ES2628365T3 - Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T - Google Patents

Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T Download PDF

Info

Publication number
ES2628365T3
ES2628365T3 ES13818857T ES13818857T ES2628365T3 ES 2628365 T3 ES2628365 T3 ES 2628365T3 ES 13818857 T ES13818857 T ES 13818857T ES 13818857 T ES13818857 T ES 13818857T ES 2628365 T3 ES2628365 T3 ES 2628365T3
Authority
ES
Spain
Prior art keywords
alkyl
optionally substituted
pyridyl
och3
independently selected
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES13818857T
Other languages
English (en)
Inventor
Kristi A. Leonard
Kent Barbay
James P. Edwards
Kevin D. Kreutter
David A. Kummer
Umar Maharoof
Rachel NISHIMURA
Maud Urbanski
Hariharan Venkatesan
Aihua Wang
Ronald L. Wolin
Craig R. Woods
Anne Fourie
Xiaohua XUE
Taraneh Mirzadegan
Kelly Lynn GANAMET
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Application granted granted Critical
Publication of ES2628365T3 publication Critical patent/ES2628365T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and 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
    • A61K31/495—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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Los compuestos de Fórmula 1: **Fórmula** en donde: R1 es pirrolilo, pirazolilo, imidazolilo, triazolilo, tiazolilo, piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinailo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, tetrahidropiranilo, tetrahidrofuranilo, furanilo, fenilo, oxazolilo, isoxazolilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, tiadiazolilo, oxadiazolilo o quinolinilo; en el que dicho piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinailo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, imidazolilo, fenilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, quinolinilo, y pirazolilo están opcionalmente sustituidos con C(O)C(1-4)alquilo, C(O)NH2, C(O)NHC(1-2)alquilo, C(O)N(C(1-2)alquilo)2, NHC(O)C(1-4)alilo, NHSO2C(1-4)alquilo, C(1-4)alquilo, CF3, CH2CF3, Cl, F, -CN, OC(1-4)alquilo, N(C(1-4)alquilo)2, (CH2)3OCH3, SC(1-4)alquilo, OH, CO2H, CO2C(1-4)alquilo, C(O)CF3, SO2CF3, OCF3, OCHF2, SO2CH3, SO2NH2, SO2NHC(1-2)alquilo, SO2N(C(1-2)alquilo)2, C(O)NHSO2CH3, o OCH2OCH3; y opcionalmente sustituidos con hasta dos sustituyentes adicionales seleccionados independientemente del grupo que consiste en Cl, C(1-2)alquilo, SCH3, OC(1-2)alquilo, CF3, -CN, y F; y en los que dichos triazolilo, oxazolilo, isoxazolilo, pirrolilo, y tiazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, alquilo C(O)NH2, -CN, OC(1-2), (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, y C(1-2)alquilo; y dicho tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con C(1-2)alquilo; y dichos piridilo, piridiloóxido, pirimidinilo, piridazilo, y pirazinilo están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en C(O)NHC(1-2)alquilo, C(O)N(C(1-2)alquilo)2, NHC(O)C(1-4)alquilo, NHSO2C(1-4)alquilo, C(O)CF3, SO2CF3, SO2NHC(1-2)alquilo, SO2N(C(1-2)alquilo)2, C(O)NHSO2CH3, SO2CH3, SO2NH2, C(O)NH2, -35 CN, OC(1-4)alquilo, (CH2)(2-3)OCH3, SC(1-4)alquilo, CF3, F, Cl, y C(1-4)alquilo; R2es triazolilo, piridilo, piridiloóxido, pirazolilo, pirimidinilo, oxazolilo, isoxazolilo, piperidinilo de N-acetilo, 1-H-piperidinilo, N-Boc-piperidinilo, N-C(1-3)alquilpiperidinilo, tiazolilo, piridazilo, pirazinilo, 1-(3-metoxipropilo)-imidazolilo, tiadiazolilo, oxadiazolilo, o imidazolilo; en el que dicho imidazolilo está opcionalmente sustituido con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en C(1-2)alquilo, SCH3, OC(1-2)alquilo, CF3, -CN, F, y Cl; y dicho piridilo, piridiloóxido, pirimidinilo, piridazilo, y pirazinilo, están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alquilo, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, o C(1-2)alquilo; y dichos triazolilo, tiazolilo, oxazolilo e isoxazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo que consiste en SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alquilo, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, y C(1-2)alquilo; y dicho tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con C(1-2)alquilo; y dicho pirazolilo está opcionalmente sustituido con hasta tres grupos CH3; R3es H, OH, OCH3, o NH2; R4es H o F; R5es H, Cl, -CN, CF3, SC(1-4)alquilo, OC(1-4)alquilo, OH, C(1-4)alquilo, N(CH3)OCH3, NH(C(1-4)alquilo), N(C(1-4)alquilo)2, o 4-hidroxi-piperidinilo;
ES13818857T 2012-10-16 2013-10-15 Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T Active ES2628365T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261714433P 2012-10-16 2012-10-16
US201261725537P 2012-11-13 2012-11-13
PCT/US2013/065026 WO2014062667A1 (en) 2012-10-16 2013-10-15 Phenyl linked quinolinyl modulators of ror-gamma-t

Publications (1)

Publication Number Publication Date
ES2628365T3 true ES2628365T3 (es) 2017-08-02

Family

ID=49943493

Family Applications (1)

Application Number Title Priority Date Filing Date
ES13818857T Active ES2628365T3 (es) 2012-10-16 2013-10-15 Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T

Country Status (21)

Country Link
US (1) US9309222B2 (es)
EP (1) EP2909193B1 (es)
JP (1) JP6251277B2 (es)
KR (1) KR20150070350A (es)
CN (1) CN105073729A (es)
AU (1) AU2013331505A1 (es)
CA (1) CA2888485C (es)
CL (1) CL2015000946A1 (es)
CO (1) CO7350658A2 (es)
CR (1) CR20150192A (es)
EA (1) EA201590750A1 (es)
EC (1) ECSP15015155A (es)
ES (1) ES2628365T3 (es)
GT (1) GT201500092A (es)
HK (1) HK1213887A1 (es)
IL (1) IL238122A0 (es)
MX (1) MX2015004784A (es)
PE (1) PE20151203A1 (es)
PH (1) PH12015500776A1 (es)
SG (1) SG11201502935VA (es)
WO (1) WO2014062667A1 (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112016008258A2 (pt) 2013-10-15 2017-10-10 Janssen Pharmaceutica Nv moduladores de ror?t de quinolinila
JP6320523B2 (ja) * 2013-10-15 2018-05-09 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγＴの第二級アルコールキノリニルモジュレータ
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
BR112016008215A2 (pt) * 2013-10-15 2017-09-26 Janssen Pharmaceutica Nv moduladores de quinolinila ligados por alquila de roryt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
CA2927152C (en) * 2013-10-15 2021-09-14 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of ror-gamma-t
EP3180335B1 (en) 2014-08-11 2021-05-05 Angion Biomedica Corporation Cytochrome p450 inhibitors and uses thereof
TWI705057B (zh) * 2014-10-30 2020-09-21 比利時商健生藥品公司 用作ＲＯＲγｔ調節劑之三氟甲基醇
CA2970819A1 (en) 2014-12-31 2016-07-07 Angion Biomedica Corp. Methods and agents for treating disease
WO2016110821A1 (en) 2015-01-08 2016-07-14 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
WO2016128908A1 (en) 2015-02-12 2016-08-18 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
TWI757266B (zh) * 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
IL264178B2 (en) * 2016-07-14 2024-05-01 Crinetics Pharmaceuticals Inc Somatostatin modulators and uses thereof
WO2018112842A1 (en) * 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor
EP3658560A4 (en) 2017-07-25 2021-01-06 Crinetics Pharmaceuticals, Inc. SOMATOSTAT IN MODULATORS AND USES THEREOF
PT3740475T (pt) 2018-01-17 2022-07-18 Crinetics Pharmaceuticals Inc Processo de produção de moduladores da somatostatina
CN108503581A (zh) * 2018-04-12 2018-09-07 苏州康润医药有限公司 一种3-溴-6-氟-2-吡啶乙酮的合成方法
CA3191084A1 (en) 2020-09-09 2022-03-17 Gerald Burke Formulations of a somatostatin modulator
CN117682980B (zh) * 2024-02-02 2024-05-10 济南悟通生物科技有限公司 一种2-乙酰基四氢吡啶的制备方法

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3472859A (en) 1966-11-01 1969-10-14 Sterling Drug Inc 1-alkyl-1,4-dihydro-4-oxo-3 quinoline-carboxylic acids and esters
JPS4826772Y1 (es) 1969-04-04 1973-08-06
ATE27451T1 (de) 1981-03-24 1987-06-15 Ciba Geigy Ag Acyl-chinolinonderivate, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische praeparate und ihre verwendung.
US4656283A (en) 1982-05-25 1987-04-07 American Cyanamid Company Alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid
US4910327A (en) 1982-05-25 1990-03-20 American Cyanamid Company Alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid: dialkyl 3-(substituted)phenylaminobut-2-ene-dioates and methods for the preparation thereof
US4710507A (en) 1983-12-22 1987-12-01 Pfizer Inc. Quinolone inotropic agents
FR2634483B2 (fr) 1987-12-29 1994-03-04 Esteve Labor Dr Derives des acides 7-(1-azetidinyl)-1,4-dihydro-4-oxoquinoleine-3-carboxyliques, leur preparation et leur application en tant que medicaments
CA2002864C (en) 1988-11-29 1999-11-16 Eddy J. E. Freyne (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives
SG64322A1 (en) 1991-05-10 1999-04-27 Rhone Poulenc Rorer Int Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US5478832A (en) 1992-05-08 1995-12-26 The Green Cross Corporation Quinoline compounds
JPH0826772A (ja) 1994-07-22 1996-01-30 Sony Corp 融着用ガラス、その製造方法及び製造装置、並びに磁気ヘッドの製造方法
DE69512495T2 (de) 1994-10-27 2000-02-03 Asahi Glass Co. Ltd., Tokio/Tokyo Verfahren zur Herstellung von Chinolin-2-yl-benzoesäure
GB9523267D0 (en) 1995-11-14 1996-01-17 Sandoz Ltd Organic compounds
SK283335B6 (sk) 1995-12-08 2003-06-03 Janssen Pharmaceutica N. V. (Imidazol-5-yl)metyl-2-chinolinónové deriváty, spôsob a medziprodukty na ich prípravu, ich použitie a farmaceutické kompozície na ich báze
AU710926B2 (en) 1996-05-20 1999-09-30 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU740603B2 (en) 1997-06-02 2001-11-08 Janssen Pharmaceutica N.V. (imidazol-5-yl)methyl-2-quinolinone derivatives as inhibitors of smooth muscle cell proliferation
PL341364A1 (en) 1997-12-22 2001-04-09 Upjohn Co 4-hydroxyqinoline-3-carboxamides and hydrazides as antiviral agents
FR2776388B1 (fr) 1998-03-20 2006-04-28 Lipha Utilisation de recepteurs de la famille ror pour le criblage de substances utiles pour le traitement de l'atherosclerose
US6399629B1 (en) 1998-06-01 2002-06-04 Microcide Pharmaceuticals, Inc. Efflux pump inhibitors
ID26987A (id) 1998-07-06 2001-02-22 Janssen Pharmaceutica Nv Inhibitor-inhibitor transferase protein farnesil dengan sifat-sifat peka terhadap sinar radiasi in vivo
HRP20000904A2 (en) * 1998-07-06 2001-12-31 Janssen Pharmaceutica Nv Farnesyl protein transferase inhibitors for treating arthropathies
JP2000169451A (ja) 1998-09-30 2000-06-20 Kyorin Pharmaceut Co Ltd ６，７―ジ置換キノリンカルボン酸誘導体とその付加塩及びそれらの製造方法
ID29241A (id) 1998-12-23 2001-08-16 Janssen Pharmaceutica Nv Turunan-turunan kinolin teranelasi-1,2
US6248739B1 (en) 1999-01-08 2001-06-19 Pharmacia & Upjohn Company Quinolinecarboxamides as antiviral agents
US6248736B1 (en) 1999-01-08 2001-06-19 Pharmacia & Upjohn Company 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents
PL349839A1 (en) 1999-02-11 2002-09-23 Pfizer Prod Inc Heteroaryl-substituted quinolin-2-one derivatives useful as anticancer agents
PT1106612E (pt) 1999-11-30 2004-06-30 Pfizer Prod Inc Derivados de quinolina uteis para inibir a farnesil-proteina-transferase
JP5491681B2 (ja) 2000-02-04 2014-05-14 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 乳ガンの治療のためのファルネシルタンパク質トランスフェラーゼ阻害剤
US6838467B2 (en) 2000-02-24 2005-01-04 Janssen Pharmaceutica N. V. Dosing regimen
US20030078281A1 (en) 2000-02-29 2003-04-24 Rybak Mary Ellen Margaret Farnesyl protein transferase inhibitor combinations with anti-tumor alkylating agents
WO2001064194A2 (en) 2000-02-29 2001-09-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with camptothecin compounds
CA2397448A1 (en) 2000-02-29 2001-09-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with further anti-cancer agents
JP2003525252A (ja) 2000-02-29 2003-08-26 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｈｅｒ２抗体とのファルネシルタンパク質トランスフェラーゼ阻害剤組み合わせ剤
EP1261343A2 (en) 2000-02-29 2002-12-04 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with anti-tumor nucleoside derivatives
US20030027808A1 (en) 2000-02-29 2003-02-06 Palmer Peter Albert Farnesyl protein transferase inhibitor combinations with platinum compounds
JP2003525239A (ja) 2000-02-29 2003-08-26 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ タキサン化合物とのファルネシルタンパク質トランスフェラーゼ阻害剤の組み合わせ剤
WO2001064196A2 (en) 2000-02-29 2001-09-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with vinca alkaloids
EP1267871A2 (en) 2000-02-29 2003-01-02 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with anti-tumor podophyllotoxin derivatives
AU2001252147A1 (en) 2000-02-29 2001-09-12 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations
AU2001244167A1 (en) 2000-02-29 2001-09-12 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with anti-tumor anthracycline derivatives
US6844357B2 (en) 2000-05-01 2005-01-18 Pfizer Inc. Substituted quinolin-2-one derivatives useful as antiproliferative agents
US6525049B2 (en) 2000-07-05 2003-02-25 Pharmacia & Upjohn Company Pyrroloquinolones as antiviral agents
US6624159B2 (en) 2000-07-12 2003-09-23 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
ATE276262T1 (de) 2000-07-12 2004-10-15 Upjohn Co Oxazinochinolone für die behandlung viraler infektionen
WO2002024682A1 (en) 2000-09-25 2002-03-28 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors
WO2002024686A2 (en) 2000-09-25 2002-03-28 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-heterocyclylmethyl quinoline and quinazoline derivatives
US7067531B2 (en) 2000-09-25 2006-06-27 Angibaud Patrick Rene Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives
CZ20031145A3 (cs) 2000-10-02 2003-12-17 Janssen Pharmaceutica N.V. Antagonisté metabotropního glutamátového receptoru
DK1339407T3 (da) 2000-11-28 2006-08-14 Janssen Pharmaceutica Nv Farnesylproteintransferaseinhibitorer til behandling af inflammatorisk tarmsygdom
ES2260316T3 (es) 2000-12-27 2006-11-01 Janssen Pharmaceutica N.V. Derivados de quinazolina y quinolina 4-sustituidos que inhiben la farnesil transferasa.
JP4969016B2 (ja) 2001-02-15 2012-07-04 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 抗エストロゲン剤とファルネシルプロテイントランスフェラーゼ阻害剤の組み合わせ物
US6544990B2 (en) 2001-03-01 2003-04-08 Pharmacia & Upjohn Company Substituted quinolinecarboxamides as antiviral agents
EP1390033A1 (en) 2001-04-25 2004-02-25 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitors for treating cachexia
EP1412367A4 (en) 2001-06-21 2006-05-03 Ariad Pharma Inc NEW CHINOLINE AND ITS USE
AU2002350244A1 (en) 2001-12-20 2003-07-09 Pharmacia And Upjohn Company Pyridoquinoxaline antivirals
EP1456208A1 (en) 2001-12-20 2004-09-15 PHARMACIA & UPJOHN COMPANY Pyridoquinoxaline antivirals
CA2479109C (en) 2002-03-29 2011-08-02 Janssen Pharmaceutica N.V. Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands
ATE404537T1 (de) 2002-08-13 2008-08-15 Shionogi & Co Heterocyclische verbindungen mit hiv-integrase- hemmender wirkung
AU2003262947A1 (en) 2002-08-30 2004-03-19 Pharmacia And Upjohn Company Method of preventing or treating atherosclerosis or restenosis
GB0222516D0 (en) 2002-09-27 2002-11-06 Karobio Ab Novel compounds
RS20060018A (sr) 2003-07-14 2007-12-31 Arena Pharmaceuticals Inc., Derivati spojenih arila i heteroarila kao modulatori metabolizma u profilaksi i lečenju sa njima povezanih stanja
BRPI0416206A (pt) 2003-11-20 2006-12-26 Janssen Pharmaceutica Nv 2-quinolinonas e 2-quinoxalinonas substituìdas por 6-alquenila e 6-fenilalquila como inibidores de polimerase de poli(adp-ribose)
SG151249A1 (en) 2003-12-05 2009-04-30 Janssen Pharmaceutica Nv 6-substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors
US7652014B2 (en) 2003-12-10 2010-01-26 Janssen Pharmaceutica Substituted 6-cyclohexylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors
AU2004298486A1 (en) 2003-12-12 2005-06-30 Wyeth Quinolines useful in treating cardiovascular disease
EA011277B1 (ru) 2004-01-23 2009-02-27 Янссен Фармацевтика Н.В. Производные хинолина и их применение в качестве ингибиторов микобактерий
EA011572B9 (ru) 2004-01-29 2018-01-31 Янссен Фармацевтика Н.В. Производные хинолина для применения в качестве микобактериальных ингибиторов
ATE540936T1 (de) 2004-06-30 2012-01-15 Janssen Pharmaceutica Nv Substituierte 2-alkyl-chinazolinonderivate als parp-hemmer
ES2407813T3 (es) 2004-08-04 2013-06-14 Meiji Seika Pharma Co., Ltd. Derivados de quinolina e insecticida que contienen los mismos como constituyente activo
KR100686531B1 (ko) 2004-08-31 2007-02-23 한국화학연구원 히스톤 디아세틸라제 저해활성을 갖는 아릴아미노메틸프로페닐 벤즈하이드록시아마이드 유도체 및 그의 제조방법
HRP20130399T1 (hr) 2004-11-05 2013-06-30 Janssen Pharmaceutica Nv Terapeutska upotreba inhibitora farenziltransferaze i postupci praä†enja njihove efikasnosti
JO2855B1 (en) 2005-08-03 2015-03-15 شركة جانسين فارماسوتيكا ان. في Quinoline derivatives acting as antibacterial agents
JO2952B1 (en) 2005-08-03 2016-03-15 جانسين فارماسوتيكا ان. في Quinoline derivatives acting as antibacterial agents
WO2007088978A1 (ja) 2006-02-03 2007-08-09 Meiji Seika Kaisha, Ltd. 新規キノリン誘導体およびこれを有効成分として含有する農園芸用殺菌剤
US8389739B1 (en) 2006-10-05 2013-03-05 Orphagen Pharmaceuticals Modulators of retinoid-related orphan receptor gamma
KR101083177B1 (ko) 2006-10-23 2011-11-11 에스지엑스 파마슈티컬스, 인코포레이티드 트리아졸로-피리다진 단백질 키나제 조정제
JO3271B1 (ar) 2006-12-06 2018-09-16 Janssen Pharmaceutica Nv مشتقات الكوينولين المضادة للجراثيم
AR065093A1 (es) 2007-02-05 2009-05-13 Merck Frosst Canada Ltd Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
EP2155197A4 (en) 2007-03-09 2011-10-12 Link Medicine Corp TREATMENT OF LYSOSOMAL STORAGE DISEASES
EP2162132A4 (en) 2007-05-21 2013-01-16 Sgx Pharmaceuticals Inc Heterocyclic kinase modulators
CN101143845B (zh) 2007-10-15 2010-08-25 中国药科大学 取代喹啉甲酰胍衍生物、其制备方法及其医药用途
AU2009205539B2 (en) 2008-01-18 2013-12-05 Allergan.Inc Substitued-aryl-(imidazole)-methyl)-phenyl compounds as subtype selective modulators of alpha 2B and/or alpha 2C adrenergic receptors
JP2011511056A (ja) 2008-02-05 2011-04-07 ファイザー・インク Ｃｎｓ障害および代謝障害治療のためのピリジニルアミド
BRPI0912604A2 (pt) 2008-05-13 2019-09-10 Allergan Inc quinolinilmetilimidazóis como agentes terapêuticos
WO2010068296A1 (en) 2008-12-11 2010-06-17 Stiefel Laboratories, Inc. Piperazine carboxamidines as antimicrobial agents
WO2010127208A1 (en) 2009-04-30 2010-11-04 Forest Laboratories Holdings Limited Inhibitors of acetyl-coa carboxylase
CN101899011B (zh) 2009-05-26 2013-01-16 北京大学 氨基二硫代甲酸酯类化合物、其制备方法和应用
AR077004A1 (es) 2009-06-09 2011-07-27 Hoffmann La Roche Compuestos heterociclicos antivirales
SG176986A1 (en) 2009-06-25 2012-02-28 Amgen Inc Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases
CA2771432A1 (en) 2009-08-20 2011-02-24 Novartis Ag Heterocyclic oxime compounds
EP2368886A1 (en) 2010-03-01 2011-09-28 Phenex Pharmaceuticals AG Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
US9101600B2 (en) 2010-03-11 2015-08-11 New York University Compounds as RORγt modulators and uses thereof
CN105962259A (zh) 2010-04-15 2016-09-28 卓莫赛尔公司 用于减小或消除苦味的化合物、组合物和方法
WO2012064744A2 (en) * 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
US11179500B2 (en) 2011-02-24 2021-11-23 Emory University JAB1 inhibitory compositions for ossification and methods related thereto
PE20141637A1 (es) 2011-04-28 2014-11-20 Japan Tobacco Inc Compuesto de amida y aplicacion farmaceutica para el mismo
WO2012158784A2 (en) 2011-05-16 2012-11-22 Theodore Mark Kamenecka Modulators of the nuclear hormone receptor ror
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
WO2013064231A1 (en) 2011-10-31 2013-05-10 Phenex Pharmaceuticals Ag SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3)
EP2800745B1 (en) 2011-12-02 2020-02-12 Phenex Pharmaceuticals AG Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rory, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases

Also Published As

Publication number Publication date
EP2909193B1 (en) 2017-04-19
PH12015500776A1 (en) 2015-06-22
US9309222B2 (en) 2016-04-12
CA2888485C (en) 2021-01-26
KR20150070350A (ko) 2015-06-24
PE20151203A1 (es) 2015-08-31
EA201590750A1 (ru) 2015-09-30
CN105073729A (zh) 2015-11-18
GT201500092A (es) 2015-12-31
US20140107097A1 (en) 2014-04-17
CL2015000946A1 (es) 2015-10-02
HK1213887A1 (zh) 2016-07-15
JP2015536321A (ja) 2015-12-21
JP6251277B2 (ja) 2017-12-20
EP2909193A1 (en) 2015-08-26
MX2015004784A (es) 2015-08-14
CA2888485A1 (en) 2014-04-24
CO7350658A2 (es) 2015-08-10
CR20150192A (es) 2015-05-18
WO2014062667A1 (en) 2014-04-24
IL238122A0 (en) 2015-05-31
ECSP15015155A (es) 2016-01-29
AU2013331505A1 (en) 2015-04-30
SG11201502935VA (en) 2015-09-29

Similar Documents

Publication Publication Date Title
ES2628365T3 (es) Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T
AR095424A1 (es) 7-azabiciclos sustituidos y su uso como moduladores del receptor de orexina
AR093403A1 (es) COMPUESTOS DE PIRIDILO SUSTITUIDOS CON ALQUILAMIDA UTILES COMO MODULADORES DE LAS RESPUESTAS DE IL-12, IL23 Y/O INFa
ES2659397T3 (es) 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas
PY1030698A (es) Mezclas pesticidas mesoionicos
AR095530A1 (es) Moduladores de p2x7
NZ732810A (en) Picolinamides and other compounds
ES2855732T3 (es) Compuestos y composiciones para tratar afecciones asociadas con la actividad de NLRP
AR109180A1 (es) Derivados de piperidina como moduladores del receptor cxcl11 / cxcl12 cxcr7
ES2526352T3 (es) Derivados de piridazinona
AR105845A1 (es) Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4
NI200800036A (es) Inhibidores macrociclicos del virus de la hepatitis c
AR096902A1 (es) Derivados de triazina y pirimidina como inhibidores de la idh1 y/o idh2 mutantes y su uso en el tratamiento del cáncer
ES2530519T3 (es) Compuestos macrocíclicos completamente sintéticos, con conformación restringida
AR104447A1 (es) Azabenzimidazoles y sus usos como moduladores de los receptores ampa
AR110789A1 (es) Compuestos moduladores del receptor de hidrocarburos de arilo (ahr)
AR070634A1 (es) Derivados de carboxamida-heteroarilo,proceso para prepararlos,medicamentos que los contienen y usos de los mismos en el tratamiento de la diabetes,obesidad,neuropatias y/o nefropatias.
AR110963A1 (es) Compuestos heterocíclicos, su método de preparación y composición farmacéutica que los comprende
AR102480A1 (es) ALCOHOLES TRIFLUOROMETÍLICOS COMO MODULADORES DE RORgt
AR101798A1 (es) Quinolinas herbicidas
AR089889A1 (es) Compuestos fungicidas de pirimidina
PE20120657A1 (es) Compuesto para el tratamiento de trastornos metabolicos
AR114374A1 (es) Compuestos herbicidas
AR096160A1 (es) Inhibidores de nicotamida fosforibosiltransferasa, composiciones, productos y usos de los mismos
AR103414A1 (es) Derivados de hidroxialquil-piperazina como moduladores del receptor cxcr3