JP2006527722A - Ａｌｋ−５受容体の阻害剤としての４−（ヘテロサイクル−縮合フェニル）−３−（フェニルまたはピリド−２−イル）ピラゾール - Google Patents
Ａｌｋ−５受容体の阻害剤としての４−（ヘテロサイクル−縮合フェニル）−３−（フェニルまたはピリド−２−イル）ピラゾール Download PDFInfo
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- JP2006527722A JP2006527722A JP2006515936A JP2006515936A JP2006527722A JP 2006527722 A JP2006527722 A JP 2006527722A JP 2006515936 A JP2006515936 A JP 2006515936A JP 2006515936 A JP2006515936 A JP 2006515936A JP 2006527722 A JP2006527722 A JP 2006527722A
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- methyl
- pyrazol
- pyrazole
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- 239000003112 inhibitor Substances 0.000 title abstract description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 title 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
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- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 150000003355 serines Chemical group 0.000 description 1
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M sodium bicarbonate Substances [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- WGRULTCAYDOGQK-UHFFFAOYSA-M sodium;sodium;hydroxide Chemical compound [OH-].[Na].[Na+] WGRULTCAYDOGQK-UHFFFAOYSA-M 0.000 description 1
- 239000007790 solid phase Substances 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000001593 sorbitan monooleate Substances 0.000 description 1
- 235000011069 sorbitan monooleate Nutrition 0.000 description 1
- 229940035049 sorbitan monooleate Drugs 0.000 description 1
- 230000000707 stereoselective effect Effects 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 150000003460 sulfonic acids Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229960001367 tartaric acid Drugs 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
- PHCBRBWANGJMHS-UHFFFAOYSA-J tetrasodium;disulfate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O PHCBRBWANGJMHS-UHFFFAOYSA-J 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- FWPIDFUJEMBDLS-UHFFFAOYSA-L tin(II) chloride dihydrate Substances O.O.Cl[Sn]Cl FWPIDFUJEMBDLS-UHFFFAOYSA-L 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 238000001890 transfection Methods 0.000 description 1
- 238000011830 transgenic mouse model Methods 0.000 description 1
- QIWRFOJWQSSRJZ-UHFFFAOYSA-N tributyl(ethenyl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C=C QIWRFOJWQSSRJZ-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 230000037314 wound repair Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Urology & Nephrology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0313915.1A GB0313915D0 (en) | 2003-06-16 | 2003-06-16 | Compounds |
| PCT/EP2004/006427 WO2004111036A1 (fr) | 2003-06-16 | 2004-06-14 | 4-(heterocyclyle-phenyle fusionne)-3-phenyle ou pyrid-2-yle)pyrazoles utilises comme inhibiteurs du recepteur de alk-5 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2006527722A true JP2006527722A (ja) | 2006-12-07 |
Family
ID=27636631
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006515936A Withdrawn JP2006527722A (ja) | 2003-06-16 | 2004-06-14 | Ａｌｋ−５受容体の阻害剤としての４−（ヘテロサイクル−縮合フェニル）−３−（フェニルまたはピリド−２−イル）ピラゾール |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1656367A1 (fr) |
| JP (1) | JP2006527722A (fr) |
| GB (1) | GB0313915D0 (fr) |
| WO (1) | WO2004111036A1 (fr) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170045348A (ko) * | 2014-10-07 | 2017-04-26 | 일라이 릴리 앤드 캄파니 | 아미노피리딜옥시피라졸 화합물 |
| JP2019522038A (ja) * | 2016-07-29 | 2019-08-08 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 窒素含有芳香族複素環式化合物、その製造方法、薬物組成物および使用 |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
| TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| US20100056505A1 (en) * | 2005-11-21 | 2010-03-04 | Biogen Idec Ma Inc. | Substituted Pyrazalones |
| MX2008012104A (es) | 2006-03-28 | 2008-10-03 | Wyeth Corp | Moduladores del gdf-9/bmp-15 para el tratamiento de trastornos de los huesos. |
| EP1878733A1 (fr) * | 2006-07-14 | 2008-01-16 | Novartis AG | Dérivés de pyrimidine comme inhibiteurs de ALK-5 |
| MX2009000310A (es) | 2006-07-14 | 2009-01-26 | Novartis Ag | Derivados de pirimidina como inhibidores de alk-5. |
| UY32656A (es) * | 2009-05-27 | 2010-12-31 | Sanofi Aventis | Procedimiento para producir benzofuranos |
| WO2020123453A2 (fr) * | 2018-12-11 | 2020-06-18 | Theravance Biopharma R&D Ip, Llc | Inhibiteurs d'alk5 |
| EP4061809A1 (fr) * | 2019-11-22 | 2022-09-28 | Theravance Biopharma R&D IP, LLC | 1,5-naphtyridines ou quinoléines substituées en tant qu'inhibiteurs d'alk5 |
| EP4173675A1 (fr) * | 2021-10-26 | 2023-05-03 | Perha Pharmaceuticals | Dérivés d'imidazolone d'en tant qu'inhibiteurs de kinases de protéine en particulier, dyrk1a, clk1 et/ou clk4 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3734180B2 (ja) * | 1994-12-28 | 2006-01-11 | エーザイ株式会社 | 新規ピラゾール誘導体 |
| GB0027987D0 (en) * | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
| GB0102672D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| DE60207390T2 (de) * | 2001-03-09 | 2006-07-20 | Pfizer Products Inc., Groton | Entzündungshemmende benzimidazolverbindungen |
| US7247734B2 (en) * | 2001-12-21 | 2007-07-24 | Vernalis (Cambridge) Limited | 3,4-diarylpyrazoles and their use in the therapy of cancer |
| CA2496295C (fr) * | 2002-09-18 | 2010-11-23 | Michael John Munchhof | Nouveaux composes de pyrazole utilises comme inhibiteurs du facteur de croissance transformant (tgf) |
| CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
-
2003
- 2003-06-16 GB GBGB0313915.1A patent/GB0313915D0/en not_active Ceased
-
2004
- 2004-06-14 JP JP2006515936A patent/JP2006527722A/ja not_active Withdrawn
- 2004-06-14 EP EP04739898A patent/EP1656367A1/fr not_active Withdrawn
- 2004-06-14 WO PCT/EP2004/006427 patent/WO2004111036A1/fr active Application Filing
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170045348A (ko) * | 2014-10-07 | 2017-04-26 | 일라이 릴리 앤드 캄파니 | 아미노피리딜옥시피라졸 화합물 |
| KR101921847B1 (ko) | 2014-10-07 | 2018-11-23 | 일라이 릴리 앤드 캄파니 | 아미노피리딜옥시피라졸 화합물 |
| JP2019522038A (ja) * | 2016-07-29 | 2019-08-08 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 窒素含有芳香族複素環式化合物、その製造方法、薬物組成物および使用 |
| JP7007359B2 (ja) | 2016-07-29 | 2022-01-24 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 窒素含有芳香族複素環式化合物、その製造方法、薬物組成物および使用 |
| US11466003B2 (en) | 2016-07-29 | 2022-10-11 | Shanghai Yingli Pharmaceutical Co., Ltd | Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1656367A1 (fr) | 2006-05-17 |
| WO2004111036A1 (fr) | 2004-12-23 |
| GB0313915D0 (en) | 2003-07-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A300 | Application deemed to be withdrawn because no request for examination was validly filed |
Free format text: JAPANESE INTERMEDIATE CODE: A300 Effective date: 20070904 |