AR054195A1 - Derivados de indol como inhibidores de la fosfolipasa a2 citosolica y composicion farmaceutica que los contiene - Google Patents
Derivados de indol como inhibidores de la fosfolipasa a2 citosolica y composicion farmaceutica que los contieneInfo
- Publication number
- AR054195A1 AR054195A1 ARP060102198A ARP060102198A AR054195A1 AR 054195 A1 AR054195 A1 AR 054195A1 AR P060102198 A ARP060102198 A AR P060102198A AR P060102198 A ARP060102198 A AR P060102198A AR 054195 A1 AR054195 A1 AR 054195A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- inhibitors
- phospholipase
- 3alkyl
- quinolin
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 102100037611 Lysophospholipase Human genes 0.000 title abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- 108010058864 Phospholipases A2 Proteins 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 quinolin-5-yl Chemical group 0.000 abstract 8
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 3
- 229910052801 chlorine Inorganic materials 0.000 abstract 3
- 239000000460 chlorine Substances 0.000 abstract 3
- 229910052731 fluorine Inorganic materials 0.000 abstract 3
- 239000011737 fluorine Substances 0.000 abstract 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 108020002496 Lysophospholipase Proteins 0.000 abstract 2
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- AQTFKGDWFRRIHR-UHFFFAOYSA-L 3-[18-(2-carboxylatoethyl)-8,13-bis(ethenyl)-3,7,12,17-tetramethylporphyrin-21,24-diid-2-yl]propanoate;cobalt(2+);hydron Chemical compound [Co+2].[N-]1C(C=C2C(=C(C)C(C=C3C(=C(C)C(=C4)[N-]3)C=C)=N2)C=C)=C(C)C(CCC(O)=O)=C1C=C1C(CCC(O)=O)=C(C)C4=N1 AQTFKGDWFRRIHR-UHFFFAOYSA-L 0.000 abstract 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 102000003658 Group IV Phospholipases A2 Human genes 0.000 abstract 1
- 108010082107 Group IV Phospholipases A2 Proteins 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 108010064785 Phospholipases Proteins 0.000 abstract 1
- 102000015439 Phospholipases Human genes 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 229940054051 antipsychotic indole derivative Drugs 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 239000013000 chemical inhibitor Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000001086 cytosolic effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000002475 indoles Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Derivados de indol como inhibidores químicos de la actividad de diversas enzimas fosfolipasa, particularmente de las enzimas fosfolipasa A2 citosolica (cPLA2), más particularmente incluyendo inhibidores de las enzimas fosfolipasa A2 alfa citosolica (cPLA2alfa). En algunas modalidades, los inhibidores poseen la formula (1). Se proveen también posicion farmacéutica que los contiene. Reivindicacion 1: Un compuesto que tiene la formula (1), en la cual: n1 es 1 o 2; n2 es 1 o 2; n3 es 1 o 2; n5 es 0, 1, o 2; X2 es un enlace O, -CH2- o SO2; cada R5 es independientemente H o alquilo C1-3; R6 es H alquilo C1-6; R7 es seleccionado del grupo que consiste de OH, benciloxi, CH3, CF3, OCF3, alcoxi C1-3, halogeno, COH, COalquilC1-3, CO(OalquilC1-3), quinolin-5-ilo, quinolin-8-ilo, 3,5-dimetilsoxazol-4-ilo, tiofen-3-ilo, piridin-4-ilo, piridin-3-ilo, -CH2-Q, y fenilo opcionalmente sustituido con desde uno hasta tres grupos R30 independientemente seleccionados; R8 es seleccionado del grupo que consiste de H, OH, NO2, CF3, OCF3, alcoxi C1-3, halogeno, COalquilC1-3, CO(OalquilC1-3), quinolin-5-ilo, quinolin-8-ilo, 3,5-dimetilsoxazol-4-ilo, tiofen-3-ilo, -CH2-Q, y fenilo sustituido por desde uno hasta tres grupos R30 independientemente seleccionados; Q es OH, dialquilamino, o un grupo de formulas (2) o (3); R20 es seleccionado del grupo que consiste de H, alquilo C1-3 y COalquilC1-3); y R30 es seleccionado del grupo que consiste de dialquilamino, CN y OCF3; con la condicion que: a) cuando cada R5 es H, R6 es H, n5 es 0, y R8 es H, entonces R7 no puede ser cloro; b) cuando cada R5 es H, R6 es H, n5 es 0, X2 es O o -CH2-, y R8 es H, entonces R7 no puede ser CH3; c) cuando cada R5 es H, y R6 es H, entonces R7 y R8 no pueden ser ambos fluor; d) cuando cada R5 es H, R6 es H, y X2 es O, entonces R7 y R8 no pueden ser ambos cloro; e) cuando cada R5 es H, R6 es H, X2 es O, y R8 es NO2, entonces R7 no puede ser fluor; y f) cuando cada R5 es H, R6 es H, X2 es SO2, y R8 es H, entonces R7 no puede ser fluor o cloro; o una sal farmacéuticamente aceptable de lo mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68556405P | 2005-05-27 | 2005-05-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR054195A1 true AR054195A1 (es) | 2007-06-06 |
Family
ID=37188759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102198A AR054195A1 (es) | 2005-05-27 | 2006-05-26 | Derivados de indol como inhibidores de la fosfolipasa a2 citosolica y composicion farmaceutica que los contiene |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US7557135B2 (es) |
| EP (2) | EP1891006B1 (es) |
| JP (1) | JP5116666B2 (es) |
| KR (1) | KR101353982B1 (es) |
| CN (2) | CN101184729B (es) |
| AR (1) | AR054195A1 (es) |
| AT (1) | ATE489364T1 (es) |
| AU (1) | AU2006251946B2 (es) |
| BR (1) | BRPI0610049A2 (es) |
| CA (1) | CA2607857C (es) |
| CR (1) | CR9520A (es) |
| CY (1) | CY1111151T1 (es) |
| DE (1) | DE602006018451D1 (es) |
| DK (1) | DK1891006T3 (es) |
| ES (1) | ES2354908T3 (es) |
| GT (1) | GT200600228A (es) |
| HN (1) | HN2006019513A (es) |
| IL (1) | IL186912A (es) |
| MX (1) | MX2007014589A (es) |
| MY (1) | MY144672A (es) |
| NI (1) | NI200700287A (es) |
| NO (1) | NO20075627L (es) |
| NZ (1) | NZ563736A (es) |
| PE (1) | PE20061426A1 (es) |
| PL (1) | PL1891006T3 (es) |
| PT (1) | PT1891006E (es) |
| RU (1) | RU2433997C2 (es) |
| SI (1) | SI1891006T1 (es) |
| SV (1) | SV2008002551A (es) |
| TW (1) | TW200718687A (es) |
| UA (1) | UA91053C2 (es) |
| WO (1) | WO2006128142A2 (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7713964B2 (en) * | 2001-12-03 | 2010-05-11 | Wyeth Llc | Methods for treating asthmatic conditions |
| US7605156B2 (en) | 2001-12-03 | 2009-10-20 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 |
| HN2004000536A (es) | 2003-12-16 | 2009-02-18 | Wyeth Corp | Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles |
| IL161579A0 (en) | 2004-04-22 | 2004-09-27 | Mor Research Applic Ltd | ANTISENSE OLIGONUCLEOTIDES AGAINST cPLA2, COMPOSITIONS AND USES THEREOF |
| EP1744761A4 (en) | 2004-04-28 | 2010-01-13 | Molecules For Health Inc | METHOD FOR THE TREATMENT OR PREVENTION OF RESTENOSIS AND OTHER PROLIFERATIVE VASCULAR DISORDER |
| TW200718687A (en) | 2005-05-27 | 2007-05-16 | Wyeth Corp | Inhibitors of cytosolic phospholipase A2 |
| US20080009485A1 (en) * | 2006-05-26 | 2008-01-10 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis |
| IL178401A (en) | 2006-09-28 | 2012-04-30 | Univ Ben Gurion | Use of antisense oligonucleotides against 2 cPLA in the treatment of cancer |
| CL2007003146A1 (es) * | 2006-10-31 | 2008-01-25 | Wyeth Corp | Composición farmacéutica que comprende un compuesto derivado de indol y un sistema portador que comprende 15-25% de un mejorador de la viscosidad, 5-15% de un solubilizante, 10-50% de un diluyente y 1-10% de un estabilizante; proceso de preparación; y forma de dosificación. |
| US20100113443A1 (en) * | 2006-10-31 | 2010-05-06 | Wyeth | Liquid formulations of phospholipase enzyme inhibitors |
| CA2681979A1 (en) | 2007-03-29 | 2008-10-09 | Asubio Pharma Co., Ltd. | Indole derivatives having cpla2 inhibiting activity and applications and production methods of the same |
| EP2030615A3 (en) * | 2007-08-13 | 2009-12-02 | ELFORD, Howard L. | Ribonucleotide reductase inhibitors for use in the treatment or prevention of neuroinflammatory or autoimmune diseases |
| US9011821B2 (en) | 2010-06-18 | 2015-04-21 | Whitehead Institute For Biomedical Research | PLA2G16 as a target for antiviral compounds |
| WO2012031763A1 (en) | 2010-09-08 | 2012-03-15 | Twincore Zentrum Fuer Experimentelle Und Klinische Infektionsforschung Gmbh | Use of inhibitors of phospholipase a2 for the treatment or prevention of flavivirus infection |
| GB201401904D0 (en) | 2014-02-04 | 2014-03-19 | Ziarco Pharma Ltd | Pharmaceutical composition for topical administration |
| JP6380524B2 (ja) * | 2014-02-28 | 2018-08-29 | 住友化学株式会社 | ２−（ハロゲノメチル）−３−メチルニトロベンゼンの製造方法 |
| CN103804150A (zh) * | 2014-03-01 | 2014-05-21 | 江苏斯威森生物医药工程研究中心有限公司 | 一种3,4-二甲氧基苄基溴的制备方法 |
| CN108017522B (zh) * | 2017-11-16 | 2021-01-05 | 贵州大学 | 一种2,6-二溴苯甲磺酰氯的制备工艺 |
| WO2020236777A1 (en) * | 2019-05-20 | 2020-11-26 | Saint Louis University | Reprogramming of lipid metabolism to inhibit t cell senescence and enhance tumor immunotherapy |
| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| KR20220161438A (ko) | 2020-03-30 | 2022-12-06 | 길리애드 사이언시즈, 인코포레이티드 | Cot 억제제 화합물, (S)-6-(((1-(바이사이클로[1.1.1]펜탄-1-일)-1H-1,2,3-트라이아졸-4-일)2-메틸-1-옥소-1,2-다이하이드로아이소퀴놀린-5-일)메틸)))아미노8-클로로-(네오펜틸아미노)퀴놀린-3-카르보니트릴의 고체 형태 |
| WO2021202688A1 (en) * | 2020-04-02 | 2021-10-07 | Gilead Sciences, Inc. | Process for preparing a cot inhibitor compound |
| US20230338529A1 (en) * | 2020-08-06 | 2023-10-26 | The Children's Medical Center Corporation | Compositions for altering a microglial cell, and methods of use therefore |
Family Cites Families (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH48411A (fr) | 1909-07-19 | 1910-10-17 | Stephen Alley | Outillage pour mettre en place et enlever les bandages élastiques des roues de véhicules |
| GB1148909A (en) | 1965-04-19 | 1969-04-16 | Sumitomo Chemical Co | Process for production of novel phenylhydrazone and phenylhydrazine derivatives |
| FR1492929A (fr) | 1966-05-11 | 1967-08-25 | Roussel Uclaf | Nouveaux 1-(omega-carboxyalcoyl) indoles substitués et procédé de préparation |
| US3505354A (en) | 1967-05-18 | 1970-04-07 | Geigy Chem Corp | 2-methyl-3-p-halobenzoylindole-n-aliphatic acids |
| DE1816335A1 (de) | 1968-12-21 | 1970-07-09 | Thiemann Gmbh Chem Pharm Fabri | Verfahren zur Herstellung von [2-Methyl-5-alkoxy-3-acyl-indol-1]-essigsaeuren und deren Estern |
| US3931229A (en) | 1973-08-23 | 1976-01-06 | Warner-Lambert Company | 3-Thiomethyl-2[2-(dialkylamino)ethyl]indoles |
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| US4271263A (en) | 1980-05-15 | 1981-06-02 | Minnesota Mining And Manufacturing Company | Thermally developable photosensitive compositions containing acutance agents |
| US4501728A (en) | 1983-01-06 | 1985-02-26 | Technology Unlimited, Inc. | Masking of liposomes from RES recognition |
| US4654360A (en) | 1984-06-01 | 1987-03-31 | Syntex (U.S.A.) Inc. | 1,2,3-trisubstituted indoles for treatment of inflammation |
| US4737323A (en) | 1986-02-13 | 1988-04-12 | Liposome Technology, Inc. | Liposome extrusion method |
| US4837028A (en) | 1986-12-24 | 1989-06-06 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| US4894386A (en) | 1987-04-15 | 1990-01-16 | Ici Americas Inc. | Aliphatic carboxamides |
| ES2045420T3 (es) | 1988-04-13 | 1994-01-16 | Ici America Inc | Amidas ciclicas. |
| GB8906032D0 (en) | 1988-04-14 | 1989-04-26 | Ici America Inc | Hetera-aliphatic carboxamides |
| US5166170A (en) | 1989-07-03 | 1992-11-24 | Hoechst-Roussel Pharmaceuticals Incorporated | 2-(aminoaryl) indoles and indolines as topical antiinflammatory agents for the treatment of skin disorders |
| GB8916774D0 (en) | 1989-07-21 | 1989-09-06 | Bayer Ag | New indole derivatives,a process for their preparation and their use in medicaments |
| US5229516A (en) | 1989-10-27 | 1993-07-20 | American Home Products Corporation | Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase |
| US5420289A (en) | 1989-10-27 | 1995-05-30 | American Home Products Corporation | Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase |
| PT95692A (pt) | 1989-10-27 | 1991-09-13 | American Home Prod | Processo para a preparacao de derivados de acidos indole-,indeno-,piranoindole- e tetra-hidrocarbazole-alcanoicos, ou quais sao uteis como inibidores de pla2 e da lipoxigenase |
| US5081145A (en) | 1990-02-01 | 1992-01-14 | Merck Frosst Canada, Inc. | Indole-2-alkanoic acids compositions of and anti allergic use thereof |
| US5622832A (en) | 1990-02-28 | 1997-04-22 | Genetics Institute, Inc. | Arachidonic acid releasing phospholipase A2 enzyme and methods of use |
| US5190968A (en) | 1991-09-30 | 1993-03-02 | Merck Frosst Canada, Inc. | (Polycyclic-arylmethoxy) indoles as inhibitors of leukotriene biosynthesis |
| US5290798A (en) | 1991-09-30 | 1994-03-01 | Merck Frosst Canada, Inc. | (hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis |
| US5206377A (en) | 1991-12-05 | 1993-04-27 | Whitby Research, Inc. | Compounds useful as antiproliferative agents |
| AU672599B2 (en) | 1992-05-13 | 1996-10-10 | Syntex (U.S.A.) Inc. | Substituted indoles and azaindoles as angiotensin II antagonists |
| US5212195A (en) | 1992-05-13 | 1993-05-18 | Syntex (U.S.A.) Inc. | Substituted indole antagonists derivatives which are angiotensin II |
| US5288743A (en) | 1992-11-20 | 1994-02-22 | Abbott Laboratories | Indole carboxylate derivatives which inhibit leukotriene biosynthesis |
| ZA939516B (en) | 1992-12-22 | 1994-06-06 | Smithkline Beecham Corp | Endothelin receptor antagonists |
| IL109311A0 (en) | 1993-04-16 | 1994-07-31 | Lilly Co Eli | 1H-indole-3-acetamide sPla2 inhibitors |
| IL109309A (en) * | 1993-04-16 | 2000-06-29 | Lilly Co Eli | 1-H-indole-3-acetic acid hydrazide SPLA2 inhibitors and pharmaceutical compositions containing them |
| US5424329A (en) | 1993-08-18 | 1995-06-13 | Warner-Lambert Company | Indole-2-carboxamides as inhibitors of cell adhesion |
| DE4338770A1 (de) | 1993-11-12 | 1995-05-18 | Matthias Dr Lehr | Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶ |
| US5686481A (en) | 1993-12-21 | 1997-11-11 | Smithkline Beecham Corporation | Endothelin receptor antagonists |
| US5641800A (en) | 1994-07-21 | 1997-06-24 | Eli Lilly And Company | 1H-indole-1-functional sPLA2 inhibitors |
| US5482960A (en) | 1994-11-14 | 1996-01-09 | Warner-Lambert Company | Nonpeptide endothelin antagonists |
| AU3767997A (en) | 1996-08-01 | 1998-02-25 | Merckle Gmbh | Acylpyrroldicarboxylic acids and acylindoldicarboxylic acids and their derivatives and inhibitors of the cytosolic phospholipase a2 |
| AU717430B2 (en) | 1996-08-26 | 2000-03-23 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
| US6630496B1 (en) | 1996-08-26 | 2003-10-07 | Genetics Institute Llc | Inhibitors of phospholipase enzymes |
| US5994398A (en) | 1996-12-11 | 1999-11-30 | Elan Pharmaceuticals, Inc. | Arylsulfonamides as phospholipase A2 inhibitors |
| SK12742000A3 (sk) * | 1998-02-25 | 2001-05-10 | Genetics Institute, Inc. | Inhibítory fosfolipázových enzýmov, farmaceutický prostriedok s ich obsahom a ich použitie |
| EA200000873A1 (ru) | 1998-02-25 | 2001-04-23 | Дженетикс Инститьют, Инк. | Ингибиторы фосфолипазы a |
| PL343007A1 (en) | 1998-02-25 | 2001-07-30 | Genetics Inst | Inhibitors of phospholipase enzymes |
| US6500853B1 (en) | 1998-02-28 | 2002-12-31 | Genetics Institute, Llc | Inhibitors of phospholipase enzymes |
| CN1178915C (zh) | 1999-01-27 | 2004-12-08 | 惠氏控股有限公司 | 含有炔基的异羟肟酸衍生物、其制备及其作为基质金属蛋白酶抑制剂/TNF-α转变酶抑制剂的用途 |
| US6424105B1 (en) | 1999-06-08 | 2002-07-23 | Camco International, Inc. | Real-time control of feedback signals to a motor for optimum performance |
| KR20020086665A (ko) | 2001-01-22 | 2002-11-18 | 소니 가부시끼 가이샤 | 용제 흡수성 수지 및 그 제조 방법 |
| US7101875B2 (en) * | 2001-12-03 | 2006-09-05 | Wyeth | Methods for treating arthritic disorders |
| US7713964B2 (en) * | 2001-12-03 | 2010-05-11 | Wyeth Llc | Methods for treating asthmatic conditions |
| US6797708B2 (en) * | 2001-12-03 | 2004-09-28 | Wyeth | Inhibitors of cytosolic phospholipase A2 |
| US6635771B2 (en) | 2001-12-03 | 2003-10-21 | Wyeth | N-benzhydryl indole compounds |
| US7605156B2 (en) | 2001-12-03 | 2009-10-20 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 |
| ES2401454T3 (es) * | 2001-12-03 | 2013-04-19 | Wyeth Llc | Inhibidores de la fosfolipasa A2 citosólica |
| US6984735B2 (en) | 2001-12-03 | 2006-01-10 | Wyeth | Process for making an aldehyde |
| WO2004060878A2 (en) | 2002-12-31 | 2004-07-22 | Vertex Pharmaceuticals Incorporated | Inhibitors of phosphatases |
| US7439249B2 (en) | 2002-12-31 | 2008-10-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of phosphatases |
| TW200510305A (en) | 2003-07-25 | 2005-03-16 | Wyeth Corp | Process for the preparation of CPLA2 inhibitors |
| US7582771B2 (en) | 2003-09-03 | 2009-09-01 | Wyeth | Process for the synthesis of cPLA2 inhibitors |
| US20050053600A1 (en) | 2003-09-09 | 2005-03-10 | Lane Thomas E. | Methods for treating rheumatoid arthritis |
| US7342119B2 (en) | 2003-09-30 | 2008-03-11 | Wyeth Holdings Corporation | Process for the synthesis of a CPLA2 inhibitor |
| HN2004000536A (es) | 2003-12-16 | 2009-02-18 | Wyeth Corp | Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles |
| AR053410A1 (es) | 2004-08-19 | 2007-05-09 | Wyeth Corp | Proceso para la sintesis de indoles n-alquilados c-2, c-3 sustituidos. compuestos intermediarios |
| TW200718687A (en) | 2005-05-27 | 2007-05-16 | Wyeth Corp | Inhibitors of cytosolic phospholipase A2 |
| US20080009485A1 (en) * | 2006-05-26 | 2008-01-10 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis |
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