TWI397529B - 〔４-（６-鹵代-７-取代-２，４-二側氧-１，４-二氫-２ｈ-喹唑啉-３-基）-苯基〕-５-氯-噻吩-２-基-磺醯脲，以及與其相關的形式及方法 - Google Patents
〔４-（６-鹵代-７-取代-２，４-二側氧-１，４-二氫-２ｈ-喹唑啉-３-基）-苯基〕-５-氯-噻吩-２-基-磺醯脲，以及與其相關的形式及方法 Download PDFInfo
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- TWI397529B TWI397529B TW095140753A TW95140753A TWI397529B TW I397529 B TWI397529 B TW I397529B TW 095140753 A TW095140753 A TW 095140753A TW 95140753 A TW95140753 A TW 95140753A TW I397529 B TWI397529 B TW I397529B
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- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 150000003109 potassium Chemical class 0.000 description 1
- NTTOTNSKUYCDAV-UHFFFAOYSA-N potassium hydride Chemical compound [KH] NTTOTNSKUYCDAV-UHFFFAOYSA-N 0.000 description 1
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- 239000002243 precursor Substances 0.000 description 1
- 150000003141 primary amines Chemical class 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
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- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
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- ODZPKZBBUMBTMG-UHFFFAOYSA-N sodium amide Chemical compound [NH2-].[Na+] ODZPKZBBUMBTMG-UHFFFAOYSA-N 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
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- 229910052712 strontium Inorganic materials 0.000 description 1
- CIOAGBVUUVVLOB-UHFFFAOYSA-N strontium atom Chemical compound [Sr] CIOAGBVUUVVLOB-UHFFFAOYSA-N 0.000 description 1
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- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
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- 238000004448 titration Methods 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
-
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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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- 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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- Veterinary Medicine (AREA)
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- Biomedical Technology (AREA)
- 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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| CN1968922A (zh) | 2004-06-18 | 2007-05-23 | 米伦纽姆医药公司 | 因子xa抑制剂 |
| EA017402B1 (ru) * | 2005-11-03 | 2012-12-28 | Портола Фармасьютикалз, Инк. | [4-(6-галоген-7-замещенные-2,4-диоксо-1,4-дигидро-2н-хиназолин-3-ил)фенил]-5-хлортиофен-2-илсульфонилмочевины, их формы, способы получения соединений, фармацевтические композиции, содержащие эти соединения, и их применение |
| NZ572418A (en) | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| TW200911755A (en) | 2007-04-19 | 2009-03-16 | Astellas Pharma Inc | Bicyclic heterocyclic compounds |
| 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 |
| WO2008137753A2 (en) | 2007-05-02 | 2008-11-13 | Portola Pharmaceuticals, Inc. | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
| CN101720324A (zh) * | 2007-05-02 | 2010-06-02 | 波托拉医药品公司 | [4-(6-氟-7-甲基氨基-2,4-二氧代-1,4-二氢-2h-喹唑啉-3-基)-苯基]-5-氯-噻吩-2-基-磺酰基脲盐、其相关的形式和方法 |
| NZ599556A (en) | 2007-05-02 | 2013-10-25 | Portola Pharm Inc | Combination therapy with a compound acting as a platelet adp receptor inhibitor |
| AU2008266515B2 (en) * | 2007-06-18 | 2014-05-01 | Sanofi | Pyrrole derivatives as P2Y12 antagonists |
| CN101654441B (zh) * | 2008-08-19 | 2012-10-03 | 信谊药厂 | 抗凝化合物、组合物及其用途 |
| AR074347A1 (es) * | 2008-11-14 | 2011-01-12 | Portola Pharm Inc | Composicion solida para liberacion controlada de agentes activos ionizables con solubilidad acuosa deficiente a ph bajo y sus metodos de uso |
| WO2011006169A1 (en) | 2009-07-10 | 2011-01-13 | Portola Pharmaceuticals, Inc. | Methods for diagnosis and treatment of thrombotic disorders mediated by cyp2c19*2 |
| TW201109339A (en) | 2009-08-28 | 2011-03-16 | Daiichi Sankyo Co Ltd | 3-(biaryloxy) propionic acid derivative |
| CN102762550B (zh) | 2009-12-17 | 2015-04-01 | 米伦纽姆医药公司 | Xa因子抑制剂的盐和结晶形式 |
| US8742120B2 (en) | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| US20130165459A1 (en) | 2010-01-12 | 2013-06-27 | Norvartis Pharma Ag | 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 |
| US8987285B2 (en) * | 2010-12-03 | 2015-03-24 | Portola Pharmaceuticals, Inc. | Pharmaceutical compositions, dosage forms and new forms of the compound of formula (I), and methods of use thereof |
| WO2014042176A1 (ja) * | 2012-09-14 | 2014-03-20 | 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 |
| WO2017003723A1 (en) | 2015-07-01 | 2017-01-05 | 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 |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| 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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| US4542139A (en) * | 1981-09-02 | 1985-09-17 | Hoechst Aktiengesellschaft | Sulfonylureas pharmaceutical formulations based on these compounds and their use for treatment of diabetes |
| US20020077486A1 (en) * | 2000-02-04 | 2002-06-20 | Scarborough Robert M. | Platelet ADP receptor inhibitors |
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2006
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- 2006-11-03 JP JP2008539089A patent/JP5509406B2/ja active Active
- 2006-11-03 WO PCT/US2006/043093 patent/WO2007056219A2/en not_active Ceased
- 2006-11-03 US US11/556,490 patent/US8058284B2/en active Active
- 2006-11-03 KR KR1020087013178A patent/KR101423483B1/ko not_active Expired - Fee Related
- 2006-11-03 AR ARP060104840A patent/AR056762A1/es unknown
- 2006-11-03 NZ NZ596025A patent/NZ596025A/xx not_active IP Right Cessation
- 2006-11-03 TW TW095140749A patent/TW200728260A/zh unknown
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2011
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