FI106379B - Förfarande för framställning av som human leukocytelastasinhibitor använda trifluormetylketonderivat - Google Patents
Förfarande för framställning av som human leukocytelastasinhibitor använda trifluormetylketonderivat Download PDFInfo
- Publication number
- FI106379B FI106379B FI915996A FI915996A FI106379B FI 106379 B FI106379 B FI 106379B FI 915996 A FI915996 A FI 915996A FI 915996 A FI915996 A FI 915996A FI 106379 B FI106379 B FI 106379B
- Authority
- FI
- Finland
- Prior art keywords
- compound
- valyl
- formula
- amino
- trifluoro
- Prior art date
Links
Classifications
-
- 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
- C07K5/08—Tripeptides
-
- 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
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Hydrogenated Pyridines (AREA)
- Magnetically Actuated Valves (AREA)
- Control Of Throttle Valves Provided In The Intake System Or In The Exhaust System (AREA)
- Medicinal Preparation (AREA)
Claims (7)
106379 39
1. Förfarande för framställning av som human leukocytelas-tasinhibitor använda trifluormetylketonderivat eller deras 5 salter, vilken förening har formeln (I) ,_k R2 R3 /ΓΛ I I R1-NHC0 ( )—X-CONHCHCO-Y-CONHCHCOCF3 (D 10 där R är en {C1-C6)-alkyl, som är substituerad med karb-oxi, förestrad karboxi vald av gruppen (C^-Cg)-alkoxikar-bonyl, fenyl (C^Cg)-alkoxikarbonyl och bensoyl (C^^-Cg)-al-15 koxikarbonyl; eller morfolino-(Cj_-Cg)-alkyl, R och R är bada isopropyl, X är - eller -NH-, och Y är 20 ,-v - / \ eller I -nch2- 25 kannetecknat därav, att 1. en förening med formeln (II) eller dess sait _ R2 R3 ro // \ I I 3U H 00c—( >— x-conhchco-y-conhchcocf3 f11) omsätts med en förening med formeln
35 R1-NH2 (III) eller dess sait, 2. en förening med formeln (IV) eller dess sait 5 40 106379 R2 R3 /ΓΛ 1 1 RX-NHCO—)— X-CONHCHCO-Y-CONHCHCOCF3 (Iv oxideras 3. en förening med formeln (la) eller dess salt de-föres-tras 10 _ R2 R3 R^ -NHCO (/ y-X-CONHCHCO-Y-CONHCHCOCF3 da) 15 4. en förening med formeln (Ic) eller dess salt NO2-\ y— CH2NHCO—/ y—CONHCHCON \ R3 (Ic)
20 Viry I I conhchcocFj reduceras eller 5. en förening med formeln (Ie) eller dess salt 25 ___ R2 R3 »- x /' I HOOC-R^-NHCO-λ y— X-CONHCHCO-Y-CONHCHCOCF3 (Ie) 30 omsätts med en föreningen med formeln θφ2ΝΗ (V) « eller dess salt, varvid i ovanstäende formler är mono- eller di-föres-trad karboxi(C1-C6)-alkyl , R* är (Cx-C6)-alkylen, är (Ci-Cg)-alkyl, och R -R , X och Y avser det samma som ovan. 35 106379 41
2. Förfarande enligt patentkravet 1, kännetecknat därav, 12 3 att R , R och R avser det samma som ovan, X är - och Y är j \ 5
3. Förfarande enligt patentkravet 1, kännetecknat därav, att
10 R1 är karboximetyl, X är - och Y är 15 4. Förfarande enligt patentkravet 1 för att framställa 3(RS)-[[4-(karboximetylaminokarbonyl)fenylkarbonyl]-L-valyl-L-prolyl]amino-1,1,1-trifluor-4-metyl-2-oxopentan, kännetecknat därav, att motsvarande utgängsämnen används. 20 5. Förfarande enligt patentkravet 1 för att framställa natriumsalt av 3(RS)-[[4-karboximetylaminokarbonyl)fenylkarbonyl] -L-valyl-L-prolyl]amino-1,1,1-trifluor-4-metyl-2-oxopentan, kännetecknat därav, att motsvarande utgängsämnen används. 25 w >
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9028231 | 1990-12-31 | ||
| GB909028231A GB9028231D0 (en) | 1990-12-31 | 1990-12-31 | Trifluoromethylketone derivatives,processes for preparation thereof and use thereof |
| GB919119713A GB9119713D0 (en) | 1991-09-16 | 1991-09-16 | Trifluoremethylketone derivatives, processes for preparation thereof and use thereof |
| GB9119713 | 1991-09-16 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI915996A0 FI915996A0 (fi) | 1991-12-19 |
| FI915996A FI915996A (fi) | 1992-07-01 |
| FI106379B true FI106379B (sv) | 2001-01-31 |
Family
ID=26298196
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI915996A FI106379B (sv) | 1990-12-31 | 1991-12-19 | Förfarande för framställning av som human leukocytelastasinhibitor använda trifluormetylketonderivat |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US5296591A (sv) |
| EP (1) | EP0494071B1 (sv) |
| JP (1) | JPH0699378B2 (sv) |
| KR (1) | KR100192991B1 (sv) |
| CN (1) | CN1040003C (sv) |
| AT (1) | ATE151775T1 (sv) |
| AU (1) | AU641577B2 (sv) |
| CA (1) | CA2058560C (sv) |
| DE (1) | DE69218977T2 (sv) |
| DK (1) | DK0494071T3 (sv) |
| ES (1) | ES2099755T3 (sv) |
| FI (1) | FI106379B (sv) |
| GR (1) | GR3023719T3 (sv) |
| HU (2) | HU210263B (sv) |
| IE (1) | IE914360A1 (sv) |
| MX (1) | MX9102612A (sv) |
| NO (1) | NO309274B1 (sv) |
| RU (1) | RU2073684C1 (sv) |
| SG (1) | SG50457A1 (sv) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5296591A (en) * | 1990-12-31 | 1994-03-22 | Fujisawa Pharmaceutical Co., Ltd. | Trifluoromethylketone derivatives, processes for preparation thereof and use thereof |
| US5714470A (en) * | 1991-08-22 | 1998-02-03 | Merrell Pharmaceuticals, Inc. | Orally-active elastase inhibitors |
| US5478811A (en) * | 1991-08-22 | 1995-12-26 | Merrell Dow Pharmaceuticals Inc. | Orally-active elastase inhibitors |
| FR2694295B1 (fr) * | 1992-07-28 | 1994-09-02 | Adir | Nouveaux peptides dérivés de trifluoromethylcetones, leur procéde de préparation et les compositions pharmaceutiques qui les contiennent. |
| FR2719589B1 (fr) * | 1994-05-05 | 1996-06-14 | Adir | Nouveaux peptides dérivés de trifluorométhylcétones, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
| AU696292B2 (en) * | 1994-06-02 | 1998-09-03 | Merrell Pharmaceuticals Inc. | Acylated enol derivatives as prodrugs of elastase inhibitors |
| EP0763055B1 (en) * | 1994-06-02 | 1999-11-03 | Merrell Pharmaceuticals Inc. | Perfluoroalkyl ketone inhibitors of elastase and processes for making the same |
| US6172044B1 (en) | 1995-12-01 | 2001-01-09 | Aventis Pharmaceuticals Inc. | Acylated enol derivative of α-ketoesters and α-ketoamides |
| US5948886A (en) * | 1996-11-20 | 1999-09-07 | Hoechst Marion Roussel, Inc. | Acylated enol derivatives of α-ketoesters and α-ketoamides |
| JP2002161051A (ja) * | 1996-12-24 | 2002-06-04 | Fujisawa Pharmaceut Co Ltd | 脳虚血性疾患等の治療剤 |
| ES2421505T3 (es) * | 1998-02-24 | 2013-09-03 | Astellas Pharma Inc | Preventivos/remedios contra el envejecimiento de la piel |
| US20020045231A1 (en) * | 1999-02-02 | 2002-04-18 | Napper Andrew D. | Catalytic antibodies which hydrolyze primary amides and methods for eliciting such antibodies |
| KR20020050235A (ko) * | 1999-10-12 | 2002-06-26 | 후지야마 아키라 | 난치성 창상의 치료제 |
| IL148924A (en) * | 2002-03-26 | 2015-06-30 | Mor Research Applic Ltd | Use of substances that inhibit intracellular elastase activity in the preparation of a drug for the treatment and / or prevention of necrosis of cells and related diseases |
| DE10219464A1 (de) | 2002-04-30 | 2003-11-13 | Focke & Co | Zigarettenpackung |
| SE0202462D0 (sv) * | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | Novel use |
| WO2007140117A1 (en) * | 2006-05-23 | 2007-12-06 | Irm Llc | Compounds and compositions as channel activating protease inhibitors |
| JP4101276B2 (ja) * | 2006-08-25 | 2008-06-18 | 株式会社ステリック再生医科学研究所 | 慢性閉塞性肺疾患改善剤 |
| EP2099454A4 (en) * | 2006-11-17 | 2010-11-10 | Abbott Lab | AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS |
| JP5819305B2 (ja) * | 2009-10-13 | 2015-11-24 | リガンド・ファーマシューティカルズ・インコーポレイテッド | 造血成長因子模倣小分子化合物およびそれらの使用 |
| WO2014181788A1 (ja) * | 2013-05-08 | 2014-11-13 | キッセイ薬品工業株式会社 | α－置換グリシンアミド誘導体 |
| CN104650016A (zh) * | 2015-01-29 | 2015-05-27 | 武汉大学 | 拟三肽类化合物及其制备方法 |
| MX2018014932A (es) * | 2016-06-24 | 2019-04-24 | Pola Chem Ind Inc | Preparacion externa para la piel para mejora de arrugas. |
| CA3080894A1 (en) | 2017-11-15 | 2019-05-23 | Pola Chemical Industries, Inc. | Oil-based composition |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8600263D0 (en) * | 1985-01-22 | 1986-02-12 | Ici America Inc | Peptide derivatives |
| EP0276101A3 (en) * | 1987-01-19 | 1989-11-23 | Ici Americas Inc. | Substituted peptide derivatives |
| EP0369391A3 (en) | 1988-11-15 | 1991-09-25 | Boehringer Ingelheim Pharmaceuticals Inc. | N-substituted amides |
| US5221665A (en) * | 1989-10-27 | 1993-06-22 | Boehringer Ingelheim Pharmaceuticals, Inc. | N-substituted amides |
| US5296591A (en) * | 1990-12-31 | 1994-03-22 | Fujisawa Pharmaceutical Co., Ltd. | Trifluoromethylketone derivatives, processes for preparation thereof and use thereof |
-
1991
- 1991-12-12 US US07/805,610 patent/US5296591A/en not_active Expired - Lifetime
- 1991-12-13 IE IE436091A patent/IE914360A1/en unknown
- 1991-12-17 MX MX9102612A patent/MX9102612A/es unknown
- 1991-12-19 JP JP3361134A patent/JPH0699378B2/ja not_active Expired - Lifetime
- 1991-12-19 AU AU89853/91A patent/AU641577B2/en not_active Expired
- 1991-12-19 FI FI915996A patent/FI106379B/sv active
- 1991-12-27 KR KR1019910024710A patent/KR100192991B1/ko not_active IP Right Cessation
- 1991-12-28 RU SU5010583/04A patent/RU2073684C1/ru active
- 1991-12-30 HU HU914153A patent/HU210263B/hu unknown
- 1991-12-30 CN CN91112615A patent/CN1040003C/zh not_active Expired - Lifetime
- 1991-12-30 CA CA002058560A patent/CA2058560C/en not_active Expired - Lifetime
-
1992
- 1992-01-02 DE DE69218977T patent/DE69218977T2/de not_active Expired - Lifetime
- 1992-01-02 EP EP92100014A patent/EP0494071B1/en not_active Expired - Lifetime
- 1992-01-02 SG SG1996001866A patent/SG50457A1/en unknown
- 1992-01-02 DK DK92100014.7T patent/DK0494071T3/da active
- 1992-01-02 AT AT92100014T patent/ATE151775T1/de not_active IP Right Cessation
- 1992-01-02 NO NO19920035A patent/NO309274B1/no not_active IP Right Cessation
- 1992-01-02 ES ES92100014T patent/ES2099755T3/es not_active Expired - Lifetime
-
1993
- 1993-11-30 US US08/158,981 patent/US5430025A/en not_active Expired - Lifetime
-
1995
- 1995-06-22 HU HU95P/P00355P patent/HU211943A9/hu unknown
-
1997
- 1997-06-10 GR GR970401361T patent/GR3023719T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IE914360A1 (en) | 1992-07-01 |
| MX9102612A (es) | 1992-06-01 |
| JPH0699378B2 (ja) | 1994-12-07 |
| NO309274B1 (no) | 2001-01-08 |
| EP0494071B1 (en) | 1997-04-16 |
| DE69218977D1 (de) | 1997-05-22 |
| US5296591A (en) | 1994-03-22 |
| DE69218977T2 (de) | 1997-08-07 |
| RU2073684C1 (ru) | 1997-02-20 |
| AU8985391A (en) | 1992-07-02 |
| KR100192991B1 (ko) | 1999-06-15 |
| SG50457A1 (en) | 1998-07-20 |
| DK0494071T3 (sv) | 1997-05-12 |
| HU211943A9 (en) | 1996-01-29 |
| ATE151775T1 (de) | 1997-05-15 |
| KR920011988A (ko) | 1992-07-25 |
| JPH04297446A (ja) | 1992-10-21 |
| US5430025A (en) | 1995-07-04 |
| EP0494071A3 (en) | 1993-05-05 |
| HU914153D0 (en) | 1992-03-30 |
| CA2058560A1 (en) | 1992-07-01 |
| NO920035L (no) | 1992-07-01 |
| CN1063108A (zh) | 1992-07-29 |
| FI915996A0 (fi) | 1991-12-19 |
| AU641577B2 (en) | 1993-09-23 |
| EP0494071A2 (en) | 1992-07-08 |
| FI915996A (fi) | 1992-07-01 |
| HUT60507A (en) | 1992-09-28 |
| GR3023719T3 (en) | 1997-09-30 |
| HU210263B (en) | 1995-03-28 |
| ES2099755T3 (es) | 1997-06-01 |
| CA2058560C (en) | 2000-12-12 |
| NO920035D0 (no) | 1992-01-02 |
| CN1040003C (zh) | 1998-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PC | Transfer of assignment of patent |
Owner name: ASTELLAS PHARMA INC. Free format text: ASTELLAS PHARMA INC. |