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PE20121132A1 - Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis - Google Patents

Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis

Info

Publication number
PE20121132A1
PE20121132A1 PE2012000206A PE2012000206A PE20121132A1 PE 20121132 A1 PE20121132 A1 PE 20121132A1 PE 2012000206 A PE2012000206 A PE 2012000206A PE 2012000206 A PE2012000206 A PE 2012000206A PE 20121132 A1 PE20121132 A1 PE 20121132A1
Authority
PE
Peru
Prior art keywords
apoptosis
compound
solid oral
oral formulations
crystal forms
Prior art date
Application number
PE2012000206A
Other languages
English (en)
Inventor
Jeewan Thakur
Dong Yang
Lili Feng
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
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=PE20121132(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20121132A1 publication Critical patent/PE20121132A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, 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
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)

Abstract

SE REFIERE A LA FORMA CRISTALINA DE UN COMPUESTO DE HEMI-HIDRATO HA DE LA (S) -N-((S)-1-CICLOHEXIL-2-{(S)-2-[4-(4-FLUORO-BENZOIL)-TIAZOL-2-IL]-PIRROLIDIN-1-IL}-2-OXO-ETIL)-2-METIL-AMINO-PROPIONAMIDA DE FORMULA (I) QUE COMPRENDE: (A) UN PATRON DE DIFRACCION EN POLVO DE RAYOS X (XRPD) QUE COMPRENDE TRES O MAS VALORES 2THETA SELECCIONADOS A PARTIR DEL GRUPO QUE CONSISTE EN: 8.3 ± 0.2, 9.5±0.2, 13.5±0.2, 17.3±0.2, 18.5±0.2 Y 18.9±0.2; (B) UNA FORMA CRISTALINA A DEL COMPUESTO (I) QUE PRESENTA UN XRPD QUE COMPRENDE TRES O MAS VALORES 2THETA SELECCIONADOS A PARTIR DEL GRUPO QUE CONSISTE EN: 5.3±0.2, 6.7±0.2, 9.1±0.2, 13.4±0.2, 13.6±0.2, 15.0±0.2, 15.3±0.2, 17.4±0.2, 18.2±0.2, 18.7±0.2, 18.9±0.2, 20.2±0.2, 21.3±0.2, 21.8±0.2, 23.0±0.2, 23.5±0.2, 24.6±0.2 Y 27.6±0.2. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE LA PROTEINA DE APOPTOSIS (IAPS) SIENDO UTIL PARA TRATAR ENFERMEDADES RELACIONADAS CON LA PROTEINA DE APOPTOSIS
PE2012000206A 2009-08-12 2010-08-11 Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis PE20121132A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US27405109P 2009-08-12 2009-08-12

Publications (1)

Publication Number Publication Date
PE20121132A1 true PE20121132A1 (es) 2012-09-04

Family

ID=42937834

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2012000206A PE20121132A1 (es) 2009-08-12 2010-08-11 Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis
PE2017000424A PE20170777A1 (es) 2009-08-12 2010-08-11 Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2017000424A PE20170777A1 (es) 2009-08-12 2010-08-11 Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis

Country Status (24)

Country Link
US (4) US8623385B2 (es)
EP (1) EP2464644A1 (es)
JP (3) JP2013501751A (es)
KR (2) KR20180020315A (es)
CN (2) CN105646471A (es)
AR (1) AR077869A1 (es)
AU (4) AU2010283748A1 (es)
BR (1) BR112012003118A2 (es)
CA (1) CA2769616A1 (es)
CL (1) CL2012000349A1 (es)
CO (1) CO6612189A2 (es)
IL (1) IL217760A0 (es)
IN (1) IN2012DN00858A (es)
MA (1) MA33511B1 (es)
MX (2) MX2012001844A (es)
MY (1) MY160475A (es)
PE (2) PE20121132A1 (es)
PH (1) PH12014501890B1 (es)
RU (1) RU2671196C1 (es)
SG (1) SG177713A1 (es)
TN (1) TN2012000026A1 (es)
TW (1) TWI607006B (es)
WO (1) WO2011018474A1 (es)
ZA (1) ZA201200390B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017182418A1 (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
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
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
CA2491041A1 (en) 2002-07-02 2004-01-15 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
SG152225A1 (en) * 2004-04-07 2009-05-29 Novartis Ag Inhibitors of iap
KR20120127754A (ko) 2004-12-20 2012-11-23 제넨테크, 인크. Iap의 피롤리딘 억제제
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
AU2017254950B2 (en) 2018-09-20
US20140093570A1 (en) 2014-04-03
RU2671196C1 (ru) 2018-10-30
CO6612189A2 (es) 2013-02-01
CA2769616A1 (en) 2011-02-17
AR077869A1 (es) 2011-09-28
PH12014501890A1 (en) 2015-09-14
RU2012108931A (ru) 2013-09-27
MX2012001844A (es) 2012-02-29
US9540363B2 (en) 2017-01-10
US20120128742A1 (en) 2012-05-24
AU2017254950A1 (en) 2017-11-23
MA33511B1 (fr) 2012-08-01
WO2011018474A1 (en) 2011-02-17
CN102471331B (zh) 2016-01-13
MX351274B (es) 2017-10-06
SG177713A1 (en) 2012-02-28
KR20180020315A (ko) 2018-02-27
IL217760A0 (en) 2012-03-29
CL2012000349A1 (es) 2012-09-07
US20180370960A1 (en) 2018-12-27
JP2013501751A (ja) 2013-01-17
US20170081319A1 (en) 2017-03-23
JP2018172403A (ja) 2018-11-08
CN105646471A (zh) 2016-06-08
ZA201200390B (en) 2012-10-31
JP2016179976A (ja) 2016-10-13
AU2010283748A1 (en) 2012-02-09
CN102471331A (zh) 2012-05-23
BR112012003118A2 (pt) 2016-02-23
MY160475A (en) 2017-03-15
KR20120048008A (ko) 2012-05-14
PH12014501890B1 (en) 2015-09-14
US8623385B2 (en) 2014-01-07
TWI607006B (zh) 2017-12-01
TN2012000026A1 (en) 2013-09-19
TW201118091A (en) 2011-06-01
WO2011018474A8 (en) 2011-09-22
PE20170777A1 (es) 2017-07-04
AU2014213533A1 (en) 2014-09-04
US10093665B2 (en) 2018-10-09
AU2016203145A1 (en) 2016-06-02
EP2464644A1 (en) 2012-06-20
IN2012DN00858A (es) 2015-07-10

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