ES2659397T3 - 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas - Google Patents

2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas Download PDF

Info

Publication number
ES2659397T3
ES2659397T3 ES14717576.4T ES14717576T ES2659397T3 ES 2659397 T3 ES2659397 T3 ES 2659397T3 ES 14717576 T ES14717576 T ES 14717576T ES 2659397 T3 ES2659397 T3 ES 2659397T3
Authority
ES
Spain
Prior art keywords
alkyl
pyridyl
oxadiazolyl
pyridazinyl
pyrimidinyl
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
ES14717576.4T
Other languages
English (en)
Inventor
Christine F. GELIN
Terry P. LEBOLD
Brock T. Shireman
Jeannie M. ZIFF
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 ES2659397T3 publication Critical patent/ES2659397T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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 groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto de fórmula I**Fórmula** o un enantiómero, diastereómero, tautómero o variante isotópica de los mismos; o una sal o solvato farmacéuticamente aceptable del mismo; donde X es N o CR1; Y es N o CR2; R1 es H, alcoxi, halo, triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo, en donde triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo está opcionalmente sustituido con hasta dos sustituyentes seleccionados de entre el grupo constituido por halo y alquilo; R2 es H, alquilo, alcoxi, o halo; Z es NH, N-CH3, N-CH2CH3, N-CH2-ciclopropilo, NC(>=O)CH3, N-CH2CH2OCH3 o O; R3 es H, alquilo, alcoxi, halo, triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo, en donde triazolilo, tiazolilo, piridazinilo, pirimidinilo, oxazolilo, isoxazolilo, oxadiazolilo, piridilo, fenilo o pirazolilo está opcionalmente sustituido con hasta dos sustituyentes seleccionados de entre el grupo constituido por halo y alquilo; R4 es H o alquilo; o R3 y R4, junto con los átomos a los que están unidos, forman un anillo arilo de 6 miembros o un anillo heteroarilo de 5 ó 6 miembros; R5 es fenilo, piridilo, pirazinilo, benzoxazolilo, piridazinilo, naftiridinilo o pirimidinilo, en el que el piridilo, pirazinilo, benzoxazolilo, piridazinilo, naftiridinilo o pirimidinilo está opcionalmente sustituido con hasta dos grupos seleccionados de entre el grupo constituido por halo, alcoxi, hidroximetilo y alquilo; y n es 1 o 2, en donde "alquilo" es un grupo de cadena lineal o ramificada de alquilo que tiene de 1 a 12 átomos de carbono en la cadena o un grupo hidrocarburo mono-cíclico no aromático que tiene de 3 a 7 átomos de carbono y está opcionalmente sustituido con uno o más átomos de halógeno.
ES14717576.4T 2013-03-13 2014-03-12 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas Active ES2659397T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361780378P 2013-03-13 2013-03-13
US201361780378P 2013-03-13
PCT/US2014/024293 WO2014165070A1 (en) 2013-03-13 2014-03-12 Substituted 2-azabicycles and their use as orexin receptor modulators

Publications (1)

Publication Number Publication Date
ES2659397T3 true ES2659397T3 (es) 2018-03-15

Family

ID=50487148

Family Applications (3)

Application Number Title Priority Date Filing Date
ES19193122T Active ES2950032T3 (es) 2013-03-13 2014-03-12 2-Azabiciclos sustituidos y su uso como moduladores del receptor de orexina
ES14717576.4T Active ES2659397T3 (es) 2013-03-13 2014-03-12 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas
ES17206491T Active ES2760564T3 (es) 2013-03-13 2014-03-12 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES19193122T Active ES2950032T3 (es) 2013-03-13 2014-03-12 2-Azabiciclos sustituidos y su uso como moduladores del receptor de orexina

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES17206491T Active ES2760564T3 (es) 2013-03-13 2014-03-12 2-azabicíclicos sustituidos y su uso como moduladores receptores de orexinas

Country Status (38)

Country Link
US (5) US9611277B2 (es)
EP (4) EP3363438B1 (es)
JP (1) JP6275815B2 (es)
KR (1) KR102209424B1 (es)
CN (3) CN108864093A (es)
AR (1) AR095423A1 (es)
AU (2) AU2014248680B2 (es)
BR (1) BR112015022294B1 (es)
CA (1) CA2904618C (es)
CL (1) CL2015002609A1 (es)
CR (2) CR20210523A (es)
CY (3) CY1120024T1 (es)
DK (2) DK2970314T3 (es)
EA (1) EA029276B1 (es)
ES (3) ES2950032T3 (es)
HR (3) HRP20180303T1 (es)
HU (3) HUE036193T2 (es)
IL (2) IL240466B (es)
JO (1) JOP20140092B1 (es)
LT (2) LT2970314T (es)
ME (2) ME03011B (es)
MX (2) MX368466B (es)
MY (1) MY183725A (es)
NI (1) NI201500130A (es)
NO (1) NO3107630T3 (es)
PE (1) PE20151599A1 (es)
PH (1) PH12015501929B1 (es)
PL (3) PL3363438T3 (es)
PT (2) PT3363438T (es)
RS (3) RS56875B1 (es)
SG (1) SG11201507415QA (es)
SI (2) SI3363438T1 (es)
SM (3) SMT201800056T1 (es)
TW (1) TWI621618B (es)
UA (1) UA118669C2 (es)
UY (1) UY35409A (es)
WO (1) WO2014165070A1 (es)
ZA (1) ZA201507562B (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2585806T3 (es) 2009-10-23 2016-10-10 Janssen Pharmaceutica N.V. Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
TWI621618B (zh) * 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途
TW201444821A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
JP6262885B2 (ja) * 2014-03-06 2018-01-17 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. オレキシン受容体拮抗剤としてのピペリジン誘導体
AU2015314851B2 (en) * 2014-09-11 2020-01-02 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators
US9938276B2 (en) * 2014-12-19 2018-04-10 Merck Sharp & Dohme Corp. 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
WO2017012502A1 (en) 2015-07-17 2017-01-26 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
WO2017028732A1 (zh) * 2015-08-14 2017-02-23 上海海雁医药科技有限公司 食欲素受体拮抗剂化合物的晶型及其制备方法和应用
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼの阻害剤
SG11201804223TA (en) 2015-11-23 2018-06-28 Sunshine Lake Pharma Co Ltd OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
HRP20220642T1 (hr) 2016-03-10 2022-06-24 Janssen Pharmaceutica Nv Postupci za liječenje depresije uporabom antagonista receptora oreksina 2
CA3252823A1 (en) 2016-06-13 2025-02-25 Gilead Sciences, Inc. Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds
BR112018075734A2 (pt) 2016-06-13 2019-04-02 Gilead Sciences, Inc. composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto.
EP3544971B1 (en) 2016-11-22 2022-07-06 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof
CN110461328A (zh) 2017-03-28 2019-11-15 吉利德科学公司 治疗肝疾病的治疗组合
GB2558975B (en) * 2017-09-01 2019-01-23 Chronos Therapeutics Ltd Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists
EP3676261B1 (en) * 2017-09-01 2024-12-18 Chronos Therapeutics Limited Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists
JP7590185B2 (ja) 2018-06-25 2024-11-26 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド Taireファミリーキナーゼインヒビターおよびそれらの使用
AU2019395255B2 (en) * 2018-12-14 2025-02-27 Dana-Farber Cancer Institute, Inc. Pyrazolopyridine inhibitors of c-Jun-N-terminal kinases and uses thereof
WO2020140098A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
EP4360632B1 (en) 2019-01-15 2025-10-29 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
US11524005B2 (en) 2019-02-19 2022-12-13 Gilead Sciences, Inc. Solid forms of FXR agonists

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3674793A (en) 1967-03-29 1972-07-04 Sterling Drug Inc 6-hydroxy-2-azabicyclo(2.2.2)octan-3-ones and 2-azabicyclo(2.2.2.)octane-3,6-diones
US6505492B2 (en) 2001-04-11 2003-01-14 Bethlehem Steel Corporation Method and apparatus for forming deep-drawn articles
EP1396488A1 (en) 2001-05-23 2004-03-10 Mitsubishi Pharma Corporation Fused heterocyclic compound and medicinal use thereof
WO2004069816A1 (en) 2003-02-07 2004-08-19 Ranbaxy Laboratories Limited Oxazolidinone derivatives as antimicrobials
BRPI0407714A (pt) 2003-02-21 2006-02-14 Pharmacia & Up John Company Ll "exo-2r (+)-2-amino-7-azabiciclo[2.2.1]heptano-7-carboxilato de t-butila, intermediário, e processo para os preparar e isolar
AR058554A1 (es) 2005-12-20 2008-02-13 Novartis Ag Compuestos heterociclicos nitrogenados de 6 miembros sustituidos, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por mglur5.
EP2272509A1 (en) 2006-09-11 2011-01-12 Novartis AG New Uses of metabotropic glutamate receptors
US8133901B2 (en) 2006-12-01 2012-03-13 Actelion Pharmaceuticals Ltd. 3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors
TW200833328A (en) 2006-12-28 2008-08-16 Actelion Pharmaceuticals Ltd 2-aza-bicyclo[3.1.0]hexane derivatives
US8030495B2 (en) 2007-05-23 2011-10-04 Coleman Paul J Cyclopropyl pyrrolidine orexin receptor antagonists
TW200904440A (en) 2007-07-17 2009-02-01 Bristol Myers Squibb Co Method for modulating GPR119 G protein-coupled receptor and selected compounds
CA2705411A1 (en) 2007-12-21 2009-07-02 F. Hoffmann-La Roche Ag Heteroaryl derivatives as orexin receptor antagonists
BRPI0908096A2 (pt) * 2008-02-21 2015-08-25 Actelion Pharmaceuticals Ltd Derivado de 2-aza-biciclo [2.2.1] heptano
CN102015645B (zh) 2008-04-30 2012-11-14 埃科特莱茵药品有限公司 哌啶和吡咯烷化合物
MX2011000664A (es) 2008-07-16 2011-02-24 Schering Corp Derivados biciclicos heterociclicos y uso de los mismos como moduladores de gpr119.
WO2010048016A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
JP2012506375A (ja) 2008-10-21 2012-03-15 メルク・シャープ・エンド・ドーム・コーポレイション 2,5−二置換ピペリジンオレキシン受容体アンタゴニスト
CA2745433A1 (en) 2008-12-02 2010-06-10 Glaxo Group Ltd. N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof
AR076024A1 (es) 2009-04-03 2011-05-11 Schering Corp Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos
US20120040991A1 (en) 2009-04-24 2012-02-16 Glaxo Group Limited 3-azabicyclo [4.1.0] heptanes used as orexin antagonists
WO2011050202A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
EP2491034B1 (en) 2009-10-23 2013-12-18 Janssen Pharmaceutica, N.V. Fused heterocyclic compounds as orexin receptor modulators
ES2585806T3 (es) 2009-10-23 2016-10-10 Janssen Pharmaceutica N.V. Octahidropirrolo [3,4-c] pirroles disustituidos como moduladores de receptores de orexina
CA2778684A1 (en) 2009-10-29 2011-05-05 Schering Corporation Bridged bicyclic piperidine derivatives and methods of use thereof
WO2011066137A1 (en) 2009-11-24 2011-06-03 Schering Corporation Substituted biaryl derivatives and methods of use thereof
AU2010332010A1 (en) 2009-12-14 2012-08-02 Inspire Pharmaceuticals, Inc. Bridged bicyclic Rho kinase inhibitor compounds, composition and use
WO2011087812A1 (en) 2009-12-21 2011-07-21 Vanderbilt University Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective m1 agonists and methods of making and using same
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
US20130096141A1 (en) 2010-06-18 2013-04-18 Bernard R. Neustadt Bicyclic heterocycle derivatives and methods of use thereof
WO2012089606A1 (en) 2010-12-28 2012-07-05 Glaxo Group Limited Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists
WO2012145581A1 (en) 2011-04-20 2012-10-26 Janssen Pharmaceutica Nv Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
WO2014066196A1 (en) 2012-10-23 2014-05-01 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-substituted-4-nitrile orexin receptor antagonists
MX2015006191A (es) 2012-11-16 2015-08-10 Merck Sharp & Dohme Inhibidores de purina de fosfatidilinositol 3-quinasa delta humana.
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途
JP6532474B2 (ja) 2014-02-06 2019-06-19 アッヴィ・インコーポレイテッド 6−ヘテロアリールオキシ−および6−アリールオキシ−キノリン−2−カルボキシアミドならびにその使用
AU2015314851B2 (en) 2014-09-11 2020-01-02 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators

Also Published As

Publication number Publication date
EP3363438B1 (en) 2019-09-18
EP4272824A3 (en) 2024-01-10
RS56875B1 (sr) 2018-04-30
US9447117B2 (en) 2016-09-20
AU2014248680A1 (en) 2015-08-27
KR20150126694A (ko) 2015-11-12
CY1126106T1 (el) 2023-11-15
CN108864093A (zh) 2018-11-23
EP3622956C0 (en) 2023-06-07
US9845333B2 (en) 2017-12-19
SI3363438T1 (sl) 2019-11-29
MY183725A (en) 2021-03-10
AU2018204835B2 (en) 2019-08-08
EP3622956A1 (en) 2020-03-18
HUE036193T2 (hu) 2018-06-28
EP2970314A1 (en) 2016-01-20
IL240466A0 (en) 2015-09-24
CY1122392T1 (el) 2021-01-27
CA2904618A1 (en) 2014-10-09
US20150174129A1 (en) 2015-06-25
UA118669C2 (uk) 2019-02-25
US20160052939A1 (en) 2016-02-25
CN105308048A (zh) 2016-02-03
EP3622956B1 (en) 2023-06-07
PL3622956T3 (pl) 2023-09-18
RS64551B9 (sr) 2023-12-29
KR102209424B1 (ko) 2021-01-29
PH12015501929A1 (en) 2016-01-04
CN105308048B (zh) 2019-10-08
US20170015651A1 (en) 2017-01-19
SMT202300223T1 (it) 2023-09-06
JP6275815B2 (ja) 2018-02-07
MX2015011815A (es) 2016-11-07
PT2970314T (pt) 2018-03-05
IL240466B (en) 2019-03-31
US20170204096A1 (en) 2017-07-20
PE20151599A1 (es) 2015-11-12
PL3363438T3 (pl) 2020-02-28
NO3107630T3 (es) 2018-01-06
PT3363438T (pt) 2019-12-11
EP4272824A2 (en) 2023-11-08
CR20150433A (es) 2015-10-26
AU2018204835A1 (en) 2018-07-19
PH12015501929B1 (en) 2016-01-04
WO2014165070A1 (en) 2014-10-09
NI201500130A (es) 2015-11-30
SI2970314T1 (en) 2018-02-28
US20140275118A1 (en) 2014-09-18
EP3363438A1 (en) 2018-08-22
TWI621618B (zh) 2018-04-21
US9611277B2 (en) 2017-04-04
SG11201507415QA (en) 2015-10-29
CR20210523A (es) 2021-11-19
MX368466B (es) 2019-10-03
BR112015022294B1 (pt) 2022-09-13
AR095423A1 (es) 2015-10-14
CY1120024T1 (el) 2018-12-12
SMT201800056T1 (it) 2018-03-08
HRP20180303T1 (hr) 2018-03-23
DK3363438T3 (da) 2019-11-11
ZA201507562B (en) 2019-04-24
AU2014248680B2 (en) 2018-07-26
CL2015002609A1 (es) 2016-03-28
EP2970314B1 (en) 2017-12-13
HUE063608T2 (hu) 2024-01-28
US8969352B2 (en) 2015-03-03
CN110669052A (zh) 2020-01-10
EA201591703A1 (ru) 2016-02-29
HRP20192032T1 (hr) 2020-02-07
ES2950032T3 (es) 2023-10-04
NZ710872A (en) 2020-10-30
HUE047592T2 (hu) 2020-05-28
TW201446757A (zh) 2014-12-16
JOP20140092B1 (ar) 2021-08-17
CA2904618C (en) 2021-12-07
ES2760564T3 (es) 2020-05-14
IL264606A (en) 2019-02-28
RS64551B1 (sr) 2023-10-31
LT3363438T (lt) 2019-11-11
MX361529B (es) 2018-12-07
BR112015022294A2 (pt) 2017-07-18
DK2970314T3 (en) 2018-02-26
ME03011B (me) 2018-10-20
JP2016512535A (ja) 2016-04-28
SMT201900655T1 (it) 2020-01-14
US10183953B2 (en) 2019-01-22
HK1219725A1 (en) 2017-04-13
EP3622956B9 (en) 2023-09-27
ME03572B (me) 2020-07-20
UY35409A (es) 2014-09-30
LT2970314T (lt) 2018-02-12
CN110669052B (zh) 2022-10-11
PL2970314T3 (pl) 2018-05-30
EA029276B1 (ru) 2018-03-30
HRP20230633T1 (hr) 2023-09-29
RS59466B1 (sr) 2019-11-29

Similar Documents

Publication Publication Date Title
NI201500130A (es) 2-azabiciclo sustituidos y su uso como moduladores del receptor de orexina
AR115662A2 (es) Derivados de piperidina
ES2659222T3 (es) 7-azabicíclicos sustituidos y su uso para moduladores de receptores de orexina
AR095422A1 (es) Compuestos de piperidina sustituidos y su uso como moduladores de receptores de orexina
ES2635318T3 (es) Moduladores P2X7
CR20160548A (es) Nuevos Derivados de Pirazolo Pirimidina y su Uso como Inhibidores de MALT1
AR088226A1 (es) Derivados piperidinicos heterociclicos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades neurodegenerativas
AR099677A1 (es) Compuesto heterocíclico fusionado y su uso para el control de plagas
EA201591429A1 (ru) 2,3-дизамещенные производные 1-ацил-4-амино-1,2,3,4-тетрагидрохинолинов и их применение в качестве ингибиторов бромодомена
AR097866A1 (es) Derivados de 4-azaindol
ES2662444T3 (es) Derivado de piridina
AR110282A1 (es) Compuestos de amida bicíclica y uso de éstos en el tratamiento de enfermedades mediadas por rip1
AR103742A1 (es) Derivados de trifluorometilpropanamida
CL2020002588A1 (es) Compuestos derivados de indol, composiciones que los contienen, útiles en el tratamiento de infestación por helmintos, preferentemente trematodos, en mamíferos. (divisional de solicitud n° 03258-2016)
MX2016017405A (es) Compuestos derivados de 2-(3-piridinil)-1h-benzimidazol y medicamentos que los contienen.
AR113811A1 (es) Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos
AR095570A1 (es) Derivados de urea
AR063374A1 (es) Derivados de benzoxazina y sus usos
AR083861A1 (es) OXAZOLIDINONAS COMO MODULADORES DE mGluR5 Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
ES2667276T3 (es) Derivados de sulfonilindol y método para prepararlos
ES2721525T3 (es) Novedosos agonistas de EP4 como compuestos terapéuticos
AR099820A1 (es) Ciano que contiene compuestos de azabenzofuran para el tratamiento de la hepatitis c
AR094381A1 (es) Derivados benzodioxano-piperidina y sus aplicaciones terapéuticas para el tratamiento de trastornos neuropsiquiátricos
AR110226A1 (es) Inhibidores selectivos de hdac1,2
AR107187A1 (es) Compuesto de oxadiazol y uso del mismo