UA87884C2 - Безводная кристаллическая калиевая соль ингибитора вич-интегразы - Google Patents
Безводная кристаллическая калиевая соль ингибитора вич-интегразы Download PDFInfo
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- UA87884C2 UA87884C2 UAA200707372A UAA200707372A UA87884C2 UA 87884 C2 UA87884 C2 UA 87884C2 UA A200707372 A UAA200707372 A UA A200707372A UA A200707372 A UAA200707372 A UA A200707372A UA 87884 C2 UA87884 C2 UA 87884C2
- Authority
- UA
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- Prior art keywords
- compound
- potassium salt
- aids
- hiv
- solution
- Prior art date
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- SUJUHGSWHZTSEU-FYBSXPHGSA-N tipranavir Chemical compound C([C@@]1(CCC)OC(=O)C([C@H](CC)C=2C=C(NS(=O)(=O)C=3N=CC(=CC=3)C(F)(F)F)C=CC=2)=C(O)C1)CC1=CC=CC=C1 SUJUHGSWHZTSEU-FYBSXPHGSA-N 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 102000035160 transmembrane proteins Human genes 0.000 description 1
- 108091005703 transmembrane proteins Proteins 0.000 description 1
- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
- YFNGWGVTFYSJHE-UHFFFAOYSA-K trisodium;phosphonoformate Chemical compound [Na+].[Na+].[Na+].OP(O)(=O)C([O-])=O.OP(O)(=O)C([O-])=O.OP(O)(=O)C([O-])=O YFNGWGVTFYSJHE-UHFFFAOYSA-K 0.000 description 1
- 229940093257 valacyclovir Drugs 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 208000016261 weight loss Diseases 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 238000001238 wet grinding Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
- C07D313/02—Seven-membered rings
- C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
- C07D313/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D313/12—[b,e]-condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Раскрыта безводная кристаллическая калиевая соль соединения А, где соединение А имеет формулу (І). Соединение А представляет собой ингибитор ВИЧ-интегразы, применяемый для лечения или профилактики ВИЧ-инфекции, для задержания начала СПИДа и для лечения или профилактики СПИДа.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63313204P | 2004-12-03 | 2004-12-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA87884C2 true UA87884C2 (ru) | 2009-08-25 |
Family
ID=36171569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA200707372A UA87884C2 (ru) | 2004-12-03 | 2005-02-12 | Безводная кристаллическая калиевая соль ингибитора вич-интегразы |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US7754731B2 (ru) |
| EP (2) | EP1819683B1 (ru) |
| JP (1) | JP4705956B2 (ru) |
| KR (2) | KR20130122031A (ru) |
| CN (1) | CN101068793B (ru) |
| AR (2) | AR052034A1 (ru) |
| AT (2) | ATE534645T1 (ru) |
| AU (1) | AU2005311671B8 (ru) |
| BR (1) | BRPI0518760A8 (ru) |
| CA (1) | CA2588398C (ru) |
| CR (1) | CR9146A (ru) |
| CY (1) | CY1112859T1 (ru) |
| DK (1) | DK1819700T3 (ru) |
| EA (1) | EA012418B1 (ru) |
| ES (2) | ES2370136T3 (ru) |
| GE (1) | GEP20105086B (ru) |
| HK (1) | HK1115011A1 (ru) |
| HR (1) | HRP20120066T1 (ru) |
| IL (1) | IL183614A (ru) |
| MA (1) | MA29120B1 (ru) |
| ME (1) | ME01985B (ru) |
| MX (1) | MX2007006639A (ru) |
| MY (1) | MY144320A (ru) |
| NI (1) | NI200700138A (ru) |
| NO (1) | NO338784B1 (ru) |
| NZ (1) | NZ555376A (ru) |
| PE (1) | PE20061148A1 (ru) |
| PL (1) | PL1819700T3 (ru) |
| PT (1) | PT1819700E (ru) |
| RS (1) | RS52197B (ru) |
| SI (1) | SI1819700T1 (ru) |
| TN (1) | TNSN07215A1 (ru) |
| TW (1) | TWI344463B (ru) |
| UA (1) | UA87884C2 (ru) |
| WO (2) | WO2006060730A2 (ru) |
| ZA (1) | ZA200704130B (ru) |
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| KR20070085702A (ko) * | 2004-12-03 | 2007-08-27 | 머크 앤드 캄파니 인코포레이티드 | Ｕｇｔ1ａ1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도 |
| CA2588465C (en) * | 2004-12-03 | 2013-10-01 | Merck & Co., Inc. | Pharmaceutical composition containing an anti-nucleating agent |
| CN101453986A (zh) * | 2006-03-14 | 2009-06-10 | 默克公司 | 通过微研磨和在微晶种上结晶生产结晶有机微粒组合物的方法和设备及其应用 |
| MX2009000661A (es) | 2006-07-19 | 2009-03-27 | Univ Georgia Res Found | Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion. |
| CA2702317A1 (en) * | 2007-07-09 | 2009-01-15 | Concert Pharmaceuticals, Inc. | Novel pyrimidinecarboxamide derivatives |
| CN101918372B (zh) * | 2008-01-08 | 2014-03-26 | 默沙东公司 | 用于制备n-取代的羟基嘧啶酮羧酰胺类化合物的方法 |
| ES2549387T3 (es) | 2009-06-02 | 2015-10-27 | Hetero Research Foundation | Procedimiento de preparación de raltegravir potásico amorfo |
| WO2011024192A2 (en) | 2009-07-27 | 2011-03-03 | Matrix Laboratories Ltd | Novel polymorphs of raltegravir |
| RU2602865C2 (ru) | 2009-10-26 | 2016-11-20 | Мерк Шарп И Доум Корп. | Твердые фармацевтические композиции, содержащие ингибитор интегразы |
| DE102009056636A1 (de) | 2009-12-02 | 2011-06-09 | Ratiopharm Gmbh | Raltegravir-Polymorphe |
| AU2010328325B2 (en) | 2009-12-07 | 2015-02-05 | University Of Georgia Research Foundation, Inc. | Pyridinone hydroxycyclopentyl carboxamides: HIV integrase inhibitors with therapeutic applications |
| ES2362598B1 (es) * | 2009-12-17 | 2012-06-13 | Consejo Superior De Investigaciones Científicas (Csic) | Uso del raltegravir y derivados para la elaboración de medicamentos destinados al tratamiento de infecciones por herpesvirus. |
| SI2796458T1 (en) * | 2010-04-01 | 2018-04-30 | Teva Pharmaceutical Industries Ltd. | CRYSTALINIC SODIUM RALTEGRAVIR SOLUTIONS |
| EP2552915B1 (en) * | 2010-04-01 | 2017-07-19 | Critical Outcome Technologies Inc. | Compounds for the treatment of hiv |
| EP2575465A4 (en) * | 2010-05-25 | 2013-11-20 | Hetero Research Foundation | Raltegravir SALTS |
| WO2012009446A1 (en) | 2010-07-16 | 2012-01-19 | Concert Pharmaceuticals Inc. | Novel pyrimidinecarboxamide derivatives |
| CN101914067B (zh) * | 2010-08-26 | 2012-07-11 | 陈岱岭 | N-甲基嘧啶酮的合成方法 |
| JO3209B1 (ar) * | 2010-11-05 | 2018-03-08 | H Lundbeck As | طريقة لتصنيع نالتريكسون |
| WO2012103105A1 (en) | 2011-01-24 | 2012-08-02 | Assia Chemical Industries Ltd. | Processes for preparing raltegravir and intermediates in the processes |
| WO2012106534A2 (en) * | 2011-02-02 | 2012-08-09 | The Regents Of The University Of California | Hiv integrase inhibitors |
| US9163009B2 (en) | 2011-04-06 | 2015-10-20 | Lupin Limited | Salts of raltegravir |
| WO2012145446A1 (en) * | 2011-04-22 | 2012-10-26 | Merck Sharp & Dohme Corp. | Taste-masked formulations of raltegravir |
| US9968607B2 (en) | 2011-04-25 | 2018-05-15 | Hetero Research Foundation | Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof |
| EP2522665A1 (en) | 2011-05-03 | 2012-11-14 | Sandoz Ag | Crystalline sodium salt of an HIV integrase inhibitor |
| ES2450944T3 (es) | 2011-06-01 | 2014-03-25 | Ratiopharm Gmbh | Composición y comprimido que comprenden raltegravir |
| WO2013037731A1 (de) | 2011-09-16 | 2013-03-21 | Hexal Ag | Neue polymorphe form von raltegravir-kalium |
| CN103130788B (zh) * | 2011-11-24 | 2015-09-02 | 南开大学 | 嘧啶酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性 |
| CN103130787B (zh) * | 2011-11-24 | 2015-06-10 | 南开大学 | 嘧啶酮酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性 |
| EP2804607B1 (en) | 2011-12-26 | 2020-09-16 | Emcure Pharmaceuticals Limited | Synthesis of raltegravir |
| AU2013213255A1 (en) | 2012-01-25 | 2014-08-07 | Lupin Limited | Stable amorphous Raltegravir potassium premix and process for the preparation thereof |
| WO2014064711A2 (en) * | 2012-10-22 | 2014-05-01 | Hetero Research Foundation | Methods of administering raltegravir and raltegravir compositions |
| EP2818470A1 (en) | 2013-06-27 | 2014-12-31 | Basf Se | Cocrystals of raltegravir potassium |
| EP3022209B1 (en) * | 2013-07-17 | 2018-03-07 | ratiopharm GmbH | Dolutegravir potassium salt |
| US20170253585A1 (en) | 2014-02-03 | 2017-09-07 | Mylan Laboratories Ltd. | Processes for the preparation of intermediates of raltegravir |
| WO2015140765A1 (en) | 2014-03-21 | 2015-09-24 | Mylan Laboratories Ltd. | A premix of crystalline raltegravir potassium salt and a process for the preparation thereof |
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| US11246869B2 (en) | 2017-11-14 | 2022-02-15 | Cambrex Profarmaco Milano S.R.L. | Process for the preparation of Raltegravir |
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| US20230073216A1 (en) | 2020-01-23 | 2023-03-09 | Lupin Limited | Pharmaceutical Compositions of Raltegravir |
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| WO2006060711A2 (en) | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
| CA2588465C (en) | 2004-12-03 | 2013-10-01 | Merck & Co., Inc. | Pharmaceutical composition containing an anti-nucleating agent |
| KR20070085702A (ko) | 2004-12-03 | 2007-08-27 | 머크 앤드 캄파니 인코포레이티드 | Ｕｇｔ1ａ1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도 |
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2005
- 2005-02-12 UA UAA200707372A patent/UA87884C2/ru unknown
- 2005-11-24 AR ARP050104911A patent/AR052034A1/es not_active Application Discontinuation
- 2005-11-25 TW TW094141625A patent/TWI344463B/zh active
- 2005-11-25 MY MYPI20055516A patent/MY144320A/en unknown
- 2005-12-01 PE PE2005001398A patent/PE20061148A1/es not_active Application Discontinuation
- 2005-12-02 KR KR1020137028450A patent/KR20130122031A/ko not_active Application Discontinuation
- 2005-12-02 AU AU2005311671A patent/AU2005311671B8/en active Active
- 2005-12-02 ES ES05852866T patent/ES2370136T3/es active Active
- 2005-12-02 US US11/293,678 patent/US7754731B2/en active Active
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