BR9812127A - Arylpyridazinones as inhibitors of prostaglein biosynthesis endoperoxide h synthase - Google Patents
Arylpyridazinones as inhibitors of prostaglein biosynthesis endoperoxide h synthaseInfo
- Publication number
- BR9812127A BR9812127A BR9812127-8A BR9812127A BR9812127A BR 9812127 A BR9812127 A BR 9812127A BR 9812127 A BR9812127 A BR 9812127A BR 9812127 A BR9812127 A BR 9812127A
- Authority
- BR
- Brazil
- Prior art keywords
- cox
- inhibitors
- prostaglein
- endoperoxide
- cyclooxygenase
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 102100038280 Prostaglandin G/H synthase 2 Human genes 0.000 abstract 3
- 102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 abstract 3
- 108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 abstract 3
- 108010037464 Cyclooxygenase 1 Proteins 0.000 abstract 2
- 102100038277 Prostaglandin G/H synthase 1 Human genes 0.000 abstract 2
- 108050003267 Prostaglandin G/H synthase 2 Proteins 0.000 abstract 2
- 102000001708 Protein Isoforms Human genes 0.000 abstract 2
- 108010029485 Protein Isoforms Proteins 0.000 abstract 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 abstract 2
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 abstract 1
- 108010037462 Cyclooxygenase 2 Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 210000003734 kidney Anatomy 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
- C07D237/14—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
- C07D237/18—Sulfur atoms
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
"ARILPIRIDAZINONAS COMO INIBIDORES DA BIOSSìNTESE DE PROSTAGLEINA ENDOPERóXIDO H SINTASE" A presente invenção divulga compostos de piridazinona, os quais são inibidores da ciclooxigenase (COX) e, em particular, são inibidores seletivos da ciclooxigenase-2 (COX/2). A COX-2 é a isoforma capaz de ser induzida associada com a inflamação, em oposição à isoforma constitutiva, a ciclooxigenase-1 (COX-1), que é uma enzima "zeladora" importante em muitos tecidos, incluindo o trato gastrointestinal (GI) e os rins. A seletividade destes compostos para a COX-2 minimiza os efeitos colaterais GI e renais não desejados, vistos com as drogas antiinflamatórias não-esteroidais (NSAIDs) atualmente vendidas."ARYLYPYRIDAZINES AS INHIBITORS OF PROSTAGLEIN ENDOPEROXIDE H SYNTHESIS BIOSYNTHESIS" The present invention discloses pyridazinone compounds, which are inhibitors of cyclooxygenase (COX) and, in particular, are selective inhibitors of cyclooxygenase-2 (COX / 2). COX-2 is the isoform capable of being induced associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1), which is an important "janitor" enzyme in many tissues, including the gastrointestinal tract (GI ) and the kidneys. The selectivity of these compounds for COX-2 minimizes unwanted GI and renal side effects, seen with the currently sold non-steroidal anti-inflammatory drugs (NSAIDs).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91702397A | 1997-08-22 | 1997-08-22 | |
| PCT/US1998/016479 WO1999010331A1 (en) | 1997-08-22 | 1998-08-10 | Arylpyridazinones as prostaglandin endoperoxide h synthase biosynthesis inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9812127A true BR9812127A (en) | 2000-07-18 |
Family
ID=25438243
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9812127-8A BR9812127A (en) | 1997-08-22 | 1998-08-10 | Arylpyridazinones as inhibitors of prostaglein biosynthesis endoperoxide h synthase |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1007515A1 (en) |
| BR (1) | BR9812127A (en) |
| CA (1) | CA2299300C (en) |
| CO (1) | CO4970740A1 (en) |
| SA (1) | SA98190764B1 (en) |
| TW (1) | TWI232216B (en) |
| WO (1) | WO1999010331A1 (en) |
| ZA (1) | ZA987555B (en) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6307047B1 (en) * | 1997-08-22 | 2001-10-23 | Abbott Laboratories | Prostaglandin endoperoxide H synthase biosynthesis inhibitors |
| US6525053B1 (en) * | 1997-08-22 | 2003-02-25 | Abbott Laboratories | Prostaglandin endoperoxide H synthase biosynthesis inhibitors |
| NZ504045A (en) | 1997-11-19 | 2001-06-29 | Kowa Co | Pyridazine derivatives with inhibitory action against interleukin-1-beta production |
| TWI241295B (en) | 1998-03-02 | 2005-10-11 | Kowa Co | Pyridazine derivative and medicine containing the same as effect component |
| EP1130015A4 (en) * | 1998-08-14 | 2006-02-08 | Nihon Nohyaku Co Ltd | Pyridazinone derivatives |
| HK1041876B (en) * | 1998-10-27 | 2006-06-23 | Abbott Laboratories | Prostaglandin endoperoxide h synthase biosynthesis inhibitors |
| US6833373B1 (en) | 1998-12-23 | 2004-12-21 | G.D. Searle & Co. | Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia |
| US6858598B1 (en) | 1998-12-23 | 2005-02-22 | G. D. Searle & Co. | Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia |
| JP2000247959A (en) | 1999-02-26 | 2000-09-12 | Kowa Co | Pyridazin-3-one derivatives and pharmaceuticals containing the same |
| IL144760A0 (en) | 1999-12-08 | 2002-06-30 | Pharmacia Corp | Cyclooxygenase-2 inhibitor compositions having rapid onset of therapeutic effect |
| JP2003523958A (en) | 1999-12-23 | 2003-08-12 | ニトロメド インコーポレーテッド | Inhibitors, compositions and uses of nitrosated and nitrosylated cyclooxygenase-2 |
| US6664256B1 (en) | 2000-07-10 | 2003-12-16 | Kowa Co., Ltd. | Phenylpyridazine compounds and medicines containing the same |
| ITMI20010733A1 (en) | 2001-04-05 | 2002-10-05 | Recordati Chem Pharm | USE OF ISOENZIN COX-2 INHIBITORS FOR THE TREATMENT OF URINARY INCONTINENCE |
| AR038957A1 (en) | 2001-08-15 | 2005-02-02 | Pharmacia Corp | COMBINATION THERAPY FOR CANCER TREATMENT |
| JP2005519895A (en) * | 2002-01-18 | 2005-07-07 | ファルマシア・コーポレーション | Substituted pyridazinones as P38 inhibitors |
| US7211598B2 (en) | 2002-06-28 | 2007-05-01 | Nitromed, Inc. | Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use |
| US7211577B2 (en) | 2003-03-18 | 2007-05-01 | Kowa Co., Ltd. | Water-soluble phenylpyridazine derivative and medicine containing the same |
| ES2275218T3 (en) | 2003-05-07 | 2007-06-01 | Osteologix A/S | HYDROSOLUBLE STRONTIUM SALTS FOR THE TREATMENT OF CARTILAGOS AND / OR BONE AFFECTIONS. |
| WO2005007632A1 (en) * | 2003-07-18 | 2005-01-27 | Pharmacia Corporation | Substituted pyridazinones as inhibitors of p38 |
| DE602005014359D1 (en) | 2004-06-09 | 2009-06-18 | Sumitomo Chemical Co | PYRIDAZINE COMPOUND AND ITS USE |
| US7795258B2 (en) | 2004-06-28 | 2010-09-14 | Sumitomo Chemical Company, Limited | Pyridazine compound and use thereof |
| PT1928454E (en) | 2005-05-10 | 2014-12-04 | Intermune Inc | Pyridone derivatives for modulating stress-activated protein kinase system |
| CA2623813A1 (en) | 2005-10-03 | 2007-04-12 | Ono Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic compound and pharmaceutical application thereof |
| BRPI0619516B1 (en) | 2005-12-07 | 2015-09-15 | Sumitomo Chemical Co | pyridazine compound and its use, as well as plant disease control agent and method |
| DK1958948T3 (en) | 2005-12-07 | 2011-10-31 | Sumitomo Chemical Co | Pyridazine compound and its use |
| DE102007008839A1 (en) | 2007-02-23 | 2008-08-28 | Bayer Healthcare Ag | Process for the preparation of 4- (3-hydroxy-3-methylbutoxy) -5- [4- (methylsulfonyl) phenyl] -2-arylpyridazine-3 (2H) -ones |
| DE102007008840A1 (en) * | 2007-02-23 | 2008-08-28 | Bayer Healthcare Ag | Novel polymorphic form of 2- (4-fluorophenyl) -4-3-hydroxy-3-methyl-1-butoxy) -5- [4-methylsulphonyl) phenyl] -3 (2H) -pyridazinone (FHMP) |
| DE102007008843A1 (en) | 2007-02-23 | 2008-08-28 | Bayer Healthcare Ag | Process for the preparation of 4,5-dihalo-2-aryl-2H-pyridazin-3-ones |
| DE102007020690A1 (en) * | 2007-05-03 | 2008-11-06 | Bayer Healthcare Ag | New amorphous form of 2- (4-fluorophenyl) -4-3-hydroxy-3-methyl-1-butoxy) -6 [4-methylsulfonyl) phenyl] -3 (2H) -pyridazinone (FHMP) |
| DE102007020689A1 (en) * | 2007-05-03 | 2008-11-06 | Bayer Healthcare Ag | Novel polymorphic form of 2- (4-fluorophenyl) -4-3-hydroxy-3-methyl-1-butoxy-5- [4-methylsulfonyl) phenyl] 3 / 2H) -pyridazinone (FHMP) |
| US8304413B2 (en) | 2008-06-03 | 2012-11-06 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
| JO3115B1 (en) | 2011-08-22 | 2017-09-20 | Takeda Pharmaceuticals Co | Pyridazinone Compounds and Their Use as DAAO Inhibitors |
| JP6169492B2 (en) | 2011-11-15 | 2017-07-26 | 武田薬品工業株式会社 | Dihydroxy aromatic heterocyclic compounds |
| AR092742A1 (en) | 2012-10-02 | 2015-04-29 | Intermune Inc | ANTIFIBROTIC PYRIDINONES |
| KR102373700B1 (en) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | Anti-fibrotic pyridinones |
| US11096924B2 (en) | 2016-09-07 | 2021-08-24 | Trustees Of Tufts College | Combination therapies using immuno-dash inhibitors and PGE2 antagonists |
| IL305573A (en) | 2021-03-15 | 2023-10-01 | Saul Yedgar | Hyaluronic acid conjugated with dipalmitoyl phosphatidyl ethanolamine in combination with non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment or suppression of inflammatory diseases |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1988009675A1 (en) * | 1987-06-05 | 1988-12-15 | Medicis Corporation | Inhibition of arachidonic acid metabolism |
| AU691673B2 (en) * | 1994-11-14 | 1998-05-21 | Dow Agrosciences Llc | Pyridazinones and their use as fungicides |
| US5622948A (en) * | 1994-12-01 | 1997-04-22 | Syntex (U.S.A.) Inc. | Pyrrole pyridazine and pyridazinone anti-inflammatory agents |
-
1998
- 1998-08-10 EP EP98938451A patent/EP1007515A1/en not_active Withdrawn
- 1998-08-10 WO PCT/US1998/016479 patent/WO1999010331A1/en not_active Ceased
- 1998-08-10 CA CA002299300A patent/CA2299300C/en not_active Expired - Fee Related
- 1998-08-10 BR BR9812127-8A patent/BR9812127A/en not_active Application Discontinuation
- 1998-08-20 ZA ZA987555A patent/ZA987555B/en unknown
- 1998-08-20 CO CO98047584A patent/CO4970740A1/en unknown
- 1998-09-10 TW TW087113837A patent/TWI232216B/en not_active IP Right Cessation
- 1998-11-16 SA SA98190764A patent/SA98190764B1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SA98190764B1 (en) | 2006-08-06 |
| WO1999010331A1 (en) | 1999-03-04 |
| CO4970740A1 (en) | 2000-11-07 |
| EP1007515A1 (en) | 2000-06-14 |
| CA2299300A1 (en) | 1999-03-04 |
| ZA987555B (en) | 1999-02-23 |
| TWI232216B (en) | 2005-05-11 |
| CA2299300C (en) | 2007-04-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09B | Patent application refused [chapter 9.2 patent gazette] |
Free format text: INDEFERIMENTO DO PRESENTE PEDIDO, UMA VEZ QUE DIANTE DO QUE FOI EXPOSTO, OPINO POR NAO ACOLHER A PRESENTACAO DO INTERESSADO E, CONSIDERANDO QUE NAO FORAM APRESENTADOS ARGUMENTOS PERTINENTES, CONCLUI- SE QUE O PEDIDO EM LIDE NAO APRESENTA REQUISITOS QUE JUSTIFIQUEM O SEU REEXAME |
|
| B12B | Appeal against refusal [chapter 12.2 patent gazette] |