IN2012DN05209A - - Google Patents

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Publication number
IN2012DN05209A
IN2012DN05209A IN5209DEN2012A IN2012DN05209A IN 2012DN05209 A IN2012DN05209 A IN 2012DN05209A IN 5209DEN2012 A IN5209DEN2012 A IN 5209DEN2012A IN 2012DN05209 A IN2012DN05209 A IN 2012DN05209A
Authority
IN
India
Prior art keywords
crystalline form
bimatoprost
new
date
designated
Prior art date
Application number
Inventor
F Ambrus Gyorgy
Karami Kiomars
Wu Ke
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=IN2012DN05209(A) "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 IN2012DN05209A publication Critical patent/IN2012DN05209A/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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

The present invention provides a new crystalline form of bimatoprost, designated as crystalline form 11. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystalline form I1 is readily prepared from crystalline form I.
IN5209DEN2012 2009-11-23 2010-11-19 IN2012DN05209A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26347109P 2009-11-23 2009-11-23
PCT/US2010/057494 WO2011063276A1 (en) 2009-11-23 2010-11-19 7-[3,5-dihydroxy-2- (3-hydroxy-5-phenyl-pent-1-enyl)- cyclopentyl]-n-ethyl-hept-5-enamide (bimatoprost) in crystalline form ii, methods for preparation, and methods for use thereof

Publications (1)

Publication Number Publication Date
IN2012DN05209A true IN2012DN05209A (en) 2015-10-23

Family

ID=43639099

Family Applications (1)

Application Number Title Priority Date Filing Date
IN5209DEN2012 IN2012DN05209A (en) 2009-11-23 2010-11-19

Country Status (20)

Country Link
US (2) US8629185B2 (en)
EP (1) EP2504313A1 (en)
JP (2) JP5921439B2 (en)
KR (1) KR20120085330A (en)
CN (2) CN102712584B (en)
AU (1) AU2010321831B2 (en)
BR (1) BR112012012387A2 (en)
CA (1) CA2781698A1 (en)
CL (1) CL2012001339A1 (en)
CO (1) CO6551754A2 (en)
HK (1) HK1207570A1 (en)
IL (2) IL219959A (en)
IN (1) IN2012DN05209A (en)
MX (1) MX2012005968A (en)
NZ (1) NZ600263A (en)
PH (1) PH12012501098A1 (en)
RU (1) RU2577546C2 (en)
UA (1) UA110696C2 (en)
WO (1) WO2011063276A1 (en)
ZA (1) ZA201203883B (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102712584B (en) * 2009-11-23 2014-10-29 阿勒根公司 7-[3,5-Dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-N-ethyl-hept-5-enamide of Form II (bimatoprost), methods of preparation and methods of use thereof
CN106278982B (en) 2011-06-02 2019-06-14 奇诺因私人有限公司 It is used to prepare the new method of prostaglandin amide
PL2911623T3 (en) 2012-10-26 2020-03-31 Forsight Vision5, Inc. Ophthalmic system for sustained release of drug to eye
KR101891144B1 (en) * 2012-12-19 2018-08-23 에스에이알코드 바이오사이언스 인코포레이티드 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
WO2016168141A1 (en) 2015-04-13 2016-10-20 Forsight Vision5, Inc. Ocular insert composition of semi-crystalline or crystalline pharmaceutically active agent
CN115677549A (en) * 2022-10-27 2023-02-03 神隆医药（常熟）有限公司 Preparation method of bimatoprost chiral isomer

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7166730B2 (en) * 2000-01-27 2007-01-23 Fine Tech Laboratories, Ltd Process for the preparation of prostaglandin derivatives
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
MXPA03000729A (en) * 2000-07-28 2004-11-01 Inspire Pharmaceuticals Inc Method for reducing intraocular pressure using indole derivatives.
BRPI0418339A (en) * 2003-12-30 2007-05-02 Metabolix Inc nucleating agents
IL177762A0 (en) * 2006-08-29 2006-12-31 Arieh Gutman Bimatoprost crystalline form i
CN102712584B (en) * 2009-11-23 2014-10-29 阿勒根公司 7-[3,5-Dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-N-ethyl-hept-5-enamide of Form II (bimatoprost), methods of preparation and methods of use thereof

Also Published As

Publication number Publication date
US20140113974A1 (en) 2014-04-24
CN102712584B (en) 2014-10-29
NZ600263A (en) 2014-08-29
AU2010321831A1 (en) 2012-06-21
IL219959A (en) 2015-07-30
CN102712584A (en) 2012-10-03
KR20120085330A (en) 2012-07-31
MX2012005968A (en) 2012-08-15
JP5921439B2 (en) 2016-05-24
UA110696C2 (en) 2016-02-10
US20110152376A1 (en) 2011-06-23
US8629185B2 (en) 2014-01-14
PH12012501098A1 (en) 2014-10-14
WO2011063276A1 (en) 2011-05-26
RU2577546C2 (en) 2016-03-20
HK1207570A1 (en) 2016-02-05
CA2781698A1 (en) 2011-05-26
JP2016094471A (en) 2016-05-26
IL239892A0 (en) 2015-08-31
AU2010321831B2 (en) 2016-07-07
US9181176B2 (en) 2015-11-10
RU2012125185A (en) 2013-12-27
JP2013511573A (en) 2013-04-04
CL2012001339A1 (en) 2012-08-10
ZA201203883B (en) 2013-01-31
EP2504313A1 (en) 2012-10-03
CN104367580A (en) 2015-02-25
BR112012012387A2 (en) 2019-09-24
IL219959A0 (en) 2012-07-31
CO6551754A2 (en) 2012-10-31

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