JP2013501751A - 経口用固体製剤および結晶形態のアポトーシスタンパク質インヒビター - Google Patents
経口用固体製剤および結晶形態のアポトーシスタンパク質インヒビター Download PDFInfo
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- JP2013501751A JP2013501751A JP2012524227A JP2012524227A JP2013501751A JP 2013501751 A JP2013501751 A JP 2013501751A JP 2012524227 A JP2012524227 A JP 2012524227A JP 2012524227 A JP2012524227 A JP 2012524227A JP 2013501751 A JP2013501751 A JP 2013501751A
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- 239000000126 substance Substances 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 229950000244 sulfanilic acid Drugs 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- MYOWBHNETUSQPA-UHFFFAOYSA-N tetradecane-1-sulfonic acid Chemical compound CCCCCCCCCCCCCCS(O)(=O)=O MYOWBHNETUSQPA-UHFFFAOYSA-N 0.000 description 1
- CBXCPBUEXACCNR-UHFFFAOYSA-N tetraethylammonium Chemical compound CC[N+](CC)(CC)CC CBXCPBUEXACCNR-UHFFFAOYSA-N 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 229940035024 thioglycerol Drugs 0.000 description 1
- AOBORMOPSGHCAX-DGHZZKTQSA-N tocofersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-DGHZZKTQSA-N 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 239000012485 toluene extract Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000002699 waste material Substances 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- 235000004835 α-tocopherol Nutrition 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2004—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
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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)
- Biophysics (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27405109P | 2009-08-12 | 2009-08-12 | |
| US61/274,051 | 2009-08-12 | ||
| PCT/EP2010/061679 WO2011018474A1 (en) | 2009-08-12 | 2010-08-11 | Solid oral formulations and crystalline forms of an inhibitor of apoptosis protein |
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| JP2016060543A Ceased JP2016179976A (ja) | 2009-08-12 | 2016-03-24 | 経口用固体製剤および結晶形態のアポトーシスタンパク質インヒビター |
| JP2018116705A Pending JP2018172403A (ja) | 2009-08-12 | 2018-06-20 | 経口用固体製剤および結晶形態のアポトーシスタンパク質インヒビター |
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| JP2016060543A Ceased JP2016179976A (ja) | 2009-08-12 | 2016-03-24 | 経口用固体製剤および結晶形態のアポトーシスタンパク質インヒビター |
| JP2018116705A Pending JP2018172403A (ja) | 2009-08-12 | 2018-06-20 | 経口用固体製剤および結晶形態のアポトーシスタンパク質インヒビター |
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| AU (4) | AU2010283748A1 (enExample) |
| BR (1) | BR112012003118A2 (enExample) |
| CA (1) | CA2769616A1 (enExample) |
| CL (1) | CL2012000349A1 (enExample) |
| CO (1) | CO6612189A2 (enExample) |
| IL (1) | IL217760A0 (enExample) |
| IN (1) | IN2012DN00858A (enExample) |
| MA (1) | MA33511B1 (enExample) |
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| MY (1) | MY160475A (enExample) |
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| SG (1) | SG177713A1 (enExample) |
| TN (1) | TN2012000026A1 (enExample) |
| TW (1) | TWI607006B (enExample) |
| WO (1) | WO2011018474A1 (enExample) |
| ZA (1) | ZA201200390B (enExample) |
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| CN109311867A (zh) | 2016-04-20 | 2019-02-05 | 葛兰素史克知识产权开发有限公司 | 包含ripk2抑制剂的共轭物 |
| CN108484640B (zh) * | 2018-05-22 | 2020-09-15 | 南京华威医药科技集团有限公司 | 一种抗肿瘤的细胞凋亡蛋白抑制剂 |
| BR112020024296A2 (pt) | 2018-08-27 | 2021-03-09 | Regeneron Pharmaceuticals, Inc. | Métodos para produção de um intermediário de purificação de proteína concentrado, para monitoramento e controle dos atributos de qualidade críticos em um intermediário de purificação de proteína e para monitorar e controlar os níveis de excipientes no fluido de cultura de células colhido e/ou intermediário de purificação de proteína, e, intermediário de purificação de proteína |
| WO2021220178A1 (en) | 2020-04-29 | 2021-11-04 | Cominnex Zrt. | Iap antagonists and their therapeutic applications |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005502861A (ja) * | 2001-08-10 | 2005-01-27 | サイミックス テクノロジーズ， インコーポレイテッド | 事前処方物を作製および試験するための装置および方法ならびにそのためのシステム |
| JP2007532504A (ja) * | 2004-04-07 | 2007-11-15 | ノバルティス アクチエンゲゼルシャフト | Ｉａｐの阻害剤 |
| WO2008016893A1 (en) * | 2006-08-02 | 2008-02-07 | Novartis Ag | Smac peptidomimetics useful as iap inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2491041A1 (en) | 2002-07-02 | 2004-01-15 | Novartis Ag | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| ATE477254T1 (de) * | 2004-12-20 | 2010-08-15 | Genentech Inc | Pyrrolidine als inhibitoren von iap |
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2010
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- 2010-08-11 PE PE2012000206A patent/PE20121132A1/es not_active Application Discontinuation
- 2010-08-11 MX MX2013011692A patent/MX351274B/es unknown
- 2010-08-11 MY MYPI2012000350A patent/MY160475A/en unknown
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- 2010-08-11 SG SG2012004222A patent/SG177713A1/en unknown
- 2010-08-11 JP JP2012524227A patent/JP2013501751A/ja not_active Withdrawn
- 2010-08-11 IN IN858DEN2012 patent/IN2012DN00858A/en unknown
- 2010-08-11 AU AU2010283748A patent/AU2010283748A1/en not_active Abandoned
- 2010-08-11 RU RU2015155182A patent/RU2671196C1/ru not_active IP Right Cessation
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- 2010-08-11 CN CN201080035867.0A patent/CN102471331B/zh not_active Expired - Fee Related
- 2010-08-11 KR KR1020187004166A patent/KR20180020315A/ko not_active Ceased
- 2010-08-11 EP EP10751839A patent/EP2464644A1/en not_active Withdrawn
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- 2010-08-11 PE PE2017000424A patent/PE20170777A1/es not_active Application Discontinuation
- 2010-08-12 TW TW099126987A patent/TWI607006B/zh not_active IP Right Cessation
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2012
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- 2012-01-26 IL IL217760A patent/IL217760A0/en unknown
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- 2012-02-10 CL CL2012000349A patent/CL2012000349A1/es unknown
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2013
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2014
- 2014-08-14 AU AU2014213533A patent/AU2014213533A1/en not_active Abandoned
- 2014-08-20 PH PH12014501890A patent/PH12014501890B1/en unknown
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2016
- 2016-03-24 JP JP2016060543A patent/JP2016179976A/ja not_active Ceased
- 2016-05-13 AU AU2016203145A patent/AU2016203145A1/en not_active Abandoned
- 2016-11-30 US US15/364,841 patent/US10093665B2/en not_active Expired - Fee Related
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2017
- 2017-11-03 AU AU2017254950A patent/AU2017254950B2/en not_active Ceased
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2018
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- 2018-08-31 US US16/120,073 patent/US20180370960A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005502861A (ja) * | 2001-08-10 | 2005-01-27 | サイミックス テクノロジーズ， インコーポレイテッド | 事前処方物を作製および試験するための装置および方法ならびにそのためのシステム |
| JP2007532504A (ja) * | 2004-04-07 | 2007-11-15 | ノバルティス アクチエンゲゼルシャフト | Ｉａｐの阻害剤 |
| WO2008016893A1 (en) * | 2006-08-02 | 2008-02-07 | Novartis Ag | Smac peptidomimetics useful as iap inhibitors |
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| BASTIN,R.J. ET AL: "Salt selection and optimization procedures for pharmaceutical new chemical entities", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 4, no. 5, JPN6009059058, 2000, pages 427 - 435, ISSN: 0003199187 * |
| CAIRA，M. R.: ""Crystalline Polymorphism of Organic Compounds"", TOPICS IN CURRENT CHEMISTRY, vol. 198, JPN5012016574, 1 January 1998 (1998-01-01), pages 163 - 208, ISSN: 0002934998 * |
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