CL2012001339A1 - Forma cristalina ii de 7-[3,5-dihidroxi-2-(3-hidroxi-5-fenil-pent-1-enil)-ciclopentil]-n-etil-hept-5-enamida (bimatoprost); método de conversion de la forma cristalina i del compuesto a la forma cristalina ii; composición farmacéutica; y su uso para tratar hipertensión ocular y glaucoma. - Google Patents

Forma cristalina ii de 7-[3,5-dihidroxi-2-(3-hidroxi-5-fenil-pent-1-enil)-ciclopentil]-n-etil-hept-5-enamida (bimatoprost); método de conversion de la forma cristalina i del compuesto a la forma cristalina ii; composición farmacéutica; y su uso para tratar hipertensión ocular y glaucoma.

Info

Publication number
CL2012001339A1
CL2012001339A1 CL2012001339A CL2012001339A CL2012001339A1 CL 2012001339 A1 CL2012001339 A1 CL 2012001339A1 CL 2012001339 A CL2012001339 A CL 2012001339A CL 2012001339 A CL2012001339 A CL 2012001339A CL 2012001339 A1 CL2012001339 A1 CL 2012001339A1
Authority
CL
Chile
Prior art keywords
crystalline form
bimatoprost
enamide
pent
hept
Prior art date
Application number
CL2012001339A
Other languages
English (en)
Inventor
Gyorgy F Ambrus
Kiomars Karami
Ke Wu
Original Assignee
Allergan Inc
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=43639099&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CL2012001339(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Allergan Inc filed Critical Allergan Inc
Publication of CL2012001339A1 publication Critical patent/CL2012001339A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00—Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
    • C07C405/0008—Analogues having the carboxyl group in the side-chains replaced by other functional groups
    • C07C405/0041—Analogues having the carboxyl group in the side-chains replaced by other functional groups containing nitrogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/22—Separation; Purification; Stabilisation; Use of additives
    • C07C231/24—Separation; Purification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/39—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00—Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Forma cristalina II de 7-[3.5-dihidroxi-2-(3-hidroxi-5-fenil-pent 1-enil) ciclopentil]-N-etil-hept-5-enamida (bimatoprost); método para convertir bimatroprost de la forma cristalina I a la forma cristalina II; composición farmacéutica; y su uso para tratar la hipertensión ocular.
CL2012001339A 2009-11-23 2012-05-23 Forma cristalina ii de 7-[3,5-dihidroxi-2-(3-hidroxi-5-fenil-pent-1-enil)-ciclopentil]-n-etil-hept-5-enamida (bimatoprost); método de conversion de la forma cristalina i del compuesto a la forma cristalina ii; composición farmacéutica; y su uso para tratar hipertensión ocular y glaucoma. CL2012001339A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26347109P 2009-11-23 2009-11-23

Publications (1)

Publication Number Publication Date
CL2012001339A1 true CL2012001339A1 (es) 2012-08-10

Family

ID=43639099

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2012001339A CL2012001339A1 (es) 2009-11-23 2012-05-23 Forma cristalina ii de 7-[3,5-dihidroxi-2-(3-hidroxi-5-fenil-pent-1-enil)-ciclopentil]-n-etil-hept-5-enamida (bimatoprost); método de conversion de la forma cristalina i del compuesto a la forma cristalina ii; composición farmacéutica; y su uso para tratar hipertensión ocular y glaucoma.

Country Status (19)

Country Link
US (2) US8629185B2 (es)
EP (1) EP2504313A1 (es)
JP (2) JP5921439B2 (es)
KR (1) KR20120085330A (es)
CN (2) CN102712584B (es)
AU (1) AU2010321831B2 (es)
BR (1) BR112012012387A2 (es)
CA (1) CA2781698A1 (es)
CL (1) CL2012001339A1 (es)
CO (1) CO6551754A2 (es)
HK (1) HK1207570A1 (es)
IL (2) IL219959A (es)
IN (1) IN2012DN05209A (es)
MX (1) MX2012005968A (es)
NZ (1) NZ600263A (es)
RU (1) RU2577546C2 (es)
UA (1) UA110696C2 (es)
WO (1) WO2011063276A1 (es)
ZA (1) ZA201203883B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20120085330A (ko) * 2009-11-23 2012-07-31 알러간, 인코포레이티드 결정형 ｉｉ의 ７?〔３,５?다이하이드록시?２?(３?하이드록시?５?페닐?펜트?１?에닐)?사이클로펜틸〕?ｎ?에틸?헵트?５?엔아마이드(비마토프로스트), 그의 제조방법 및 이용방법
EP2723714B1 (en) 2011-06-02 2017-06-21 Chinoin Zrt. Novel processes for the preparation of prostaglandin amides
US9750636B2 (en) 2012-10-26 2017-09-05 Forsight Vision5, Inc. Ophthalmic system for sustained release of drug to eye
NZ708821A (en) * 2012-12-19 2020-03-27 Novartis Ag Lfa-1 inhibitor formulations
US9120738B2 (en) 2012-12-28 2015-09-01 Allergan, Inc. Crystalline forms of bimatoprost acid, methods for preparation, and methods for use thereof
US9447014B2 (en) 2012-12-28 2016-09-20 Allergan, Inc. Tromethamine salt of bimatoprost acid in crystalline form, methods for preparation, and methods for use thereof
US10273206B2 (en) 2014-06-27 2019-04-30 Allergan, Inc. Tromethamine salt of bimatoprost acid in crystalline form 1, methods for preparation, and methods for use thereof
US20160296532A1 (en) 2015-04-13 2016-10-13 Forsight Vision5, Inc. Ocular Insert Composition of a Semi-Crystalline or Crystalline Pharmaceutically Active Agent
CN115677549A (zh) * 2022-10-27 2023-02-03 神隆医药（常熟）有限公司 一种贝美前列素手性异构体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU403156A3 (es) * 1968-07-29 1973-10-19
IL143477A (en) * 2001-05-31 2009-07-20 Finetech Pharmaceutical Ltd Process for the preparation of 17-phenyl-18,19,20-trinor-pgf2?? and its derivatives
US7166730B2 (en) * 2000-01-27 2007-01-23 Fine Tech Laboratories, Ltd Process for the preparation of prostaglandin derivatives
CN1450896A (zh) * 2000-07-28 2003-10-22 印斯拜尔药品股份有限公司 用吲哚衍生物降低眼内压的方法
EP1964879B1 (en) * 2003-12-30 2012-06-13 Metabolix, Inc. Nucleating agents
IL177762A0 (en) 2006-08-29 2006-12-31 Arieh Gutman Bimatoprost crystalline form i
KR20120085330A (ko) * 2009-11-23 2012-07-31 알러간, 인코포레이티드 결정형 ｉｉ의 ７?〔３,５?다이하이드록시?２?(３?하이드록시?５?페닐?펜트?１?에닐)?사이클로펜틸〕?ｎ?에틸?헵트?５?엔아마이드(비마토프로스트), 그의 제조방법 및 이용방법

Also Published As

Publication number Publication date
BR112012012387A2 (pt) 2019-09-24
EP2504313A1 (en) 2012-10-03
WO2011063276A1 (en) 2011-05-26
US20110152376A1 (en) 2011-06-23
AU2010321831B2 (en) 2016-07-07
CN102712584B (zh) 2014-10-29
CO6551754A2 (es) 2012-10-31
UA110696C2 (uk) 2016-02-10
JP2016094471A (ja) 2016-05-26
NZ600263A (en) 2014-08-29
RU2012125185A (ru) 2013-12-27
IN2012DN05209A (es) 2015-10-23
CN104367580A (zh) 2015-02-25
KR20120085330A (ko) 2012-07-31
MX2012005968A (es) 2012-08-15
CA2781698A1 (en) 2011-05-26
RU2577546C2 (ru) 2016-03-20
US20140113974A1 (en) 2014-04-24
JP2013511573A (ja) 2013-04-04
AU2010321831A1 (en) 2012-06-21
US8629185B2 (en) 2014-01-14
US9181176B2 (en) 2015-11-10
CN102712584A (zh) 2012-10-03
IL219959A0 (en) 2012-07-31
JP5921439B2 (ja) 2016-05-24
IL239892A0 (en) 2015-08-31
ZA201203883B (en) 2013-01-31
HK1207570A1 (en) 2016-02-05
IL219959A (en) 2015-07-30

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