CN101068550B - 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂 - Google Patents

含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂 Download PDF

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Publication number
CN101068550B
CN101068550B CN2005800412301A CN200580041230A CN101068550B CN 101068550 B CN101068550 B CN 101068550B CN 2005800412301 A CN2005800412301 A CN 2005800412301A CN 200580041230 A CN200580041230 A CN 200580041230A CN 101068550 B CN101068550 B CN 101068550B
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amount
preparation
compound
compd
poloxamer
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Expired - Fee Related
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English (en)
Chinese (zh)
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CN101068550A (zh
Inventor
N·普尔卡沃斯
J·R·尼
M·T·克吕安斯
Y·吴
S·A·帕尔卡
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Merck Sharp and Dohme LLC
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Schering Corp
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN2005800412301A 2004-12-03 2005-12-02 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂 Expired - Fee Related CN101068550B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US63294404P 2004-12-03 2004-12-03
US60/632,944 2004-12-03
PCT/US2005/043727 WO2006060711A2 (en) 2004-12-03 2005-12-02 Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition

Publications (2)

Publication Number Publication Date
CN101068550A CN101068550A (zh) 2007-11-07
CN101068550B true CN101068550B (zh) 2011-03-30

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CN2005800412301A Expired - Fee Related CN101068550B (zh) 2004-12-03 2005-12-02 含有释放速度控制组分的羧酰胺人类免疫缺陷整合酶抑制剂药物制剂

Country Status (16)

Country Link
US (1) US8852632B2 (enExample)
EP (2) EP1904067B2 (enExample)
JP (1) JP5228488B2 (enExample)
KR (1) KR101351059B1 (enExample)
CN (1) CN101068550B (enExample)
AU (1) AU2005311652B2 (enExample)
BR (1) BRPI0518781A2 (enExample)
CA (1) CA2588445C (enExample)
ES (1) ES2755273T3 (enExample)
IL (1) IL183615A (enExample)
MX (1) MX2007006635A (enExample)
NO (1) NO20073405L (enExample)
NZ (1) NZ555120A (enExample)
RU (1) RU2382648C2 (enExample)
WO (1) WO2006060711A2 (enExample)
ZA (1) ZA200703866B (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1819323B2 (en) * 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
KR20070085702A (ko) * 2004-12-03 2007-08-27 머크 앤드 캄파니 인코포레이티드 Ｕｇｔ1ａ1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도
US7687509B2 (en) 2007-07-09 2010-03-30 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives
EP3970702A1 (en) 2009-10-26 2022-03-23 Merck Sharp & Dohme Corp. Solid pharmaceutical compositions containing an integrase inhibitor
CA2999435A1 (en) * 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
WO2012009446A1 (en) 2010-07-16 2012-01-19 Concert Pharmaceuticals Inc. Novel pyrimidinecarboxamide derivatives
US9968607B2 (en) 2011-04-25 2018-05-15 Hetero Research Foundation Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof
EP2529741B1 (en) * 2011-06-01 2014-02-12 Ratiopharm GmbH Composition and Tablet Comprising Raltegravir
HUE064694T2 (hu) 2012-03-22 2024-04-28 Novo Nordisk As Továbbítószert tartalmazó készítmények és elõállításuk
WO2014030172A2 (en) * 2012-08-23 2014-02-27 Hetero Research Foundation Pharmaceutical formulations of rufinamide
US9763934B2 (en) * 2014-03-05 2017-09-19 Professional Compounding Centers Of America Synergistic effect of poloxamer-based composition and itraconazole on fungus and yeast
KR102293907B1 (ko) 2015-06-30 2021-08-26 한미약품 주식회사 이리노테칸 함유 경구용 고형제제 및 그 제조방법
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
WO2019236395A1 (en) * 2018-06-06 2019-12-12 Merck Sharp & Dohme Corp. Formulations of raltegravir

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035077A1 (en) * 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
WO2004058756A1 (en) * 2002-12-27 2004-07-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA56992C2 (uk) * 1995-05-08 2003-06-16 Фармація Енд Апджон Компані <font face="Symbol">a</font>-ПІРИМІДИНТІОАЛКІЛЗАМІЩЕНІ ТА <font face="Symbol">a</font>-ПІРИМІДИНОКСОАЛКІЛЗАМІЩЕНІ СПОЛУКИ
IE970588A1 (en) * 1997-08-01 2000-08-23 Elan Corp Plc Controlled release pharmaceutical compositions containing tiagabine
MXPA02005291A (es) * 1999-12-03 2004-06-21 Polichem Sa Metodos para elaborar composiciones farmaceuticas de liberacion sostenida de alcaloides de cornezuelo de centeno que tienen biodisponibilidad mejorada y composiciones de los mismos.
CN1255185C (zh) * 2001-05-03 2006-05-10 弗·哈夫曼-拉罗切有限公司 无定形甲磺酸奈非那韦的药物剂型
SE0102887D0 (sv) * 2001-08-29 2001-08-29 Astrazeneca Ab New formulation
US6673369B2 (en) * 2001-08-29 2004-01-06 Ranbaxy Laboratories Limited Controlled release formulation
DK1441734T3 (da) * 2001-10-26 2007-06-11 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
WO2003086319A2 (en) * 2002-04-10 2003-10-23 Merck & Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
ATE500819T1 (de) * 2003-12-31 2011-03-15 Bend Res Inc Stabilisierte pharmazeutische feste zusammensetzungen von arzneimitteln mit geringer löslichkeit, poloxameren und stabilisierenden polymeren
KR20070085702A (ko) 2004-12-03 2007-08-27 머크 앤드 캄파니 인코포레이티드 Ｕｇｔ1ａ1에 의해 대사된 약물의 약력학을 개선시키기위한 아타자나비르의 용도
EP1819323B2 (en) * 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035077A1 (en) * 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
WO2004058756A1 (en) * 2002-12-27 2004-07-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors

Also Published As

Publication number Publication date
RU2382648C2 (ru) 2010-02-27
EP1904067A2 (en) 2008-04-02
ZA200703866B (en) 2008-03-26
IL183615A0 (en) 2007-10-31
WO2006060711A3 (en) 2006-09-08
AU2005311652A1 (en) 2006-06-08
MX2007006635A (es) 2007-06-19
NO20073405L (no) 2007-07-02
RU2007125122A (ru) 2009-01-10
CN101068550A (zh) 2007-11-07
KR20070085695A (ko) 2007-08-27
NZ555120A (en) 2009-11-27
BRPI0518781A2 (pt) 2008-12-09
JP5228488B2 (ja) 2013-07-03
EP2586444B1 (en) 2019-09-25
EP1904067B1 (en) 2013-11-20
WO2006060711A2 (en) 2006-06-08
US8852632B2 (en) 2014-10-07
EP1904067B2 (en) 2017-10-11
IL183615A (en) 2013-01-31
US20070292504A1 (en) 2007-12-20
ES2755273T3 (es) 2020-04-22
KR101351059B1 (ko) 2014-02-17
JP2008521932A (ja) 2008-06-26
AU2005311652B2 (en) 2010-12-02
CA2588445C (en) 2013-06-25
EP2586444A1 (en) 2013-05-01
CA2588445A1 (en) 2006-06-08

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Owner name: SCHERING CORP (US)

Free format text: FORMER OWNER: MSD CORP.

Effective date: 20121031

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Address after: New jersey, USA

Patentee after: MERCK SHARP & DOHME Corp.

Address before: New jersey, USA

Patentee before: SCHERING Corp.

TR01 Transfer of patent right

Effective date of registration: 20121031

Address after: New jersey, USA

Patentee after: SCHERING Corp.

Address before: New jersey, USA

Patentee before: MERCK SHARP & DOHME Corp.

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20110330

Termination date: 20161202

CF01 Termination of patent right due to non-payment of annual fee