JP2008519826A5 - - Google Patents
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- Publication number
- JP2008519826A5 JP2008519826A5 JP2007540808A JP2007540808A JP2008519826A5 JP 2008519826 A5 JP2008519826 A5 JP 2008519826A5 JP 2007540808 A JP2007540808 A JP 2007540808A JP 2007540808 A JP2007540808 A JP 2007540808A JP 2008519826 A5 JP2008519826 A5 JP 2008519826A5
- Authority
- JP
- Japan
- Prior art keywords
- general formula
- enantiomers
- pharmaceutically acceptable
- racemates
- mixtures
- 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
- 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 16
- 239000000203 mixture Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical class NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 201000006474 Brain Ischemia Diseases 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims 2
- 208000002177 Cataract Diseases 0.000 claims 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 2
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 2
- 108010036949 Cyclosporine Proteins 0.000 claims 2
- 206010011878 Deafness Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 208000002249 Diabetes Complications Diseases 0.000 claims 2
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- 208000003782 Raynaud disease Diseases 0.000 claims 2
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 2
- 208000001647 Renal Insufficiency Diseases 0.000 claims 2
- 206010038419 Renal colic Diseases 0.000 claims 2
- 206010063897 Renal ischaemia Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 208000007107 Stomach Ulcer Diseases 0.000 claims 2
- 208000032851 Subarachnoid Hemorrhage Diseases 0.000 claims 2
- 208000025865 Ulcer Diseases 0.000 claims 2
- 238000002399 angioplasty Methods 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 238000007675 cardiac surgery Methods 0.000 claims 2
- 206010008118 cerebral infarction Diseases 0.000 claims 2
- 208000007451 chronic bronchitis Diseases 0.000 claims 2
- 229960001265 ciclosporin Drugs 0.000 claims 2
- 208000018631 connective tissue disease Diseases 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 229930182912 cyclosporin Natural products 0.000 claims 2
- 208000000718 duodenal ulcer Diseases 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 201000005917 gastric ulcer Diseases 0.000 claims 2
- 230000010370 hearing loss Effects 0.000 claims 2
- 231100000888 hearing loss Toxicity 0.000 claims 2
- 208000016354 hearing loss disease Diseases 0.000 claims 2
- 201000001881 impotence Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 201000006370 kidney failure Diseases 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000007232 portal hypertension Diseases 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 230000035939 shock Effects 0.000 claims 2
- 208000007056 sickle cell anemia Diseases 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- 231100000397 ulcer Toxicity 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- 238000007631 vascular surgery Methods 0.000 claims 2
- -1 2-methoxyphenoxy, 3-methoxyphenoxy, 2-chloro-5-methoxy-phenoxy Chemical group 0.000 claims 1
- NZNJQXHLVGOHMX-UHFFFAOYSA-N 3-(sulfoamino)propanoic acid Chemical compound OC(=O)CCNS(O)(=O)=O NZNJQXHLVGOHMX-UHFFFAOYSA-N 0.000 claims 1
- JIJWAGNGLPTXDB-UHFFFAOYSA-N 3-[[5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]pyrimidin-4-yl]sulfamoylamino]propan-1-ol Chemical compound C=1C=C(Br)C=CC=1C=1C(NS(=O)(=O)NCCCO)=NC=NC=1OCCOC1=NC=C(Br)C=N1 JIJWAGNGLPTXDB-UHFFFAOYSA-N 0.000 claims 1
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- LFEPQTGGEXKQEY-UHFFFAOYSA-N 5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]pyrimidin-4-amine Chemical compound C=1C=C(Br)C=CC=1C=1C(N)=NC=NC=1OCCOC1=NC=C(Br)C=N1 LFEPQTGGEXKQEY-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EPPCT/EP2004/012774 | 2004-11-11 | ||
| EP2004012774 | 2004-11-11 | ||
| PCT/IB2005/053716 WO2006051502A2 (en) | 2004-11-11 | 2005-11-11 | Sulfamides as endothelin receptor antagonists for the treatment of cardiovascular diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008519826A JP2008519826A (ja) | 2008-06-12 |
| JP2008519826A5 true JP2008519826A5 (enExample) | 2008-12-25 |
| JP5020089B2 JP5020089B2 (ja) | 2012-09-05 |
Family
ID=36177271
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007540808A Expired - Fee Related JP5020089B2 (ja) | 2004-11-11 | 2005-11-11 | 心臓血管疾患の治療のためのエンドセリン受容体アンタゴニストとしてのスルファミド類 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7868012B2 (enExample) |
| EP (1) | EP1833821B1 (enExample) |
| JP (1) | JP5020089B2 (enExample) |
| KR (1) | KR101285463B1 (enExample) |
| CN (1) | CN101056872A (enExample) |
| AR (1) | AR051764A1 (enExample) |
| AT (1) | ATE503752T1 (enExample) |
| AU (1) | AU2005303435A1 (enExample) |
| BR (1) | BRPI0517565A (enExample) |
| CA (1) | CA2586106C (enExample) |
| CY (1) | CY1111578T1 (enExample) |
| DE (1) | DE602005027251D1 (enExample) |
| DK (1) | DK1833821T3 (enExample) |
| ES (1) | ES2362103T3 (enExample) |
| MX (1) | MX2007005566A (enExample) |
| PL (1) | PL1833821T3 (enExample) |
| PT (1) | PT1833821E (enExample) |
| RU (1) | RU2007121842A (enExample) |
| SI (1) | SI1833821T1 (enExample) |
| TW (1) | TW200628467A (enExample) |
| WO (1) | WO2006051502A2 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008120093A1 (en) * | 2007-04-03 | 2008-10-09 | Pfizer Inc. | Sulfonamides and pharmaceutical compositions thereof |
| WO2010018549A2 (en) * | 2008-08-13 | 2010-02-18 | Actelion Pharmaceuticals Ltd | Therapeutic compositions containing macitentan |
| AR095727A1 (es) * | 2013-03-27 | 2015-11-04 | Actelion Pharmaceuticals Ltd | Preparación de intermediarios de pirimidina |
| US9899745B2 (en) | 2013-09-13 | 2018-02-20 | Raytheon Company | Low profile high efficiency multi-band reflector antennas |
| CN103724281A (zh) * | 2013-12-03 | 2014-04-16 | 镇江圣安医药有限公司 | N-[5-（4-溴苯基）-6-[2-[（5-溴-2-嘧啶基）氧基]乙氧基]-4-嘧啶基]-n′-丙基磺酰胺的新型衍生物及其应用 |
| CN104447572A (zh) * | 2014-12-15 | 2015-03-25 | 南京艾德凯腾生物医药有限责任公司 | 一种马西替坦的制备方法 |
| HRP20230318T1 (hr) * | 2017-11-21 | 2023-05-12 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Derivat pirimidin sulfamida, postupak pripreme i njegova medicinska primjena |
| CN108997223B (zh) * | 2018-08-09 | 2020-06-30 | 浙江先锋科技股份有限公司 | 5-(4-溴苯基)-4，6-二氯嘧啶的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2086544C1 (ru) | 1991-06-13 | 1997-08-10 | Хоффманн-Ля Рош АГ | Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина |
| TW394761B (en) | 1993-06-28 | 2000-06-21 | Hoffmann La Roche | Novel Sulfonylamino Pyrimidines |
| IL111959A (en) | 1993-12-17 | 2000-07-16 | Tanabe Seiyaku Co | N-(polysubstituted pyrimidin-4-yl) benzenesulfonamide derivatives their preparation and pharmaceutical compositions containing them |
| TW313568B (enExample) | 1994-12-20 | 1997-08-21 | Hoffmann La Roche | |
| US5739333A (en) | 1995-05-16 | 1998-04-14 | Tanabe Seiyaku Co., Ltd. | Sulfonamide derivative and process for preparing the same |
| RU2172735C2 (ru) | 1995-12-20 | 2001-08-27 | Яманоути Фармасьютикал Ко., Лтд. | Арилэтенсульфонамидные производные и фармацевтическая композиция |
| JPH10226649A (ja) * | 1996-12-12 | 1998-08-25 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| BRPI0116237B8 (pt) * | 2000-12-18 | 2021-05-25 | Actelion Pharmaceuticals Ltd | "composto de sulfamida, composição farmacêutica contendo o mesmo e seu uso como medicamento antagonista de receptor de endotelina". |
| AU2003285321B2 (en) * | 2002-12-02 | 2010-04-08 | Actelion Pharmaceuticals Ltd | Pyrimidine-sulfamides and their use as endothelian receptor antagonist |
-
2005
- 2005-11-10 TW TW094139488A patent/TW200628467A/zh unknown
- 2005-11-11 DE DE602005027251T patent/DE602005027251D1/de not_active Expired - Lifetime
- 2005-11-11 WO PCT/IB2005/053716 patent/WO2006051502A2/en not_active Ceased
- 2005-11-11 ES ES05802290T patent/ES2362103T3/es not_active Expired - Lifetime
- 2005-11-11 AR ARP050104726A patent/AR051764A1/es not_active Application Discontinuation
- 2005-11-11 SI SI200531305T patent/SI1833821T1/sl unknown
- 2005-11-11 KR KR1020077012690A patent/KR101285463B1/ko not_active Expired - Fee Related
- 2005-11-11 PL PL05802290T patent/PL1833821T3/pl unknown
- 2005-11-11 DK DK05802290.6T patent/DK1833821T3/da active
- 2005-11-11 AT AT05802290T patent/ATE503752T1/de active
- 2005-11-11 PT PT05802290T patent/PT1833821E/pt unknown
- 2005-11-11 EP EP05802290A patent/EP1833821B1/en not_active Expired - Lifetime
- 2005-11-11 BR BRPI0517565-8A patent/BRPI0517565A/pt not_active Application Discontinuation
- 2005-11-11 JP JP2007540808A patent/JP5020089B2/ja not_active Expired - Fee Related
- 2005-11-11 CN CNA200580038466XA patent/CN101056872A/zh active Pending
- 2005-11-11 CA CA2586106A patent/CA2586106C/en not_active Expired - Fee Related
- 2005-11-11 MX MX2007005566A patent/MX2007005566A/es not_active Application Discontinuation
- 2005-11-11 AU AU2005303435A patent/AU2005303435A1/en not_active Abandoned
- 2005-11-11 RU RU2007121842/04A patent/RU2007121842A/ru not_active Application Discontinuation
- 2005-11-11 US US11/718,922 patent/US7868012B2/en active Active
-
2011
- 2011-06-16 CY CY20111100575T patent/CY1111578T1/el unknown
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