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 (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

Family Cites Families (5)

* 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)
PE20110224A1 (es) * 2006-08-02 2011-04-05 Novartis Ag PROCEDIMIENTO PARA LA SINTESIS DE UN PEPTIDOMIMETICO DE Smac INHIBIDOR DE IAP, Y COMPUESTOS INTERMEDIARIOS PARA LA SINTESIS DEL MISMO

Also Published As

Publication number Publication date
US20140093570A1 (en) 2014-04-03
AU2014213533A1 (en) 2014-09-04
PE20170777A1 (es) 2017-07-04
AR077869A1 (es) 2011-09-28
CN102471331B (zh) 2016-01-13
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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A107 Divisional application of patent
PA0104 Divisional application for international application

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
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20180314

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20180514

Patent event code: PE09021S01D

E601 Decision to refuse application
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Patent event date: 20190624

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20180514

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I