CN101203211B - 药物组合物 - Google Patents
药物组合物 Download PDFInfo
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- CN101203211B CN101203211B CN2006800219417A CN200680021941A CN101203211B CN 101203211 B CN101203211 B CN 101203211B CN 2006800219417 A CN2006800219417 A CN 2006800219417A CN 200680021941 A CN200680021941 A CN 200680021941A CN 101203211 B CN101203211 B CN 101203211B
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- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 description 1
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- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
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Classifications
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/20—Pills, tablets, discs, rods
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A—HUMAN NECESSITIES
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- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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- A—HUMAN NECESSITIES
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A—HUMAN NECESSITIES
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
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- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US67280505P | 2005-04-19 | 2005-04-19 | |
| US60/672,805 | 2005-04-19 | ||
| PCT/US2006/014447 WO2006113649A1 (en) | 2005-04-19 | 2006-04-18 | Pharmaceutical composition |
Publications (2)
| Publication Number | Publication Date |
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| CN101203211A CN101203211A (zh) | 2008-06-18 |
| CN101203211B true CN101203211B (zh) | 2012-08-08 |
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| CN2006800219417A Active CN101203211B (zh) | 2005-04-19 | 2006-04-18 | 药物组合物 |
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| NO (1) | NO20075111L (enExample) |
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| TW200716204A (en) * | 2005-04-19 | 2007-05-01 | Smithkline Beecham Cork Ltd | Pharmaceutical composition |
| US8252805B2 (en) | 2008-05-07 | 2012-08-28 | Teva Pharmaceutical Industries Ltd. | Forms of lapatinib ditosylate and processes for preparation thereof |
| EP2158912A1 (en) * | 2008-08-25 | 2010-03-03 | Ratiopharm GmbH | Pharmaceutical composition comprising N-[3-chhloro-4-[3-fluorophenyl)methoxy)phenyl]6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine |
| EP2158913A1 (en) | 2008-08-25 | 2010-03-03 | Ratiopharm GmbH | Pharmaceutical composition comprising N-[3-chhloro-4-[(3-fluorophenyl)methoxy]phenyl]6-(5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine |
| WO2010099150A1 (en) * | 2009-02-24 | 2010-09-02 | Smithkline Beecham (Cork) Limited | Pharmaceutical tablet and process |
| US20120245351A1 (en) * | 2009-09-29 | 2012-09-27 | Natco Pharma Limited | Process for the preparation of lapatinib and its pharmaceutically acceptable salts |
| JP5858989B2 (ja) | 2010-05-21 | 2016-02-10 | ノバルティス アーゲー | 組合せ |
| JP2013526578A (ja) | 2010-05-21 | 2013-06-24 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 組合せ |
| US9907767B2 (en) | 2010-08-03 | 2018-03-06 | Velicept Therapeutics, Inc. | Pharmaceutical compositions and the treatment of overactive bladder |
| KR20180008918A (ko) | 2010-08-03 | 2018-01-24 | 앨씨알엑스, 인크. | 과민성 방광 치료를 위한 베타-3 아드레날린 수용체 작용제 및 무스카린 수용체 길항제의 약학적 배합제 |
| EA029119B1 (ru) * | 2013-02-19 | 2018-02-28 | Хексаль Аг | Фармацевтическая композиция, содержащая n-[3-хлор-4-(3-фторбензилокси)фенил]-6-[5({[2-(метилсульфонил)этил]амино}метил)-2-фурил]хиназолин-4-амин или его фармацевтически приемлемые соль, сольват или сольватированную соль |
| WO2014170910A1 (en) | 2013-04-04 | 2014-10-23 | Natco Pharma Limited | Process for the preparation of lapatinib |
| US9636340B2 (en) | 2013-11-12 | 2017-05-02 | Ayyappan K. Rajasekaran | Kinase inhibitors |
| CN107205964A (zh) | 2014-12-03 | 2017-09-26 | 威力塞帕特治疗股份有限公司 | 使用调节释放索拉贝隆用于下尿路症状的组合物和方法 |
| CN106389373B (zh) * | 2015-07-29 | 2019-07-02 | 四川科伦药物研究院有限公司 | 一种二甲苯磺酸拉帕替尼片剂及其制备方法 |
| CN106511289A (zh) * | 2015-09-10 | 2017-03-22 | 湖北生物医药产业技术研究院有限公司 | 甲苯磺酸拉帕替尼片剂及其制备方法 |
| WO2017070689A2 (en) | 2015-10-23 | 2017-04-27 | Velicept Therapeutics, Inc. | Solabegron zwitterion and uses thereof |
Citations (1)
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| CN1440403A (zh) * | 2000-06-30 | 2003-09-03 | 葛兰素集团有限公司 | 喹唑啉二甲苯磺酸盐化合物 |
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| US5506248A (en) * | 1993-08-02 | 1996-04-09 | Bristol-Myers Squibb Company | Pharmaceutical compositions having good dissolution properties |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| NZ336233A (en) | 1997-04-25 | 2001-01-26 | Janssen Pharmaceutica Nv | Phenyl substituted quinazolines on 4-position and 2-quinazolinone moiety bearing a carbon or nitrogen-linked imidazolyl moiety |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| GB9800569D0 (en) * | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| WO2002056912A2 (en) | 2001-01-16 | 2002-07-25 | Glaxo Group Limited | Pharmaceutical combination for the treatment of cancer containing a 4-quinazolineamine and another anti-neoplastic agent |
| EP1492568A1 (en) | 2002-04-08 | 2005-01-05 | SmithKline Beecham Corporation | Cancer treatment method comprising administration of an erb-family inhibitor and a raf and/or ras inhibitor |
| US20060094068A1 (en) | 2002-06-19 | 2006-05-04 | Bacus Sarah S | Predictive markers in cancer therapy |
| TW200716204A (en) * | 2005-04-19 | 2007-05-01 | Smithkline Beecham Cork Ltd | Pharmaceutical composition |
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- 2006-04-18 PT PT67504753T patent/PT1871347T/pt unknown
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1440403A (zh) * | 2000-06-30 | 2003-09-03 | 葛兰素集团有限公司 | 喹唑啉二甲苯磺酸盐化合物 |
Non-Patent Citations (2)
| Title |
|---|
| 邹立家.药剂学 1.中国医药科技出版社,1996,231-238, 257. |
| 邹立家.药剂学 1.中国医药科技出版社,1996,231-238, 257. * |
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