[go: up one dir, main page]

RU2382783C2 - Органические соединения - Google Patents

Органические соединения Download PDF

Info

Publication number
RU2382783C2
RU2382783C2 RU2006109545/04A RU2006109545A RU2382783C2 RU 2382783 C2 RU2382783 C2 RU 2382783C2 RU 2006109545/04 A RU2006109545/04 A RU 2006109545/04A RU 2006109545 A RU2006109545 A RU 2006109545A RU 2382783 C2 RU2382783 C2 RU 2382783C2
Authority
RU
Russia
Prior art keywords
disease
compound
pharmaceutically acceptable
acceptable salt
phosphatidylinositol
Prior art date
Application number
RU2006109545/04A
Other languages
English (en)
Other versions
RU2006109545A (ru
Inventor
Грэм Чарлз БЛУМФИЛД (GB)
Грэм Чарлз Блумфилд
Айан БРУС (GB)
Айан БРУС
Джуди Фокс ХАЙЛЕР (GB)
Джуди Фокс ХАЙЛЕР
Катрин ЛЕБЛАН (GB)
Катрин Леблан
Даррен Марк ЛЕ-ГРАНД (GB)
Даррен Марк ЛЕ-ГРАНД
Клайв МАККАРТИ (CH)
Клайв Маккарти
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of RU2006109545A publication Critical patent/RU2006109545A/ru
Application granted granted Critical
Publication of RU2382783C2 publication Critical patent/RU2382783C2/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к соединению, представляющему собой 1-[2-(2-этил-2H-тетразол-5-ил)этил]-3-[5-(3-фтор-4-метансульфонилфенил)-4-метилтиазол-2-ил]мочевину в свободной форме или в форме фармацевтически приемлемой соли. Изобретение также относится к фармацевтической композиции, обладающей ингибирующим действием в отношении фосфатидилинозит-3-киназы, включающей в качестве активного ингредиента соединение изобретения, к применению соединения для получения фармацевтической композиции, предназначенной для лечения заболевания, опосредованного фосфатидилинозит-3-киназой и его способу получения. 4 н. и 2 з.п. ф-лы, 9 табл.

Description

Текст описания приведен в факсимильном виде.
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091

Claims (6)

1. Соединение, представляющее собой 1-[2-(2-этил-2H-тетразол-5-ил)этил]-3-[5-(3-фтор-4-метансульфонилфенил)-4-метилтиазол-2-ил]мочевину в свободной форме или в форме фармацевтически приемлемой соли.
2. Фармацевтическая композиция, обладающая ингибирующим действием в отношении фосфатидилинозит-3-киназы, включающая в качестве активного ингредиента соединение по п.1 в свободной форме или в форме фармацевтически приемлемой соли, необязательно вместе с фармацевтически приемлемым носителем или разбавителем.
3. Применение соединения по п.1 в свободной форме или в форме фарамцевтически приемлемой соли для получения фармацевтической композиции, предназначенной для лечения заболевания, опосредованного фосфатидилинозит-3-киназой.
4. Применение по п.3, где заболевание, опосредованное фосфатидилинозит-3-киназой, представляет собой респираторное заболевание.
5. Применение по п.4, где респираторное заболевание выбрано из астмы, острой травмы легкого (ALI), респираторного дистресс-синдром взрослых (ARDS), хронического обструктивного легочного заболевания, хронического обструктивного заболевания дыхательных путей или хронического обструктивного заболевания легкого (COPD, COAD или COLD), включая ассоциированный с ними хронический бронхит или отдышку, эмфиземы, а также обострения повышенной реактивности дыхательных путей, являющееся результатом другой лекарственной терапии, острого, арахидового, катарального, крупозного, хронического или гнойного бронхитов, алюминоза, антракоза, асбестоза, халикоза, муковисцидоза, птилоза, сидероза, силикоза, табакоза и биссиноза.
6. Способ получения соединения по п.1, в свободной форме или в форме фармацевтически приемлемой соли, включающий две стадии:
(i) взаимодействие соединения формулы II
Figure 00000092

где Т означает 5- или 6-членное гетероциклическое кольцо, имеющее один или несколько кольцевых гетероатомов, выбранных из группы, состоящей из кислорода, азота и серы,
с соединением формулы III
Figure 00000093

при соответствующих условиях;
(ii) выделение полученного соединения.
RU2006109545/04A 2003-08-28 2004-08-27 Органические соединения RU2382783C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0320197.7A GB0320197D0 (en) 2003-08-28 2003-08-28 Organic compounds
GB0320197.7 2003-08-28

Publications (2)

Publication Number Publication Date
RU2006109545A RU2006109545A (ru) 2007-10-10
RU2382783C2 true RU2382783C2 (ru) 2010-02-27

Family

ID=28686509

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2006109545/04A RU2382783C2 (ru) 2003-08-28 2004-08-27 Органические соединения

Country Status (33)

Country Link
US (3) US7902375B2 (ru)
EP (1) EP1689391B1 (ru)
JP (1) JP4574618B2 (ru)
KR (1) KR100774038B1 (ru)
CN (1) CN1838953B (ru)
AR (1) AR045510A1 (ru)
AT (1) ATE429225T1 (ru)
AU (1) AU2004268050B2 (ru)
BR (1) BRPI0413934A (ru)
CA (1) CA2533175A1 (ru)
CY (1) CY1109227T1 (ru)
DE (1) DE602004020793D1 (ru)
DK (1) DK1689391T3 (ru)
EC (1) ECSP066383A (ru)
ES (1) ES2323000T3 (ru)
GB (1) GB0320197D0 (ru)
HR (1) HRP20090340T1 (ru)
IL (1) IL173035A0 (ru)
IS (1) IS2690B (ru)
MA (1) MA28007A1 (ru)
MX (1) MXPA06002217A (ru)
MY (1) MY135050A (ru)
NO (1) NO20061406L (ru)
NZ (1) NZ545139A (ru)
PE (1) PE20050872A1 (ru)
PL (1) PL1689391T3 (ru)
PT (1) PT1689391E (ru)
RU (1) RU2382783C2 (ru)
SI (1) SI1689391T1 (ru)
TN (1) TNSN06064A1 (ru)
TW (1) TWI347941B (ru)
WO (1) WO2005021519A2 (ru)
ZA (1) ZA200600415B (ru)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
WO2005118543A1 (ja) * 2004-06-03 2005-12-15 Ono Pharmaceutical Co., Ltd. キナーゼ阻害薬およびその用途
WO2006037468A1 (en) * 2004-09-30 2006-04-13 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv reverse transcriptase inhibitors
EP1888546B1 (en) 2005-05-24 2015-07-08 Merck Serono SA Thiazole derivatives and use thereof
EA014350B1 (ru) 2005-05-24 2010-10-29 Мерк Сероно С.А. Производные тиазола и их применение
UA100358C2 (xx) 2005-08-26 2012-12-25 Мерк Сероно Са Похідні піразину та їх застосування
GB0525671D0 (en) * 2005-12-16 2006-01-25 Novartis Ag Organic compounds
EP1991528A2 (en) * 2006-01-18 2008-11-19 Siena Biotech S.p.A. Modulators of alpha7 nicotinic acetylcholine receptors and therapeutic uses thereof
GB0608854D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd P13 kinase inhibitors
GB0608823D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of P13 kinase
GB0610243D0 (en) * 2006-05-23 2006-07-05 Novartis Ag Organic compounds
GB0612630D0 (en) * 2006-06-26 2006-08-02 Novartis Ag Organic compounds
CA2675884C (en) 2007-02-22 2016-04-26 Merck Serono S.A. Quinoxaline compounds and use thereof
EP2572712A3 (en) 2007-06-01 2013-11-20 The Trustees Of Princeton University Treatment of viral infections by modulation of host cell metabolic pathways
CN101939319A (zh) * 2007-12-20 2011-01-05 诺瓦提斯公司 联噻唑衍生物、它们的制备方法以及它们作为药物的用途
EA201000947A1 (ru) * 2007-12-20 2011-02-28 Новартис Аг Производные тиазола, применимые в качестве ингибиторов киназы pi3
UA104147C2 (ru) 2008-09-10 2014-01-10 Новартис Аг Производная пирролидиндикарбоновой кислоты и ее применение в лечении пролиферативных заболеваний
CN101684106B (zh) * 2008-09-22 2013-06-12 北京摩力克科技有限公司 噻唑鎓盐类化合物及其治疗蛋白老化相关疾病的用途
WO2010091996A1 (en) 2009-02-12 2010-08-19 Merck Serono S.A. 2-morpholino-pyrido[3,2-d]pyrimidines
TWI516487B (zh) * 2009-04-30 2016-01-11 葛蘭素集團有限公司 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途
EP2440556A1 (en) * 2009-06-10 2012-04-18 Vertex Pharmaceuticals Incorporated Inhibitors of phosphatidylinositol 3-kinase
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
CA2766853A1 (en) 2009-07-02 2011-01-06 Novartis Ag 2-carboxamide cycloamino ureas useful as pi3k inhibitors
JPWO2011048936A1 (ja) 2009-10-19 2013-03-07 大正製薬株式会社 アミノチアゾール誘導体
ES2607952T3 (es) 2009-11-13 2017-04-04 Merck Serono S.A. Derivados tricíclicos de Pirazol Amina
EP2992878A1 (en) 2010-02-03 2016-03-09 Signal Pharmaceuticals, LLC Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
GB201018124D0 (en) * 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
EP2727920B1 (en) * 2011-07-29 2016-11-02 FUJIFILM Corporation 1,5-naphthyridine derivative or salt thereof
AU2012290056B2 (en) 2011-08-03 2015-03-19 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for LKB1 status
US9926309B2 (en) 2011-10-05 2018-03-27 The Board Of Trustees Of The Leland Stanford Junior University Pi-kinase inhibitors with anti-infective activity
EP2763532B1 (en) 2011-10-05 2018-09-19 The Board of Trustees of the Leland Stanford Junior University Pi-kinase inhibitors with broad spectrum anti-infective activity
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
KR102459285B1 (ko) 2013-04-17 2022-10-27 시그날 파마소티칼 엘엘씨 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법
WO2014172431A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
CA2909579A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
TWI654979B (zh) 2013-04-17 2019-04-01 美商標誌製藥公司 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法
JP6382945B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ，エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
WO2014172432A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
CN113831345A (zh) 2013-05-29 2021-12-24 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
EP3131551A4 (en) 2014-04-16 2017-09-20 Signal Pharmaceuticals, LLC SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
JP6827948B2 (ja) * 2015-03-23 2021-02-10 ザ ユニヴァーシティー オブ メルボルン 呼吸器疾患の治療
CA2987914C (en) * 2015-06-30 2022-09-13 Dana-Farber Cancer Institute, Inc. Inhibitors of egfr and methods of use thereof
US11091472B2 (en) 2016-02-26 2021-08-17 The Regents Of The University Of California PI-kinase inhibitors with anti-infective activity
JOP20190052A1 (ar) * 2016-09-22 2019-03-21 Astrazeneca Ab 5-[2-(بيريدين-2-يلامينو )-3،1 ثيازول-5-يال]-3،2 – ثنائي هيدرو- 1h- إيزوإندول 1--مشتق واحد واستخدامها كمثبطات مزدوجة للدلتا وغاما فوسفاتيديلينوسيتول 3-كيناز
SG11201912403SA (en) 2017-06-22 2020-01-30 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
JP7701051B2 (ja) 2019-03-21 2025-07-01 ザ ボード オブ トラスティス オブ ザ リーランド スタンフォード ジュニア ユニヴァーシティー Ｐｉ４－キナーゼ阻害剤及びその使用方法
IL296139A (en) 2020-03-03 2022-11-01 Pic Therapeutics Inc Eif4e inhibitors and uses thereof
WO2023028238A1 (en) 2021-08-25 2023-03-02 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
AU2022334296A1 (en) 2021-08-25 2024-03-07 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
CN116874442B (zh) * 2023-07-27 2025-10-24 武汉呈瑞生物医药科技有限公司 一种有机化合物及其应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1279531A3 (ru) * 1983-02-14 1986-12-23 Ниппон Сода Компани Лимитед (Фирма) Способ получени производных тиазолинотриазина
EA200100486A1 (ru) * 1998-10-30 2001-12-24 Фармация Энд Апджон С.П.А. Производные 2-уреидотиазола, способ их получения и применение указанных веществ в качестве противоопухолевых средств
WO2001098270A2 (en) * 2000-06-21 2001-12-27 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
WO2002010162A1 (en) * 2000-07-26 2002-02-07 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl] carboxamide inhibitors of cyclin dependent kinases

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0519449A1 (en) * 1991-06-21 1992-12-23 Boehringer Mannheim Italia S.P.A. 2-Amino-4-aryl thiazoles with antiasthmatic and antiinflammatory activities on the respiratory tract
CN1390215A (zh) 1999-09-10 2003-01-08 麦克公司 酪氨酸激酶抑制剂
US6667300B2 (en) * 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
WO2003015778A1 (en) * 2001-08-17 2003-02-27 Merck & Co., Inc. Tyrosine kinase inhibitors
AR038703A1 (es) * 2002-02-28 2005-01-26 Novartis Ag Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1279531A3 (ru) * 1983-02-14 1986-12-23 Ниппон Сода Компани Лимитед (Фирма) Способ получени производных тиазолинотриазина
EA200100486A1 (ru) * 1998-10-30 2001-12-24 Фармация Энд Апджон С.П.А. Производные 2-уреидотиазола, способ их получения и применение указанных веществ в качестве противоопухолевых средств
WO2001098270A2 (en) * 2000-06-21 2001-12-27 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
WO2002010162A1 (en) * 2000-07-26 2002-02-07 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl] carboxamide inhibitors of cyclin dependent kinases

Also Published As

Publication number Publication date
CY1109227T1 (el) 2014-07-02
ECSP066383A (es) 2006-08-30
AR045510A1 (es) 2005-11-02
US20080280871A1 (en) 2008-11-13
JP2007504109A (ja) 2007-03-01
RU2006109545A (ru) 2007-10-10
ZA200600415B (en) 2007-12-27
KR20060060704A (ko) 2006-06-05
US20110124693A1 (en) 2011-05-26
TW200517386A (en) 2005-06-01
MA28007A1 (fr) 2006-07-03
TWI347941B (en) 2011-09-01
MXPA06002217A (es) 2006-04-27
SI1689391T1 (sl) 2009-08-31
DE602004020793D1 (de) 2009-06-04
HK1093688A1 (en) 2007-03-09
IL173035A0 (en) 2006-06-11
PE20050872A1 (es) 2005-11-22
KR100774038B1 (ko) 2007-11-06
EP1689391B1 (en) 2009-04-22
PL1689391T3 (pl) 2009-09-30
BRPI0413934A (pt) 2006-10-24
CA2533175A1 (en) 2005-03-10
ATE429225T1 (de) 2009-05-15
GB0320197D0 (en) 2003-10-01
IS2690B (is) 2010-10-15
NO20061406L (no) 2006-08-25
JP4574618B2 (ja) 2010-11-04
MY135050A (en) 2008-01-31
PT1689391E (pt) 2009-06-19
AU2004268050A1 (en) 2005-03-10
WO2005021519A2 (en) 2005-03-10
US20110124624A1 (en) 2011-05-26
CN1838953B (zh) 2011-02-02
DK1689391T3 (da) 2009-07-27
WO2005021519A3 (en) 2005-05-12
EP1689391A2 (en) 2006-08-16
NZ545139A (en) 2009-11-27
HRP20090340T1 (hr) 2009-07-31
TNSN06064A1 (en) 2007-10-03
IS8372A (is) 2006-03-24
US7902375B2 (en) 2011-03-08
CN1838953A (zh) 2006-09-27
ES2323000T3 (es) 2009-07-03
AU2004268050B2 (en) 2006-11-16

Similar Documents

Publication Publication Date Title
RU2382783C2 (ru) Органические соединения
RU2481346C2 (ru) Ингибиторы фосфатидилинозитол-3-киназы
WO2021207409A2 (en) Small molecule inhibitors of sars-cov-2 viral replication and uses thereof
ES2616036T3 (es) Nuevos ácidos 5-aminotetrahidroquinolin-2-carboxílicos y su uso
EA008939B1 (ru) Производные никотинамида, полезные в качестве ингибиторов pde4
CN113292565B (zh) 核苷类化合物及其制备方法和应用
RU2008129620A (ru) Пиразиноилгуанидиновые соединения, применяемые в лечении воспалительных или аллергических заболеваний
RU2472783C2 (ru) Аминные производные и их применение в бета-2-адренорецептор-опосредованных заболеваниях
RU2011117927A (ru) Карбаматное соединение или его соль
JP2008502614A5 (ru)
RU2430923C2 (ru) Тиазолилдигидрохиназолины
JP2005509642A5 (ru)
RU2006134020A (ru) Конденсированные производные пиразола
BRPI0409227B8 (pt) &#34;composto, composição farmacêutica, uso de um composto e processo para a preparação de um composto de fórmula (i)&#34;
TW200304811A (en) Treatment of chemokine mediated diseases
CA2376305A1 (en) Sulfonamide and sulfamide substituted imidazoquinolines
HRP20041005A2 (en) Quinoline and isoquinoline derivatives, method forthe production thereof and use thereof as anti-inflammatory agents
CA2568608A1 (en) Six membered amino-amide derivatives as angiogenesis inhibitors
CA2418652A1 (en) Novel 3-substituted urea derivatives and medicinal use thereof
TW200307545A (en) Nicotinamide derivatives and a tiotropium salt in combination for the treatment of diseases
KR940703814A (ko) 히스타민 H3 작용제/길항제로서의 이미다졸릴-알킬-피페라진 및 -디아제핀 유도체(Imidazolyl-alkyl-piperazine and-diazepine derivatives as histamine H3 agonists/antagonists)
RU2007130144A (ru) Гетероциклические соединения в качестве антагонистов cccr2b
RU2006130000A (ru) Органические соединения
US20160185748A1 (en) Pyridyl reverse sulfonamides for hbv treatment
JP2024170457A5 (ru)

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20120828