BRPI0618210A2 - compostos, composição farmacêutica, métodos de produção de um composto e de preparação de uma composição farmacêutica, uso de um composto ou de um sal farmaceuticamente aceitável do mesmo - Google Patents
compostos, composição farmacêutica, métodos de produção de um composto e de preparação de uma composição farmacêutica, uso de um composto ou de um sal farmaceuticamente aceitável do mesmo Download PDFInfo
- Publication number
- BRPI0618210A2 BRPI0618210A2 BRPI0618210-0A BRPI0618210A BRPI0618210A2 BR PI0618210 A2 BRPI0618210 A2 BR PI0618210A2 BR PI0618210 A BRPI0618210 A BR PI0618210A BR PI0618210 A2 BRPI0618210 A2 BR PI0618210A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- formula
- group
- dioxo
- methylamino
- Prior art date
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- 238000000034 method Methods 0.000 title claims abstract description 106
- 150000003839 salts Chemical class 0.000 title claims abstract description 59
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- 238000011282 treatment Methods 0.000 claims abstract description 25
- 238000002360 preparation method Methods 0.000 claims abstract description 23
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 15
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- 102000007466 Purinergic P2 Receptors Human genes 0.000 claims abstract 2
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 73
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 73
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 70
- -1 6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl Chemical group 0.000 claims description 64
- 239000002904 solvent Substances 0.000 claims description 52
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- WUPZRLYEGIXBNO-UHFFFAOYSA-N 1-(5-chlorothiophen-2-yl)sulfonyl-1-[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1h-quinazolin-3-yl]phenyl]urea Chemical compound O=C1C=2C=C(F)C(NC)=CC=2NC(=O)N1C(C=C1)=CC=C1N(C(N)=O)S(=O)(=O)C1=CC=C(Cl)S1 WUPZRLYEGIXBNO-UHFFFAOYSA-N 0.000 claims description 25
- 238000002329 infrared spectrum Methods 0.000 claims description 24
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims description 24
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- WLMZTKAZJUWXCB-KQYNXXCUSA-N [(2r,3s,4r,5r)-5-(6-amino-2-methylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate Chemical compound C12=NC(SC)=NC(N)=C2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O WLMZTKAZJUWXCB-KQYNXXCUSA-N 0.000 claims description 6
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- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims description 4
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- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 3
- KLPPUPBECAHKEF-UHFFFAOYSA-N thiophen-2-ylsulfonylurea Chemical compound NC(=O)NS(=O)(=O)C1=CC=CS1 KLPPUPBECAHKEF-UHFFFAOYSA-N 0.000 claims 3
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- TYMLOMAKGOJONV-UHFFFAOYSA-N 4-nitroaniline Chemical compound NC1=CC=C([N+]([O-])=O)C=C1 TYMLOMAKGOJONV-UHFFFAOYSA-N 0.000 claims 1
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- PPADHTVWIWCEDE-UHFFFAOYSA-M potassium;(5-chlorothiophen-2-yl)sulfonyl-[[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1h-quinazolin-3-yl]phenyl]carbamoyl]azanide Chemical compound [K+].O=C1C=2C=C(F)C(NC)=CC=2NC(=O)N1C(C=C1)=CC=C1NC(=O)[N-]S(=O)(=O)C1=CC=C(Cl)S1 PPADHTVWIWCEDE-UHFFFAOYSA-M 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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Classifications
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
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- A—HUMAN NECESSITIES
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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- A—HUMAN NECESSITIES
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- 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
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- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Urology & Nephrology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
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| EP (2) | EP1951254B1 (enExample) |
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| KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｘａ 인자 억제제 |
| CA2627719C (en) | 2005-11-03 | 2016-07-12 | Portola Pharmaceuticals, Inc. | [4-(6-halo-7-substituted-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylureas and forms and methods related thereto |
| EP2016072B1 (en) | 2006-05-05 | 2014-07-16 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| WO2008133155A1 (ja) | 2007-04-19 | 2008-11-06 | Astellas Pharma Inc. | 二環式ヘテロ環化合物 |
| US20090156620A1 (en) * | 2007-05-02 | 2009-06-18 | Portola Pharmaceuticals, Inc. | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea salts, forms and methods related thereto |
| CA2686221A1 (en) * | 2007-05-02 | 2008-11-13 | Portola Pharmaceuticals, Inc. | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea salts, forms and methods related thereto |
| KR101509829B1 (ko) * | 2007-05-02 | 2015-04-06 | 포톨라 파마슈티컬스, 인코포레이티드 | 혈소판 ａｄｐ 수용체 억제제로 작용하는 화합물을 이용한 병용요법 |
| US20090048216A1 (en) | 2007-05-02 | 2009-02-19 | Portola Pharmaceuticals, Inc. | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
| MX2009013431A (es) * | 2007-06-18 | 2010-01-15 | Sanofi Aventis | Derivados de pirrol como antagonistas de p2y12. |
| CN101654441B (zh) * | 2008-08-19 | 2012-10-03 | 信谊药厂 | 抗凝化合物、组合物及其用途 |
| RU2011123377A (ru) * | 2008-11-14 | 2012-12-20 | Портола Фармасьютиклз, Инк. | ТВЕРДАЯ КОМПОЗИЦИЯ ДЛЯ КОНТРОЛИРУЕМОГО ВЫСВОБОЖДЕНИЯ АКТИВНЫХ ИОНИЗИРУЕМЫХ АГЕНТОВ, ХАРАКТЕРИЗУЮЩИХСЯ НИЗКОЙ РАСТВОРИМОСТЬЮ В ВОДЕ ПРИ НИЗКИХ ЗНАЧЕНИЯХ pН, И СПОСОБЫ ЕЕ ПРИМЕНЕНИЯ |
| WO2011006169A1 (en) | 2009-07-10 | 2011-01-13 | Portola Pharmaceuticals, Inc. | Methods for diagnosis and treatment of thrombotic disorders mediated by cyp2c19*2 |
| JP5597202B2 (ja) | 2009-08-28 | 2014-10-01 | 第一三共株式会社 | ３−（ビアリールオキシ）プロピオン酸誘導体 |
| EP2513094B1 (en) | 2009-12-17 | 2015-12-16 | Millennium Pharmaceuticals, Inc. | Crystalline salts of a factor xa inhibitor |
| US8742120B2 (en) | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| WO2011088152A1 (en) | 2010-01-12 | 2011-07-21 | Portola Pharmaceuticals, Inc. | Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof |
| WO2011137459A1 (en) | 2010-04-30 | 2011-11-03 | Portola Pharmaceuticals, Inc. | Dosage forms of elinogrel and methods of injectable administration thereof |
| JP2013544271A (ja) * | 2010-12-03 | 2013-12-12 | ポートラ ファーマシューティカルズ， インコーポレイテッド | 式（ｉ）の化合物の薬学的組成物、投薬形態、および新規の形態、ならびにその使用方法 |
| JP6268093B2 (ja) * | 2012-09-14 | 2018-01-24 | キッセイ薬品工業株式会社 | 縮合複素環誘導体の製造方法およびその製造中間体 |
| RU2556198C1 (ru) * | 2014-04-10 | 2015-07-10 | Федеральное государственное бюджетное учреждение "Научно-исследовательский институт кардиологии" Сибирского отделения Российской академии медицинских наук | Способ профилактики развития постперикардиотомного синдрома у больных ишемической болезнью сердца, подвергшихся коронарному шунтированию |
| US9957267B2 (en) | 2015-07-01 | 2018-05-01 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN AND USES THEREOF |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
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| DE845042C (de) | 1950-07-14 | 1952-07-28 | Basf Ag | Verfahren zur Herstellung von Sulfonylurethanen, -harnstoffen oder -carbonsaeureamiden |
| US3847925A (en) * | 1971-07-15 | 1974-11-12 | En Nom Collectif Science Et Ci | Benzenesulfonyl semicarbazides |
| DE3134780A1 (de) * | 1981-09-02 | 1983-03-10 | Hoechst Ag, 6000 Frankfurt | "sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung" |
| US4720450A (en) * | 1985-06-03 | 1988-01-19 | Polaroid Corporation | Thermal imaging method |
| GB9413975D0 (en) | 1994-07-11 | 1994-08-31 | Fujisawa Pharmaceutical Co | New heterobicyclic derivatives |
| US5314902A (en) * | 1993-01-27 | 1994-05-24 | Monsanto Company | Urea derivatives useful as platelet aggregation inhibitors |
| US6268380B1 (en) | 1993-02-19 | 2001-07-31 | G. D. Searle & Co. | Urea derivatives useful as platelet aggregation inhibitors |
| WO1994021602A1 (en) | 1993-03-15 | 1994-09-29 | G.D. Searle & Co. | Urea derivatives useful as platelet aggregation inhibitors |
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2006
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- 2006-11-03 US US11/556,518 patent/US20070208045A1/en not_active Abandoned
- 2006-11-03 TW TW095140749A patent/TW200728260A/zh unknown
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- 2006-11-03 EP EP06827506A patent/EP1951254B1/en active Active
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- 2006-11-03 ZA ZA200804241A patent/ZA200804241B/xx unknown
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- 2006-11-03 EA EA200801245A patent/EA017402B1/ru not_active IP Right Cessation
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- 2006-11-03 ES ES06827506T patent/ES2380814T3/es active Active
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