PE20160682A1 - Composiciones y metodos para modular los receptores x farnesoides - Google Patents

Composiciones y metodos para modular los receptores x farnesoides

Info

Publication number
PE20160682A1
PE20160682A1 PE2016000596A PE2016000596A PE20160682A1 PE 20160682 A1 PE20160682 A1 PE 20160682A1 PE 2016000596 A PE2016000596 A PE 2016000596A PE 2016000596 A PE2016000596 A PE 2016000596A PE 20160682 A1 PE20160682 A1 PE 20160682A1
Authority
PE
Peru
Prior art keywords
receptors
modulate
pharnesoid
compositions
methods
Prior art date
Application number
PE2016000596A
Other languages
English (en)
Inventor
David Tully
Jason Roland
John Nelson
Xiaodong Liu
Donatella Chianelli
Paul Rucker
Valentina Molteni
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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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=PE20160682(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20160682A1 publication Critical patent/PE20160682A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Se refiere a compuestos de formula (I) donde: R0 es alquilo C1-C6, entre otros; Anillo B es arilo, entre otros; X es –C(O)-, entre otros; Y es –O-, entre otros; Z1, Z2, Z3 y Z4 son –N-, entre otros; L1 es *1-(CR4R5)1-2, donde “*1” indica el punto de union de L1 a N, entre otros; L2 es *2-(CR4R5)1-2, donde “*2” indica el punto de union de L2 a N, entre otros; L3 es –C(O)-, entre otros; R4 y R5 son hidrogeno o alquilo C1-C6. Son compuestos preferidos: acido 4-fluoro-3-(2-(8-fluoro-N-(3-fluorobencil)-1-metil-1,4-dihidrocromeno[4,3-c]pirazol-3-carboxamida)acetamida)benzoico; acido 3- (2-(8-cloro-1-metil-N-(3-metilbencil)-1,4-dihidrocromeno[4,3-c]pirazol-3- carboxamida)acetamida)benzoico; entre otros. Dichos compuestos modulan la actividad de los receptores X farsenoides (FXRS) siendo utiles en el tratamiento de enfermedades hepaticas
PE2016000596A 2013-11-05 2014-11-04 Composiciones y metodos para modular los receptores x farnesoides PE20160682A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361900013P 2013-11-05 2013-11-05

Publications (1)

Publication Number Publication Date
PE20160682A1 true PE20160682A1 (es) 2016-07-23

Family

ID=51982773

Family Applications (1)

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PE2016000596A PE20160682A1 (es) 2013-11-05 2014-11-04 Composiciones y metodos para modular los receptores x farnesoides

Country Status (42)

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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) PH12016500777A1 (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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PH12016500777B1 (en) 2016-05-30
CN105682656A (zh) 2016-06-15
IL245242B (en) 2019-03-31
JP6424231B2 (ja) 2018-11-14
US20200247757A1 (en) 2020-08-06
TWI662027B (zh) 2019-06-11
PT3065738T (pt) 2018-06-04
TN2016000143A1 (en) 2017-10-06
TR201807321T4 (tr) 2018-06-21
SG11201603026PA (en) 2016-05-30
US10683271B2 (en) 2020-06-16
US10077240B2 (en) 2018-09-18
US20160340317A1 (en) 2016-11-24
CN105682656B (zh) 2019-11-05
CU20160063A7 (es) 2016-09-30
EP3065738B1 (en) 2018-02-28
ES2670984T3 (es) 2018-06-04
CY1120273T1 (el) 2019-07-10
JP2016535784A (ja) 2016-11-17
WO2015069666A1 (en) 2015-05-14
PH12016500777A1 (en) 2016-05-30
AU2014346919B2 (en) 2017-02-02
PL3065738T3 (pl) 2018-07-31
EA201690930A1 (ru) 2016-08-31
EP3065738A1 (en) 2016-09-14
MX364834B (es) 2019-05-08
IL245242A0 (en) 2016-06-30
MA39088B1 (fr) 2018-06-29
ZA201602555B (en) 2017-06-28
NZ719078A (en) 2018-07-27
US11021446B2 (en) 2021-06-01
NO3105103T3 (es) 2018-05-12
CR20160212A (es) 2016-07-22
TW201612163A (en) 2016-04-01
AR098316A1 (es) 2016-05-26
UY35818A (es) 2015-05-29
CA2927705C (en) 2021-09-21
SV2016005192A (es) 2016-11-21
KR20160079091A (ko) 2016-07-05
US9682939B2 (en) 2017-06-20
CA2927705A1 (en) 2015-05-14
BR112016009630B1 (pt) 2021-02-09
AU2014346919A1 (en) 2016-05-12
JO3454B1 (ar) 2020-07-05
HUE039155T2 (hu) 2018-12-28
MY175903A (en) 2020-07-15
AP2016009165A0 (en) 2016-04-30
LT3065738T (lt) 2018-05-10
HRP20180817T1 (hr) 2018-06-29
RS57179B1 (sr) 2018-07-31
CU24375B1 (es) 2018-12-05
KR102350357B1 (ko) 2022-01-14
US20190062283A1 (en) 2019-02-28
MA39088A1 (fr) 2017-07-31
GT201600085A (es) 2019-07-19
US20170275256A1 (en) 2017-09-28
SI3065738T1 (en) 2018-06-29
EA030430B1 (ru) 2018-08-31
DK3065738T3 (en) 2018-06-06
MX2016005865A (es) 2016-07-13
CL2016000982A1 (es) 2016-10-07
US20210253534A1 (en) 2021-08-19
BR112016009630A8 (pt) 2020-04-07

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