ES2628365T3 - Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T - Google Patents
Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T Download PDFInfo
- 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
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
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;
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
EP3057421B1 (en) * | 2013-10-15 | 2019-11-20 | Janssen Pharmaceutica NV | Alkyl linked quinolinyl modulators of ror(gamma)t |
US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
JP6377152B2 (ja) * | 2013-10-15 | 2018-08-22 | ヤンセン ファーマシューティカ エヌ.ベー. | RORγtのフェニル結合キノリニルモジュレータ |
KR20160068956A (ko) | 2013-10-15 | 2016-06-15 | 얀센 파마슈티카 엔.브이. | RORyT의 퀴놀리닐 조절제 |
JP6578349B2 (ja) | 2014-08-11 | 2019-09-18 | アンジオン バイオメディカ コーポレーション | チトクロームp450阻害剤およびその使用 |
JOP20200117A1 (ar) * | 2014-10-30 | 2017-06-16 | Janssen Pharmaceutica Nv | كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t |
EP3240778A4 (en) | 2014-12-31 | 2018-07-11 | Angion Biomedica Corp. | Methods and agents for treating disease |
BR112017014770A2 (pt) | 2015-01-08 | 2018-01-16 | Advinus Therapeutics Ltd | compostos bicíclicos, composições e aplicações médicas dos mesmos |
WO2016128908A1 (en) | 2015-02-12 | 2016-08-18 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
TW202220968A (zh) * | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
HRP20221279T1 (hr) | 2016-07-14 | 2022-12-23 | Crinetics Pharmaceuticals, Inc. | Modulatori somatostatina i njihove uporabe |
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 |
WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN AND USES THEREOF |
MX2020007586A (es) | 2018-01-17 | 2020-09-03 | Crinetics Pharmaceuticals Inc | Proceso de fabricacion de moduladores de 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 |
JP2023540137A (ja) | 2020-09-09 | 2023-09-21 | クリネティックス ファーマシューティカルズ,インク. | ソマトスタチン調節因子の製剤 |
CN117682980A (zh) * | 2024-02-02 | 2024-03-12 | 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)
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 |
JPS4826772U (es) | 1971-08-02 | 1973-03-31 | ||
ATE27451T1 (de) | 1981-03-24 | 1987-06-15 | Ciba Geigy Ag | Acyl-chinolinonderivate, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische praeparate und ihre verwendung. |
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 |
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 |
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 |
ES2136782T3 (es) | 1994-10-27 | 1999-12-01 | Asahi Glass Co Ltd | Procedimiento para producir compuestos de acido quinolin-2-il-benzoico. |
GB9523267D0 (en) | 1995-11-14 | 1996-01-17 | Sandoz Ltd | Organic compounds |
CA2231105C (en) | 1995-12-08 | 2005-09-13 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives |
CA2254769A1 (en) | 1996-05-20 | 1997-11-27 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
CA2290992C (en) * | 1997-06-02 | 2008-02-12 | Janssen Pharmaceutica N.V. | (imidazol-5-yl)methyl-2-quinolinone derivatives as inhibitors of smooth muscle cell proliferation |
RU2220960C2 (ru) | 1997-12-22 | 2004-01-10 | Фармация Энд Апджон Компани | 4-гидрокси-3-хинолинкарбоксамиды и гидразиды, фармацевтическая композиция и способ лечения на их основе |
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 |
CA2337800C (en) * | 1998-07-06 | 2007-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitors for treating arthropathies |
TR200003879T2 (tr) | 1998-07-06 | 2007-01-22 | Janssen Pharmaceutica N.V. | İn vivo ışın tedavisine duyarlılaştırıcı özelliklere sahip farnesil protein transferaz inhibitörleri@ |
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 |
ATE240327T1 (de) | 1998-12-23 | 2003-05-15 | Janssen Pharmaceutica Nv | 1,2-annelierte chinolinderivate |
US6248736B1 (en) | 1999-01-08 | 2001-06-19 | Pharmacia & Upjohn Company | 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents |
US6248739B1 (en) | 1999-01-08 | 2001-06-19 | Pharmacia & Upjohn Company | Quinolinecarboxamides as antiviral agents |
EA200100766A1 (ru) | 1999-02-11 | 2002-02-28 | Пфайзер Продактс Инк. | Хинолин-2-он замещенные гетероарильные производные, используемые в качестве противоопухолевых агентов |
PT1106612E (pt) | 1999-11-30 | 2004-06-30 | Pfizer Prod Inc | Derivados de quinolina uteis para inibir a farnesil-proteina-transferase |
ES2262626T3 (es) | 2000-02-04 | 2006-12-01 | Janssen Pharmaceutica N.V. | Inhibidores de farnesil proteina transferasa para tratar cancer de mama. |
DE60130976T2 (de) | 2000-02-24 | 2008-07-17 | Janssen Pharmaceutica N.V. | Dosierschema enthaldend farnesyl protein transferase inhibitoren für die behandlung von krebs |
WO2001064198A2 (en) | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with anti-tumor podophyllotoxin derivatives |
CA2397475A1 (en) | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with vinca alkaloids |
AU2001240658A1 (en) | 2000-02-29 | 2001-09-12 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with camptothecin compounds |
CA2397425A1 (en) | 2000-02-29 | 2001-09-07 | Ivan David Horak | Farnesyl protein transferase inhibitor combinations with taxane compounds |
JP2003525237A (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 | 抗腫瘍性アントラサイクリン誘導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 |
AU2001252147A1 (en) | 2000-02-29 | 2001-09-12 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations |
AU2001256166A1 (en) | 2000-02-29 | 2001-09-12 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with anti-tumor nucleoside derivatives |
US20030022918A1 (en) | 2000-02-29 | 2003-01-30 | Horak Ivan David | Farnesyl protein transferase inhibitor combinations with an her2 antibody |
EP1261356A2 (en) | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with platinum compounds |
EP1261374A2 (en) | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with further anti-cancer agents |
EP1261348A2 (en) | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Combinations of a farnesyl protein transferase inhibitor with nitrogen mustard or nitrosourea alkylating agents |
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 |
ATE321038T1 (de) | 2000-09-25 | 2006-04-15 | Janssen Pharmaceutica Nv | Chinolin- und chinazolinderivate und deren verwendung als farnesyl transferase inhibitoren |
ES2313991T3 (es) | 2000-09-25 | 2009-03-16 | Janssen Pharmaceutica Nv | Derivados de 6-heterociclilmetil-quinolina y quinazolina que inhiben la farnesil transferasa. |
AU2001293835A1 (en) | 2000-09-25 | 2002-04-02 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives |
BR0114253A (pt) | 2000-10-02 | 2003-07-01 | Janssen Pharmaceutica Nv | Antagonistas de receptor de glutamato metabotrópico |
WO2002043733A1 (en) | 2000-11-28 | 2002-06-06 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitors for the treatment of inflammatory bowel disease |
WO2002051835A1 (en) | 2000-12-27 | 2002-07-04 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 4-substituted quinoline and quinazoline derivatives |
EP1365763B1 (en) | 2001-02-15 | 2008-11-26 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with antiestrogen agents |
WO2002070487A1 (en) | 2001-03-01 | 2002-09-12 | 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 |
WO2003000705A1 (en) | 2001-06-21 | 2003-01-03 | Ariad Pharmaceuticals, Inc. | Novel quinolines and uses thereof |
BR0215067A (pt) | 2001-12-20 | 2004-11-09 | Upjohn Co | Piridoquinoxalinas antivirais |
JP2005530681A (ja) | 2001-12-20 | 2005-10-13 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | ピリドキノキサリン抗ウイルス剤 |
NZ535438A (en) | 2002-03-29 | 2006-08-31 | Janssen Pharmaceutica Nv | Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands |
EP2045242A1 (en) | 2002-08-13 | 2009-04-08 | Shionogi&Co., Ltd. | Heterocyclic compounds having inhibitory activity against HIV integrase |
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 |
EP2287165A3 (en) | 2003-07-14 | 2011-06-22 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
WO2005054201A1 (en) | 2003-11-20 | 2005-06-16 | Janssen Pharmaceutica N.V. | 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors |
CN1890224B (zh) | 2003-12-05 | 2011-06-08 | 詹森药业有限公司 | 用作聚(adp-核糖)聚合酶抑制剂的6-取代的2-喹啉酮和2-喹喔啉酮 |
UA91007C2 (ru) | 2003-12-10 | 2010-06-25 | Янссен Фармацевтика Н.В. | Замещенные 6-циклогексилалкилом замещенные 2-хинолиноны и 2-хиноксалиноны как ингибиторы поли-(адф-рибоза)полимеразы |
TW200529845A (en) | 2003-12-12 | 2005-09-16 | Wyeth Corp | Quinolines useful in treating cardiovascular disease |
DK1711181T3 (da) | 2004-01-23 | 2010-02-01 | Janssen Pharmaceutica Nv | Quinolin-derivater og anvendelse af disse som mycobakterielle inhibitorer |
CA2554049C (en) | 2004-01-29 | 2012-12-18 | Janssen Pharmaceutica N.V. | Quinoline derivatives for use as mycobacterial inhibitors |
DE602005026391D1 (de) | 2004-06-30 | 2011-03-31 | Janssen Pharmaceutica Nv | Chinazolinonderivate als parp-hemmer |
WO2006013896A1 (ja) | 2004-08-04 | 2006-02-09 | Meiji Seika Kaisha, Ltd. | キノリン誘導体およびそれを有効成分として含んでなる殺虫剤 |
KR100686531B1 (ko) | 2004-08-31 | 2007-02-23 | 한국화학연구원 | 히스톤 디아세틸라제 저해활성을 갖는 아릴아미노메틸프로페닐 벤즈하이드록시아마이드 유도체 및 그의 제조방법 |
EP1815247B1 (en) | 2004-11-05 | 2013-02-20 | Janssen Pharmaceutica NV | Therapeutic use of farnesyltransferase inhibitors and methods of monitoring the efficacy thereof |
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 |
JP5112083B2 (ja) | 2006-02-03 | 2013-01-09 | Meiji Seikaファルマ株式会社 | 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 |
PT2081937E (pt) | 2006-10-23 | 2012-10-15 | Sgx Pharmaceuticals Inc | Moduladores de proteína-cinase de triazolo-piridazina |
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 |
WO2008112525A2 (en) | 2007-03-09 | 2008-09-18 | Link Medicine Corporation | Treatment of lysosomal storage diseases |
JP2010528991A (ja) | 2007-05-21 | 2010-08-26 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | 複素環式キナーゼ調節因子 |
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 |
US8227499B2 (en) | 2008-01-18 | 2012-07-24 | Allergan, Inc. | Substituted-aryl-(imidazole)-methyl)-phenyl compounds as subtype selective modulators of alpha 2B and/or alpha 2C adrenergic receptors |
CA2714232A1 (en) | 2008-02-05 | 2009-08-13 | Pfizer Inc. | Pyridinyl amides for the treatment of cns and metabolic disorders |
CA2724293A1 (en) | 2008-05-13 | 2009-11-19 | Allergan, Inc. | Quinolynylmethylimidizoles as therapeutic agents |
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 |
TW201111362A (en) | 2009-06-25 | 2011-04-01 | Amgen Inc | Heterocyclic compounds and their uses |
KR20120089463A (ko) | 2009-08-20 | 2012-08-10 | 노파르티스 아게 | 헤테로시클릭 옥심 화합물 |
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 |
WO2011112264A1 (en) | 2010-03-11 | 2011-09-15 | New York University | Compounds as rorϒt modulators and uses thereof |
JP2013523192A (ja) | 2010-04-15 | 2013-06-17 | クロモセル コーポレーション | 苦味を低減または排除する化合物、組成物、および方法 |
JP6063870B2 (ja) * | 2010-11-08 | 2017-01-18 | ライセラ・コーポレイション | RORγ活性の阻害用のN−スルホニル化テトラヒドロキノリンおよび関連二環化合物および病気の治療 |
EP2678052B1 (en) | 2011-02-24 | 2018-09-26 | Emory University | Jab1 blocking compositions for ossification and methods related thereto |
US8604069B2 (en) | 2011-04-28 | 2013-12-10 | Japan Tobacco Inc. | Amide compound and medicinal use thereof |
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) |
WO2013079223A1 (en) | 2011-12-02 | 2013-06-06 | Phenex Pharmaceuticals Ag | Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rorϒ, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases |
-
2013
- 2013-10-15 SG SG11201502935VA patent/SG11201502935VA/en unknown
- 2013-10-15 EP EP13818857.8A patent/EP2909193B1/en active Active
- 2013-10-15 JP JP2015537770A patent/JP6251277B2/ja not_active Expired - Fee Related
- 2013-10-15 CA CA2888485A patent/CA2888485C/en active Active
- 2013-10-15 AU AU2013331505A patent/AU2013331505A1/en not_active Abandoned
- 2013-10-15 CN CN201380065774.6A patent/CN105073729A/zh active Pending
- 2013-10-15 KR KR1020157012866A patent/KR20150070350A/ko not_active Application Discontinuation
- 2013-10-15 ES ES13818857T patent/ES2628365T3/es active Active
- 2013-10-15 WO PCT/US2013/065026 patent/WO2014062667A1/en active Application Filing
- 2013-10-15 US US14/053,707 patent/US9309222B2/en active Active
- 2013-10-15 MX MX2015004784A patent/MX2015004784A/es unknown
- 2013-10-15 PE PE2015000492A patent/PE20151203A1/es not_active Application Discontinuation
- 2013-10-15 EA EA201590750A patent/EA201590750A1/ru unknown
-
2015
- 2015-04-02 IL IL238122A patent/IL238122A0/en unknown
- 2015-04-08 PH PH12015500776A patent/PH12015500776A1/en unknown
- 2015-04-13 CR CR20150192A patent/CR20150192A/es unknown
- 2015-04-15 CO CO15084078A patent/CO7350658A2/es unknown
- 2015-04-15 CL CL2015000946A patent/CL2015000946A1/es unknown
- 2015-04-15 GT GT201500092A patent/GT201500092A/es unknown
- 2015-04-16 EC ECIEPI201515155A patent/ECSP15015155A/es unknown
-
2016
- 2016-02-18 HK HK16101837.7A patent/HK1213887A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
CL2015000946A1 (es) | 2015-10-02 |
CA2888485C (en) | 2021-01-26 |
GT201500092A (es) | 2015-12-31 |
EA201590750A1 (ru) | 2015-09-30 |
PE20151203A1 (es) | 2015-08-31 |
HK1213887A1 (zh) | 2016-07-15 |
KR20150070350A (ko) | 2015-06-24 |
US20140107097A1 (en) | 2014-04-17 |
PH12015500776A1 (en) | 2015-06-22 |
CA2888485A1 (en) | 2014-04-24 |
EP2909193A1 (en) | 2015-08-26 |
EP2909193B1 (en) | 2017-04-19 |
IL238122A0 (en) | 2015-05-31 |
CR20150192A (es) | 2015-05-18 |
CO7350658A2 (es) | 2015-08-10 |
ECSP15015155A (es) | 2016-01-29 |
JP2015536321A (ja) | 2015-12-21 |
JP6251277B2 (ja) | 2017-12-20 |
WO2014062667A1 (en) | 2014-04-24 |
AU2013331505A1 (en) | 2015-04-30 |
MX2015004784A (es) | 2015-08-14 |
CN105073729A (zh) | 2015-11-18 |
US9309222B2 (en) | 2016-04-12 |
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 | |
ES2619610T3 (es) | Moduladores de ROR-gamma-t de quinolinilo enlazado con heteroarilo | |
ES2632269T3 (es) | Moduladores de quinolinailo enlazados a metileno de ROR-gamma-t | |
ES2659397T3 (es) | 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas | |
AR101586A1 (es) | Derivados heterocíclicos con sustituyentes que contienen azufre activos como plaguicidas | |
AR092266A1 (es) | Inhibidores de ddr2 para el tratamiento de osteoartritis | |
ES2635318T3 (es) | Moduladores P2X7 | |
AR090867A1 (es) | Compuestos y composiciones plaguicidas y procesos relacionados | |
NZ732810A (en) | Picolinamides and other compounds | |
NZ732649A (en) | Picolinamides and related compounds | |
ES2526352T3 (es) | Derivados de piridazinona | |
AR052898A1 (es) | Derivados de la n-[(4,5-difenil -2-tienil) metil] amina, su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para enfermedades mediadas por los receptores canabinoides cb1 | |
AR095208A1 (es) | Pirrolotriazinas como inhibidores del canal del ión potasio | |
ES2530519T3 (es) | Compuestos macrocíclicos completamente sintéticos, con conformación restringida | |
AR115662A2 (es) | Derivados de piperidina | |
AR089889A1 (es) | Compuestos fungicidas de pirimidina | |
PE20120657A1 (es) | Compuesto para el tratamiento de trastornos metabolicos | |
AR102480A1 (es) | ALCOHOLES TRIFLUOROMETÍLICOS COMO MODULADORES DE RORgt | |
AR077364A1 (es) | Derivados de 6-oxo-1,6- dihidro -pirimidin-2-il-) amida, su preparacion y su utilizacion farmaceutica como inhibidores de fosforilacion de akt (pkb) | |
AR103414A1 (es) | Derivados de hidroxialquil-piperazina como moduladores del receptor cxcr3 | |
AR114430A1 (es) | Compuestos herbicidas | |
AR076310A1 (es) | 4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2,composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes,obesidad y otras enfermedades. | |
AR114374A1 (es) | Compuestos herbicidas |