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PE20141281A1 - Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a - Google Patents

Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a

Info

Publication number
PE20141281A1
PE20141281A1 PE2014000114A PE2014000114A PE20141281A1 PE 20141281 A1 PE20141281 A1 PE 20141281A1 PE 2014000114 A PE2014000114 A PE 2014000114A PE 2014000114 A PE2014000114 A PE 2014000114A PE 20141281 A1 PE20141281 A1 PE 20141281A1
Authority
PE
Peru
Prior art keywords
alkyl
tetrahydropyride
pyrimidine
pyridine
dimethylphenyl
Prior art date
Application number
PE2014000114A
Other languages
English (en)
Inventor
Christine Gelin
Alec Flyer
Christopher Michael Adams
Veronique Darsigny
Timothy Brian Hurley
Rajeshri Ganesh Karki
Nan Jiang
Toshio Kawanami
Erik Meredith
Michael H Serrano-Wu
Chang Rao
Catherine Solovay
George Tien-San Lee
Christopher Towler
Denis Har
Lichun Shen
Bin Hu
Xinglong Jiang
Christina Cappaci-Daniel
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=46604083&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20141281(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 PE20141281A1 publication Critical patent/PE20141281A1/es

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE TETRAHIDROPIRIDO-PIRIDINA Y TETRAHIDROPIRIDO-PIRIMIDINA DE FORMULA (I) DONDE X ES N O CH; Z1 ES N O CR1c, EN DONDE R1c ES H, HALOGENO O ALQUILO(C1-C6); Z2 ES N O CR1d, EN DONDE R1d ES H, ALQUILO(C1-C6), ALCOXILO(C1-C6), ENTRE OTROS; R1a ES H, ALQUILO(C1-C6), ALCOXILO(C1-C6), CN, ENTRE OTROS; R1b ES H, AMINO, ALQUILAMINO(C1-C4), ENTRE OTROS; R1e ES H, HALOGENO, CN, ALQUILO(C1-C6), ENTRE OTROS; R2 ES H, ALQUILO(C1-C6); CICLOALQUILO(C3-C7), ENTRE OTROS; R3 ES FENILO, HETEROARILO O FENILALQUILO(C1-C3); R4 ES H O ALQUILO(C1-C4); R5 ES H, O R4 Y R5 EN COMBINACION SON OXO; R6 ES H O AMBOS R6 FORMAN UN CARBONILO. SON COMPUESTOS PREFERIDOS: 1-(2-(2,6-DIMETILFENIL)-6-(3-ISOPROPIL-1-METIL-1H-PIRAZOL-5-IL)-5,6,7,8-TETRAHIDROPIRIDO[4,3-d]PIRIMIDIN-4-IL)-2-METILPIPERIDIN-4-OL RACEMICO; 2-(2,6-DIMETILFENIL)-4-(3,3-DIMETILPIPERIDIN-1-IL)-6-(3-ISOPROPIL-1-METIL-1H-PIRAZOL-5-IL)-5,6,7,8-TETRAHIDROPIRIDO[4,3-d]PIRIMIDINA; (S)-2-(2,6-DIMETILFENIL)-6-(3-ISOPROPIL-1-METIL-1H-PIRAZOL-5-IL)-4-(2-METILPIPERIDIN-1-IL)-5,6,7,8-TETRAHIDROPIRIDO[4,3-d]PIRIMIDINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE RECEPTORES DE C5A DEL COMPLEMENTO MAMIFERO SIENDO UTILES EN EL TRATAMIENTO DE RETINOPATIA DIABETICA, RETINITIS PIGMENTOSA, PENFIGO OCULAR
PE2014000114A 2011-07-22 2012-07-20 Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a PE20141281A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161510643P 2011-07-22 2011-07-22
US201161539732P 2011-09-27 2011-09-27

Publications (1)

Publication Number Publication Date
PE20141281A1 true PE20141281A1 (es) 2014-09-24

Family

ID=46604083

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000114A PE20141281A1 (es) 2011-07-22 2012-07-20 Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a

Country Status (26)

Country Link
US (2) US8846656B2 (es)
EP (1) EP2734521B1 (es)
JP (1) JP6040237B2 (es)
KR (1) KR20140096020A (es)
CN (1) CN103814027B (es)
AP (1) AP2014007398A0 (es)
AR (1) AR087288A1 (es)
AU (1) AU2012287183B2 (es)
BR (1) BR112014001468A2 (es)
CA (1) CA2842528A1 (es)
CL (1) CL2014000171A1 (es)
CO (1) CO6862157A2 (es)
CR (1) CR20140032A (es)
EA (1) EA201490320A1 (es)
ES (1) ES2637167T3 (es)
IL (1) IL230501A0 (es)
MA (1) MA35275B1 (es)
MX (1) MX336497B (es)
PE (1) PE20141281A1 (es)
PH (1) PH12014500200A1 (es)
PL (1) PL2734521T3 (es)
PT (1) PT2734521T (es)
TN (1) TN2014000030A1 (es)
TW (1) TW201311688A (es)
UY (1) UY34209A (es)
WO (1) WO2013016197A1 (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8946260B2 (en) * 2010-09-16 2015-02-03 Novartis Ag 17α-hydroxylase/C17,20-lyase inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
UY34781A (es) * 2012-05-04 2013-12-31 Novartis Ag Moduladores de la via del complemento y usos de los mismos
NZ702747A (en) 2012-06-13 2017-03-31 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9475806B2 (en) 2013-03-14 2016-10-25 Novartis Ag Complement factor B inhibitors and uses there of
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
EP3060276B1 (en) 2013-10-24 2023-05-24 Trustees of Boston University Infusion system for preventing mischanneling of multiple medicaments
US9676728B2 (en) 2013-10-30 2017-06-13 Novartis Ag 2-benzyl-benzimidazole complement factor B inhibitors and uses thereof
TWI656121B (zh) * 2014-08-04 2019-04-11 德商拜耳製藥公司 ２－（嗎啉－４－基）－１，７－萘啶
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3240537B1 (en) 2014-12-30 2020-09-09 F. Hoffmann-La Roche AG Novel tetrahydropyridopyrimidines and tetrahydropyridopyridines for the treatment and prophylaxis of hepatitis b virus infection
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
JP7219218B2 (ja) 2016-12-22 2023-02-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規のベンジルアミノ置換キナゾリンおよびｓｏｓ１阻害剤としての誘導体
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
MX392259B (es) * 2017-05-31 2025-03-24 Chemocentryx Inc ANILLOS 6-5 FUSIONADOS COMO INHIBIDORES C5a
EP3630774B1 (en) * 2017-05-31 2022-11-23 ChemoCentryx, Inc. 5-5 fused rings as c5a inhibitors
US10829487B2 (en) 2017-12-21 2020-11-10 Boehringer Ingelheim International Gmbh Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
JP7254082B2 (ja) * 2017-12-22 2023-04-07 ケモセントリックス，インコーポレイティド Ｃ５ａＲ阻害剤としてのジアリール置換６，５－縮合環化合物
IL275516B2 (en) 2017-12-22 2023-12-01 Chemocentryx Inc Diaryl substituted 5,5-fused ring compounds as c5ar inhibitors
UA124694C2 (uk) * 2018-01-10 2021-10-27 Ідорсія Фармасьютікалз Лтд 2,4,6,7-ТЕТРАГІДРОПІРАЗОЛО[4,3-d]ПІРИМІДИН-5-ОНОВІ ПОХІДНІ ТА СПОРІДНЕНІ СПОЛУКИ ЯК МОДУЛЯТОРИ РЕЦЕПТОРА C5A ДЛЯ ЛІКУВАННЯ ВАСКУЛІТУ ТА ЗАПАЛЬНИХ ЗАХВОРЮВАНЬ
KR102809631B1 (ko) 2018-04-02 2025-05-16 케모센트릭스, 인크. 융합된-바이사이클릭 C5aR 길항제의 프로드러그
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
AU2021222818A1 (en) * 2020-02-17 2022-09-01 Alesta Therapeutics BV GCN2 modulator compounds
US20240287058A1 (en) * 2020-04-29 2024-08-29 Relay Therapeutics, Inc. Pi3k-alpha inhibitors and methods of use thereof
CN116323623B (zh) 2020-09-18 2025-09-26 拜耳公司 作为SOS1抑制剂的吡啶并[2,3-d]嘧啶-4-胺
US20230382856A1 (en) * 2020-10-30 2023-11-30 Daiichi Sankyo Company, Limited Method of producing 3-methyl-4-halo-indole derivative
GB202104286D0 (en) * 2021-03-26 2021-05-12 Syngenta Crop Protection Ag Chemical process
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CN117820340A (zh) * 2022-12-01 2024-04-05 成都硕德药业有限公司 Atr抑制剂及其用途
KR20250000614A (ko) * 2023-06-27 2025-01-03 서울대학교병원 신규한 망막질환 예방 또는 치료용 조성물

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US4727149A (en) 1982-03-11 1988-02-23 John Wyeth & Brother Limited Preparation of nitriles of fused ring pyridine derivatives
US5853740A (en) 1996-08-07 1998-12-29 Abbott Laboratories Delivery system for pharmaceutical agents encapsulated with oils
EP1317450B1 (en) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2004016596A1 (en) 2002-08-19 2004-02-26 Glenmark Pharmaceuticals Limited Condensed heterocyclic compounds as pde-iv inhibitors for the treatment of inflammatory and allergic disorders
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
JP2006521398A (ja) 2003-03-28 2006-09-21 サイオス・インコーポレーテツド ＴＧＦβの二−環式ピリミジン阻害剤
ES2388547T3 (es) 2003-04-18 2012-10-16 Eli Lilly And Company Compuestos de (piperidiniloxi)fenilo, (piperidiniloxi)piridinilo, (piperidinilsulfanil)fenilo y (piperidinilsulfanil)piridinilo como agonistas de 5-HT 1F
KR20060118398A (ko) * 2003-08-05 2006-11-23 버텍스 파마슈티칼스 인코포레이티드 전압 개폐 이온 채널 억제제로서의 축합 피라미딘 화합물
GB0403038D0 (en) 2004-02-11 2004-03-17 Novartis Ag Organic compounds
AU2005244104B2 (en) * 2004-05-08 2012-03-15 Novartis International Pharmaceutical Ltd. 4,5-disubstituted-2-aryl pyrimidines
US7429666B2 (en) 2004-06-10 2008-09-30 Merck Frosst Canada Ltd. Pyridine analogs as C5a antagonists
AU2005288858B2 (en) 2004-09-30 2011-04-21 Janssen R&D Ireland HCV inhibiting bi-cyclic pyrimidines
WO2007021710A1 (en) 2005-08-12 2007-02-22 Merck & Co., Inc. Heterobicyclic compounds useful as p38 kinase inhibiting agents
KR101176697B1 (ko) 2006-04-20 2012-08-23 에프. 호프만-라 로슈 아게 케모카인 수용체의 다이아제판 유도체 조절자
US20090124610A1 (en) 2006-04-25 2009-05-14 Gordon Saxty Pharmaceutical compounds
US8563566B2 (en) 2007-08-01 2013-10-22 Valeant Pharmaceuticals International Naphthyridine derivatives as potassium channel modulators
WO2009023669A1 (en) 2007-08-13 2009-02-19 Janssen Pharmaceutica N.V. Substituted 5,6,7,8-tetrahydroquinoline derivatives, compositions, and methods of use thereof
EP2318377B1 (en) 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
US7989463B2 (en) 2008-09-03 2011-08-02 Dr. Reddy's Laboratories Limited Biccyclic compounds as GATA modulators
AR073304A1 (es) 2008-09-22 2010-10-28 Jerini Ag Moduladores del receptor de bradiquinina b2 de molecula pequena
WO2010120994A2 (en) 2009-04-17 2010-10-21 Wyeth Llc Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis
EP2424556A4 (en) 2009-04-27 2013-07-31 Jerini Ophthalmic Inc EXTENDED RELEASE FORMULATIONS OF PEPTIDOMIMETIC MEDICAMENTS AND USES THEREOF
EP2434885B1 (en) 2009-05-27 2014-03-26 Merck Sharp & Dohme Corp. Alkoxy tetrahydro-pyridopyrimidine pde10 inhibitors
US8691827B2 (en) 2009-08-17 2014-04-08 Merck Sharp & Dohme Corp. Amino tetrahydro-pyridopyrimidine PDE10 inhibitors
JP2013032290A (ja) 2009-11-20 2013-02-14 Dainippon Sumitomo Pharma Co Ltd 新規縮合ピリミジン誘導体
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
JP2014528410A (ja) 2011-09-30 2014-10-27 キネタ・インコーポレイテツド 抗ウイルス化合物
US10220002B2 (en) 2011-12-02 2019-03-05 Board Of Regents Of The University Of Nebraska Controlled-release peptide compositions and uses thereof

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