JP2005515994A5 - - Google Patents
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- Publication number
- JP2005515994A5 JP2005515994A5 JP2003548825A JP2003548825A JP2005515994A5 JP 2005515994 A5 JP2005515994 A5 JP 2005515994A5 JP 2003548825 A JP2003548825 A JP 2003548825A JP 2003548825 A JP2003548825 A JP 2003548825A JP 2005515994 A5 JP2005515994 A5 JP 2005515994A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- heteroaryl
- pharmaceutical composition
- composition according
- 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.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- -1 nitro, sulfoxy, sulfonyl Chemical group 0.000 claims 5
- 206010039710 Scleroderma Diseases 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000001302 tertiary amino group Chemical group 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims 2
- 230000005856 abnormality Effects 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- VUAFHZCUKUDDBC-SCSAIBSYSA-N (2s)-2-[(2-methyl-2-sulfanylpropanoyl)amino]-3-sulfanylpropanoic acid Chemical compound CC(C)(S)C(=O)N[C@H](CS)C(O)=O VUAFHZCUKUDDBC-SCSAIBSYSA-N 0.000 claims 1
- XCPPIJCBCWUBNT-UHFFFAOYSA-N 2-(1,3-benzothiazol-2-yl)-2-[2-[[4-(morpholin-4-ylmethyl)phenyl]methoxy]pyrimidin-4-yl]acetonitrile Chemical group N=1C2=CC=CC=C2SC=1C(C#N)C(N=1)=CC=NC=1OCC(C=C1)=CC=C1CN1CCOCC1 XCPPIJCBCWUBNT-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 239000005541 ACE inhibitor Substances 0.000 claims 1
- XKJMBINCVNINCA-UHFFFAOYSA-N Alfalone Chemical compound CON(C)C(=O)NC1=CC=C(Cl)C(Cl)=C1 XKJMBINCVNINCA-UHFFFAOYSA-N 0.000 claims 1
- 229940124638 COX inhibitor Drugs 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 208000032544 Cicatrix Diseases 0.000 claims 1
- 208000001708 Dupuytren contracture Diseases 0.000 claims 1
- 102400000686 Endothelin-1 Human genes 0.000 claims 1
- 101800004490 Endothelin-1 Proteins 0.000 claims 1
- 229940122091 Geranylgeranyltransferase inhibitor Drugs 0.000 claims 1
- 229940122439 Hydroxylase inhibitor Drugs 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 229940121922 Lysyl oxidase inhibitor Drugs 0.000 claims 1
- BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 claims 1
- 206010060932 Postoperative adhesion Diseases 0.000 claims 1
- 102000004079 Prolyl Hydroxylases Human genes 0.000 claims 1
- 108010043005 Prolyl Hydroxylases Proteins 0.000 claims 1
- 102000003743 Relaxin Human genes 0.000 claims 1
- 108090000103 Relaxin Proteins 0.000 claims 1
- 229930189237 Rotalin Natural products 0.000 claims 1
- 206010062553 Scleroderma renal crisis Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 208000005392 Spasm Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 239000004098 Tetracycline Substances 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 210000003403 autonomic nervous system Anatomy 0.000 claims 1
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical class C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 1
- 229960004272 bucillamine Drugs 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 208000003295 carpal tunnel syndrome Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- KAQKFAOMNZTLHT-VVUHWYTRSA-N epoprostenol Chemical compound O1C(=CCCCC(O)=O)C[C@@H]2[C@@H](/C=C/[C@@H](O)CCCCC)[C@H](O)C[C@@H]21 KAQKFAOMNZTLHT-VVUHWYTRSA-N 0.000 claims 1
- 229960001123 epoprostenol Drugs 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- LVASCWIMLIKXLA-LSDHHAIUSA-N halofuginone Chemical compound O[C@@H]1CCCN[C@H]1CC(=O)CN1C(=O)C2=CC(Cl)=C(Br)C=C2N=C1 LVASCWIMLIKXLA-LSDHHAIUSA-N 0.000 claims 1
- 229950010152 halofuginone Drugs 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 239000000612 proton pump inhibitor Substances 0.000 claims 1
- 229940126409 proton pump inhibitor Drugs 0.000 claims 1
- 201000003086 pulmonary systemic sclerosis Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 231100000241 scar Toxicity 0.000 claims 1
- 230000037387 scars Effects 0.000 claims 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 229960002180 tetracycline Drugs 0.000 claims 1
- 229930101283 tetracycline Natural products 0.000 claims 1
- 235000019364 tetracycline Nutrition 0.000 claims 1
- 150000003522 tetracyclines Chemical class 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- LBLWIGSPWVYIPO-UHFFFAOYSA-N Cc1nc(I)ncc1 Chemical compound Cc1nc(I)ncc1 LBLWIGSPWVYIPO-UHFFFAOYSA-N 0.000 description 4
- 0 *C(C#N)=C1SC2=CC=C(*)CC=C2N1 Chemical compound *C(C#N)=C1SC2=CC=C(*)CC=C2N1 0.000 description 3
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01000727 | 2001-12-07 | ||
| PCT/EP2002/013857 WO2003047570A1 (en) | 2001-12-07 | 2002-12-06 | Benzazole derivatives for the treatment of scleroderma |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010127168A Division JP2010248205A (ja) | 2001-12-07 | 2010-06-02 | 強皮症の治療のためのベンザゾール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005515994A JP2005515994A (ja) | 2005-06-02 |
| JP2005515994A5 true JP2005515994A5 (https=) | 2006-01-26 |
| JP4589002B2 JP4589002B2 (ja) | 2010-12-01 |
Family
ID=8176107
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003548825A Expired - Lifetime JP4589002B2 (ja) | 2001-12-07 | 2002-12-06 | 強皮症の治療のためのベンザゾール誘導体 |
| JP2010127168A Pending JP2010248205A (ja) | 2001-12-07 | 2010-06-02 | 強皮症の治療のためのベンザゾール誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010127168A Pending JP2010248205A (ja) | 2001-12-07 | 2010-06-02 | 強皮症の治療のためのベンザゾール誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7776854B2 (https=) |
| EP (1) | EP1450792B1 (https=) |
| JP (2) | JP4589002B2 (https=) |
| AT (1) | ATE340572T1 (https=) |
| AU (1) | AU2002352227B2 (https=) |
| CA (1) | CA2468826C (https=) |
| DE (1) | DE60215042T2 (https=) |
| DK (1) | DK1450792T3 (https=) |
| ES (1) | ES2268127T3 (https=) |
| IL (1) | IL162259A0 (https=) |
| PT (1) | PT1450792E (https=) |
| SI (1) | SI1450792T1 (https=) |
| WO (1) | WO2003047570A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5021307B2 (ja) * | 2003-09-12 | 2012-09-05 | メルク セローノ ソシエテ アノニム | 糖尿病治療のためのベンゾチアゾール誘導体 |
| US7878978B2 (en) | 2004-03-18 | 2011-02-01 | University Of Pittsburgh- Of The Commonwealth System Of Higher Education | Use of relaxin to increase arterial compliance |
| US20070203134A1 (en) * | 2004-09-10 | 2007-08-30 | Applied Research Systems Ars Holding N.V. | Benzimidazole Acetonitriles |
| US7838522B2 (en) | 2004-11-17 | 2010-11-23 | Ares Trading S.A. | Benzothiazole formulations and use thereof |
| JP5144271B2 (ja) * | 2004-11-17 | 2013-02-13 | アレス トレーディング ソシエテ アノニム | ベンゾチアゾ−ル製剤、及びそれらの使用 |
| KR20080044836A (ko) | 2005-07-15 | 2008-05-21 | 라보라뚜와르 세로노 에스. 에이. | 자궁내막증 치료용 ｊｎｋ 억제제 |
| BRPI0613042A2 (pt) | 2005-07-15 | 2010-12-14 | Serono Lab | inibidores de jnk para o tratamento de endometriose |
| WO2007141224A2 (en) * | 2006-06-02 | 2007-12-13 | Laboratoires Serono Sa | Jnk inhibitors for treatment of skin diseases |
| US20080305186A1 (en) * | 2007-06-11 | 2008-12-11 | Board Of Regents, The University Of Texas System | Method and Composition for the Treatment of Cardiac Hypertrophy |
| JP2011520902A (ja) * | 2008-05-16 | 2011-07-21 | コーセラ，インコーポレーテッド | 創傷の治癒を促進する方法 |
| US8680076B2 (en) | 2010-10-25 | 2014-03-25 | Signal Pharmaceuticals, Llc | Methods of treatment, improvement and prevention using haloaryl substituted aminopurines |
| WO2014114186A1 (zh) * | 2013-01-24 | 2014-07-31 | 山东亨利医药科技有限责任公司 | Jnk抑制剂 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0666812B2 (ja) | 1988-01-11 | 1994-08-24 | 日本電気株式会社 | パケット交換方法並びにパケット交換装置 |
| US5985592A (en) | 1997-06-05 | 1999-11-16 | Dalhousie University | Uses for pentoxifylline or functional derivatives/metabolites thereof |
| WO2000075118A1 (en) * | 1999-06-03 | 2000-12-14 | Vertex Pharmaceuticals Incorporated | INHIBITORS OF c-JUN N-TERMINAL KINASES (JNK) |
| EP1110957A1 (en) | 1999-12-24 | 2001-06-27 | Applied Research Systems ARS Holding N.V. | Benzazole derivatives and their use as JNK modulators |
| US20020111353A1 (en) * | 2000-12-05 | 2002-08-15 | Mark Ledeboer | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
-
2002
- 2002-12-06 AT AT02787919T patent/ATE340572T1/de active
- 2002-12-06 DE DE60215042T patent/DE60215042T2/de not_active Expired - Lifetime
- 2002-12-06 IL IL16225902A patent/IL162259A0/xx unknown
- 2002-12-06 JP JP2003548825A patent/JP4589002B2/ja not_active Expired - Lifetime
- 2002-12-06 AU AU2002352227A patent/AU2002352227B2/en not_active Expired
- 2002-12-06 CA CA2468826A patent/CA2468826C/en not_active Expired - Lifetime
- 2002-12-06 SI SI200230413T patent/SI1450792T1/sl unknown
- 2002-12-06 EP EP02787919A patent/EP1450792B1/en not_active Expired - Lifetime
- 2002-12-06 US US10/496,785 patent/US7776854B2/en not_active Expired - Lifetime
- 2002-12-06 PT PT02787919T patent/PT1450792E/pt unknown
- 2002-12-06 DK DK02787919T patent/DK1450792T3/da active
- 2002-12-06 ES ES02787919T patent/ES2268127T3/es not_active Expired - Lifetime
- 2002-12-06 WO PCT/EP2002/013857 patent/WO2003047570A1/en not_active Ceased
-
2010
- 2010-06-02 JP JP2010127168A patent/JP2010248205A/ja active Pending
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