 (en) * | 1992-12-11 | 1994-06-23 | University Of Florida | Materials and methods for control of pests |
| US5559209A (en) * | 1993-02-18 | 1996-09-24 | The General Hospital Corporation | Regulator regions of G proteins |
-
1995
- 1995-03-06 US US08/395,533 patent/US5770575A/en not_active Expired - Lifetime
- 1995-03-14 AT AT95914023T patent/ATE180470T1/de not_active IP Right Cessation
- 1995-03-14 DE DE69509875T patent/DE69509875T2/de not_active Expired - Fee Related
- 1995-03-14 DK DK95914023T patent/DK0746545T3/da active
- 1995-03-14 WO PCT/US1995/003145 patent/WO1995025091A2/en active IP Right Grant
- 1995-03-14 MX MX9504800A patent/MX9504800A/es not_active IP Right Cessation
- 1995-03-14 NZ NZ283209A patent/NZ283209A/en unknown
- 1995-03-14 KR KR1019950705100A patent/KR100328287B1/ko not_active IP Right Cessation
- 1995-03-14 CA CA002163027A patent/CA2163027A1/en not_active Abandoned
- 1995-03-14 RU RU95122287A patent/RU2135470C1/ru not_active IP Right Cessation
- 1995-03-14 EP EP95914023A patent/EP0746545B1/en not_active Expired - Lifetime
- 1995-03-14 JP JP7524128A patent/JPH09510453A/ja active Pending
- 1995-03-14 ES ES95914023T patent/ES2131313T3/es not_active Expired - Lifetime
- 1995-03-14 CN CN95190367A patent/CN1083834C/zh not_active Expired - Fee Related
- 1995-03-14 AU AU21191/95A patent/AU703397B2/en not_active Ceased
- 1995-03-14 HU HU9503270A patent/HUT74871A/hu unknown
- 1995-11-15 NO NO954609A patent/NO304885B1/no unknown
- 1995-11-15 FI FI955498A patent/FI113763B/sv active
- 1995-12-18 TW TW084113492A patent/TW318179B/zh active
-
1999
- 1999-06-17 GR GR990401649T patent/GR3030566T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX9504800A (es) | 1997-05-31 |
| AU2119195A (en) | 1995-10-03 |
| ES2131313T3 (es) | 1999-07-16 |
| NO304885B1 (no) | 1999-03-01 |
| WO1995025091A3 (en) | 1995-10-12 |
| KR100328287B1 (ko) | 2002-10-11 |
| FI955498A (sv) | 1996-01-15 |
| HU9503270D0 (en) | 1996-05-28 |
| DE69509875D1 (de) | 1999-07-01 |
| DE69509875T2 (de) | 1999-12-09 |
| EP0746545B1 (en) | 1999-05-26 |
| WO1995025091A2 (en) | 1995-09-21 |
| JPH09510453A (ja) | 1997-10-21 |
| FI955498A0 (sv) | 1995-11-15 |
| EP0746545A1 (en) | 1996-12-11 |
| HUT74871A (en) | 1997-02-28 |
| CN1128022A (zh) | 1996-07-31 |
| NO954609L (no) | 1996-01-05 |
| CN1083834C (zh) | 2002-05-01 |
| TW318179B (en) | 1997-10-21 |
| CA2163027A1 (en) | 1995-09-21 |
| NZ283209A (en) | 1998-04-27 |
| DK0746545T3 (da) | 1999-11-08 |
| RU2135470C1 (ru) | 1999-08-27 |
| NO954609D0 (no) | 1995-11-15 |
| AU703397B2 (en) | 1999-03-25 |
| US5770575A (en) | 1998-06-23 |
| ATE180470T1 (de) | 1999-06-15 |
| GR3030566T3 (en) | 1999-10-29 |
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