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

    • 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
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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) KR20120048008A (es)
CN (2) CN102471331B (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) MX351274B (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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019514878A (ja) 2016-04-20 2019-06-06 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｒｉｐｋ２阻害剤を含むコンジュゲート
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
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
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
JP5007235B2 (ja) * 2004-12-20 2012-08-22 ジェネンテック， インコーポレイテッド Ｉａｐのピロリジンインヒビター
PE20110218A1 (es) * 2006-08-02 2011-04-01 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
WO2011018474A8 (en) 2011-09-22
RU2012108931A (ru) 2013-09-27
TWI607006B (zh) 2017-12-01
IN2012DN00858A (es) 2015-07-10
US20120128742A1 (en) 2012-05-24
CA2769616A1 (en) 2011-02-17
KR20120048008A (ko) 2012-05-14
JP2013501751A (ja) 2013-01-17
PH12014501890A1 (en) 2015-09-14
BR112012003118A2 (pt) 2016-02-23
MX351274B (es) 2017-10-06
KR20180020315A (ko) 2018-02-27
SG177713A1 (en) 2012-02-28
PH12014501890B1 (en) 2015-09-14
MA33511B1 (fr) 2012-08-01
JP2016179976A (ja) 2016-10-13
IL217760A0 (en) 2012-03-29
AU2017254950A1 (en) 2017-11-23
US20140093570A1 (en) 2014-04-03
TW201118091A (en) 2011-06-01
CN105646471A (zh) 2016-06-08
JP2018172403A (ja) 2018-11-08
RU2671196C1 (ru) 2018-10-30
US8623385B2 (en) 2014-01-07
US20170081319A1 (en) 2017-03-23
EP2464644A1 (en) 2012-06-20
ZA201200390B (en) 2012-10-31
CL2012000349A1 (es) 2012-09-07
AR077869A1 (es) 2011-09-28
PE20170777A1 (es) 2017-07-04
US20180370960A1 (en) 2018-12-27
AU2010283748A1 (en) 2012-02-09
WO2011018474A1 (en) 2011-02-17
CO6612189A2 (es) 2013-02-01
US10093665B2 (en) 2018-10-09
AU2017254950B2 (en) 2018-09-20
US9540363B2 (en) 2017-01-10
MY160475A (en) 2017-03-15
TN2012000026A1 (en) 2013-09-19
MX2012001844A (es) 2012-02-29
AU2016203145A1 (en) 2016-06-02
AU2014213533A1 (en) 2014-09-04
CN102471331A (zh) 2012-05-23
CN102471331B (zh) 2016-01-13

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