PE12462016A1 - Acrylamides pyrrolo [2,3-d] pyrimidinyl, pyrrolo [2,3-b] pyrazinyl and pyrrolo [2,3-d] pyridinyl - Google Patents

Acrylamides pyrrolo [2,3-d] pyrimidinyl, pyrrolo [2,3-b] pyrazinyl and pyrrolo [2,3-d] pyridinyl

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Publication number
PE12462016A1
PE12462016A1 PE2016000723A PE0007232016A PE12462016A1 PE 12462016 A1 PE12462016 A1 PE 12462016A1 PE 2016000723 A PE2016000723 A PE 2016000723A PE 0007232016 A PE0007232016 A PE 0007232016A PE 12462016 A1 PE12462016 A1 PE 12462016A1
Authority
PE
Peru
Prior art keywords
pyrrolo
c1
c6
deuterium
compounds
Prior art date
Application number
PE2016000723A
Other languages
Spanish (es)
Inventor
Matthew Frank Brown
Agustin Casimiro-Garcia
Ye Che
Jotham Wadsworth Coe
Mark Edward Flanagan
Adam Matthew Gilbert
Rayomand Jal Unwalla
Jonathan David Langille
Justin Ian Montgomery
Jean-Baptiste Telliez
Atli Thorarensen
John I Trujillo
Matthew Merrill Hayward
Original Assignee
Pfizer
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
Priority to US201361912074P priority Critical
Application filed by Pfizer filed Critical Pfizer
Publication of PE12462016A1 publication Critical patent/PE12462016A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Abstract

SE REFIERE A COMPUESTOS ACRILAMIDAS DE PIRROLO[2,3-d]PIRIMIDINILO, PIRROLO[2,3-b]PIRAZINILO Y PIRROLO[2,3-d]PIRIDINILO DE FORMULA (I) DONDE R2 ES H, DEUTERIO, ALQUILO C1-C6, ENTRE OTROS; Refers to compounds acrylamides pyrrolo [2,3-d] pyrimidinyl, pyrrolo [2,3-b] pyrazinyl and pyrrolo [2,3-d] pyridinyl of formula (I) wherein R2 is H, deuterium, C1- C6, among others; R3 ES H, DEUTERIO, HALOGENO, ENTRE OTROS; R3 is H, deuterium, halogen, among others; A ES -(CRaRb)q-(CRcRd)-, EN DONDE Ra, Rb, Rc Y Rd SON CADA UNO H, ALQUILO C1-C6, ENTRE OTROS; A is - (CRaRb) q- (CRcRd) -, wherein Ra, Rb, Rc and Rd are each H, C1-C6 alkyl, among others; R0, R1, R4, R5, R6, R7, R8, R9 Y R10 SON CADA UNO H, ALQUILO C1-C6, ARILO C6-C10, ENTRE OTROS; R0, R1, R4, R5, R6, R7, R8, R9 and R10 are each H, C1-C6 alkyl, C6-C10, among others; R11 ES HO DEUTERIO; R11 is H or deuterium; Y ES OUN; AND IS OUN; UNO DE LOS ENLACES PUNTEADOS AZY Z' ES UN ENLACE INDIVIDUAL; ONE OF THE LINKS DOTTED AZY Z 'is a single bond; ZY Z' SON CADA UNO C, NO CR16, EN DONDE R16 ES ALQUILO C1-C4, ARILO C6-C10, ENTRE OTROS; ZY Z 'are each C, NO CR16, wherein R16 is C1-C4 alkyl, C6-C10, among others; X ES O, ENTRE OTROS; X is O, among others; n, p Y q SON DE 0 A 2. SON COMPUESTOS PREFERIDOS: 2-(1-ACRILOILPIPERIDIN-4-ILAMINO)-N-ISOPROPIL-5H-PIRROLO[2,3-b]PIRAZINA-7-CARBOXAMIDA; n, p and q are 0 to 2. Preferred compounds are: 2- (1-ACRILOILPIPERIDIN-4-ylamino) -N-isopropyl-5H-pyrrolo [2,3-b] pyrazine-7-carboxamide; N-ISOPROPIL-2-(3-(N-METILACRILAMIDO)AZETIDIN-1-IL)-5H-PIRROLO[2,3-b]PIRAZINA-7-CARBOXAMIDA; N-Isopropyl-2- (3- (N-methylacrylamido) azetidin-1-yl) -5H-pyrrolo [2,3-b] pyrazine-7-carboxamide; ENTRE OTROS. AMONG OTHERS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ALSO it REFERS TO A PHARMACEUTICAL COMPOSITION. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASA JANUS (JAK) SIENDO UTILES EN EL TRATAMIENTO DE ARTRITIS REUMATOIDE, ENFERMEDAD DE ALZHEIMER Such compounds are inhibitors of Janus kinase (JAK) to be useful in the treatment of rheumatoid arthritis, ALZHEIMER'S DISEASE
PE2016000723A 2013-12-05 2014-11-20 Acrylamides pyrrolo [2,3-d] pyrimidinyl, pyrrolo [2,3-b] pyrazinyl and pyrrolo [2,3-d] pyridinyl PE12462016A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US201361912074P true 2013-12-05 2013-12-05

Publications (1)

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PE12462016A1 true PE12462016A1 (en) 2016-11-25

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PE2016000723A PE12462016A1 (en) 2013-12-05 2014-11-20 Acrylamides pyrrolo [2,3-d] pyrimidinyl, pyrrolo [2,3-b] pyrazinyl and pyrrolo [2,3-d] pyridinyl

Country Status (40)

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US (2) US9617258B2 (en)
EP (2) EP3318565A1 (en)
JP (2) JP6192839B2 (en)
KR (1) KR101930603B1 (en)
CN (2) CN107417684A (en)
AP (1) AP201609269A0 (en)
AR (1) AR099363A1 (en)
AU (1) AU2014358792B2 (en)
CA (1) CA2932425C (en)
CL (1) CL2016001216A1 (en)
CR (1) CR20160250A (en)
CU (1) CU24396B1 (en)
CY (1) CY1119778T1 (en)
DK (1) DK3077395T3 (en)
DO (1) DOP2016000124A (en)
EA (1) EA030472B1 (en)
ES (1) ES2654051T3 (en)
GE (1) GEP20186840B (en)
HR (1) HRP20171846T1 (en)
HU (1) HUE035264T2 (en)
IL (1) IL246038D0 (en)
LT (1) LT3077395T (en)
MA (1) MA39092B1 (en)
MD (1) MD20160058A2 (en)
ME (1) ME02883B (en)
MX (1) MX2016007156A (en)
NO (1) NO3134430T3 (en)
NZ (1) NZ720092A (en)
PE (1) PE12462016A1 (en)
PH (1) PH12016500938A1 (en)
PL (1) PL3077395T3 (en)
PT (1) PT3077395T (en)
RS (1) RS56728B1 (en)
SI (1) SI3077395T1 (en)
SV (1) SV2016005209A (en)
TN (1) TN2016000227A1 (en)
TW (1) TWI548636B (en)
UA (1) UA117040C2 (en)
UY (1) UY35861A (en)
WO (1) WO2015083028A1 (en)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201601980XA (en) 2013-09-18 2016-04-28 Beijing Hanmi Pharmaceutical Co Ltd Compound inhibiting activities of btk and/or jak3 kinases
CN107417684A (en) * 2013-12-05 2017-12-01 辉瑞公司 Heterocyclic acrylamide
CN105777756B (en) * 2014-07-02 2019-03-01 广东东阳光药业有限公司 Heteroaryl compound and its application in drug
SG11201701315VA (en) 2014-08-28 2017-03-30 Asceneuron Sa Glycosidase inhibitors
CN105712998A (en) * 2014-12-05 2016-06-29 上海润诺生物科技有限公司 Azaindole derivatives, preparation method and applications thereof in medicine
JP2018502853A (en) 2015-01-23 2018-02-01 コンフルエンス・ライフ・サイエンシズ,インコーポレーテッド Heterocyclic itk inhibitors to treat inflammation and cancer
CN105837574B (en) * 2015-02-02 2018-03-02 四川大学 N- (3- piperidinyl) - and aromatic amine derivatives, preparation and use
WO2016178110A1 (en) * 2015-05-01 2016-11-10 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, pyrrolo[2,3-b]pyridinyl acrylamides and epoxides thereof
CN107531711A (en) * 2015-05-29 2018-01-02 无锡福祈制药有限公司 Janus kinase inhibitor
CN106432246A (en) * 2015-08-05 2017-02-22 广东东阳光药业有限公司 Heteroaromatic compound and application thereof to drug
KR101771219B1 (en) * 2015-08-21 2017-09-05 양지화학 주식회사 Janus kinase 1 selective inhibitors and their pharmaceutical use
AU2016350816A1 (en) 2015-11-03 2018-05-17 Theravance Biopharma R&D Ip, Llc JAK kinase inhibitor compounds for treatment of respiratory disease
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
SG11201811470PA (en) * 2016-06-30 2019-01-30 Daewoong Pharmaceutical Co Ltd Pyrazolopyrimidine derivatives as kinase inhibitor
WO2018095345A1 (en) * 2016-11-23 2018-05-31 无锡福祈制药有限公司 Crystal form and salt form of 7h-pyrrolo[2,3-d]pyrimidine compound and preparation method therefor
WO2018134352A1 (en) 2017-01-20 2018-07-26 Leo Pharma A/S Bicyclic amines as novel jak kinase inhibitors
AU2018223192A1 (en) 2017-02-27 2019-06-20 Janssen Pharmaceutica Nv [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as OGA inhibitors
US10196393B2 (en) 2017-03-09 2019-02-05 Theravance Biopharma R&D Ip, Llc JAK inhibitors containing a 4-membered heterocyclic amide
WO2018204236A1 (en) 2017-05-01 2018-11-08 Theravance Biopharma R&D Ip, Llc Crystalline forms of a jak inhibitor compound
CN107857778A (en) * 2017-11-21 2018-03-30 江苏乐斯化学有限公司 Preparation method of alpha-amino-nitrile containing phosphonyl

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR200003719T2 (en) 1998-06-19 2001-03-21 Pfizer Products Inc. Pyrrolo [2,3-d] pyrimidine compounds
PA8474101A1 (en) 1998-06-19 2000-09-29 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine
TR200400105T4 (en) 1999-12-10 2004-02-23 Prizer Products Inc. Pyrrolo [2,3-d] pyrimidine compounds
OA12292A (en) 2000-06-26 2003-11-11 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents.
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
RS20050380A (en) 2002-11-21 2007-11-15 Pfizer Products Inc., 3-amino piperidine derivatives and methods of manufacture
AR054416A1 (en) 2004-12-22 2007-06-27 Incyte Corp Pyrrolo [2,3-b] pyridin-4-yl-amines and pyrrolo [2,3-b] pyrimidin-4-yl-amines as inhibitors of janus kinases. pharmaceutical compositions.
US8232394B2 (en) 2005-07-29 2012-07-31 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
PL2530083T3 (en) 2006-09-22 2016-11-30 Inhibitors of bruton's tyrosine kinase
WO2010016005A1 (en) 2008-08-06 2010-02-11 Pfizer Inc. 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors
US20100185419A1 (en) 2008-09-05 2010-07-22 Avila Therapeutics, Inc. Algorithm for designing irreversible inhibitors
CN102232076B (en) 2008-12-05 2014-12-31 霍夫曼-拉罗奇有限公司 Pyrrolopyrazinyl urea kinase inhibitors
KR101705158B1 (en) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr inhibitors and methods of treating diseases
EP2448473A4 (en) 2009-06-30 2014-06-25 Edwards Lifesciences Corp Systems and methods for monitoring and displaying a patient's status
TW201105674A (en) * 2009-07-08 2011-02-16 Leo Pharma As Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof
EP3461824A1 (en) 2009-09-04 2019-04-03 Biogen MA Inc. Bruton's tyrosine kinase inhibitors
JP5967827B2 (en) * 2009-12-09 2016-08-10 アジオス ファーマシューティカルズ, インコーポレイテッド Therapeutically active compounds for treating cancer characterized by having a Idh mutant
UY33213A (en) 2010-02-18 2011-09-30 Almirall Sa Pyrazole derivatives as inhibitors of Jak
CA2799904A1 (en) * 2010-05-20 2011-11-24 F. Hoffmann-La Roche Ag Pyrrolo [2, 3 - b] pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
JP2013533868A (en) * 2010-07-09 2013-08-29 レオ ファーマ アクティーゼルスカブ New homopiperazine derivatives and use thereof a medicament as protein tyrosine kinase inhibitors
EP2629777B1 (en) * 2010-10-22 2018-12-19 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
EP2788000B1 (en) * 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
WO2013091539A1 (en) 2011-12-21 2013-06-27 江苏恒瑞医药股份有限公司 Pyrrole six-membered heteroaryl ring derivative, preparation method therefor, and medicinal uses thereof
JP6318156B2 (en) * 2012-09-06 2018-04-25 プレキシコン インコーポレーテッドPlexxikon Inc. Compounds and methods for modulating kinases, and indicators that
AU2013348116A1 (en) 2012-11-20 2015-06-11 Principia Biopharma Inc. Azaindole derivatives as JAK3 inhibitors
CN103896946B (en) * 2012-12-28 2018-04-03 浙江导明医药科技有限公司 The new compounds for the prevention and treatment of various autoimmune diseases
CN107417684A (en) * 2013-12-05 2017-12-01 辉瑞公司 Heterocyclic acrylamide

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PH12016500938A1 (en) 2016-06-27
EP3077395B1 (en) 2017-11-15
CR20160250A (en) 2016-09-19
EA201600373A1 (en) 2016-10-31
TN2016000227A1 (en) 2017-10-06
SI3077395T1 (en) 2018-03-30
AP201609269A0 (en) 2016-06-30
CY1119778T1 (en) 2018-06-27
PL3077395T3 (en) 2018-04-30
KR20160092012A (en) 2016-08-03
EP3077395A1 (en) 2016-10-12
CA2932425A1 (en) 2015-06-11
KR101930603B1 (en) 2018-12-18
DOP2016000124A (en) 2016-10-31
CN106061973A (en) 2016-10-26
JP2016539137A (en) 2016-12-15
UY35861A (en) 2015-07-31
CU24396B1 (en) 2019-04-04
GEP20186840B (en) 2018-04-10
US20150158864A1 (en) 2015-06-11
AU2014358792A1 (en) 2016-06-02
MX2016007156A (en) 2016-07-21
TW201524977A (en) 2015-07-01
MD20160058A2 (en) 2016-11-30
AU2014358792B2 (en) 2017-06-08
MA39092B1 (en) 2018-09-28
IL246038D0 (en) 2016-08-02
CA2932425C (en) 2018-07-17
PT3077395T (en) 2018-01-03
TWI548636B (en) 2016-09-11
JP6192839B2 (en) 2017-09-06
LT3077395T (en) 2018-02-12
SV2016005209A (en) 2018-04-11
MA39092A1 (en) 2018-06-29
NZ720092A (en) 2019-05-31
JP2018008996A (en) 2018-01-18
EA030472B1 (en) 2018-08-31
WO2015083028A1 (en) 2015-06-11
RS56728B1 (en) 2018-03-30
DK3077395T3 (en) 2018-01-02
NO3134430T3 (en) 2018-08-18
US9617258B2 (en) 2017-04-11
EP3318565A1 (en) 2018-05-09
CN106061973B (en) 2019-07-09
UA117040C2 (en) 2018-06-11
HUE035264T2 (en) 2018-05-02
CL2016001216A1 (en) 2017-01-20
CU20160077A7 (en) 2017-01-10
ES2654051T3 (en) 2018-02-12
US20170247372A1 (en) 2017-08-31
HRP20171846T1 (en) 2018-01-12
PH12016500938B1 (en) 2016-06-27
CN107417684A (en) 2017-12-01
AR099363A1 (en) 2016-07-20
ME02883B (en) 2018-04-20

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