ES8802619A1 - Procedimiento para preparar peptidos difluorcetonicos - Google Patents
Procedimiento para preparar peptidos difluorcetonicosInfo
- Publication number
- ES8802619A1 ES8802619A1 ES557733A ES557733A ES8802619A1 ES 8802619 A1 ES8802619 A1 ES 8802619A1 ES 557733 A ES557733 A ES 557733A ES 557733 A ES557733 A ES 557733A ES 8802619 A1 ES8802619 A1 ES 8802619A1
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- ceto
- amino
- difluoro derivatives
- hydroxibenzotria
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
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
- C07K5/06—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/18—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/16—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
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Detergent Compositions (AREA)
- Cosmetics (AREA)
Abstract
LOS PEPTIDOS DIFLUORCETONICOS (I), (II) Y (III), DONDE NO EXCLUSIVAMENTE, R1 ES ALQUILO C1-5, R2 ALQUILO C1-6 SUSTITUIDO POR AMINO, HIDROXI O ARILO CONTENIENDO C6, C10 O C12, R3 ALQUILO C1-12, Y OPCIONALMENTE DE 1 A 4 HETEROATOMOS, A ES CETO, AMIDO, ESTER, RA ES RB.NRC.CO CON R3 ALQUILO C1-10, RC HIDROGENO O METILO; SE OBTIENEN HACIENDO REACCIONAR UN AMINO CETO ACIDO DIFLUORADO (IV) DONDE Q ES UN GRUPO (V), CON UNA AMINA RB.NH.RC POR ACOPLAMIENTO CON CARBODIIMIDA SOLUBLE EN AGUA NORMALIZADA U 1-HIDROXIBENZOTRIAZOL EN UN DISLUYENTE ADECUADO COMO TETRAHIDROFURANO ENTRE 0 Y 35GC. SON INHIBIDORES DE LA ELASTASA DE LEUCOCITOS HUMANOS (HLE) APLICABLES AL TRATAMIENTO DEL ENFISEMA PULMONAR, ATEROSCLEROSIS, ARTRITIS REUMATOIDE Y OSTEOARTRITIS. *FORMULA* N
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB858514438A GB8514438D0 (en) | 1985-06-07 | 1985-06-07 | Selected difluoro ketone dipeptide derivatives |
| GB858514440A GB8514440D0 (en) | 1985-06-07 | 1985-06-07 | Difluoro ketone tripeptide derivatives |
| GB858514436A GB8514436D0 (en) | 1985-06-07 | 1985-06-07 | Selected difluoro derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES8802619A1 true ES8802619A1 (es) | 1988-09-01 |
| ES557733A0 ES557733A0 (es) | 1988-09-01 |
Family
ID=27262698
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES555826A Expired ES8801305A1 (es) | 1985-06-07 | 1986-06-06 | Procedimiento para preparar peptidos difluorcetonicos |
| ES557734A Expired ES8900051A1 (es) | 1985-06-07 | 1987-09-16 | Procedimiento para preparar peptidos difluorcetonicos |
| ES557733A Expired ES8802619A1 (es) | 1985-06-07 | 1987-09-16 | Procedimiento para preparar peptidos difluorcetonicos |
| ES557735A Expired ES8802321A1 (es) | 1985-06-07 | 1987-09-16 | Procedimiento para preparar peptidos difluorcetonicos |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES555826A Expired ES8801305A1 (es) | 1985-06-07 | 1986-06-06 | Procedimiento para preparar peptidos difluorcetonicos |
| ES557734A Expired ES8900051A1 (es) | 1985-06-07 | 1987-09-16 | Procedimiento para preparar peptidos difluorcetonicos |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES557735A Expired ES8802321A1 (es) | 1985-06-07 | 1987-09-16 | Procedimiento para preparar peptidos difluorcetonicos |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US4880780A (es) |
| EP (1) | EP0204571B1 (es) |
| JP (1) | JPH07116159B2 (es) |
| AT (1) | ATE71934T1 (es) |
| AU (1) | AU594683B2 (es) |
| DE (1) | DE3683541D1 (es) |
| DK (1) | DK267686A (es) |
| ES (4) | ES8801305A1 (es) |
| FI (1) | FI86859C (es) |
| GR (1) | GR861488B (es) |
| HU (1) | HU208438B (es) |
| IE (1) | IE59146B1 (es) |
| IL (1) | IL79049A0 (es) |
| NO (1) | NO170585C (es) |
| NZ (1) | NZ216437A (es) |
| PT (1) | PT82724B (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8600263D0 (en) * | 1985-01-22 | 1986-02-12 | Ici America Inc | Peptide derivatives |
| US5496927A (en) * | 1985-02-04 | 1996-03-05 | Merrell Pharmaceuticals Inc. | Peptidase inhibitors |
| GB8711748D0 (en) * | 1986-06-05 | 1987-06-24 | Ici America Inc | Difluoro keto compounds |
| GB8613703D0 (en) * | 1986-06-05 | 1986-07-09 | Ici America Inc | Difluoro peptide compounds |
| GB8809316D0 (en) * | 1987-05-11 | 1988-05-25 | Ici America Inc | Heterocyclic ketones |
| EP0371179A1 (en) * | 1988-10-28 | 1990-06-06 | Merrell Dow Pharmaceuticals Inc. | Novel analogs of peptidase substrates |
| EP0369391A3 (en) * | 1988-11-15 | 1991-09-25 | Boehringer Ingelheim Pharmaceuticals Inc. | N-substituted amides |
| GB8910547D0 (en) * | 1989-05-08 | 1989-06-21 | Ici America Inc | Substituted ketones |
| US5221665A (en) * | 1989-10-27 | 1993-06-22 | Boehringer Ingelheim Pharmaceuticals, Inc. | N-substituted amides |
| US5391705A (en) * | 1991-03-15 | 1995-02-21 | Merrell Dow Pharmaceuticals Inc. | Polyfluorinated tripeptide thrombin inhibitors |
| AU655301B2 (en) * | 1991-05-23 | 1994-12-15 | Merrell Pharmaceuticals Inc. | Inhibitors of cathepsin G and elastase for preventing connective tissue degradation |
| US5478811A (en) * | 1991-08-22 | 1995-12-26 | Merrell Dow Pharmaceuticals Inc. | Orally-active elastase inhibitors |
| US5714470A (en) | 1991-08-22 | 1998-02-03 | Merrell Pharmaceuticals, Inc. | Orally-active elastase inhibitors |
| US5486529A (en) * | 1992-04-16 | 1996-01-23 | Zeneca Limited | Certain pyridyl ketones for treating diseases involving leukocyte elastase |
| IL108031A0 (en) * | 1992-12-22 | 1994-04-12 | Procter & Gamble | Difluoro pentapeptide derivatives and pharmaceutical compositions containing them |
| US6008196A (en) * | 1994-06-02 | 1999-12-28 | Hoechst Marion Roussel, Inc. | Perfluoroalkyl ketone inhibitors of elastase and processes for making the same |
| JP4221059B2 (ja) * | 1994-06-02 | 2009-02-12 | アベンティス・インコーポレイテッド | エラスターゼインヒビターのプロドラッグとしてのアシル化エノール誘導体 |
| PT804465E (pt) * | 1994-06-02 | 2003-12-31 | Aventis Pharma Inc | Novos inibidores da elastase |
| US6069232A (en) * | 1995-10-02 | 2000-05-30 | Hoechst Marion Roussel, Inc. | Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors |
| US5948886A (en) * | 1996-11-20 | 1999-09-07 | Hoechst Marion Roussel, Inc. | Acylated enol derivatives of α-ketoesters and α-ketoamides |
| US6172044B1 (en) | 1995-12-01 | 2001-01-09 | Aventis Pharmaceuticals Inc. | Acylated enol derivative of α-ketoesters and α-ketoamides |
| US6673784B1 (en) | 1996-03-19 | 2004-01-06 | G. D. Searle & Co. | Electrophilic ketones for the treatment of herpesvirus infections |
| US5739354A (en) * | 1996-03-26 | 1998-04-14 | Hoechst Marion Roussel, Inc. | Process for the preparation of N-methyl-D-phenylalanyl-N- 1- 3- (aminoiminomethyl)amino!propyl!-3,3-difluoro-2-oxohexyl!-L-prolinamide |
| EP0932617B1 (en) | 1996-10-18 | 2002-01-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| MY148123A (en) | 2003-09-05 | 2013-02-28 | Vertex Pharma | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| US7964624B1 (en) | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| AR055395A1 (es) | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
| US8039475B2 (en) | 2006-02-27 | 2011-10-18 | Vertex Pharmaceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| NZ571280A (en) * | 2006-03-16 | 2011-10-28 | Vertex Pharma | Deuterated hepatitis C protease inhibitors |
| US8754107B2 (en) * | 2006-11-17 | 2014-06-17 | Abbvie Inc. | Aminopyrrolidines as chemokine receptor antagonists |
| AU2008219704A1 (en) | 2007-02-27 | 2008-09-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| AR065498A1 (es) | 2007-02-27 | 2009-06-10 | Vertex Pharma | Co- critales de vx-950 (un inhibidor del virus de la hepatitis c) y composiciones farmaceuticas que los comprenden |
| AU2008297015B2 (en) | 2007-08-30 | 2013-08-22 | Vertex Pharmaceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| MY159837A (en) | 2009-08-29 | 2017-02-15 | Abbvie Inc | Therapeutic dll4 binding proteins |
| SG183872A1 (en) | 2010-03-02 | 2012-11-29 | Abbvie Inc | Therapeutic dll4 binding proteins |
| BR112013002578A2 (pt) | 2010-08-03 | 2019-05-14 | Abbvie Inc. | imunoglobinas de domínio variável duplo e usos das mesmas |
| TW202210507A (zh) | 2012-11-01 | 2022-03-16 | 美商艾伯維有限公司 | 抗-vegf/dll4雙重可變區域免疫球蛋白及其用途 |
| WO2016094881A2 (en) | 2014-12-11 | 2016-06-16 | Abbvie Inc. | Lrp-8 binding proteins |
| CN107531653B (zh) * | 2015-05-11 | 2021-10-19 | 豪夫迈·罗氏有限公司 | 新的二氟酮酰胺衍生物 |
| TW201710286A (zh) | 2015-06-15 | 2017-03-16 | 艾伯維有限公司 | 抗vegf、pdgf及/或其受體之結合蛋白 |
| MX2021015894A (es) * | 2019-07-01 | 2022-02-03 | Basf Se | Peptidos acetales para estabilizar enzimas. |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE787249A (fr) | 1971-08-05 | 1973-02-05 | Squibb & Sons Inc | Derives amino d'acides pyrazolopyridine carboxyliques, leurs esters et les sels de ces composes, ainsi que leurs procedes de preparation |
| US3935280A (en) | 1975-01-10 | 1976-01-27 | Aldrich-Boranes, Inc. | Reduction of amino acids in the presence of boron trifluoride |
| US4277395A (en) * | 1980-06-16 | 1981-07-07 | Richardson-Merrell Inc. | Novel enzyme inhibitors |
| DE3481913D1 (de) | 1983-04-27 | 1990-05-17 | Ici America Inc | Prolin-derivate. |
| US4518528A (en) * | 1983-05-19 | 1985-05-21 | Rasnick David W | α Amino fluoro ketones |
| GB8600263D0 (en) * | 1985-01-22 | 1986-02-12 | Ici America Inc | Peptide derivatives |
-
1986
- 1986-06-05 DE DE8686304296T patent/DE3683541D1/de not_active Expired - Fee Related
- 1986-06-05 EP EP86304296A patent/EP0204571B1/en not_active Expired - Lifetime
- 1986-06-05 AT AT86304296T patent/ATE71934T1/de not_active IP Right Cessation
- 1986-06-06 FI FI862434A patent/FI86859C/fi not_active IP Right Cessation
- 1986-06-06 JP JP61130457A patent/JPH07116159B2/ja not_active Expired - Fee Related
- 1986-06-06 GR GR861488A patent/GR861488B/el unknown
- 1986-06-06 NO NO862269A patent/NO170585C/no unknown
- 1986-06-06 HU HU862393A patent/HU208438B/hu not_active IP Right Cessation
- 1986-06-06 DK DK267686A patent/DK267686A/da not_active Application Discontinuation
- 1986-06-06 AU AU58454/86A patent/AU594683B2/en not_active Ceased
- 1986-06-06 ES ES555826A patent/ES8801305A1/es not_active Expired
- 1986-06-06 IE IE151386A patent/IE59146B1/en not_active IP Right Cessation
- 1986-06-06 PT PT82724A patent/PT82724B/pt not_active IP Right Cessation
- 1986-06-06 IL IL79049A patent/IL79049A0/xx unknown
- 1986-06-06 NZ NZ216437A patent/NZ216437A/xx unknown
-
1987
- 1987-06-04 US US07/058,079 patent/US4880780A/en not_active Expired - Lifetime
- 1987-09-16 ES ES557734A patent/ES8900051A1/es not_active Expired
- 1987-09-16 ES ES557733A patent/ES8802619A1/es not_active Expired
- 1987-09-16 ES ES557735A patent/ES8802321A1/es not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| FI862434A0 (fi) | 1986-06-06 |
| FI862434A7 (fi) | 1986-12-08 |
| ES555826A0 (es) | 1987-12-16 |
| IE59146B1 (en) | 1994-01-12 |
| ES8802321A1 (es) | 1988-05-01 |
| JPH07116159B2 (ja) | 1995-12-13 |
| FI86859C (fi) | 1992-10-26 |
| PT82724B (pt) | 1988-12-15 |
| AU5845486A (en) | 1986-12-18 |
| ES8801305A1 (es) | 1987-12-16 |
| DK267686D0 (da) | 1986-06-06 |
| PT82724A (en) | 1986-07-01 |
| NO862269L (no) | 1986-12-08 |
| EP0204571B1 (en) | 1992-01-22 |
| ES557734A0 (es) | 1988-11-16 |
| ES8900051A1 (es) | 1988-11-16 |
| ATE71934T1 (de) | 1992-02-15 |
| GR861488B (en) | 1986-09-05 |
| EP0204571A3 (en) | 1988-09-21 |
| HUT40811A (en) | 1987-02-27 |
| ES557733A0 (es) | 1988-09-01 |
| IL79049A0 (en) | 1986-09-30 |
| EP0204571A2 (en) | 1986-12-10 |
| ES557735A0 (es) | 1988-05-01 |
| FI86859B (fi) | 1992-07-15 |
| HU208438B (en) | 1993-10-28 |
| DE3683541D1 (de) | 1992-03-05 |
| AU594683B2 (en) | 1990-03-15 |
| JPS6253951A (ja) | 1987-03-09 |
| NO862269D0 (no) | 1986-06-06 |
| NZ216437A (en) | 1990-06-26 |
| NO170585B (no) | 1992-07-27 |
| IE861513L (en) | 1986-12-07 |
| DK267686A (da) | 1986-12-08 |
| US4880780A (en) | 1989-11-14 |
| NO170585C (no) | 1992-11-04 |
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