TR200001876T2 - HIV proteaz inhibitörünün bisülfat tuzu. - Google Patents
HIV proteaz inhibitörünün bisülfat tuzu.Info
- Publication number
- TR200001876T2 TR200001876T2 TR2000/01876T TR200001876T TR200001876T2 TR 200001876 T2 TR200001876 T2 TR 200001876T2 TR 2000/01876 T TR2000/01876 T TR 2000/01876T TR 200001876 T TR200001876 T TR 200001876T TR 200001876 T2 TR200001876 T2 TR 200001876T2
- Authority
- TR
- Turkey
- Prior art keywords
- protease inhibitor
- hiv protease
- bisulfate salt
- salt
- following formula
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Mevcut bulus, asagidaki formüle sahip azapeptit HIV proteaz inhibitör bilesiginin serbest baz formuna oranla beklenmedik sekilde yüksek çözünürlük/bozulma hizina ve oral biyoyararlanima sahip oldugu bulunan kristalin bisülfat tuzunu sunmaktadir:
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US7196898P | 1998-01-20 | 1998-01-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
TR200001876T2 true TR200001876T2 (tr) | 2000-11-21 |
Family
ID=22104737
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
TR2000/01876T TR200001876T2 (tr) | 1998-01-20 | 1998-12-22 | HIV proteaz inhibitörünün bisülfat tuzu. |
Country Status (39)
Country | Link |
---|---|
US (1) | US6087383A (tr) |
EP (1) | EP1056722B1 (tr) |
JP (2) | JP4860037B2 (tr) |
KR (1) | KR100559283B1 (tr) |
CN (1) | CN1116282C (tr) |
AR (1) | AR014417A1 (tr) |
AT (1) | ATE219057T1 (tr) |
AU (1) | AU735875B2 (tr) |
BG (1) | BG64774B1 (tr) |
BR (1) | BR9814736A (tr) |
CA (1) | CA2317736C (tr) |
CO (1) | CO4970820A1 (tr) |
CZ (1) | CZ293507B6 (tr) |
DE (1) | DE69806067T2 (tr) |
DK (1) | DK1056722T3 (tr) |
EE (1) | EE04434B1 (tr) |
EG (1) | EG23936A (tr) |
ES (1) | ES2178300T3 (tr) |
GE (1) | GEP20033026B (tr) |
HK (2) | HK1033667A1 (tr) |
HU (1) | HU227196B1 (tr) |
IL (2) | IL137384A0 (tr) |
LT (1) | LT4780B (tr) |
LV (1) | LV12522B (tr) |
MY (1) | MY114838A (tr) |
NO (1) | NO315605B1 (tr) |
NZ (1) | NZ504417A (tr) |
PE (1) | PE20000185A1 (tr) |
PL (1) | PL190744B1 (tr) |
PT (1) | PT1056722E (tr) |
RO (1) | RO118869B1 (tr) |
RU (1) | RU2186070C2 (tr) |
SK (1) | SK283975B6 (tr) |
TR (1) | TR200001876T2 (tr) |
TW (1) | TW531531B (tr) |
UA (1) | UA59432C2 (tr) |
UY (1) | UY25345A1 (tr) |
WO (1) | WO1999036404A1 (tr) |
ZA (1) | ZA9956B (tr) |
Families Citing this family (45)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MXPA03010733A (es) * | 2001-05-22 | 2004-07-01 | Upjohn Co | Compuestos de etilamina aza-hidroxilados. |
US7193065B2 (en) * | 2001-07-13 | 2007-03-20 | Roche Diagnostics Operations, Inc. | Protease inhibitor conjugates and antibodies useful in immunoassay |
US7157561B2 (en) * | 2001-07-13 | 2007-01-02 | Roche Diagnostics Operations, Inc. | Methods of inhibiting transmission of a costimulatory signal of lymphocytes |
ATE398455T1 (de) * | 2003-01-14 | 2008-07-15 | Gilead Sciences Inc | Zusammensetzungen und verfahren zur antiviralen kombinationstherapie |
TW200534879A (en) * | 2004-03-25 | 2005-11-01 | Bristol Myers Squibb Co | Coated tablet formulation and method |
US20050256314A1 (en) * | 2004-05-04 | 2005-11-17 | Soojin Kim | Process employing controlled crystallization in forming crystals of a pharmaceutical |
US7829720B2 (en) * | 2004-05-04 | 2010-11-09 | Bristol-Myers Squibb Company | Process for preparing atazanavir bisulfate and novel forms |
CN1980666B (zh) * | 2004-05-04 | 2011-03-30 | 布里斯托尔-迈尔斯斯奎布公司 | 制备阿扎那韦硫酸氢盐的方法和新的形式 |
US20050288343A1 (en) * | 2004-05-19 | 2005-12-29 | Andrew Rusowicz | Process of preparing substituted carbamates and intermediates thereof |
TWI415635B (zh) * | 2004-05-28 | 2013-11-21 | 必治妥施貴寶公司 | 加衣錠片調製物及製備彼之方法 |
US7642049B2 (en) | 2006-06-30 | 2010-01-05 | Bristol-Myers Squibb Company | Method for identifying HIV-1 protease inhibitors with reduced metabolic affects through detection of human resistin polymorphisms |
ES2574831T3 (es) * | 2006-07-21 | 2016-06-22 | Gilead Sciences, Inc. | Inhibidores de la proteasa antivirales |
BG66056B1 (bg) * | 2006-10-05 | 2010-12-30 | Красимир ДЕЧЕВ | Метод и инсталация за производство на трисезонна добавка към дизелово гориво |
BRPI0823520A2 (pt) | 2007-06-12 | 2013-12-17 | Concert Pharmaceuticals Inc | Composto derivado de azapeptídeos e composição farmacêutica contendo o mesmo |
EP2178512B1 (en) * | 2007-06-22 | 2011-03-09 | Bristol-Myers Squibb Company | Tableted compositions containing atazanavir |
PT2170292E (pt) * | 2007-06-22 | 2014-03-06 | Bristol Myers Squibb Holdings Ireland | Composições de comprimido contendo atazanavir |
SI2178513T1 (sl) * | 2007-06-22 | 2011-05-31 | Bristol Myers Squibb Co | Tabletni sestavki vsebujoäśi atazanavir |
DE602008005316D1 (de) * | 2007-06-22 | 2011-04-14 | Bristol Myers Squibb Co | Tablettierte atazanavirhaltige zusammensetzungen |
WO2009006203A1 (en) * | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Therapeutic compositions and the use thereof |
JP5547066B2 (ja) * | 2007-06-29 | 2014-07-09 | ギリアード サイエンシーズ, インコーポレイテッド | 治療用組成物およびその使用 |
EP2288593A1 (en) * | 2008-05-08 | 2011-03-02 | Ranbaxy Laboratories Limited | Process for the preparation of 3,4-epoxy-2-amino-1-substituted butane derivatives and intermediate compounds thereof |
WO2010070611A1 (en) | 2008-12-18 | 2010-06-24 | Ranbaxy Laboratories Limited | Atazanavir formulations |
EP2376452A4 (en) | 2009-01-12 | 2012-08-29 | Hetero Research Foundation | NEW SULFATE POLYMORPH OF ATAZANAVIR |
JP2012528160A (ja) | 2009-05-27 | 2012-11-12 | メルク・シャープ・エンド・ドーム・コーポレイション | Hivプロテアーゼ阻害薬 |
EP2272830A1 (en) | 2009-06-18 | 2011-01-12 | Esteve Química, S.A. | Preparation process of an antivirally heterocyclic azahexane derivative |
WO2011027324A1 (en) | 2009-09-03 | 2011-03-10 | Ranbaxy Laboratories Limited | Polymorphic forms of atazanavir sulfate |
PL2493312T3 (pl) | 2009-10-26 | 2022-01-03 | Merck Sharp & Dohme Corp. | Kompozycje farmaceutyczne w postaci ciała stałego zawierające inhibitor integrazy |
WO2011080562A1 (en) | 2009-12-29 | 2011-07-07 | Hetero Research Foundation | Novel aza-peptides containing 2,2-disubstituted cyclobutyl and/or substituted alkoxy benzyl derivatives as antivirals |
KR20170078868A (ko) | 2010-01-27 | 2017-07-07 | 비이브 헬쓰케어 컴퍼니 | 항바이러스 치료 |
WO2011107843A2 (en) | 2010-03-01 | 2011-09-09 | Lupin Limited | Process for the preparation of atazanavir sulfate substantially free of diastereomers |
EP2555757B1 (en) | 2010-04-09 | 2016-05-25 | Bristol-Myers Squibb Holdings Ireland | Atazanavir sulfate formulations with improved ph effect |
EP2621472A1 (en) | 2010-09-28 | 2013-08-07 | Ratiopharm GmbH | Dry processing of atazanavir |
US20140343290A1 (en) | 2011-07-27 | 2014-11-20 | Rakesh Kumar Singh | Process for the preparation of atazanavir or its bisulfate salt |
US8461347B2 (en) | 2011-08-05 | 2013-06-11 | Scinopharm Taiwan, Ltd. | Process for preparing form A of atazanavir sulfate |
EP2771332B1 (en) | 2011-10-26 | 2016-06-29 | Merck Canada Inc. | Thiophen and thiazol sulfonamid derivatives as HIV protease inhibitors for the treatment of AIDS |
EP2888230A4 (en) | 2012-08-24 | 2017-07-19 | Laurus Labs Private Limited | Improved process for the preparation of atazanavir bisulfate |
WO2014036690A1 (zh) * | 2012-09-04 | 2014-03-13 | 上海迪赛诺化学制药有限公司 | 制备阿扎那韦硫酸氢盐a型结晶的方法 |
US9890121B2 (en) | 2013-02-12 | 2018-02-13 | Cipla Limited | Process for preparing atazanavir sulphate |
CN104250224A (zh) * | 2013-06-28 | 2014-12-31 | 上海威智医药科技有限公司 | 阿扎那韦富马酸盐及其制备和应用 |
CN104250225A (zh) * | 2013-06-28 | 2014-12-31 | 上海威智医药科技有限公司 | 阿扎那韦磷酸盐及其制备和应用 |
CN104250223B (zh) * | 2013-06-28 | 2017-04-12 | 上海威智医药科技有限公司 | 阿扎那韦氢溴酸盐及其制备和应用 |
CN105859611A (zh) * | 2016-04-18 | 2016-08-17 | 上海现代制药海门有限公司 | 一种阿扎那韦硫酸氢盐a型结晶的制备方法 |
CN109251165B (zh) * | 2018-10-02 | 2022-09-23 | 国药集团川抗制药有限公司 | 阿扎那韦达二4-氨基苯磺酸盐及其制备方法 |
CN111349042B (zh) * | 2018-12-20 | 2023-07-14 | 陕西理工大学 | 一种阿扎那韦单晶及其制备方法 |
US12083099B2 (en) | 2020-10-28 | 2024-09-10 | Accencio LLC | Methods of treating symptoms of coronavirus infection with viral protease inhibitors |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5849911A (en) * | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
TW409125B (en) * | 1996-04-22 | 2000-10-21 | Novartis Ag | Antivirally active heterocyclic azahexane derivatives |
-
1998
- 1998-12-21 US US09/217,538 patent/US6087383A/en not_active Expired - Lifetime
- 1998-12-22 PL PL342019A patent/PL190744B1/pl unknown
- 1998-12-22 AU AU20101/99A patent/AU735875B2/en not_active Expired
- 1998-12-22 WO PCT/US1998/027382 patent/WO1999036404A1/en active IP Right Grant
- 1998-12-22 IL IL13738498A patent/IL137384A0/xx active IP Right Grant
- 1998-12-22 KR KR1020007007885A patent/KR100559283B1/ko not_active IP Right Cessation
- 1998-12-22 DK DK98964878T patent/DK1056722T3/da active
- 1998-12-22 RU RU2000119792/04A patent/RU2186070C2/ru active
- 1998-12-22 EP EP98964878A patent/EP1056722B1/en not_active Expired - Lifetime
- 1998-12-22 JP JP2000540121A patent/JP4860037B2/ja not_active Expired - Lifetime
- 1998-12-22 NZ NZ504417A patent/NZ504417A/en not_active IP Right Cessation
- 1998-12-22 UA UA2000084931A patent/UA59432C2/uk unknown
- 1998-12-22 TR TR2000/01876T patent/TR200001876T2/tr unknown
- 1998-12-22 CA CA002317736A patent/CA2317736C/en not_active Expired - Lifetime
- 1998-12-22 RO ROA200000717A patent/RO118869B1/ro unknown
- 1998-12-22 PT PT98964878T patent/PT1056722E/pt unknown
- 1998-12-22 AT AT98964878T patent/ATE219057T1/de active
- 1998-12-22 CN CN98812741A patent/CN1116282C/zh not_active Expired - Lifetime
- 1998-12-22 EE EEP200000798A patent/EE04434B1/xx unknown
- 1998-12-22 HU HU0101389A patent/HU227196B1/hu unknown
- 1998-12-22 ES ES98964878T patent/ES2178300T3/es not_active Expired - Lifetime
- 1998-12-22 SK SK1062-2000A patent/SK283975B6/sk not_active IP Right Cessation
- 1998-12-22 GE GEAP19985466A patent/GEP20033026B/en unknown
- 1998-12-22 CZ CZ20002564A patent/CZ293507B6/cs not_active IP Right Cessation
- 1998-12-22 BR BR9814736-6A patent/BR9814736A/pt not_active Application Discontinuation
- 1998-12-22 DE DE69806067T patent/DE69806067T2/de not_active Expired - Lifetime
-
1999
- 1999-01-05 MY MYPI99000020A patent/MY114838A/en unknown
- 1999-01-05 ZA ZA9900056A patent/ZA9956B/xx unknown
- 1999-01-12 UY UY25345A patent/UY25345A1/es not_active Application Discontinuation
- 1999-01-15 TW TW088100623A patent/TW531531B/zh not_active IP Right Cessation
- 1999-01-17 EG EG5699A patent/EG23936A/xx active
- 1999-01-18 AR ARP990100179A patent/AR014417A1/es active IP Right Grant
- 1999-01-19 CO CO99002578A patent/CO4970820A1/es unknown
- 1999-01-20 PE PE1999000047A patent/PE20000185A1/es not_active IP Right Cessation
-
2000
- 2000-06-06 LV LVP-00-78A patent/LV12522B/en unknown
- 2000-07-14 LT LT2000067A patent/LT4780B/lt not_active IP Right Cessation
- 2000-07-17 BG BG104618A patent/BG64774B1/bg unknown
- 2000-07-19 NO NO20003692A patent/NO315605B1/no not_active IP Right Cessation
- 2000-07-19 IL IL137384A patent/IL137384A/en not_active IP Right Cessation
-
2001
- 2001-04-26 HK HK01103011A patent/HK1033667A1/xx not_active IP Right Cessation
- 2001-06-15 HK HK01104126A patent/HK1033458A1/xx not_active IP Right Cessation
-
2008
- 2008-12-17 JP JP2008321240A patent/JP2009102357A/ja not_active Withdrawn
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