EA201071307A1 - Карбамоильные производные бициклических карбониламинопиразолов в качестве пролекарств - Google Patents

Карбамоильные производные бициклических карбониламинопиразолов в качестве пролекарств

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Publication number
EA201071307A1
EA201071307A1 EA201071307A EA201071307A EA201071307A1 EA 201071307 A1 EA201071307 A1 EA 201071307A1 EA 201071307 A EA201071307 A EA 201071307A EA 201071307 A EA201071307 A EA 201071307A EA 201071307 A1 EA201071307 A1 EA 201071307A1
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EA
Eurasian Patent Office
Prior art keywords
bicyclic
medicine
derivatives
carbonylaminopyrazole
carbamoic
Prior art date
Application number
EA201071307A
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English (en)
Other versions
EA019901B1 (ru
Inventor
Паоло Получчи
Маурицио Пуличи
Original Assignee
НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40886839&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201071307(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. filed Critical НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Publication of EA201071307A1 publication Critical patent/EA201071307A1/ru
Publication of EA019901B1 publication Critical patent/EA019901B1/ru

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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D497/04—Ortho-condensed systems

Abstract

Обеспечиваются бициклические карбониламинопиразолы формулы (I), где переменные имеют значения, определенные в формуле изобретения, для использования в качестве лекарственного средства, в частности для лечения заболеваний, вызванных нарушением функции протеинкиназ (РК), таких как рак, фармацевтические композиции, включающие такие карбамоильные производные, и их применение в качестве пролекарств терапевтически активных веществ. Способ лечения и некоторые новые бициклические карбониламинопиразолы также являются объектом настоящего изобретения.
EA201071307A 2008-05-15 2009-05-14 Карбамоильные производные бициклических карбониламинопиразолов в качестве пролекарств EA019901B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08156262 2008-05-15
PCT/EP2009/055802 WO2009138440A1 (en) 2008-05-15 2009-05-14 Carbamoyl derivatives of bicyclic carbonylamino-pyrazoles as prodrugs

Publications (2)

Publication Number Publication Date
EA201071307A1 true EA201071307A1 (ru) 2011-06-30
EA019901B1 EA019901B1 (ru) 2014-07-30

Family

ID=40886839

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201071307A EA019901B1 (ru) 2008-05-15 2009-05-14 Карбамоильные производные бициклических карбониламинопиразолов в качестве пролекарств

Country Status (21)

Country Link
US (2) US20110118278A1 (ru)
EP (1) EP2300436B1 (ru)
JP (1) JP5984387B2 (ru)
KR (1) KR101586634B1 (ru)
CN (1) CN102026983B (ru)
AR (1) AR071780A1 (ru)
AU (1) AU2009248060B2 (ru)
BR (1) BRPI0911986A2 (ru)
CA (1) CA2724215C (ru)
CL (1) CL2009001158A1 (ru)
EA (1) EA019901B1 (ru)
ES (1) ES2689325T3 (ru)
HK (1) HK1151793A1 (ru)
IL (1) IL209234A (ru)
MX (1) MX2010012295A (ru)
NZ (1) NZ589956A (ru)
SG (1) SG190636A1 (ru)
TW (1) TW201004951A (ru)
UA (1) UA106353C2 (ru)
WO (1) WO2009138440A1 (ru)
ZA (1) ZA201008911B (ru)

Families Citing this family (8)

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MX2009006401A (es) * 2006-12-20 2009-06-23 Nerviano Medical Sciences Srl Derivados de indazol como inhibidores de cinasa para el tratamiento del cancer.
KR101178495B1 (ko) 2010-05-03 2012-09-07 서울대학교산학협력단 3,6-이치환-4,5,6,7-테트라하이드로-1Ｈ-피라졸로［3,4-ｃ］피리딘-7-온 화합물과 이 화합물의 제조방법
MX342509B (es) * 2011-05-12 2016-10-03 Nerviano Medical Sciences Srl Compuestos de indazol sustituidos como inhibidores de las cinasas de proteina.
WO2015110467A1 (en) * 2014-01-23 2015-07-30 Nerviano Medical Sciences S.R.L. Process for the preparation of substituted n-(5-benzenesulfonyl-1h-indazol-3-yl)-benzamides
WO2016086200A1 (en) 2014-11-27 2016-06-02 Genentech, Inc. 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors
MA45146A (fr) 2016-05-24 2021-03-24 Constellation Pharmaceuticals Inc Dérivés de pyrazolopyridine pour le traitement du cancer
CN115073471B (zh) * 2021-03-11 2023-03-21 沈阳药科大学 吡唑并四氢吡咯类衍生物、其制备方法和在医药上的应用
CN113072562B (zh) * 2021-04-06 2022-01-14 山东大学 一种GSK-3β抑制剂及其制备方法与应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA05009719A (es) * 2003-03-11 2005-10-18 Pharmacia Italia Spa Derivados de biciclo-pirazol activos como inhibidores de cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
SE0301906D0 (sv) * 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
US7141568B2 (en) * 2003-07-09 2006-11-28 Pfizer Italia S.R.L. Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
EP1904503B1 (en) * 2005-07-19 2013-11-06 Nerviano Medical Sciences S.R.L. 1h-thieno[2,3-c]-pyrazole compounds useful as kinase inhibitors
EP1963326A1 (en) * 2005-12-12 2008-09-03 NERVIANO MEDICAL SCIENCES S.r.l. Substituted pyrrolo-pyrazole derivatives active as kinase inhibitors
CA2631853C (en) * 2005-12-12 2015-11-24 Nerviano Medical Sciences S.R.L. Substituted pyrazolo[4,3-c]pyridine derivatives active as kinase inhibitors
ATE478875T1 (de) * 2006-05-31 2010-09-15 Nerviano Medical Sciences Srl 1h-furoä3,2-cü pyrazolverbindungen, die sich als kinaseinhibitoren eignen
ES2367416T3 (es) * 2006-10-11 2011-11-03 Nerviano Medical Sciences S.R.L. Derivados de pirrolo-pirazol sustituidos como inhibidores de quinasas.
BRPI0811065A2 (pt) * 2007-06-08 2014-12-02 Abbott Lab Indazóis 5-heteroaril substituídos como inibidores de quinase

Also Published As

Publication number Publication date
KR20110009706A (ko) 2011-01-28
EP2300436B1 (en) 2018-07-18
ES2689325T3 (es) 2018-11-13
JP2011520838A (ja) 2011-07-21
NZ589956A (en) 2012-11-30
ZA201008911B (en) 2012-02-29
AU2009248060A1 (en) 2009-11-19
IL209234A0 (en) 2011-01-31
CN102026983A (zh) 2011-04-20
CA2724215C (en) 2016-03-29
US20110118278A1 (en) 2011-05-19
UA106353C2 (en) 2014-08-26
EP2300436A1 (en) 2011-03-30
KR101586634B1 (ko) 2016-01-20
MX2010012295A (es) 2010-12-06
US8809337B2 (en) 2014-08-19
IL209234A (en) 2015-01-29
AR071780A1 (es) 2010-07-14
TW201004951A (en) 2010-02-01
SG190636A1 (en) 2013-06-28
CN102026983B (zh) 2014-10-22
EA019901B1 (ru) 2014-07-30
CA2724215A1 (en) 2009-11-19
AU2009248060B2 (en) 2013-11-14
BRPI0911986A2 (pt) 2015-10-13
JP5984387B2 (ja) 2016-09-06
CL2009001158A1 (es) 2009-10-23
WO2009138440A1 (en) 2009-11-19
US20130203770A1 (en) 2013-08-08
HK1151793A1 (en) 2012-02-10

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