MX2014012741A - Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria. - Google Patents

Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria.

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Publication number
MX2014012741A
MX2014012741A MX2014012741A MX2014012741A MX2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A
Authority
MX
Mexico
Prior art keywords
inhibitors
imidazothiadiazole
platelet aggregation
par4
activated receptor
Prior art date
Application number
MX2014012741A
Other languages
English (en)
Inventor
R Michael Lawrence
Eldon Scott Priestley
Shoshana L Posy
Michael M Miller
Alain Martel
Francois Tremblay
Anne Marinier
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
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of MX2014012741A publication Critical patent/MX2014012741A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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

Abstract

La presente invención se refiere a compuestos de imidazotiadiazol de la Fórmula (I): (ver Fórmula) en donde W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 y X4 son como se definen en la presente, o un estereoisómero, tautómero, una sal farmacéuticamente aceptable, éster de profármaco o forma de solvato del mismo, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores de la agregación plaquetaria y, por lo tanto, se pueden usar como medicamentos para tratar o prevenir trastornos tromboembólicos.
MX2014012741A 2012-04-26 2013-04-24 Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria. MX2014012741A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261638567P 2012-04-26 2012-04-26
PCT/US2013/037884 WO2013163241A1 (en) 2012-04-26 2013-04-24 Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation

Publications (1)

Publication Number Publication Date
MX2014012741A true MX2014012741A (es) 2015-04-13

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MX2014012741A MX2014012741A (es) 2012-04-26 2013-04-24 Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria.

Country Status (14)

Country Link
US (1) US9518064B2 (es)
EP (1) EP2855489B1 (es)
JP (1) JP6101343B2 (es)
KR (1) KR20150003766A (es)
CN (1) CN104640869B (es)
AU (1) AU2013251680A1 (es)
BR (1) BR112014026651A8 (es)
CA (1) CA2871599A1 (es)
EA (1) EA201491954A1 (es)
ES (1) ES2617879T3 (es)
IL (1) IL235141A0 (es)
MX (1) MX2014012741A (es)
SG (1) SG11201406733QA (es)
WO (1) WO2013163241A1 (es)

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CN112074523B (zh) * 2018-05-16 2022-08-09 深圳信立泰药业股份有限公司 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物
CN112074522B (zh) * 2018-05-16 2022-08-26 深圳信立泰药业股份有限公司 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物
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CN111349105B (zh) * 2018-12-24 2023-04-07 江苏恒瑞医药股份有限公司 苯并呋喃类衍生物、其制备方法及其在医药上的应用
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EA201491954A1 (ru) 2015-01-30
IL235141A0 (en) 2014-12-31
JP6101343B2 (ja) 2017-03-22
US20150119390A1 (en) 2015-04-30
AU2013251680A1 (en) 2014-11-13
CA2871599A1 (en) 2013-10-31
EP2855489B1 (en) 2017-01-04
JP2015514806A (ja) 2015-05-21
US9518064B2 (en) 2016-12-13
BR112014026651A2 (pt) 2017-06-27
CN104640869A (zh) 2015-05-20
BR112014026651A8 (pt) 2018-01-16
ES2617879T3 (es) 2017-06-20
CN104640869B (zh) 2017-12-12
SG11201406733QA (en) 2014-11-27
WO2013163241A1 (en) 2013-10-31
EP2855489A1 (en) 2015-04-08
KR20150003766A (ko) 2015-01-09

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