CN102471331B - 细胞凋亡蛋白抑制剂的固体口服制剂和晶形 - Google Patents

细胞凋亡蛋白抑制剂的固体口服制剂和晶形 Download PDF

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Publication number
CN102471331B
CN102471331B CN201080035867.0A CN201080035867A CN102471331B CN 102471331 B CN102471331 B CN 102471331B CN 201080035867 A CN201080035867 A CN 201080035867A CN 102471331 B CN102471331 B CN 102471331B
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CN
China
Prior art keywords
acid
ethyl
methylamino
oxo
fluoro
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Expired - Fee Related
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CN201080035867.0A
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English (en)
Chinese (zh)
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CN102471331A (zh
Inventor
J·塔库尔
D·杨
冯丽丽
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Novartis AG
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Novartis AG
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    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
CN201080035867.0A 2009-08-12 2010-08-11 细胞凋亡蛋白抑制剂的固体口服制剂和晶形 Expired - Fee Related CN102471331B (zh)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201610031620.0A Division CN105646471A (zh) 2009-08-12 2010-08-11 细胞凋亡蛋白抑制剂的固体口服制剂和晶形

Publications (2)

Publication Number Publication Date
CN102471331A CN102471331A (zh) 2012-05-23
CN102471331B true CN102471331B (zh) 2016-01-13

Family

ID=42937834

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201080035867.0A Expired - Fee Related CN102471331B (zh) 2009-08-12 2010-08-11 细胞凋亡蛋白抑制剂的固体口服制剂和晶形
CN201610031620.0A Pending CN105646471A (zh) 2009-08-12 2010-08-11 细胞凋亡蛋白抑制剂的固体口服制剂和晶形

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201610031620.0A Pending CN105646471A (zh) 2009-08-12 2010-08-11 细胞凋亡蛋白抑制剂的固体口服制剂和晶形

Country Status (24)

Country Link
US (4) US8623385B2 (enExample)
EP (1) EP2464644A1 (enExample)
JP (3) JP2013501751A (enExample)
KR (2) KR20180020315A (enExample)
CN (2) CN102471331B (enExample)
AR (1) AR077869A1 (enExample)
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)
MX (2) MX351274B (enExample)
MY (1) MY160475A (enExample)
PE (2) PE20170777A1 (enExample)
PH (1) PH12014501890B1 (enExample)
RU (1) RU2671196C1 (enExample)
SG (1) SG177713A1 (enExample)
TN (1) TN2012000026A1 (enExample)
TW (1) TWI607006B (enExample)
WO (1) WO2011018474A1 (enExample)
ZA (1) ZA201200390B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3020792A1 (en) 2016-04-20 2017-10-26 Glaxosmithkline Intellectual Property Development Limited Conjugates comprising ripk2 inhibitors
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
IL280880B2 (en) 2018-08-27 2025-04-01 Regeneron Pharma Using Raman Spectroscopy in Downstream Purification
HUP2200468A1 (hu) 2020-04-29 2023-03-28 X Chem Zrt IAP antagonisták és gyógyászati alkalmazásuk

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008016893A1 (en) * 2006-08-02 2008-02-07 Novartis Ag Smac peptidomimetics useful as iap inhibitors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030124028A1 (en) * 2001-08-10 2003-07-03 Carlson Eric D. Apparatuses and methods for creating and testing pre-formulations and systems for same
US20060128632A1 (en) 2002-07-02 2006-06-15 Sharma Sushil K Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
WO2005097791A1 (en) * 2004-04-07 2005-10-20 Novartis Ag Inhibitors of iap
EA019420B1 (ru) 2004-12-20 2014-03-31 Дженентех, Инк. Пирролидиновые ингибиторы иап (ингибиторов апоптоза)

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008016893A1 (en) * 2006-08-02 2008-02-07 Novartis Ag Smac peptidomimetics useful as iap inhibitors

Also Published As

Publication number Publication date
US20140093570A1 (en) 2014-04-03
AU2014213533A1 (en) 2014-09-04
KR20180020315A (ko) 2018-02-27
PE20170777A1 (es) 2017-07-04
AR077869A1 (es) 2011-09-28
US20180370960A1 (en) 2018-12-27
MX351274B (es) 2017-10-06
BR112012003118A2 (pt) 2016-02-23
CO6612189A2 (es) 2013-02-01
MX2012001844A (es) 2012-02-29
AU2017254950B2 (en) 2018-09-20
IN2012DN00858A (enExample) 2015-07-10
CL2012000349A1 (es) 2012-09-07
WO2011018474A1 (en) 2011-02-17
IL217760A0 (en) 2012-03-29
SG177713A1 (en) 2012-02-28
PE20121132A1 (es) 2012-09-04
JP2013501751A (ja) 2013-01-17
PH12014501890A1 (en) 2015-09-14
RU2671196C1 (ru) 2018-10-30
TN2012000026A1 (en) 2013-09-19
US20170081319A1 (en) 2017-03-23
AU2016203145A1 (en) 2016-06-02
CN102471331A (zh) 2012-05-23
US20120128742A1 (en) 2012-05-24
MA33511B1 (fr) 2012-08-01
TW201118091A (en) 2011-06-01
KR20120048008A (ko) 2012-05-14
WO2011018474A8 (en) 2011-09-22
PH12014501890B1 (en) 2015-09-14
EP2464644A1 (en) 2012-06-20
JP2016179976A (ja) 2016-10-13
AU2017254950A1 (en) 2017-11-23
RU2012108931A (ru) 2013-09-27
US10093665B2 (en) 2018-10-09
CN105646471A (zh) 2016-06-08
JP2018172403A (ja) 2018-11-08
CA2769616A1 (en) 2011-02-17
US9540363B2 (en) 2017-01-10
ZA201200390B (en) 2012-10-31
AU2010283748A1 (en) 2012-02-09
MY160475A (en) 2017-03-15
US8623385B2 (en) 2014-01-07
TWI607006B (zh) 2017-12-01

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Granted publication date: 20160113

Termination date: 20200811