KR20180020315A - 아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태 - Google Patents

아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태 Download PDF

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Publication number
KR20180020315A
KR20180020315A KR1020187004166A KR20187004166A KR20180020315A KR 20180020315 A KR20180020315 A KR 20180020315A KR 1020187004166 A KR1020187004166 A KR 1020187004166A KR 20187004166 A KR20187004166 A KR 20187004166A KR 20180020315 A KR20180020315 A KR 20180020315A
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KR
South Korea
Prior art keywords
acid
temperature
compound
ethyl
cyclohexyl
Prior art date
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Ceased
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KR1020187004166A
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English (en)
Korean (ko)
Inventor
지완 타쿠르
동 양
릴리 펭
Original Assignee
노파르티스 아게
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42937834&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR20180020315(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20180020315A publication Critical patent/KR20180020315A/ko
Ceased legal-status Critical Current

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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

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  • 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)
KR1020187004166A 2009-08-12 2010-08-11 아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태 Ceased KR20180020315A (ko)

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 Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020127006234A Division KR20120048008A (ko) 2009-08-12 2010-08-11 아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태

Publications (1)

Publication Number Publication Date
KR20180020315A true KR20180020315A (ko) 2018-02-27

Family

ID=42937834

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020187004166A Ceased KR20180020315A (ko) 2009-08-12 2010-08-11 아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태
KR1020127006234A Ceased KR20120048008A (ko) 2009-08-12 2010-08-11 아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020127006234A Ceased KR20120048008A (ko) 2009-08-12 2010-08-11 아폽토시스 단백질의 억제제의 고체 경구 제제 및 결정질 형태

Country Status (24)

Country Link
US (4) US8623385B2 (https=)
EP (1) EP2464644A1 (https=)
JP (3) JP2013501751A (https=)
KR (2) KR20180020315A (https=)
CN (2) CN105646471A (https=)
AR (1) AR077869A1 (https=)
AU (4) AU2010283748A1 (https=)
BR (1) BR112012003118A2 (https=)
CA (1) CA2769616A1 (https=)
CL (1) CL2012000349A1 (https=)
CO (1) CO6612189A2 (https=)
IL (1) IL217760A0 (https=)
IN (1) IN2012DN00858A (https=)
MA (1) MA33511B1 (https=)
MX (2) MX2012001844A (https=)
MY (1) MY160475A (https=)
PE (2) PE20170777A1 (https=)
PH (1) PH12014501890A1 (https=)
RU (1) RU2671196C1 (https=)
SG (1) SG177713A1 (https=)
TN (1) TN2012000026A1 (https=)
TW (1) TWI607006B (https=)
WO (1) WO2011018474A1 (https=)
ZA (1) ZA201200390B (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017253560B2 (en) 2016-04-20 2019-03-21 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
CN119264211A (zh) 2018-08-27 2025-01-07 瑞泽恩制药公司 拉曼光谱在下游纯化中的应用
WO2021220178A1 (en) 2020-04-29 2021-11-04 Cominnex Zrt. Iap antagonists and their therapeutic applications

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030119060A1 (en) 2001-08-10 2003-06-26 Desrosiers Peter J. Apparatuses and methods for creating and testing pre-formulations and systems for same
WO2004005248A1 (en) 2002-07-02 2004-01-15 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
DK2253614T3 (da) * 2004-04-07 2013-01-07 Novartis Ag IAP-inhibitorer
DK1836201T4 (da) * 2004-12-20 2013-11-11 Genentech Inc Pyrrolidininhibitorer af IAP.
PE20110220A1 (es) * 2006-08-02 2011-04-11 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS

Also Published As

Publication number Publication date
MY160475A (en) 2017-03-15
US20180370960A1 (en) 2018-12-27
PH12014501890B1 (en) 2015-09-14
BR112012003118A2 (pt) 2016-02-23
JP2018172403A (ja) 2018-11-08
PH12014501890A1 (en) 2015-09-14
MX351274B (es) 2017-10-06
TN2012000026A1 (en) 2013-09-19
CN102471331A (zh) 2012-05-23
US8623385B2 (en) 2014-01-07
US9540363B2 (en) 2017-01-10
CA2769616A1 (en) 2011-02-17
RU2012108931A (ru) 2013-09-27
AR077869A1 (es) 2011-09-28
TW201118091A (en) 2011-06-01
MA33511B1 (fr) 2012-08-01
IL217760A0 (en) 2012-03-29
PE20121132A1 (es) 2012-09-04
CO6612189A2 (es) 2013-02-01
TWI607006B (zh) 2017-12-01
AU2017254950B2 (en) 2018-09-20
MX2012001844A (es) 2012-02-29
US10093665B2 (en) 2018-10-09
AU2017254950A1 (en) 2017-11-23
CL2012000349A1 (es) 2012-09-07
WO2011018474A8 (en) 2011-09-22
IN2012DN00858A (https=) 2015-07-10
PE20170777A1 (es) 2017-07-04
AU2014213533A1 (en) 2014-09-04
US20170081319A1 (en) 2017-03-23
RU2671196C1 (ru) 2018-10-30
ZA201200390B (en) 2012-10-31
US20120128742A1 (en) 2012-05-24
EP2464644A1 (en) 2012-06-20
AU2010283748A1 (en) 2012-02-09
CN102471331B (zh) 2016-01-13
JP2013501751A (ja) 2013-01-17
AU2016203145A1 (en) 2016-06-02
KR20120048008A (ko) 2012-05-14
SG177713A1 (en) 2012-02-28
US20140093570A1 (en) 2014-04-03
WO2011018474A1 (en) 2011-02-17
JP2016179976A (ja) 2016-10-13
CN105646471A (zh) 2016-06-08

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A107 Divisional application of patent
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Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20180212

Application number text: 1020127006234

Filing date: 20120309

PG1501 Laying open of application
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Patent event code: PA02012R01D

Patent event date: 20180314

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Patent event date: 20190624

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