JP5921439B2 - 結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法 - Google Patents

結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法 Download PDF

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Publication number
JP5921439B2
JP5921439B2 JP2012541130A JP2012541130A JP5921439B2 JP 5921439 B2 JP5921439 B2 JP 5921439B2 JP 2012541130 A JP2012541130 A JP 2012541130A JP 2012541130 A JP2012541130 A JP 2012541130A JP 5921439 B2 JP5921439 B2 JP 5921439B2
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polymorph
bimatoprost
crystalline form
ethyl
enamide
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Expired - Fee Related
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Japanese (ja)
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JP2013511573A (ja
Inventor
ジョルジ エフ アンブラス
ジョルジ エフ アンブラス
キオマース カラミ
キオマース カラミ
ケ ウー
ケ ウー
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Allergan Inc
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Allergan Inc
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    • 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
    • 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
    • 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
    • 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

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  • 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)
JP2012541130A 2009-11-23 2010-11-19 結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法 Expired - Fee Related JP5921439B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26347109P 2009-11-23 2009-11-23
US61/263,471 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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016021287A Division JP2016094471A (ja) 2009-11-23 2016-02-05 結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法

Publications (2)

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JP2013511573A JP2013511573A (ja) 2013-04-04
JP5921439B2 true JP5921439B2 (ja) 2016-05-24

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JP2012541130A Expired - Fee Related JP5921439B2 (ja) 2009-11-23 2010-11-19 結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法
JP2016021287A Abandoned JP2016094471A (ja) 2009-11-23 2016-02-05 結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法

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JP2016021287A Abandoned JP2016094471A (ja) 2009-11-23 2016-02-05 結晶形態ｉｉの７−［３，５−ジヒドロキシ−２−（３−ヒドロキシ−５−フェニル−ペント−１−エニル）−シクロペンチル］−ｎ−エチル−ヘプト−５−エナミド（ビマトプロスト）、その調製方法、およびその使用方法

Country Status (20)

Country Link
US (2) US8629185B2 (cg-RX-API-DMAC10.html)
EP (1) EP2504313A1 (cg-RX-API-DMAC10.html)
JP (2) JP5921439B2 (cg-RX-API-DMAC10.html)
KR (1) KR20120085330A (cg-RX-API-DMAC10.html)
CN (2) CN102712584B (cg-RX-API-DMAC10.html)
AU (1) AU2010321831B2 (cg-RX-API-DMAC10.html)
BR (1) BR112012012387A2 (cg-RX-API-DMAC10.html)
CA (1) CA2781698A1 (cg-RX-API-DMAC10.html)
CL (1) CL2012001339A1 (cg-RX-API-DMAC10.html)
CO (1) CO6551754A2 (cg-RX-API-DMAC10.html)
HK (1) HK1207570A1 (cg-RX-API-DMAC10.html)
IL (2) IL219959A (cg-RX-API-DMAC10.html)
IN (1) IN2012DN05209A (cg-RX-API-DMAC10.html)
MX (1) MX2012005968A (cg-RX-API-DMAC10.html)
NZ (1) NZ600263A (cg-RX-API-DMAC10.html)
PH (1) PH12012501098A1 (cg-RX-API-DMAC10.html)
RU (1) RU2577546C2 (cg-RX-API-DMAC10.html)
UA (1) UA110696C2 (cg-RX-API-DMAC10.html)
WO (1) WO2011063276A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA201203883B (cg-RX-API-DMAC10.html)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA110696C2 (uk) * 2009-11-23 2016-02-10 Аллерган, Інк. 7-[3,5-дигідрокси-2-(3-гідрокси-5-фенілпент-1-еніл)циклопентил]-n-етилгепт-5-енамід (біматопрост) у кристалічній формі ii, спосіб його одержання й спосіб його застосування
BR122021008918B1 (pt) 2011-06-02 2021-08-10 Chinoin Zrt Forma cristalina ii de bimatoproposta e processo para a preparação da mesma
RU2652063C2 (ru) 2012-10-26 2018-04-24 Форсайт Вижн5, Инк. Офтальмологическая система для замедленного высвобождения лекарственного средства в глазу
SI2934510T1 (sl) * 2012-12-19 2021-02-26 Novartis Ag Formulacije zaviralca LFA-1
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
EP3283004A4 (en) 2015-04-13 2018-12-05 Forsight Vision5, Inc. Ocular insert composition of 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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU2001280984A1 (en) * 2000-07-28 2002-02-13 Inspire Pharmaceuticals, Inc. Use of indole derivatives for the manufacture of a medicament for reducing intracular pressure
BRPI0418339A (pt) * 2003-12-30 2007-05-02 Metabolix Inc agentes de nucleação
IL177762A0 (en) * 2006-08-29 2006-12-31 Arieh Gutman Bimatoprost crystalline form i
UA110696C2 (uk) * 2009-11-23 2016-02-10 Аллерган, Інк. 7-[3,5-дигідрокси-2-(3-гідрокси-5-фенілпент-1-еніл)циклопентил]-n-етилгепт-5-енамід (біматопрост) у кристалічній формі ii, спосіб його одержання й спосіб його застосування

Also Published As

Publication number Publication date
RU2577546C2 (ru) 2016-03-20
EP2504313A1 (en) 2012-10-03
NZ600263A (en) 2014-08-29
WO2011063276A1 (en) 2011-05-26
US8629185B2 (en) 2014-01-14
US20110152376A1 (en) 2011-06-23
ZA201203883B (en) 2013-01-31
CN104367580A (zh) 2015-02-25
AU2010321831B2 (en) 2016-07-07
AU2010321831A1 (en) 2012-06-21
US20140113974A1 (en) 2014-04-24
IL219959A (en) 2015-07-30
CO6551754A2 (es) 2012-10-31
CL2012001339A1 (es) 2012-08-10
IL239892A0 (en) 2015-08-31
RU2012125185A (ru) 2013-12-27
CN102712584B (zh) 2014-10-29
CN102712584A (zh) 2012-10-03
PH12012501098A1 (en) 2014-10-14
US9181176B2 (en) 2015-11-10
HK1207570A1 (en) 2016-02-05
MX2012005968A (es) 2012-08-15
JP2016094471A (ja) 2016-05-26
JP2013511573A (ja) 2013-04-04
IL219959A0 (en) 2012-07-31
BR112012012387A2 (pt) 2019-09-24
KR20120085330A (ko) 2012-07-31
CA2781698A1 (en) 2011-05-26
UA110696C2 (uk) 2016-02-10
IN2012DN05209A (cg-RX-API-DMAC10.html) 2015-10-23

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