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
Links
- AQOKCDNYWBIDND-UHFFFAOYSA-N 7-[3,5-dihydroxy-2-(3-hydroxy-5-phenylpent-1-enyl)cyclopentyl]-n-ethylhept-5-enamide Chemical compound CCNC(=O)CCCC=CCC1C(O)CC(O)C1C=CC(O)CCC1=CC=CC=C1 AQOKCDNYWBIDND-UHFFFAOYSA-N 0.000 title abstract 2
- 206010030043 Ocular hypertension Diseases 0.000 title abstract 2
- AQOKCDNYWBIDND-FTOWTWDKSA-N bimatoprost Chemical compound CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1 AQOKCDNYWBIDND-FTOWTWDKSA-N 0.000 title abstract 2
- 229960002470 bimatoprost Drugs 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 208000010412 Glaucoma Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
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 (20)
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5921439B2 (ja) * | 2009-11-23 | 2016-05-24 | アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ | 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 |
| KR102038048B1 (ko) | 2011-06-02 | 2019-10-30 | 키노인 제트알티. | 프로스타글란딘 아미드의 신규한 제조 방법 |
| WO2014066775A1 (en) | 2012-10-26 | 2014-05-01 | Forsight Vision5, Inc. | Ophthalmic system for sustained release of drug to eye |
| EA201791321A1 (ru) * | 2012-12-19 | 2018-04-30 | Саркоуд Байосайенс Инк. | Составы ингибитора lfa-1 |
| 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 |
| US9120738B2 (en) * | 2012-12-28 | 2015-09-01 | Allergan, Inc. | Crystalline forms of bimatoprost acid, 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 (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)
| 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 |
| AR035651A1 (es) * | 2000-07-28 | 2004-06-23 | Univ Madrid Complutense | Uso de derivados de indol para la manufactura de un medicamento para reducir la presion intraocular y una composicion |
| CA2550009C (en) * | 2003-12-30 | 2013-05-14 | Metabolix, Inc. | Nucleating agents |
| IL177762A0 (en) * | 2006-08-29 | 2006-12-31 | Arieh Gutman | Bimatoprost crystalline form i |
| JP5921439B2 (ja) * | 2009-11-23 | 2016-05-24 | アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ | 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 |
-
2010
- 2010-11-19 JP JP2012541130A patent/JP5921439B2/ja not_active Expired - Fee Related
- 2010-11-19 IN IN5209DEN2012 patent/IN2012DN05209A/en unknown
- 2010-11-19 CN CN201080062129.5A patent/CN102712584B/zh active Active
- 2010-11-19 EP EP10785274A patent/EP2504313A1/en not_active Ceased
- 2010-11-19 AU AU2010321831A patent/AU2010321831B2/en active Active
- 2010-11-19 NZ NZ600263A patent/NZ600263A/en unknown
- 2010-11-19 KR KR1020127016191A patent/KR20120085330A/ko not_active Ceased
- 2010-11-19 MX MX2012005968A patent/MX2012005968A/es not_active Application Discontinuation
- 2010-11-19 PH PH1/2012/501098A patent/PH12012501098A1/en unknown
- 2010-11-19 CA CA2781698A patent/CA2781698A1/en not_active Abandoned
- 2010-11-19 WO PCT/US2010/057494 patent/WO2011063276A1/en not_active Ceased
- 2010-11-19 BR BR112012012387A patent/BR112012012387A2/pt not_active IP Right Cessation
- 2010-11-19 CN CN201410542159.6A patent/CN104367580A/zh active Pending
- 2010-11-19 UA UAA201207505A patent/UA110696C2/uk unknown
- 2010-11-19 RU RU2012125185/04A patent/RU2577546C2/ru active
- 2010-11-22 US US12/951,780 patent/US8629185B2/en active Active
-
2012
- 2012-05-23 IL IL219959A patent/IL219959A/en active IP Right Grant
- 2012-05-23 CL CL2012001339A patent/CL2012001339A1/es unknown
- 2012-05-28 ZA ZA2012/03883A patent/ZA201203883B/en unknown
- 2012-06-22 CO CO12104940A patent/CO6551754A2/es unknown
-
2013
- 2013-12-20 US US14/136,323 patent/US9181176B2/en active Active
-
2015
- 2015-07-12 IL IL239892A patent/IL239892A0/en unknown
- 2015-08-25 HK HK15108218.2A patent/HK1207570A1/xx unknown
-
2016
- 2016-02-05 JP JP2016021287A patent/JP2016094471A/ja not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CO6551754A2 (es) | 2012-10-31 |
| IL239892A0 (en) | 2015-08-31 |
| WO2011063276A1 (en) | 2011-05-26 |
| KR20120085330A (ko) | 2012-07-31 |
| CN102712584B (zh) | 2014-10-29 |
| JP2016094471A (ja) | 2016-05-26 |
| NZ600263A (en) | 2014-08-29 |
| HK1207570A1 (en) | 2016-02-05 |
| AU2010321831A1 (en) | 2012-06-21 |
| JP5921439B2 (ja) | 2016-05-24 |
| CN102712584A (zh) | 2012-10-03 |
| PH12012501098A1 (en) | 2014-10-14 |
| CA2781698A1 (en) | 2011-05-26 |
| US20140113974A1 (en) | 2014-04-24 |
| US9181176B2 (en) | 2015-11-10 |
| ZA201203883B (en) | 2013-01-31 |
| RU2577546C2 (ru) | 2016-03-20 |
| IN2012DN05209A (cg-RX-API-DMAC10.html) | 2015-10-23 |
| IL219959A (en) | 2015-07-30 |
| IL219959A0 (en) | 2012-07-31 |
| BR112012012387A2 (pt) | 2019-09-24 |
| MX2012005968A (es) | 2012-08-15 |
| CN104367580A (zh) | 2015-02-25 |
| AU2010321831B2 (en) | 2016-07-07 |
| US8629185B2 (en) | 2014-01-14 |
| UA110696C2 (uk) | 2016-02-10 |
| EP2504313A1 (en) | 2012-10-03 |
| RU2012125185A (ru) | 2013-12-27 |
| US20110152376A1 (en) | 2011-06-23 |
| JP2013511573A (ja) | 2013-04-04 |
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