CN104922054A - 凝血酶受体拮抗剂的即释片剂 - Google Patents

凝血酶受体拮抗剂的即释片剂 Download PDF

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Publication number
CN104922054A
CN104922054A CN201510409546.7A CN201510409546A CN104922054A CN 104922054 A CN104922054 A CN 104922054A CN 201510409546 A CN201510409546 A CN 201510409546A CN 104922054 A CN104922054 A CN 104922054A
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CN
China
Prior art keywords
formulation
compound
pharmaceutical formulation
tablet
solid pharmaceutical
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.)
Pending
Application number
CN201510409546.7A
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English (en)
Chinese (zh)
Inventor
R.古塔
S.查德瑞
S.S.道吉雷拉
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.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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Publication of CN104922054A publication Critical patent/CN104922054A/zh
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201510409546.7A 2006-06-30 2007-06-29 凝血酶受体拮抗剂的即释片剂 Pending CN104922054A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US81782106P 2006-06-30 2006-06-30
US60/817821 2006-06-30
CNA2007800325694A CN101511345A (zh) 2006-06-30 2007-06-29 凝血酶受体拮抗剂的即释片剂

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNA2007800325694A Division CN101511345A (zh) 2006-06-30 2007-06-29 凝血酶受体拮抗剂的即释片剂

Publications (1)

Publication Number Publication Date
CN104922054A true CN104922054A (zh) 2015-09-23

Family

ID=38895141

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201510409546.7A Pending CN104922054A (zh) 2006-06-30 2007-06-29 凝血酶受体拮抗剂的即释片剂
CNA2007800325694A Pending CN101511345A (zh) 2006-06-30 2007-06-29 凝血酶受体拮抗剂的即释片剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CNA2007800325694A Pending CN101511345A (zh) 2006-06-30 2007-06-29 凝血酶受体拮抗剂的即释片剂

Country Status (18)

Country Link
US (2) US20080031943A1 (https=)
EP (2) EP2491922B1 (https=)
JP (2) JP5116764B2 (https=)
KR (1) KR20090023670A (https=)
CN (2) CN104922054A (https=)
AR (1) AR061790A1 (https=)
AU (1) AU2007269733B2 (https=)
BR (1) BRPI0713935A2 (https=)
CA (1) CA2656395C (https=)
CL (1) CL2007001923A1 (https=)
CO (1) CO6150126A2 (https=)
ES (2) ES2616405T3 (https=)
MX (1) MX2009000131A (https=)
NO (1) NO20090467L (https=)
PE (1) PE20080376A1 (https=)
TW (1) TWI367112B (https=)
WO (1) WO2008005353A2 (https=)
ZA (1) ZA200900350B (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
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TWI343262B (en) * 2006-09-26 2011-06-11 Schering Corp Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist
EP2120879A2 (en) * 2006-12-22 2009-11-25 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
US8624050B2 (en) * 2007-06-22 2014-01-07 General Electric Company Solution process for transparent conductive oxide coatings
WO2009078999A1 (en) 2007-12-17 2009-06-25 Janssen Pharmaceutica N.V. Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1
EP2438060B1 (en) 2009-06-04 2013-10-02 Merck Sharp & Dohme Corp. Active metabolite of a thrombin receptor antagonist
JP2012529431A (ja) 2009-06-08 2012-11-22 メルク・シャープ・アンド・ドーム・コーポレーション トロンビン受容体アンタゴニストおよびクロピドグレルの固定用量錠剤
CN102442965B (zh) * 2010-09-30 2013-12-11 天津药物研究院 用于治疗血栓性疾病的par-1拮抗剂及其制备方法和用途
WO2017134200A1 (en) 2016-02-05 2017-08-10 Sanovel Ilac Sanayi Ve Ticaret A.S. A novel pharmaceutical composition of vorapaxar and metoprolol
TR201601548A2 (tr) 2016-02-05 2018-03-21 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Vorapaksar ve metoprololün bi̇r farmasöti̇k kompozi̇syonu
MX2020008137A (es) * 2018-02-02 2020-10-19 Eustralis Pharmaceuticals Ltd Trading As Pressura Neuro Formulaciones orales y usos de las mismas.

Citations (3)

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US20020160963A1 (en) * 2001-02-23 2002-10-31 Maryanoff Bruce E. Aminomethyl-pyrroloquinazoline compounds as thrombin receptor antagonists
CN1436185A (zh) * 2000-06-15 2003-08-13 先灵公司 凝血酶受体拮抗药
EP1495018A1 (en) * 2002-04-16 2005-01-12 Schering Corporation Tricyclic thrombin receptor antagonists

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US20080026050A1 (en) * 2006-06-30 2008-01-31 Rajan Gupta Solid dose formulations of a thrombin receptor antagonist
TWI343262B (en) * 2006-09-26 2011-06-11 Schering Corp Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist
EP2120879A2 (en) * 2006-12-22 2009-11-25 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
BRPI0809095A2 (pt) * 2007-03-23 2014-09-09 Schering Corp Redução de eventos adversos após intervenção percutânea através de uso de um antagonista de receptor de trombina

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CN1436185A (zh) * 2000-06-15 2003-08-13 先灵公司 凝血酶受体拮抗药
US20020160963A1 (en) * 2001-02-23 2002-10-31 Maryanoff Bruce E. Aminomethyl-pyrroloquinazoline compounds as thrombin receptor antagonists
EP1495018A1 (en) * 2002-04-16 2005-01-12 Schering Corporation Tricyclic thrombin receptor antagonists
CN1659162A (zh) * 2002-04-16 2005-08-24 先灵公司 三环凝血酶受体拮抗剂

Also Published As

Publication number Publication date
BRPI0713935A2 (pt) 2012-12-04
EP2491922A1 (en) 2012-08-29
ZA200900350B (en) 2010-01-27
US20170224666A9 (en) 2017-08-10
WO2008005353A2 (en) 2008-01-10
CO6150126A2 (es) 2010-04-20
CA2656395A1 (en) 2008-01-10
WO2008005353A3 (en) 2008-06-26
EP2034969A2 (en) 2009-03-18
JP2009542678A (ja) 2009-12-03
CL2007001923A1 (es) 2008-02-08
EP2491922B1 (en) 2017-01-04
AU2007269733B2 (en) 2013-02-21
US20160193196A1 (en) 2016-07-07
JP2012126752A (ja) 2012-07-05
US20080031943A1 (en) 2008-02-07
MX2009000131A (es) 2009-01-26
CN101511345A (zh) 2009-08-19
AR061790A1 (es) 2008-09-24
JP5116764B2 (ja) 2013-01-09
TW200810792A (en) 2008-03-01
NO20090467L (no) 2009-03-19
KR20090023670A (ko) 2009-03-05
CA2656395C (en) 2016-12-13
ES2616354T3 (es) 2017-06-12
ES2616405T3 (es) 2017-06-13
EP2034969B1 (en) 2017-01-11
AU2007269733A1 (en) 2008-01-10
TWI367112B (en) 2012-07-01
PE20080376A1 (es) 2008-06-13

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Application publication date: 20150923