UA87884C2 - Безводна кристалічна калієва сіль інгібітора віл-інтегрази - Google Patents
Безводна кристалічна калієва сіль інгібітора віл-інтегрази 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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 (uk) | 2009-08-25 |
Family
ID=36171569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA200707372A UA87884C2 (uk) | 2004-12-03 | 2005-02-12 | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
Country Status (35)
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| EP2272827A1 (en) | 2004-03-11 | 2011-01-12 | 4Sc Ag | Sulphonylpyrroles as hdac inhibitors |
| WO2006060711A2 (en) * | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
| EP1819323B2 (en) * | 2004-12-03 | 2023-03-22 | Merck Sharp & Dohme Corp. | 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 |
| EP1993513A4 (en) * | 2006-03-14 | 2012-06-27 | Merck Sharp & Dohme | METHOD AND DEVICE FOR PREPARING CRYSTALLINE ORGANIC MICROPARTICLE COMPOSITIONS USING MICROMATES AND CRYSTALLIZING MICROSAMEN AND THEIR USE |
| JP2009543865A (ja) | 2006-07-19 | 2009-12-10 | ユニバーシティ オブ ジョージア リサーチ ファウンデーション， インコーポレーテッド | ピリジノンジケト酸：併用療法におけるｈｉｖ複製の阻害剤 |
| US7687509B2 (en) | 2007-07-09 | 2010-03-30 | Concert Pharmaceuticals Inc. | Pyrimidinecarboxamide derivatives |
| CN103254138A (zh) * | 2008-01-08 | 2013-08-21 | 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 |
| EP3970702A1 (en) | 2009-10-26 | 2022-03-23 | Merck Sharp & Dohme Corp. | Solid pharmaceutical compositions containing an integrase inhibitor |
| 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. |
| JP5889275B2 (ja) * | 2010-04-01 | 2016-03-22 | テバ ファーマシューティカル インダストリーズ リミティド | ラルテグラビル塩およびその結晶形 |
| CA2999435A1 (en) * | 2010-04-01 | 2011-10-06 | Critical Outcome Technologies Inc. | Compounds and method for 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 |
| CA2833006A1 (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 |
| EP2529741B1 (en) | 2011-06-01 | 2014-02-12 | Ratiopharm GmbH | Composition and Tablet Comprising 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 |
| ES2825029T3 (es) | 2011-12-26 | 2021-05-14 | Emcure Pharmaceuticals Ltd | Síntesis de raltegravir |
| KR20140114406A (ko) | 2012-01-25 | 2014-09-26 | 루핀 리미티드 | 안정한 비정질 랄테그라빌 포타슘 프리믹스 및 이의 제조 방법 |
| 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 |
| WO2015009927A1 (en) * | 2013-07-17 | 2015-01-22 | Ratiopharm Gmbh | Dolutegravir salts |
| WO2015114608A1 (en) | 2014-02-03 | 2015-08-06 | Mylan Laboratories Ltd | Processes for the preparation of intermediates of raltegravir |
| US10391178B2 (en) * | 2014-03-21 | 2019-08-27 | Mylan Laboratories Limited | Premix of crystalline raltegravir potassium salt and a process for the preparation thereof |
| US10257840B2 (en) | 2014-10-22 | 2019-04-09 | Telefonaktiebolaget Lm Ericsson (Publ) | Operation of wireless local area network in the presence of periodic interference |
| WO2016075605A1 (en) | 2014-11-10 | 2016-05-19 | Aurobindo Pharma Ltd | An improved process for the preparation of raltegravir |
| EP3472134B1 (en) | 2016-06-21 | 2021-10-20 | Pharmathen S.A. | Process for preparing compounds useful as intermediates for the preparation of raltegravir |
| EP3512854A1 (en) | 2016-09-15 | 2019-07-24 | Lupin Limited | Process for the preparation of pure and stable crystalline raltegravir potassium form 3 |
| CN108610338A (zh) * | 2016-12-12 | 2018-10-02 | 天津国际生物医药联合研究院 | 一种嘧啶酮酰胺类化合物的制备方法 |
| EP3710445B1 (en) | 2017-11-14 | 2022-03-16 | Cambrex Profarmaco Milano S.r.l. | Process for the preparation of raltegravir |
| WO2019236395A1 (en) * | 2018-06-06 | 2019-12-12 | Merck Sharp & Dohme Corp. | Formulations of raltegravir |
| GB201907305D0 (en) * | 2019-05-23 | 2019-07-10 | Douglas Pharmaceuticals Ltd | Treatment of conditions |
| US12465565B2 (en) | 2020-01-23 | 2025-11-11 | Lupin Limited | Pharmaceutical compositions of raltegravir |
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| CH624391A5 (enExample) * | 1976-12-14 | 1981-07-31 | Ciba Geigy Ag | |
| US5717097A (en) * | 1991-11-08 | 1998-02-10 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| US5413999A (en) * | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| IL121789A (en) * | 1996-10-03 | 2001-06-14 | Rohm & Haas | A medicinal product for inhibiting mammalian cell tumors |
| US6620841B1 (en) * | 1998-12-25 | 2003-09-16 | Shionogi & Co., Ltd. | Aromatic heterocycle compounds having HIV integrase inhibiting activities |
| IT1318424B1 (it) * | 2000-03-24 | 2003-08-25 | Unihart Corp | Composti con attivita' anti-hiv. |
| WO2002030931A2 (en) | 2000-10-12 | 2002-04-18 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| GB0028483D0 (en) * | 2000-11-22 | 2001-01-10 | Hoffmann La Roche | Hydroxyethylamine HIV protease inhibitors |
| CA2463976C (en) * | 2001-10-26 | 2007-02-13 | Benedetta Crescenzi | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
| US7354932B2 (en) * | 2001-12-21 | 2008-04-08 | Anormed, Inc. | Chemokine receptor binding heterocyclic compounds with enhanced efficacy |
| IL161784A0 (en) * | 2001-12-21 | 2005-11-20 | Anormed Inc | Chemokine receptor binding heterocyclic compounds with enhanced efficacy |
| AR042095A1 (es) * | 2002-11-20 | 2005-06-08 | Japan Tobacco Inc | Compuesto 4-oxoquinolina y aplicacion del mismo como inhibidor de integrasa de vih |
| KR20050087865A (ko) * | 2002-12-27 | 2005-08-31 | 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이. | ＨＩＶ 인테그라제 억제제로서 유용한테트라하이드로-4Ｈ-피리도[1,2-ａ]피리미딘 및 관련화합물 |
| TW200423930A (en) * | 2003-02-18 | 2004-11-16 | Hoffmann La Roche | Non-nucleoside reverse transcriptase inhibitors |
| EP1819323B2 (en) | 2004-12-03 | 2023-03-22 | Merck Sharp & Dohme Corp. | 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 |
| WO2006060711A2 (en) * | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
-
2005
- 2005-02-12 UA UAA200707372A patent/UA87884C2/uk unknown
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- 2005-11-25 TW TW094141625A patent/TWI344463B/zh active
- 2005-12-01 PE PE2005001398A patent/PE20061148A1/es not_active Application Discontinuation
- 2005-12-02 WO PCT/US2005/043781 patent/WO2006060730A2/en not_active Ceased
- 2005-12-02 RS RS20120021A patent/RS52197B/sr unknown
- 2005-12-02 AU AU2005311671A patent/AU2005311671B8/en not_active Expired
- 2005-12-02 ES ES05852840T patent/ES2375788T3/es not_active Expired - Lifetime
- 2005-12-02 EP EP05852840A patent/EP1819700B1/en not_active Expired - Lifetime
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- 2005-12-02 ME MEP-2012-21A patent/ME01985B/me unknown
- 2005-12-02 AT AT05852866T patent/ATE518844T1/de active
- 2005-12-02 KR KR1020137028450A patent/KR20130122031A/ko not_active Withdrawn
- 2005-12-02 SI SI200531435T patent/SI1819700T1/sl unknown
- 2005-12-02 CN CN2005800416393A patent/CN101068793B/zh not_active Expired - Lifetime
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- 2005-12-02 JP JP2007544570A patent/JP4705956B2/ja not_active Expired - Lifetime
- 2005-12-02 US US11/293,678 patent/US7754731B2/en active Active
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- 2005-12-02 EA EA200701204A patent/EA012418B1/ru not_active IP Right Cessation
- 2005-12-02 CA CA2588398A patent/CA2588398C/en not_active Expired - Lifetime
- 2005-12-02 AT AT05852840T patent/ATE534645T1/de active
- 2005-12-02 MX MX2007006639A patent/MX2007006639A/es active IP Right Grant
- 2005-12-02 DK DK05852840.7T patent/DK1819700T3/da active
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- 2005-12-02 KR KR1020077015278A patent/KR101350420B1/ko not_active Expired - Lifetime
- 2005-12-02 NZ NZ555376A patent/NZ555376A/en unknown
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- 2007-05-22 ZA ZA200704130A patent/ZA200704130B/xx unknown
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