[go: up one dir, main page]

PE20091687A1 - Derivados de piridina o pirazina como inhibidores de cinasa-pi-3 - Google Patents

Derivados de piridina o pirazina como inhibidores de cinasa-pi-3

Info

Publication number
PE20091687A1
PE20091687A1 PE2009000404A PE2009000404A PE20091687A1 PE 20091687 A1 PE20091687 A1 PE 20091687A1 PE 2009000404 A PE2009000404 A PE 2009000404A PE 2009000404 A PE2009000404 A PE 2009000404A PE 20091687 A1 PE20091687 A1 PE 20091687A1
Authority
PE
Peru
Prior art keywords
pyridin
amino
kinase
alkyl
pirazine
Prior art date
Application number
PE2009000404A
Other languages
English (en)
Inventor
Ian Bruce
Lee Edwards
Catherine Howsham
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39512639&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20091687(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20091687A1 publication Critical patent/PE20091687A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

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

Abstract

REFERIDA A UN DERIVADO DE PIRIDINA O PIRAZINA DE FORMULA (I), DONDE R1 Y R2 SON H, ALQUILO C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS; Y ES H, -O-ALQUILO C1-C6, -O-CICLOALQUILO C3-C8, ENTRE OTROS; A ES N O CR5; R5 ES H, ALQUILO C1-C6, HALOALQUILO C1-C6, ENTRE OTROS; Ar' ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS CON OH, HALOGENO, CIANO, NITRO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [3-AMINO-6-(6-AMINO-5-TRIFLUORO-METIL-PIRIDIN-3-IL)-PIRAZIN-2-IL]-PIRIDINIL-3-IL-METANONA, {3-AMINO-6-[2-METIL-5-(MORFOLIN-4-SULFONIL)-FENIL]-PIRAZIN-2-IL}-PIRIDIN-3-IL-METANONA, N-{5-[5-AMINO-6-(PIRIDIN-3-CARBONIL)-PIRAZIN-2-IL]-2-CLORO-PIRIDIN-3-IL}-BENCEN-SULFONAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS ENZIMAS CINASA DE FOSFATIDIL-INOSITOL 3 (CINASA-PI 3) Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS U OBSTRUCTIVAS DE LAS VIAS RESPIRATORIAS, ENTRE OTRAS
PE2009000404A 2008-03-19 2009-03-18 Derivados de piridina o pirazina como inhibidores de cinasa-pi-3 PE20091687A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08153045 2008-03-19

Publications (1)

Publication Number Publication Date
PE20091687A1 true PE20091687A1 (es) 2009-11-27

Family

ID=39512639

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000404A PE20091687A1 (es) 2008-03-19 2009-03-18 Derivados de piridina o pirazina como inhibidores de cinasa-pi-3

Country Status (23)

Country Link
US (2) US8268834B2 (es)
EP (2) EP2257529B1 (es)
JP (1) JP2011515362A (es)
KR (1) KR101284517B1 (es)
CN (1) CN102036961B (es)
AR (1) AR070923A1 (es)
AU (1) AU2009226958B2 (es)
BR (1) BRPI0909417A2 (es)
CA (1) CA2718526A1 (es)
CL (1) CL2009000650A1 (es)
CO (1) CO6300942A2 (es)
CR (1) CR11683A (es)
EA (1) EA018065B1 (es)
EC (1) ECSP10010556A (es)
ES (1) ES2455721T3 (es)
IL (1) IL208107A0 (es)
MA (1) MA32231B1 (es)
MX (1) MX2010010155A (es)
NZ (1) NZ587926A (es)
PE (1) PE20091687A1 (es)
TW (1) TW200948800A (es)
WO (1) WO2009115517A2 (es)
ZA (1) ZA201006506B (es)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8263585B2 (en) * 2007-05-04 2012-09-11 Novartis Ag Organic compounds
PE20091628A1 (es) 2008-03-19 2009-11-19 Novartis Ag Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
MX315904B (es) 2008-05-30 2013-11-29 Amgen Inc Inhibidores de fosfoinosituro-3 cinasa.
AU2009327357C1 (en) 2008-12-19 2017-02-02 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of ATR kinase
US8729074B2 (en) 2009-03-20 2014-05-20 Amgen Inc. Inhibitors of PI3 kinase
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
EP2493878B1 (en) * 2009-10-30 2016-10-12 Janssen Pharmaceutica NV Pyrazines as delta opioid receptor modulators
RS56432B1 (sr) 2009-11-05 2018-01-31 Rhizen Pharmaceuticals S A Novi benzopiran modulatori kinaze
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
KR20130066633A (ko) 2010-05-12 2013-06-20 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
JP2013529200A (ja) * 2010-05-12 2013-07-18 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
CN102718745A (zh) * 2011-03-30 2012-10-10 中国科学院上海药物研究所 新型胺基吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
KR101992311B1 (ko) 2011-05-04 2019-09-27 리젠 파마슈티컬스 소시에떼 아노님 단백질 키나아제의 조절제로서 신규한 화합물
CN103957917A (zh) 2011-09-30 2014-07-30 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CA3124539A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Process for making 4-[chloro-n-hydroxycarbonimidoyl]phenyl derivative
BR112014020773A2 (pt) 2012-02-22 2020-10-27 Sanford-Burnham Medical Research Institute compostos de sulfonamida e seus usos como inibidores tnap
US20140044802A1 (en) 2012-04-05 2014-02-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
SI3459942T1 (sl) 2012-04-24 2021-05-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
AU2013285081B2 (en) 2012-07-04 2017-01-12 Rhizen Pharmaceuticals Sa Selective PI3K delta inhibitors
EP2904406B1 (en) 2012-10-04 2018-03-21 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
ME03336B (me) 2013-03-12 2019-10-20 Vertex Pharma Inhibitori dnk-pk
EP2970196B1 (en) 2013-03-15 2020-11-25 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
GEP201706761B (en) * 2013-03-29 2017-10-25 Takeda Pharmaceuticals Co 6-(5-hydroxy-1h-pyrazol-1-yl) nicotinamide derivatives and their use as phd inhibitors
RU2675270C2 (ru) 2013-10-17 2018-12-18 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы и содержащие их фармацевтические композиции
EA202092627A1 (ru) 2013-11-18 2021-09-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CR20160363A (es) 2014-01-14 2016-10-12 Millennium Pharm Inc Heteroarilos y usos de estos
FI3102208T4 (fi) * 2014-02-07 2024-09-23 Global Blood Therapeutics Inc 2-hydroksi-6-((2-(1-isopropyyli-1h-pyratsol-5-yyli)pyridin-3-yyli)metoksi)bentsaldehydin vapaan emäksen kiteinen polymorfi
CN103804312B (zh) * 2014-02-17 2016-04-20 四川百利药业有限责任公司 一类氮杂环化合物及其制备方法和用途
KR20160141855A (ko) 2014-04-24 2016-12-09 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피라진 유도체
KR20160141856A (ko) 2014-04-24 2016-12-09 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 피라진 유도체
MX2016013981A (es) 2014-04-24 2016-11-15 Novartis Ag Derivados de amino-piridina como inhibidores de fosfatidil-inositol-3-cinasa.
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
WO2018064092A1 (en) 2016-09-27 2018-04-05 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors
GB201715410D0 (en) * 2017-09-22 2017-11-08 Syngenta Participations Ag Improvements in or relating to organic compounds
US11306079B2 (en) 2017-12-21 2022-04-19 Incyte Corporation 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors
IL275522B2 (en) 2017-12-22 2024-02-01 Petra Pharma Corp Amine derivatives of ARYL–BIPYRIDINE as phosphatidylinositol phosphate kinase inhibitors
SMT202200134T1 (it) 2018-03-08 2022-05-12 Incyte Corp Composti di amminopirazindiolo come inibitori di pi3k-y
WO2020010003A1 (en) * 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
KR20220100544A (ko) 2021-01-08 2022-07-15 고려대학교 산학협력단 PI3K/Akt 매개 후기 나트륨 전류 억제를 통한 부정맥 치료용 약학 조성물 및 치료방법

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US30583A (en) * 1860-11-06 Milkibtg-stool
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
BE757702A (fr) 1969-10-20 1971-04-19 Sandoz Sa Derives de la pyrido (2,3-d) pyrimidine, leur preparation et medicaments les contenant.
US4297360A (en) * 1980-03-28 1981-10-27 Sterling Drug Inc. 5-(Pyridinyl)pyridine-2,3-diamines, preparation thereof and their cardiotonic use
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
WO1997043267A1 (en) 1996-05-11 1997-11-20 Kings College London Pyrazines
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
CZ20013940A3 (cs) 1999-05-04 2002-04-17 Schering Corporation Piperazinové deriváty uľitečné jako CCR5 antagonisté
TR200103213T2 (tr) 1999-05-04 2002-03-21 Schering Corporation CCR5 antagonistleri olarak yararlì piperidin trevleri.
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
WO2001046691A1 (en) 1999-12-22 2001-06-28 Biosignal Packard Inc. A bioluminescence resonance energy transfer (bret) system with broad spectral resolution between donor and acceptor emission wavelengths and its use
UA72632C2 (uk) 2000-06-27 2005-03-15 Лабораторіос С.А.Л.В.А.Т., С.А. Карбамати, похідні від арилалкіламінів
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
ES2523930T3 (es) 2000-08-05 2014-12-02 Glaxo Group Limited Éster s-fluorometílico del ácido 6-alfa,9-alfa-difluoro-17-alfa-[(2-furanilcarbonil)oxi]-11-beta-hidroxi-16-alfa-metil-3-oxo-androst-1,4-dien-17-carbotioico como agente antiinflamatorio
NZ525656A (en) 2000-11-07 2004-12-24 Novartis Ag Indolylmaleimide derivatives as protein kinase C inhibitors
KR100869722B1 (ko) 2000-12-22 2008-11-21 알미랄 에이쥐 퀴누클리딘 카르바메이트 유도체 및 ｍ3 길항제로서 그의사용
DK1353919T3 (da) 2000-12-28 2006-11-20 Almirall Prodesfarma Ag Hidtil ukendte quinuclidinderivater og medicinale sammensætninger indeholdende samme
PT1383786E (pt) 2001-04-30 2008-12-30 Glaxo Group Ltd Derivados anti-inflamatórios de éster 17.beta-carbotioato de androstano com um grupo éster ciclíco na posição 17.alfa
US20040248867A1 (en) 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
JP4405258B2 (ja) 2001-06-21 2010-01-27 ヴェレニウム コーポレイション ニトリラーゼ
RU2004110717A (ru) 2001-10-17 2005-10-20 Юсиби, С.А. (Be) Производные хинуклидина, способы их получения и их применение в качестве и нгибиторов м2- и/или м3- мускариновых рецепторов
MY130622A (en) 2001-11-05 2007-07-31 Novartis Ag Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors
UA76571C2 (en) 2001-12-20 2006-08-15 Derivatives of 1-alkyl-1-azoniabicyclo [2.2.2.]octanecarbamate and use thereof as antagonists of muscarin receptor
PE20040079A1 (es) 2002-04-03 2004-04-19 Novartis Ag Derivados de indolilmaleimida
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
WO2003093297A2 (en) 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
MXPA05005477A (es) 2002-11-21 2005-07-25 Chiron Corp Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer.
RU2005121672A (ru) 2002-12-09 2005-11-20 Зе Бод оф Риджентс оф зи Юнивесити оф Тексэс Систим (US) Способ ингибирования в условиях in vitro функции и/или пролиферации клетки, экспрессирующей тирозинкиназу janus 3 (jak3) (варианты), способ тестирования соединений in vitro в качестве перспективных терапевтических иммунодепрессантов и идентификации in vitro нового иммунодепрессивного лекарственного средства (варианты), стериозомер и фармацевтическая композиция на его основе, применение вышеуказанных объектов в качестве средства подавления нежелательной функции клетки у млекопитающего
DK2476667T3 (da) * 2003-02-26 2014-09-15 Sugen Inc Aminoheteroaryl-forbindelser som proteinkinase-inhibitorer
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
WO2005003101A2 (en) 2003-07-02 2005-01-13 Biofocus Discovery Limited Pyrazine and pyridine derivatives as rho kinase inhibitors
DK1704145T3 (da) 2004-01-12 2012-09-24 Ym Biosciences Australia Pty Selektive kinaseinhibitorer
DE102004017934A1 (de) * 2004-04-14 2005-11-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
US7361763B2 (en) 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
SI1784396T1 (sl) 2004-08-26 2011-03-31 Pfizer S pirazolom substituirane aminoheteroarilne spojine kot zaviralci protein-kinaze
BRPI0514687A (pt) 2004-08-26 2008-06-17 Pfizer compostos amino heteroarila como inibidores de proteìna tirosina cinase
MX2007004302A (es) 2004-10-12 2007-06-07 Applied Research Systems Inhibidores de pi3 cinasa gamma para el tratamiento de anemia.
SE0402735D0 (sv) 2004-11-09 2004-11-09 Astrazeneca Ab Novel compounds
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
US20090222270A2 (en) 2006-02-14 2009-09-03 Ivc Inc. Voice command interface device
PL2049502T3 (pl) 2006-07-28 2012-06-29 Novartis Ag 2,4-Podstawione chinazoliny jako inhibitory kinazy lipidowej
KR100932093B1 (ko) 2006-09-27 2009-12-16 주식회사종근당 미세소관 형성 저해제로서 유용한 벤조페논 유도체
GB0621607D0 (en) 2006-10-31 2006-12-06 Chroma Therapeutics Ltd Inhibitors of c-Met
EP2121613A2 (en) 2007-01-31 2009-11-25 Vertex Pharmaceuticals, Inc. 2-aminopyridine derivatives useful as kinase inhibitors
US8263585B2 (en) 2007-05-04 2012-09-11 Novartis Ag Organic compounds
JP5485884B2 (ja) * 2007-07-26 2014-05-07 ノバルティス アーゲー 炎症性またはアレルギー性状態の処置に有用なピリミジン誘導体
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
AU2009227013B2 (en) * 2008-03-21 2013-01-10 Novartis Ag Novel heterocyclic compounds and uses therof

Also Published As

Publication number Publication date
CR11683A (es) 2010-10-29
EP2257529B1 (en) 2014-01-01
KR101284517B1 (ko) 2013-07-23
ZA201006506B (en) 2011-06-29
US8846687B2 (en) 2014-09-30
IL208107A0 (en) 2010-12-30
CO6300942A2 (es) 2011-07-21
US20120214800A1 (en) 2012-08-23
MX2010010155A (es) 2010-11-04
EP2257529A2 (en) 2010-12-08
KR20100133439A (ko) 2010-12-21
JP2011515362A (ja) 2011-05-19
WO2009115517A3 (en) 2010-01-07
AU2009226958A1 (en) 2009-09-24
US20090239847A1 (en) 2009-09-24
EA201001455A1 (ru) 2011-06-30
TW200948800A (en) 2009-12-01
CL2009000650A1 (es) 2010-03-26
WO2009115517A2 (en) 2009-09-24
EA018065B1 (ru) 2013-05-30
AU2009226958B2 (en) 2012-06-14
NZ587926A (en) 2012-08-31
MA32231B1 (fr) 2011-04-01
US8268834B2 (en) 2012-09-18
AR070923A1 (es) 2010-05-12
ES2455721T3 (es) 2014-04-16
CN102036961A (zh) 2011-04-27
AU2009226958A8 (en) 2010-10-14
BRPI0909417A2 (pt) 2015-12-08
EP2597085A1 (en) 2013-05-29
CA2718526A1 (en) 2009-09-24
ECSP10010556A (es) 2010-11-30
CN102036961B (zh) 2014-02-26

Similar Documents

Publication Publication Date Title
PE20091687A1 (es) Derivados de piridina o pirazina como inhibidores de cinasa-pi-3
NO20076450L (no) Heterosykliske forbindelser som nikotinsyrereseptoragonister for behandling av dyslipidemi
NO20091244L (no) Adenosinderivater som A2A reseptoragonister
PE20080315A1 (es) DERIVADOS DE PIRAZOLO-[3,4-d]-PIRIMIDINAS COMO INHIBIDORES DE CINASA PI-3
TW200833675A (en) Nicotinamide derivatives
PE20130650A1 (es) Derivados de tetrahidro-pirido-pirimidina
TW200724541A (en) Imidazoquinolines as lipid kinase inhibitors
NO20091596L (no) Benzoylamino-heterocykliske forbindelser som Glucokinase-(GLK)-activatorer
MX2012002179A (es) Compuestos heterociclicos de oxima.
MY146645A (en) Purine derivatives for use as adenosin a2a receptor agonists
MX2009009492A (es) Compuestos organicos biciclicos adecuados para el tratamiento de condiciones inflamatorias o alergicas.
EA200801996A1 (ru) 2-замещенные производные 4-бензилфталазинонов в качестве гистаминовых h1- и h3-антагонистов
MY155836A (en) Thienopyridone derivatives as amp-activated protein kinase (ampk) activators
ATE537830T1 (de) Nicotinamid derivate und ihre verwendung als therapeutika
NO20085397L (no) Pyridinon- og pyridazinonderivater som inhibitorer av poly(ADP-ribose)polymerase (PARP)
PE20081345A1 (es) Compuestos heterociclicos que contienen nitrogeno como agonistas del receptor nicotinico
AR068115A1 (es) Derivado del acido pirazolcarboxilico metodo de produccion del mismo y fungicida
ATE473221T1 (de) 1-(1-benzylpiperidin-4-yl)benzimidazol-5- carbonsäurederivate zur behandlung von diabetes mellitus
PE20090880A1 (es) Compuestos heterociclicos como inhibidores de fosfatidilinositol 3-cinasa
CY1111327T1 (el) Υποκατεστημενα παραγωγα κυκλοεξυλοξεικου οξεος
TW200637863A (en) Organic compounds
EA201490630A1 (ru) 6-замещенные 3-(хинолин-6-илтио)[1,2,4]триазоло[4,3-a]пиридины в качестве ингибиторов c-met тирозинкиназы
NO20070789L (no) Nikotinreseptoragonister for behandling av betennelsessykdommer
WO2008104473A3 (en) Pyrazolopyriidine derivatives and their use as kinase inhibitors
ATE492534T1 (de) 1h-indol-5-ylpiperazin-1-ylmethanonderivate

Legal Events

Date Code Title Description
FC Refusal