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CU20160063A7 - Derivados de pirazol fusionados activos como moduladores del receptor de farnesoide x - Google Patents

Derivados de pirazol fusionados activos como moduladores del receptor de farnesoide x

Info

Publication number
CU20160063A7
CU20160063A7 CUP2016000063A CU20160063A CU20160063A7 CU 20160063 A7 CU20160063 A7 CU 20160063A7 CU P2016000063 A CUP2016000063 A CU P2016000063A CU 20160063 A CU20160063 A CU 20160063A CU 20160063 A7 CU20160063 A7 CU 20160063A7
Authority
CU
Cuba
Prior art keywords
farnesoid
fusioned
active
receptor modulators
pirazol derivatives
Prior art date
Application number
CUP2016000063A
Other languages
English (en)
Other versions
CU24375B1 (es
Inventor
Donatella Chianelli
Xiaodong Liu
Valentina Molteni
John Nelson
Jason Roland
Paul Rucker
David Tully
Original Assignee
Novartis Ag
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51982773&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CU20160063(A7) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20160063A7 publication Critical patent/CU20160063A7/es
Publication of CU24375B1 publication Critical patent/CU24375B1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)

Abstract

La presente invención se relaciona con compuestos derivados de pirazol fusionados de Ia formula I: ESPACIO PARA FÓRMULA un estereoisómero, enantiómero, una sal farmacéuticamente aceptable o un conjugado aminoácido del mismo; en donde las variables son como se definen en el presente documento; y sus composiciones farmacéuticas, que son útiles como moduladores de Ia actividad de los receptores X farnesoides (FXR).
CU2016000063A 2013-11-05 2014-11-04 Derivados de pirazol fusionados activos como moduladores del receptor de farnesoide x CU24375B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361900013P 2013-11-05 2013-11-05
PCT/US2014/063948 WO2015069666A1 (en) 2013-11-05 2014-11-04 Compositions and methods for modulating farnesoid x receptors

Publications (2)

Publication Number Publication Date
CU20160063A7 true CU20160063A7 (es) 2016-09-30
CU24375B1 CU24375B1 (es) 2018-12-05

Family

ID=51982773

Family Applications (1)

Application Number Title Priority Date Filing Date
CU2016000063A CU24375B1 (es) 2013-11-05 2014-11-04 Derivados de pirazol fusionados activos como moduladores del receptor de farnesoide x

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US (5) US9682939B2 (es)
EP (1) EP3065738B1 (es)
JP (1) JP6424231B2 (es)
KR (1) KR102350357B1 (es)
CN (1) CN105682656B (es)
AP (1) AP2016009165A0 (es)
AR (1) AR098316A1 (es)
AU (1) AU2014346919B2 (es)
BR (1) BR112016009630B1 (es)
CA (1) CA2927705C (es)
CL (1) CL2016000982A1 (es)
CR (1) CR20160212A (es)
CU (1) CU24375B1 (es)
CY (1) CY1120273T1 (es)
DK (1) DK3065738T3 (es)
EA (1) EA030430B1 (es)
ES (1) ES2670984T3 (es)
GT (1) GT201600085A (es)
HR (1) HRP20180817T1 (es)
HU (1) HUE039155T2 (es)
IL (1) IL245242B (es)
JO (1) JO3454B1 (es)
LT (1) LT3065738T (es)
MA (1) MA39088B1 (es)
MX (1) MX364834B (es)
MY (1) MY175903A (es)
NO (1) NO3105103T3 (es)
NZ (1) NZ719078A (es)
PE (1) PE20160682A1 (es)
PH (1) PH12016500777B1 (es)
PL (1) PL3065738T3 (es)
PT (1) PT3065738T (es)
RS (1) RS57179B1 (es)
SG (1) SG11201603026PA (es)
SI (1) SI3065738T1 (es)
SV (1) SV2016005192A (es)
TN (1) TN2016000143A1 (es)
TR (1) TR201807321T4 (es)
TW (1) TWI662027B (es)
UY (1) UY35818A (es)
WO (1) WO2015069666A1 (es)
ZA (1) ZA201602555B (es)

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EA030430B1 (ru) 2013-11-05 2018-08-31 Новартис Аг Композиции и способы модуляции фарнезоидных х-рецепторов
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US10351576B2 (en) 2015-04-30 2019-07-16 Novartis Ag Fused tricyclic pyrazole derivatives useful for farnesoid X receptors
RU2743075C2 (ru) 2016-02-22 2021-02-15 Новартис Аг Способы применения агонистов fxr
SG11201810600WA (en) 2016-06-13 2018-12-28 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (NR1H4)
KR20210110407A (ko) * 2016-09-14 2021-09-07 노파르티스 아게 Fxr 작용제의 신규 요법
JOP20190040A1 (ar) * 2016-09-14 2019-03-10 Novartis Ag توليفة من ناهضات fxr
MX2019003889A (es) * 2016-10-05 2019-08-12 Novartis Ag Composiciones de combinacion que comprenden agonistas de fxr para tratar o prevenir una enfermedad o trastorno fibrotico o cirrotico.
CN107973790A (zh) * 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
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EP3759077A1 (en) 2018-03-02 2021-01-06 Inflazome Limited Novel compounds
JOP20210017A1 (ar) 2018-07-25 2021-01-21 Novartis Ag مثبطات جسيم التهابي nlrp3
BR112021011762A2 (pt) 2019-01-15 2021-11-03 Gilead Sciences Inc Compostos para modulação de fxr (nr1h4)
US10610280B1 (en) 2019-02-02 2020-04-07 Ayad K. M. Agha Surgical method and apparatus for destruction and removal of intraperitoneal, visceral, and subcutaneous fat
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UY38687A (es) 2019-05-17 2023-05-15 Novartis Ag Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso
EP3999101A1 (en) 2019-07-18 2022-05-25 ENYO Pharma Method for decreasing adverse-effects of interferon
WO2021044351A1 (en) 2019-09-06 2021-03-11 Novartis Ag Methods of treating liver disease using lta4h inhibitors
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US10351576B2 (en) 2015-04-30 2019-07-16 Novartis Ag Fused tricyclic pyrazole derivatives useful for farnesoid X receptors

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SV2016005192A (es) 2016-11-21
IL245242A0 (en) 2016-06-30
NO3105103T3 (es) 2018-05-12
CY1120273T1 (el) 2019-07-10
ZA201602555B (en) 2017-06-28
ES2670984T3 (es) 2018-06-04
LT3065738T (lt) 2018-05-10
HRP20180817T1 (hr) 2018-06-29
US20200247757A1 (en) 2020-08-06
RS57179B1 (sr) 2018-07-31
BR112016009630B1 (pt) 2021-02-09
KR102350357B1 (ko) 2022-01-14
NZ719078A (en) 2018-07-27
MY175903A (en) 2020-07-15
TW201612163A (en) 2016-04-01
CU24375B1 (es) 2018-12-05
SG11201603026PA (en) 2016-05-30
DK3065738T3 (en) 2018-06-06
PL3065738T3 (pl) 2018-07-31
MA39088A1 (fr) 2017-07-31
JO3454B1 (ar) 2020-07-05
US9682939B2 (en) 2017-06-20
TWI662027B (zh) 2019-06-11
MX364834B (es) 2019-05-08
AR098316A1 (es) 2016-05-26
AU2014346919B2 (en) 2017-02-02
EA030430B1 (ru) 2018-08-31
JP6424231B2 (ja) 2018-11-14
EP3065738B1 (en) 2018-02-28
EA201690930A1 (ru) 2016-08-31
TR201807321T4 (tr) 2018-06-21
SI3065738T1 (en) 2018-06-29
CN105682656B (zh) 2019-11-05
US20210253534A1 (en) 2021-08-19
US20160340317A1 (en) 2016-11-24
CA2927705C (en) 2021-09-21
US10683271B2 (en) 2020-06-16
EP3065738A1 (en) 2016-09-14
PH12016500777A1 (en) 2016-05-30
CR20160212A (es) 2016-07-22
CA2927705A1 (en) 2015-05-14
TN2016000143A1 (en) 2017-10-06
HUE039155T2 (hu) 2018-12-28
CL2016000982A1 (es) 2016-10-07
AU2014346919A1 (en) 2016-05-12
WO2015069666A1 (en) 2015-05-14
US20170275256A1 (en) 2017-09-28
US11021446B2 (en) 2021-06-01
GT201600085A (es) 2019-07-19
US10077240B2 (en) 2018-09-18
AP2016009165A0 (en) 2016-04-30
MX2016005865A (es) 2016-07-13
CN105682656A (zh) 2016-06-15
UY35818A (es) 2015-05-29
JP2016535784A (ja) 2016-11-17
US20190062283A1 (en) 2019-02-28
PT3065738T (pt) 2018-06-04
PE20160682A1 (es) 2016-07-23
MA39088B1 (fr) 2018-06-29
PH12016500777B1 (en) 2016-05-30
IL245242B (en) 2019-03-31
BR112016009630A8 (pt) 2020-04-07
KR20160079091A (ko) 2016-07-05

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