KR20120085330A - 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 - Google Patents

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 Download PDF

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KR20120085330A
KR20120085330A KR1020127016191A KR20127016191A KR20120085330A KR 20120085330 A KR20120085330 A KR 20120085330A KR 1020127016191 A KR1020127016191 A KR 1020127016191A KR 20127016191 A KR20127016191 A KR 20127016191A KR 20120085330 A KR20120085330 A KR 20120085330A
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South Korea
Prior art keywords
ethyl
enamide
hept
enyl
dihydroxy
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Ceased
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KR1020127016191A
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Korean (ko)
Inventor
죄르지 에. 앰브러스
키오마르스 카라미
커 우
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알러간, 인코포레이티드
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Application filed by 알러간, 인코포레이티드 filed Critical 알러간, 인코포레이티드
Publication of KR20120085330A publication Critical patent/KR20120085330A/ko
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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)
KR1020127016191A 2009-11-23 2010-11-19 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 Ceased KR20120085330A (ko)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
KR20120085330A true KR20120085330A (ko) 2012-07-31

Family

ID=43639099

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127016191A Ceased KR20120085330A (ko) 2009-11-23 2010-11-19 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

Country Status (20)

Country Link
US (2) US8629185B2 (https=)
EP (1) EP2504313A1 (https=)
JP (2) JP5921439B2 (https=)
KR (1) KR20120085330A (https=)
CN (2) CN104367580A (https=)
AU (1) AU2010321831B2 (https=)
BR (1) BR112012012387A2 (https=)
CA (1) CA2781698A1 (https=)
CL (1) CL2012001339A1 (https=)
CO (1) CO6551754A2 (https=)
HK (1) HK1207570A1 (https=)
IL (2) IL219959A (https=)
IN (1) IN2012DN05209A (https=)
MX (1) MX2012005968A (https=)
NZ (1) NZ600263A (https=)
PH (1) PH12012501098A1 (https=)
RU (1) RU2577546C2 (https=)
UA (1) UA110696C2 (https=)
WO (1) WO2011063276A1 (https=)
ZA (1) ZA201203883B (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012005968A (es) * 2009-11-23 2012-08-15 Allergan Inc 7- [3,5 - dihidroxi - 2 - (3 - hidroxi - 5 - fenil - 1 - enil) - ciclopentil] - n - etil - hept - 5 - enamida (bmato prost) en la forma cristalina ii, metodos de preparacion y metodos para uso del mismo.
US9238621B2 (en) 2011-06-02 2016-01-19 Chinoin Zrt Processes for the preparation of prostaglandin amides
DK2911623T3 (da) 2012-10-26 2019-10-28 Forsight Vision5 Inc Oftalmisk system til langvarig frigivelse af lægemiddel til øjet
EA028008B1 (ru) * 2012-12-19 2017-09-29 Саркоуд Байосайенс Инк. Составы ингибитора 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
US20160296532A1 (en) 2015-04-13 2016-10-13 Forsight Vision5, Inc. Ocular Insert Composition of a Semi-Crystalline or Crystalline Pharmaceutically Active Agent
EP4346720A4 (en) 2021-05-28 2025-01-01 Sight Sciences, Inc. INTRAOCULAR DEVICES, SYSTEMS AND METHODS
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
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
KR20030046395A (ko) * 2000-07-28 2003-06-12 인스파이어 파마슈티컬스 인코퍼레이티드 인돌 유도체를 사용하여 안압을 감소시키는 방법
JP2007517126A (ja) * 2003-12-30 2007-06-28 メタボリックス インコーポレイティッド 増核剤
IL177762A0 (en) * 2006-08-29 2006-12-31 Arieh Gutman Bimatoprost crystalline form i
MX2012005968A (es) * 2009-11-23 2012-08-15 Allergan Inc 7- [3,5 - dihidroxi - 2 - (3 - hidroxi - 5 - fenil - 1 - enil) - ciclopentil] - n - etil - hept - 5 - enamida (bmato prost) en la forma cristalina ii, metodos de preparacion y metodos para uso del mismo.

Also Published As

Publication number Publication date
CO6551754A2 (es) 2012-10-31
US20140113974A1 (en) 2014-04-24
WO2011063276A1 (en) 2011-05-26
PH12012501098A1 (en) 2014-10-14
CA2781698A1 (en) 2011-05-26
UA110696C2 (uk) 2016-02-10
MX2012005968A (es) 2012-08-15
JP2013511573A (ja) 2013-04-04
AU2010321831B2 (en) 2016-07-07
CN104367580A (zh) 2015-02-25
RU2012125185A (ru) 2013-12-27
HK1207570A1 (en) 2016-02-05
JP5921439B2 (ja) 2016-05-24
IN2012DN05209A (https=) 2015-10-23
RU2577546C2 (ru) 2016-03-20
BR112012012387A2 (pt) 2019-09-24
US20110152376A1 (en) 2011-06-23
JP2016094471A (ja) 2016-05-26
IL239892A0 (en) 2015-08-31
CN102712584A (zh) 2012-10-03
EP2504313A1 (en) 2012-10-03
IL219959A (en) 2015-07-30
NZ600263A (en) 2014-08-29
CN102712584B (zh) 2014-10-29
US9181176B2 (en) 2015-11-10
CL2012001339A1 (es) 2012-08-10
IL219959A0 (en) 2012-07-31
ZA201203883B (en) 2013-01-31
US8629185B2 (en) 2014-01-14
AU2010321831A1 (en) 2012-06-21

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