BR112012023752A2 - derivados de pirrolopirazina e seu uso como inibidores de jak e syk - Google Patents

derivados de pirrolopirazina e seu uso como inibidores de jak e syk

Info

Publication number
BR112012023752A2
BR112012023752A2 BR112012023752A BR112012023752A BR112012023752A2 BR 112012023752 A2 BR112012023752 A2 BR 112012023752A2 BR 112012023752 A BR112012023752 A BR 112012023752A BR 112012023752 A BR112012023752 A BR 112012023752A BR 112012023752 A2 BR112012023752 A2 BR 112012023752A2
Authority
BR
Brazil
Prior art keywords
jak
pyrrolopyrazine derivatives
syk inhibitors
syk
derivatives
Prior art date
Application number
BR112012023752A
Other languages
English (en)
Inventor
Soth Michael
Than Hendricks Robert
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112012023752A2 publication Critical patent/BR112012023752A2/pt

Links

Classifications

    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/08—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
    • 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
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • 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

Abstract

derivados de pirrolopirazina e seu uso como inibidores de jak e syk. refere-se a presente invenção ao uso de novos derivados de pirrolopirazina da fórmula i, em que as variáveis q, r ^2^, r ^3^, e y são definidas como descritas neste contexto, que inibem jak e syk e são úteis para o tratamento de doenças autoimunes e inflamatórias.
BR112012023752A 2010-03-22 2011-03-21 derivados de pirrolopirazina e seu uso como inibidores de jak e syk BR112012023752A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31599910P 2010-03-22 2010-03-22
PCT/EP2011/054171 WO2011117160A1 (en) 2010-03-22 2011-03-21 Pyrrolopyrazine derivatives and their use as jak and syk inhibitors

Publications (1)

Publication Number Publication Date
BR112012023752A2 true BR112012023752A2 (pt) 2019-09-24

Family

ID=43983677

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012023752A BR112012023752A2 (pt) 2010-03-22 2011-03-21 derivados de pirrolopirazina e seu uso como inibidores de jak e syk

Country Status (12)

Country Link
US (1) US8481541B2 (pt)
EP (1) EP2550274A1 (pt)
JP (1) JP5667692B2 (pt)
KR (1) KR20130004342A (pt)
CN (1) CN102812029A (pt)
AR (1) AR080699A1 (pt)
BR (1) BR112012023752A2 (pt)
CA (1) CA2786402A1 (pt)
MX (1) MX2012010610A (pt)
RU (1) RU2012142550A (pt)
TW (1) TW201136936A (pt)
WO (1) WO2011117160A1 (pt)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2571881A1 (en) * 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolopyrazine derivatives as syk and jak inhibitors
KR20130083386A (ko) * 2010-05-20 2013-07-22 에프. 호프만-라 로슈 아게 피롤로[2,3-ｂ]피라진-7-카복스아마이드 유도체 및 ＪＡＫ 및 ＳＹＫ 억제제로서의 그의 용도
BR112014004569A2 (pt) * 2011-09-01 2017-06-13 F. Hoffmann-La Roche Ag composto da fórmula i, métodos para tratar condição inflamatória, artrite reumatoide, asma e distúrbio imune, composição farmacêutica e uso do composto
WO2013064445A1 (en) 2011-11-01 2013-05-10 F. Hoffmann-La Roche Ag Imidazopyridazine compounds
CN104159891B (zh) 2012-01-10 2016-09-07 霍夫曼-拉罗奇有限公司 哒嗪酰胺化合物和它们作为syk 抑制剂的用途
US20170100396A1 (en) 2015-10-07 2017-04-13 F. Hoffmann-La Roche Ag Pyrrolopyrazine derivatives for use in the treatment, amelioration or prevention of influenza
US9815850B2 (en) 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods
PL3552017T3 (pl) 2016-12-09 2022-08-08 Denali Therapeutics Inc. Związki użyteczne jako inhibitory RIPK1
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
EP4077316A1 (en) 2019-12-20 2022-10-26 Pfizer Inc. Benzimidazole derivatives
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4306172A1 (en) * 2021-03-09 2024-01-17 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Use of tricyclic heteroaryl-containing compound

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2699568C (en) 1999-12-24 2013-03-12 Aventis Pharma Limited Azaindoles
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
JP2005534618A (ja) 2002-03-28 2005-11-17 エーザイ株式会社 神経変性疾患用の、ｃ−ｊｕｎｎ−末端キナーゼ阻害剤としての７−アザインドール
CA2550361C (en) * 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
US7456289B2 (en) * 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
AR060316A1 (es) 2006-01-17 2008-06-11 Vertex Pharma Azaindoles de utilidad como inhibidores de janus quinasas
CL2007002617A1 (es) * 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
WO2008084861A1 (ja) 2007-01-12 2008-07-17 Astellas Pharma Inc. 縮合ピリジン化合物
BRPI0812014A2 (pt) 2007-05-25 2014-11-18 Elan Pharm Inc Pirazolopirrolidinas como inibidores de gama secretase, composição farmacêutica compreendendo as mesmas e uso dos referidos compostos
EA201070504A1 (ru) * 2007-10-25 2010-12-30 Эйкеоджен, Инк. КАРБАЦЕФЕМ β-ЛАКТАМОВЫЕ АНТИБИОТИКИ
EP2250172B1 (en) * 2008-02-25 2011-08-31 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
BRPI0907928A2 (pt) 2008-02-25 2015-07-28 Hoffmann La Roche Inibidores de pirrolopirazina quinase.
ES2372908T3 (es) 2008-02-25 2012-01-27 F. Hoffmann-La Roche Ag Inhibidores de la pirrolopirazina quinasa.
WO2009106445A1 (en) 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
PT2247592E (pt) 2008-02-25 2011-11-03 Hoffmann La Roche Inibidores de pirrolpirazina-cinase
US8518945B2 (en) * 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors

Also Published As

Publication number Publication date
EP2550274A1 (en) 2013-01-30
CA2786402A1 (en) 2011-09-29
RU2012142550A (ru) 2014-04-27
CN102812029A (zh) 2012-12-05
WO2011117160A1 (en) 2011-09-29
TW201136936A (en) 2011-11-01
AR080699A1 (es) 2012-05-02
MX2012010610A (es) 2012-10-03
KR20130004342A (ko) 2013-01-09
JP2013522337A (ja) 2013-06-13
JP5667692B2 (ja) 2015-02-12
US8481541B2 (en) 2013-07-09
US20110230414A1 (en) 2011-09-22

Similar Documents

Publication Publication Date Title
BR112012023752A2 (pt) derivados de pirrolopirazina e seu uso como inibidores de jak e syk
BR112012024117A2 (pt) inibidores de pirrolopirazina quinase
MX2014002442A (es) Inhibidores de pirrolopirazina cinasa.
BR112013024901A2 (pt) compostos de tiazolopirimidina
ATE517107T1 (de) Pyrrolopyrazinkinaseinhibitoren
ATE522536T1 (de) Pyrrolopyrazin-kinasehemmer
MX343561B (es) Compuestos de imidazolpiridazina.
ECSP17073191A (es) Compuestos heterocíclicos como inhibidores de lsd1
TW200942543A (en) Pyrrolopyrazine kinase inhibitors
CY1121549T1 (el) Ενωσεις 1-αρυλκαρβονυλ-4-oξυ-πιπεριδινης χρησιμες για την αγωγη νευροεκφυλιστικων παθησεων
CY1119345T1 (el) Μακροκυκλικες ενωσεις ως αναστολεις κινασης trk
ATE522534T1 (de) Pyrrolopyrazin-kinasehemmer
MX2010008198A (es) Inhibidores de cinasa de pirrolopirazina.
CR20210079A (es) Sulfamoilarilamidas y su uso como medicamentos para el tratamiento de la hepatitis b
MX352928B (es) Compuestos de piridazina-amida.
DOP2016000144A (es) Moduladores de tetrahidropiridopirazinas de gpr6
UY35257A (es) Picolinamidas macrocíclicas como fungicidas, composiciones y metodos para el control de enfermedades vegetales
CR20120659A (es) Derivados de piperidinona como inhibidores mdm2 para el tratamiento de cáncer
CU20130101A7 (es) Derivados de 1,4-oxazin-3-il-piridin-2-il-acetamida, activos como inhibidores bace-1 o bace-2
UA108101C2 (xx) Похідні n3-заміщених n1-сульфоніл-5-фторпіримідинонів
CO6491116A2 (es) Derivados de 5-fluoropirimidinona
CL2012001821A1 (es) Compuestos derivados de 5-alquinil-pirimidinas, inhibidores de quinasas; composiciones farmaceuticas que los contienen; y su uso para el tratamiento y/o prevencion de cancer, infecciones, enfermedades inflamatorias y autoinmunitarias.
CO7151502A2 (es) Compuestos que inhiben la actividad de catecol o- metiltransferasa
UY33888A (es) Derivados de (1,2,4) triazolo [4,3-a) quinoxalina como inhibidores de fosfodiesterasas
CR20140468A (es) Inhibidores de diacilglicerol aciltransferasa 2

Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2543 DE 01-10-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.