EA201692139A1 - Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы - Google Patents

Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы

Info

Publication number
EA201692139A1
EA201692139A1 EA201692139A EA201692139A EA201692139A1 EA 201692139 A1 EA201692139 A1 EA 201692139A1 EA 201692139 A EA201692139 A EA 201692139A EA 201692139 A EA201692139 A EA 201692139A EA 201692139 A1 EA201692139 A1 EA 201692139A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
pirazine
phosphatidylinositol
derivatives
kinase
Prior art date
Application number
EA201692139A
Other languages
English (en)
Other versions
EA033571B1 (ru
Inventor
Бенджамин Ричард Беллини
Ян БРЮС
Эндрю Джеймс КАЛШО
Грегори Холлингворт
Джеймс Ниф
Мэттью Спендифф
Саймон Джеймс Уотсон
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 EA201692139A1 publication Critical patent/EA201692139A1/ru
Publication of EA033571B1 publication Critical patent/EA033571B1/ru

Links

Classifications

    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond

Abstract

Изобретение относится к соединению формулы (I)которое ингибирует активность гамма-изоформы PI 3-киназы, что эффективно для лечения заболевания, опосредованного активацией гамма-изоформы PI 3-киназы.
EA201692139A 2014-04-24 2014-04-24 Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы EA033571B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IB2014/060991 WO2015162461A1 (en) 2014-04-24 2014-04-24 Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201692139A1 true EA201692139A1 (ru) 2017-02-28
EA033571B1 EA033571B1 (ru) 2019-11-06

Family

ID=50819761

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201692139A EA033571B1 (ru) 2014-04-24 2014-04-24 Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы

Country Status (14)

Country Link
US (1) US9862711B2 (ru)
EP (1) EP3134395B1 (ru)
JP (1) JP6404944B2 (ru)
KR (1) KR20160141856A (ru)
CN (1) CN106458966B (ru)
AU (1) AU2014391610B2 (ru)
BR (1) BR112016023967A2 (ru)
CA (1) CA2945257A1 (ru)
EA (1) EA033571B1 (ru)
ES (1) ES2667424T3 (ru)
MX (1) MX2016013983A (ru)
PL (1) PL3134395T3 (ru)
PT (1) PT3134395T (ru)
WO (1) WO2015162461A1 (ru)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2014391605A1 (en) 2014-04-24 2016-10-27 Novartis Ag Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors
MX2016013812A (es) 2014-04-24 2017-03-09 Novartis Ag Derivados de amino-pirazina como inhibidores de fosfatidil-inositol-3-cinasa.
AU2017229445B2 (en) 2016-03-10 2019-07-11 Astrazeneca Ab Novel inhibitors of phosphatidylinositol 3-kinase gamma
WO2019119207A1 (en) 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
MA54133B1 (fr) 2018-03-08 2022-01-31 Incyte Corp Composés d'aminopyrazine diol utilisés comme inhibiteurs de pi3k-y

Family Cites Families (140)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
IT1016489B (it) 1974-03-18 1977-05-30 Isf Spa Inalatore
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
JPH0525045A (ja) 1991-07-18 1993-02-02 Tanabe Seiyaku Co Ltd 経皮吸収製剤
WO1993018007A1 (en) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Novel carbostyril derivative
US5605923A (en) 1992-04-02 1997-02-25 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
MX9301943A (es) 1992-04-02 1994-08-31 Smithkline Beecham Corp Compuestos.
WO1993019750A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic or inflammatory diseases
US6596260B1 (en) 1993-08-27 2003-07-22 Novartis Corporation Aerosol container and a method for storage and administration of a predetermined amount of a pharmaceutically active aerosol
DK0995457T3 (da) 1995-12-07 2004-08-16 Jago Res Ag Mundstykke til inhalator til flere dosisvise afgivelser af farmakologisk törpulver
PL185384B1 (pl) 1996-02-21 2003-04-30 Schering Corp Inhalator proszku
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
WO1999016766A1 (fr) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Derives de benzodioxole
US6362371B1 (en) 1998-06-08 2002-03-26 Advanced Medicine, Inc. β2- adrenergic receptor agonists
BR9815931A (pt) 1998-06-30 2001-02-20 Dow Chemical Co Polióis poliméricos, um processo para sua produção, e espuma de poliuretanoobtida
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
DE19834047A1 (de) 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
CA2371587C (en) 1999-05-04 2005-09-13 Schering Corporation Piperidine derivatives useful as ccr5 antagonists
CA2371583C (en) 1999-05-04 2005-09-13 Schering Corporation Piperazine derivatives useful as ccr5 antagonists
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
SI1212089T1 (sl) 1999-08-21 2006-08-31 Altana Pharma Ag Sinergisticna kombinacija roflumilasta in salmeterola
DE19943639A1 (de) 1999-09-13 2001-03-15 Bayer Ag Dicarbonsäurederivate mit neuartigen pharmazeutischen Eigenschaften
DE19943636A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE19943634A1 (de) 1999-09-13 2001-04-12 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE19943635A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
WO2001083462A1 (de) 2000-04-27 2001-11-08 Boehringer Ingelheim Pharma Kg Neue, langwirksame betamimetika, verfahren zu deren herstellung und deren verwendung als arzneimittel
KR100751981B1 (ko) 2000-06-27 2007-08-28 라보라토리오스 살바트, 에스.에이. 아릴알킬아민으로부터 유도된 카바메이트
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
NZ523958A (en) 2000-08-05 2004-11-26 Glaxo Group Ltd 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derviative as anti-inflammatory agents
KR20080014934A (ko) 2000-11-07 2008-02-14 노파르티스 아게 단백질 키나제 ｃ 억제제로서의 인돌릴말레이미드 유도체
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
AR031176A1 (es) 2000-11-22 2003-09-10 Bayer Ag Nuevos derivados de pirazolpiridina sustituidos con piridina
JP4445704B2 (ja) 2000-12-22 2010-04-07 アルミラル・ソシエダッド・アノニマ キヌクリジンカルバメート誘導体およびｍ３アンダゴニストとしてのそれらの使用
UA75626C2 (en) 2000-12-28 2006-05-15 Almirall Prodesfarma Ag Quinuclidine derivatives and medicinal compositions containing the same
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
WO2002070490A1 (en) 2001-03-08 2002-09-12 Glaxo Group Limited Agonists of beta-adrenoceptors
EP1370521B1 (en) 2001-03-22 2007-12-19 Glaxo Group Limited Formanilide derivatives as beta2-adrenoreceptor agonists
WO2002088167A1 (en) 2001-04-30 2002-11-07 Glaxo Group Limited Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha
DE60227254D1 (de) 2001-06-12 2008-08-07 Glaxo Group Ltd Neue anti inflammatorische 17.alpha.-heterozyklische ester von 17.beta.-carbothioat androstan derivativen
EP2327765B1 (en) 2001-06-21 2015-04-01 BASF Enzymes LLC Nitrilases
SI1425001T1 (sl) 2001-09-14 2009-04-30 Glaxo Group Ltd Glaxo Welcome Fenetanolaminski derivati za zdravljenje respiratornih bolezni
CA2462980A1 (en) 2001-10-17 2003-04-24 Ucb, S.A. Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
KR100944580B1 (ko) 2001-12-20 2010-02-25 치에시 파마슈티시 에스.피.아. 1-알킬-1-아조니아비시클로[2.2.2]옥탄 카르바메이트유도체 및 이의 무스카린 수용체 길항제로서의 용도
WO2003072592A1 (en) 2002-01-15 2003-09-04 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
WO2003062259A2 (en) 2002-01-21 2003-07-31 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
ATE486600T1 (de) 2002-03-12 2010-11-15 Merck Sharp & Dohme Di-aryl-substituierte tetrazol-modulatoren des metabotropen glutamat-rezeptors-5
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ATE381333T1 (de) 2002-03-26 2008-01-15 Boehringer Ingelheim Pharma Glucocorticoid-mimetika, deren herstellung, pharmazeutische zusammensetzungen und verwendung
TWI324064B (en) 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
CA2481320A1 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
DE60318193T2 (de) 2002-04-25 2008-12-04 Glaxo Group Ltd., Greenford Phenethanolaminderivate
WO2003093297A2 (en) 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
US6747043B2 (en) 2002-05-28 2004-06-08 Theravance, Inc. Alkoxy aryl β2 adrenergic receptor agonists
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
EP1517895B1 (en) 2002-06-25 2007-03-14 Merck Frosst Canada Ltd. 8-(biaryl) quinoline pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
EP1521733B1 (en) 2002-07-08 2014-08-20 Pfizer Products Inc. Modulators of the glucocorticoid receptor
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
AR040962A1 (es) 2002-08-09 2005-04-27 Novartis Ag Compuestos derivados de tiazol 1,3-2-ona, composicion farmaceutica y proceso de preparacion del compuesto
PL373146A1 (en) 2002-08-10 2005-08-22 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
WO2004018457A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyrrolidinedione substituted piperidine-phthalazones as pde4 inhibitors
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
PL373597A1 (en) 2002-08-10 2005-09-05 Altana Pharma Ag Piperidine-n-oxide-derivatives
RS20050116A (en) 2002-08-17 2007-11-15 Altana Pharma Ag., Novel phenanthridines
EP1581533A2 (en) 2002-08-17 2005-10-05 ALTANA Pharma AG Novel benzonaphthyridines
WO2004018429A2 (en) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
JP2006501236A (ja) 2002-08-23 2006-01-12 ランバクシー ラボラトリーズ リミテッド ムスカリン性レセプター拮抗薬としてのフルオロおよびスルホニルアミノ含有３，６−二置換アザビシクロ（３．１．０）ヘキサン誘導体
ES2349164T3 (es) 2002-08-29 2010-12-28 Boehringer Ingelheim Pharmaceuticals Inc. Derivados de 3-(sulfonamidoetil)-indol para uso como compuestos miméticos de glucocorticoides en el tratamiento de enfermedades inflamatorias, alérgicas y proliferativas.
AU2003273805B8 (en) 2002-08-29 2010-06-17 Takeda Gmbh 3-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors
JP4587294B2 (ja) 2002-08-29 2010-11-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｄｅ４インヒビターとしての２−ヒドロキシ−６−フェニルフェナントリジン
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
KR20050057408A (ko) 2002-09-18 2005-06-16 오노 야꾸힝 고교 가부시키가이샤 트리아자스피로[5.5]운데칸 유도체 및 이를 유효 성분으로하는 약제
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規６−置換ウラシル誘導体及びアレルギー性疾患の治療剤
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規１−置換ウラシル誘導体及びアレルギー性疾患の治療剤
JP4520309B2 (ja) 2002-09-20 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−２−Ｈ−ナフト［１，２−ｆ］インドール−４−カルボキサミド誘導体
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
AP2005003283A0 (en) 2002-10-11 2005-06-30 Pfizer Indole derivatives useful for the treatment os diseases
WO2004037807A2 (en) 2002-10-22 2004-05-06 Glaxo Group Limited Medicinal arylethanolamine compounds
KR20050065624A (ko) 2002-10-23 2005-06-29 그렌마크 파머수티칼스 엘티디. 염증성 및 알레르기 질환의 치료에 유용한 신규한트리사이클릭 화합물, 이의 제조 방법 및 이를 함유하는약제 조성물
CA2503588A1 (en) 2002-10-28 2004-05-06 Glaxo Group Limited Phenethanolamine derivative for the treatment of respiratory diseases
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225287D0 (en) 2002-10-30 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
CA2506432A1 (en) 2002-12-09 2004-06-24 Robert A. Kirken Methods for selectively inhibiting janus tyrosine kinase 3 (jak3)
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
US7732432B2 (en) 2003-01-21 2010-06-08 Merck Sharp & Dohme Corp. 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
WO2004108765A2 (en) 2003-06-10 2004-12-16 Ace Biosciences A/S Extracellular aspergillus polypeptides
GB2407042B (en) 2003-10-17 2007-10-24 Vectura Ltd Inhaler
GB2424882B (en) 2004-01-12 2008-08-06 Cytopia Res Pty Ltd Selective kinase inhibitors
GB0410712D0 (en) 2004-05-13 2004-06-16 Novartis Ag Organic compounds
CN101056633A (zh) 2004-10-12 2007-10-17 应用研究系统Ars股份公司 用于贫血治疗的PI3激酶γ抑制剂
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
KR20090007347A (ko) 2006-03-22 2009-01-16 버텍스 파마슈티칼스 인코포레이티드 증식성 장애의 치료를 위한 ｃ-ＭＥＴ 단백질 키나제 억제제
WO2007110337A1 (en) 2006-03-29 2007-10-04 F. Hoffmann-La Roche Ag Pyridine and pyrimidine derivatives as mglur2 antagonists
WO2008006583A1 (en) 2006-07-14 2008-01-17 Novartis Ag Pyrimidine derivatives as alk-5 inhibitors
EP1900727A1 (en) 2006-08-30 2008-03-19 Cellzome Ag Aminopyridine derivatives as kinase inhibitors
GB0713259D0 (en) * 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
CN101765591B (zh) * 2007-07-26 2013-11-27 诺华股份有限公司 用于治疗炎性或过敏性病症的嘧啶衍生物
AU2008315746A1 (en) 2007-10-25 2009-04-30 Astrazeneca Ab Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
US8343966B2 (en) 2008-01-11 2013-01-01 Novartis Ag Organic compounds
US8268834B2 (en) * 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
CN106496210B (zh) 2008-12-19 2020-06-09 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
ES2551875T3 (es) 2010-01-18 2015-11-24 Mmv Medicines For Malaria Venture Agentes nuevos contra la malaria
PL2593452T3 (pl) 2010-07-14 2017-07-31 Novartis Ag Związki heterocykliczne będące agonistami receptora IP
DE102010033690A1 (de) 2010-08-06 2012-02-09 Saltigo Gmbh Verfahren zur Herstellung vom Aminoarylalkylverbindungen
AU2014391605A1 (en) 2014-04-24 2016-10-27 Novartis Ag Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors
MX2016013812A (es) 2014-04-24 2017-03-09 Novartis Ag Derivados de amino-pirazina como inhibidores de fosfatidil-inositol-3-cinasa.

Also Published As

Publication number Publication date
MX2016013983A (es) 2017-04-06
EP3134395A1 (en) 2017-03-01
PL3134395T3 (pl) 2018-07-31
CN106458966A (zh) 2017-02-22
US9862711B2 (en) 2018-01-09
BR112016023967A2 (pt) 2017-08-15
AU2014391610A1 (en) 2016-10-27
KR20160141856A (ko) 2016-12-09
JP2017515807A (ja) 2017-06-15
US20170029414A1 (en) 2017-02-02
PT3134395T (pt) 2018-04-16
CA2945257A1 (en) 2015-10-29
EA033571B1 (ru) 2019-11-06
AU2014391610B2 (en) 2018-01-25
JP6404944B2 (ja) 2018-10-17
ES2667424T3 (es) 2018-05-10
EP3134395B1 (en) 2018-01-31
WO2015162461A1 (en) 2015-10-29
CN106458966B (zh) 2019-05-07

Similar Documents

Publication Publication Date Title
EA201692143A1 (ru) Производные аминопиразина в качестве ингибиторов фосфатидилинозитол-3-киназы
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
PH12018500041A1 (en) Substituted aza compoounds as irak-4 inhibitors
BR112018069612A2 (pt) compostos de pirroltriazina como inibidores de tam
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
EA201691625A1 (ru) Ароматические гетероциклические соединения как противовоспалительные соединения
EA201890307A1 (ru) Индазольные и азаиндазольные соединения как ингибиторы irak-4
CL2016001790A1 (es) Compuestos derivados y composiciones de n-azaspirocicloalcano n-heteroaril sustituido para inhibir la actividad de shp2.
BR112017019286A2 (pt) composto de fórmula (i) ou um sal farmaceuticamente aceitável deste
UY35617A (es) Inhibidores de la fosfatidilinositol 3-quinasa
NZ726608A (en) Phosphatidylinositol 3-kinase inhibitors
UY35951A (es) HETEROARILOS y USOS DE ESTOS
EA201790266A1 (ru) Индолы для применения при инфекции, вызванной вирусом гриппа
TR201906366T4 (tr) Polisiklik-karbamoilpiridon bileşiklerinin sentezi.
EA201790112A1 (ru) Гетероциклические соединения и их применение в качестве ингибиторов орфанного рецептора гамма-t, родственного рецепторам ретиноидов (ror)
CY1123033T1 (el) Σπειροκυκλικοι αναστολεις της καθεψινης c
NZ726360A (en) Phosphatidylinositol 3-kinase inhibitors
EA201792021A1 (ru) Ингибитор jak
NZ726638A (en) Phosphatidylinositol 3-kinase inhibitors
PH12016501462A1 (en) Neprilysin inhibitors
EA201891278A1 (ru) Гетероциклические индолы для применения при инфекции, вызванной вирусом гриппа
DOP2016000312A (es) Compuestos derivados de 1-(ciclopent-2-en-1-il)-3-(2-hidroxi-3-(arilsulfonil)fenil)urea como inhibidores cxcr2
CL2017000484A1 (es) Compuestos de azetidiniloxifenilpirrolidina
EA201692139A1 (ru) Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы
EA201692140A1 (ru) Производные аминопиридина в качестве ингибиторов фосфатидилинозитол 3-киназы

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU