ES2178300T3 - Sal bisulfato del inhibidor de la proteasa del vih. - Google Patents

Sal bisulfato del inhibidor de la proteasa del vih.

Info

Publication number
ES2178300T3
ES2178300T3 ES98964878T ES98964878T ES2178300T3 ES 2178300 T3 ES2178300 T3 ES 2178300T3 ES 98964878 T ES98964878 T ES 98964878T ES 98964878 T ES98964878 T ES 98964878T ES 2178300 T3 ES2178300 T3 ES 2178300T3
Authority
ES
Spain
Prior art keywords
protease inhibitor
bisulfate salt
hiv protease
formula
pharmaceutical forms
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES98964878T
Other languages
English (en)
Inventor
Janak Singh
Madhusudhan Pudipeddi
Mark D Lindrud
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22104737&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2178300(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Application granted granted Critical
Publication of ES2178300T3 publication Critical patent/ES2178300T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente invención proporciona una sal bisulfato cristalina novedosa del azapéptido inhibidor de la proteasa del VIH de fórmula **(Fórmula)** que muestra unas inesperadas solubilidad/disolución en agua superiores a las de otras sales, y que mejor o significativamente la biodisponibilidad oral en animales comparado con la base libre. La sal bisulfato es por tanto de utilidad en formas farmacéuticas del anteriormente indicado inhibidor de proteasas, en particular en formas farmacéuticas orales.
ES98964878T 1998-01-20 1998-12-22 Sal bisulfato del inhibidor de la proteasa del vih. Expired - Lifetime ES2178300T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7196898P 1998-01-20 1998-01-20

Publications (1)

Publication Number Publication Date
ES2178300T3 true ES2178300T3 (es) 2002-12-16

Family

ID=22104737

Family Applications (1)

Application Number Title Priority Date Filing Date
ES98964878T Expired - Lifetime ES2178300T3 (es) 1998-01-20 1998-12-22 Sal bisulfato del inhibidor de la proteasa del vih.

Country Status (39)

Country Link
US (1) US6087383A (es)
EP (1) EP1056722B1 (es)
JP (2) JP4860037B2 (es)
KR (1) KR100559283B1 (es)
CN (1) CN1116282C (es)
AR (1) AR014417A1 (es)
AT (1) ATE219057T1 (es)
AU (1) AU735875B2 (es)
BG (1) BG64774B1 (es)
BR (1) BR9814736A (es)
CA (1) CA2317736C (es)
CO (1) CO4970820A1 (es)
CZ (1) CZ293507B6 (es)
DE (1) DE69806067T2 (es)
DK (1) DK1056722T3 (es)
EE (1) EE04434B1 (es)
EG (1) EG23936A (es)
ES (1) ES2178300T3 (es)
GE (1) GEP20033026B (es)
HK (2) HK1033667A1 (es)
HU (1) HU227196B1 (es)
IL (2) IL137384A0 (es)
LT (1) LT4780B (es)
LV (1) LV12522B (es)
MY (1) MY114838A (es)
NO (1) NO315605B1 (es)
NZ (1) NZ504417A (es)
PE (1) PE20000185A1 (es)
PL (1) PL190744B1 (es)
PT (1) PT1056722E (es)
RO (1) RO118869B1 (es)
RU (1) RU2186070C2 (es)
SK (1) SK283975B6 (es)
TR (1) TR200001876T2 (es)
TW (1) TW531531B (es)
UA (1) UA59432C2 (es)
UY (1) UY25345A1 (es)
WO (1) WO1999036404A1 (es)
ZA (1) ZA9956B (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004534771A (ja) 2001-05-22 2004-11-18 イーラン　ファーマスーティカルズ、インコーポレイテッド アザヒドロキシル化エチルアミン化合物
US7157561B2 (en) * 2001-07-13 2007-01-02 Roche Diagnostics Operations, Inc. Methods of inhibiting transmission of a costimulatory signal of lymphocytes
US7193065B2 (en) * 2001-07-13 2007-03-20 Roche Diagnostics Operations, Inc. Protease inhibitor conjugates and antibodies useful in immunoassay
US20040224916A1 (en) * 2003-01-14 2004-11-11 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
TW200534879A (en) * 2004-03-25 2005-11-01 Bristol Myers Squibb Co Coated tablet formulation and method
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
US7829720B2 (en) 2004-05-04 2010-11-09 Bristol-Myers Squibb Company Process for preparing atazanavir bisulfate and novel forms
US20050256314A1 (en) * 2004-05-04 2005-11-17 Soojin Kim Process employing controlled crystallization in forming crystals of a pharmaceutical
US20050288343A1 (en) * 2004-05-19 2005-12-29 Andrew Rusowicz Process of preparing substituted carbamates and intermediates thereof
TWI354569B (en) * 2004-05-28 2011-12-21 Bristol Myers Squibb Co Coated tablet formulation and method
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
CA2657936C (en) * 2006-07-21 2017-01-10 Gilead Sciences, Inc. Antiviral protease inhibitors
BG66056B1 (bg) * 2006-10-05 2010-12-30 Красимир ДЕЧЕВ Метод и инсталация за производство на трисезонна добавка към дизелово гориво
MX2009013565A (es) 2007-06-12 2010-06-02 Concert Pharmaceuticals Inc Derivados de azapeptidos.
US20100183715A1 (en) * 2007-06-22 2010-07-22 Bristo-Meyers Squibb Company Tableted compositions containing atazanavir
DE602008005896D1 (de) * 2007-06-22 2011-05-12 Bristol Myers Squibb Co Tablettierte atazanavirhaltige zusammensetzungen
AU2008268627A1 (en) * 2007-06-22 2008-12-31 Bristol-Myers Squibb Company Tableted compositions containing atazanavir
AU2008268630A1 (en) * 2007-06-22 2008-12-31 Bristol-Myers Squibb Company Tableted compositions containing atazanavir
KR20100028656A (ko) * 2007-06-29 2010-03-12 길리애드 사이언시즈, 인코포레이티드 치료 조성물 및 그의 용도
TW200914011A (en) * 2007-06-29 2009-04-01 Gilead Sciences Inc Therapeutic compositions and methods
WO2009136365A1 (en) * 2008-05-08 2009-11-12 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
WO2010079497A2 (en) * 2009-01-12 2010-07-15 Hetero Research Foundation Novel polymorph of atazanavir sulfate
CA2762582A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Hiv protease inhibitors
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
HRP20211826T1 (hr) 2009-10-26 2022-03-04 Merck Sharp & Dohme Corp. Čvrste farmaceutske kompozicije koje sadrže inhibitor integraze
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
NZ627826A (en) 2010-01-27 2016-01-29 Viiv Healthcare Co Antiviral combinations involving (3s,11ar)-n-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
EP2542527A2 (en) 2010-03-01 2013-01-09 Lupin Limited Process for the preparation of atazanavir sulfate substantially free of diastereomers
US20130203759A1 (en) 2010-04-09 2013-08-08 Faranak Nikfar ATAZANAVIR SULFATE FORMULATIONS WITH IMPROVED pH EFFECT
EA201390464A1 (ru) 2010-09-28 2013-08-30 Рациофарм Гмбх Способ сухой обработки атазанавира
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
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
US9382207B2 (en) 2012-08-24 2016-07-05 Laurus Labs Private Limited 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
ZA201401073B (en) 2013-02-12 2015-12-23 Cipla Ltd Process for preparing atazanavir sulphate
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
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
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

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW409125B (en) * 1996-04-22 2000-10-21 Novartis Ag Antivirally active heterocyclic azahexane derivatives
US5849911A (en) * 1996-04-22 1998-12-15 Novartis Finance Corporation Antivirally active heterocyclic azahexane derivatives

Also Published As

Publication number Publication date
GEP20033026B (en) 2003-07-25
EE04434B1 (et) 2005-02-15
NO20003692D0 (no) 2000-07-19
CZ20002564A3 (cs) 2000-10-11
CN1283188A (zh) 2001-02-07
ZA9956B (en) 2000-07-05
NO20003692L (no) 2000-07-19
DK1056722T3 (da) 2002-09-30
TW531531B (en) 2003-05-11
NZ504417A (en) 2001-09-28
JP4860037B2 (ja) 2012-01-25
IL137384A0 (en) 2001-07-24
HK1033667A1 (en) 2001-09-14
PE20000185A1 (es) 2000-05-14
EP1056722A1 (en) 2000-12-06
PT1056722E (pt) 2002-09-30
US6087383A (en) 2000-07-11
MY114838A (en) 2003-01-31
EG23936A (en) 2008-01-14
IL137384A (en) 2006-08-01
JP2009102357A (ja) 2009-05-14
PL190744B1 (pl) 2006-01-31
EP1056722A4 (en) 2001-01-10
TR200001876T2 (tr) 2000-11-21
KR100559283B1 (ko) 2006-03-15
AU735875B2 (en) 2001-07-19
AR014417A1 (es) 2001-02-28
LT2000067A (en) 2000-11-27
EE200000798A (et) 2002-06-17
LT4780B (lt) 2001-04-25
HK1033458A1 (en) 2001-08-31
UY25345A1 (es) 2000-12-29
SK283975B6 (sk) 2004-06-08
BG104618A (en) 2001-02-28
CO4970820A1 (es) 2000-11-07
JP2002509136A (ja) 2002-03-26
CA2317736C (en) 2004-11-02
SK10622000A3 (sk) 2001-02-12
PL342019A1 (en) 2001-05-07
NO315605B1 (no) 2003-09-29
CA2317736A1 (en) 1999-07-22
HUP0101389A2 (hu) 2001-08-28
DE69806067D1 (de) 2002-07-18
EP1056722B1 (en) 2002-06-12
BR9814736A (pt) 2000-10-24
UA59432C2 (uk) 2003-09-15
ATE219057T1 (de) 2002-06-15
WO1999036404A1 (en) 1999-07-22
LV12522A (en) 2000-08-20
HU227196B1 (en) 2010-10-28
CN1116282C (zh) 2003-07-30
DE69806067T2 (de) 2003-01-23
AU2010199A (en) 1999-08-02
HUP0101389A3 (en) 2003-07-28
CZ293507B6 (cs) 2004-05-12
RO118869B1 (ro) 2003-12-30
LV12522B (en) 2000-10-20
BG64774B1 (bg) 2006-03-31
KR20010034221A (ko) 2001-04-25
RU2186070C2 (ru) 2002-07-27

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