MX370535B - Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer. - Google Patents

Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.

Info

Publication number
MX370535B
MX370535B MX2016006438A MX2016006438A MX370535B MX 370535 B MX370535 B MX 370535B MX 2016006438 A MX2016006438 A MX 2016006438A MX 2016006438 A MX2016006438 A MX 2016006438A MX 370535 B MX370535 B MX 370535B
Authority
MX
Mexico
Prior art keywords
bromodomain inhibitors
bet bromodomain
tetrahydroquinoline
compositions
tetrahydroquinoline compositions
Prior art date
Application number
MX2016006438A
Other languages
English (en)
Other versions
MX2016006438A (es
Inventor
W Bair Kenneth
Herbertz Torsten
Stryker Kauffman Goss
J Kayser-Bricker Katherine
P Luke George
W Martin Matthew
S Millan David
E R Schiller Shawn
c talbot Adam
Original Assignee
Forma Therapeutics Inc
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 Forma Therapeutics Inc filed Critical Forma Therapeutics Inc
Publication of MX2016006438A publication Critical patent/MX2016006438A/es
Publication of MX370535B publication Critical patent/MX370535B/es

Links

Classifications

    • 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
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed 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
    • A61K31/495Heterocyclic 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
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/10Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28Oxygen atom
    • 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
    • C07D487/04Ortho-condensed systems
    • 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

Abstract

La presente invención se refiere a inhibidores de bromodominios de terminal extra y bromo (BET) que son útiles para el tratamiento de cáncer, enfermedades inflamatorias, diabetes y obesidad, que tienen la formula (I): Formula (I) en donde W, X, Y, Z, R1, R2, R5 y R8 son como se describe aquí.
MX2016006438A 2013-11-18 2014-11-18 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer. MX370535B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361905639P 2013-11-18 2013-11-18
US201462054811P 2014-09-24 2014-09-24
PCT/US2014/066198 WO2015074064A2 (en) 2013-11-18 2014-11-18 Tetrahydroquinoline compositions as bet bromodomain inhibitors

Publications (2)

Publication Number Publication Date
MX2016006438A MX2016006438A (es) 2016-10-21
MX370535B true MX370535B (es) 2019-12-17

Family

ID=53058297

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2016006438A MX370535B (es) 2013-11-18 2014-11-18 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo (bet) y el uso de los mismos en el tratamiento de cáncer.
MX2019015068A MX2019015068A (es) 2013-11-18 2016-05-17 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer.

Family Applications After (1)

Application Number Title Priority Date Filing Date
MX2019015068A MX2019015068A (es) 2013-11-18 2016-05-17 Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer.

Country Status (25)

Country Link
US (6) US9388161B2 (es)
EP (2) EP3799872A1 (es)
JP (2) JP6553632B2 (es)
KR (1) KR102007796B1 (es)
CN (2) CN110627770A (es)
AU (1) AU2014348191B2 (es)
BR (3) BR112016011024B1 (es)
CA (1) CA2930414C (es)
CY (1) CY1124394T1 (es)
DK (1) DK3071203T3 (es)
ES (1) ES2860695T3 (es)
HR (1) HRP20210431T1 (es)
HU (1) HUE053645T2 (es)
IL (2) IL245582B (es)
LT (1) LT3071203T (es)
MX (2) MX370535B (es)
NZ (1) NZ720004A (es)
PL (1) PL3071203T3 (es)
PT (1) PT3071203T (es)
RS (1) RS61519B1 (es)
RU (1) RU2727169C2 (es)
SI (1) SI3071203T1 (es)
TW (2) TWI684588B (es)
WO (1) WO2015074064A2 (es)
ZA (1) ZA201603278B (es)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104736569A (zh) 2012-01-12 2015-06-24 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
MX365864B (es) 2013-06-21 2019-06-18 Zenith Epigenetics Ltd Inhibidores de bromodominio biciclicos novedosos.
ES2661437T3 (es) 2013-06-21 2018-04-02 Zenith Epigenetics Corp. Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
ES2860695T3 (es) 2013-11-18 2021-10-05 Forma Therapeutics Inc Composiciones de tetrahidroquinolina como inhibidores de bromodominio BET
US20160256448A1 (en) * 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Tetrahydroquinoline compositions as bet bromodomain inhibitors
EP3071205B1 (en) 2013-11-18 2020-02-05 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
CN107207474B (zh) 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
JP7269731B2 (ja) 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
EP3331905B1 (en) 2015-08-06 2022-10-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3454862A4 (en) 2016-05-10 2020-02-12 C4 Therapeutics, Inc. SPIROCYCLIC DEGRONIMERS FOR TARGET PROTEIN REDUCTION
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
ES2919558T3 (es) * 2016-09-14 2022-07-27 Bayer Cropscience Ag Método para producir compuestos bicíclicos halogenados
EP4119552A1 (en) 2017-02-08 2023-01-18 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
WO2018207882A1 (ja) * 2017-05-12 2018-11-15 武田薬品工業株式会社 複素環化合物
CN107216331B (zh) * 2017-07-07 2019-06-18 华南理工大学 一种四氢萘啶并四氢喹唑啉衍生物及其合成方法和应用
WO2019018583A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC 1,8-NAPHTHYRIDINONE COMPOUNDS AND USES THEREOF
MX2020000690A (es) 2017-07-18 2020-07-29 Nuvation Bio Inc Compuestos heterociclicos como antagonistas de adenosina.
WO2019055869A1 (en) 2017-09-15 2019-03-21 Forma Therapeutics, Inc. TETRAHYDROIMIDAZO QUINOLINE COMPOSITIONS AS INHIBITORS OF CBP / P300
US20210179607A1 (en) 2017-11-01 2021-06-17 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE BASED MODULATORS OF PROTEOLYSIS AND METHOD OF USE
CN112236172A (zh) 2018-01-30 2021-01-15 福宏治疗公司 用于治疗病症的方法和化合物
IL310860A (en) 2018-04-13 2024-04-01 Arvinas Operations Inc Servalon ligands and bifunctional compounds containing them
WO2020006329A1 (en) * 2018-06-29 2020-01-02 Forma Therapeutics, Inc. Salts of (s)-(5-cyclobutoxy-2-methyl-6-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)-3,4-dihydroquinolin-1(2h)-yl)(cyclopropyl)methanone and solid forms thereof
BR112020026783A2 (pt) * 2018-06-29 2021-03-30 Forma Therapeutics, Inc. Inibição da proteína de ligação creb (cbp)
TW202023552A (zh) * 2018-09-13 2020-07-01 加拿大商增你智表觀遺傳學公司 用於治療雌激素受體陽性乳癌之組合療法
BR112021007982A2 (pt) 2018-10-30 2021-08-03 Nuvation Bio Inc. compostos heterocíclicos como inibidores de bet
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN DEGRADATION
EP3911323A4 (en) 2019-01-18 2022-11-16 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
EP3911324A4 (en) 2019-01-18 2022-08-17 Nuvation Bio Inc. 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES
CN113874016A (zh) * 2019-01-29 2021-12-31 福宏治疗公司 化合物及其用途
EP3917529A4 (en) * 2019-01-29 2022-11-02 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF
WO2020160193A2 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020190792A1 (en) * 2019-03-15 2020-09-24 Forma Therapeutics, Inc. Compositions and methods for treating androgen receptor positive forms of cancer
WO2021003163A1 (en) 2019-07-01 2021-01-07 Forma Therapeutics, Inc. Treating cancer with a bromodomain and extra-terminal (bet) family inhibitor
EP3997070A4 (en) 2019-07-02 2023-07-26 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS USED AS BET INHIBITORS
TW202126638A (zh) 2019-09-30 2021-07-16 日商協和麒麟股份有限公司 Bet分解劑
AU2020393384A1 (en) 2019-11-28 2022-06-09 Bayer Aktiengesellschaft Substituted aminoquinolones as DGKalpha inhibitors for immune activation
IL293961A (en) 2019-12-19 2022-08-01 Arvinas Operations Inc Compounds and methods for targeted degradation of androgen receptor
IL295101A (en) 2020-01-29 2022-09-01 Foghorn Therapeutics Inc materials and their use
CN111617305B (zh) * 2020-04-23 2021-05-11 杭州千芝雅卫生用品有限公司 一种亲肤性吸液材料的制备方法
US11787800B2 (en) 2020-07-29 2023-10-17 Foghorn Therapeutics Inc. BRD9 degraders and uses thereof
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
WO2022271801A1 (en) * 2021-06-23 2022-12-29 Blueprint Medicines Corporation Process for preparing egfr inhibitors
US11767330B2 (en) 2021-07-06 2023-09-26 Foghorn Therapeutics Inc. Citrate salt, pharmaceutical compositions, and methods of making and using the same
TW202339721A (zh) * 2022-03-31 2023-10-16 英屬開曼群島商百濟神州有限公司 Bcl-xL抑制劑

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3062981D1 (en) 1979-11-09 1983-06-09 Bayer Ag Alkyl-urea derivatives for the treatment of lipometabolic diseases; process for their preparation, their use in medicaments for the treatment of lipometabolic disorders, medicaments containing them, process for the preparation of the medicaments, and some alkyl-urea derivatives
FR2541680B1 (fr) 1983-02-24 1985-06-14 Rhone Poulenc Sante Nouveaux derives de l'amino-5 dithiole-1,2 one-3, leur preparation et les compositions medicinales qui les contiennent
EP0190105A3 (de) 1985-01-31 1988-10-26 Ciba-Geigy Ag Herbizides Mittel
JPS61227506A (ja) 1985-04-01 1986-10-09 Nippon Tokushu Noyaku Seizo Kk カルバモイルイミダゾ−ル類、その中間体、それらの製法並びに除草剤又は農園芸用殺菌剤
DE3600288A1 (de) 1986-01-08 1987-07-16 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonylharnstoff-derivaten
DE3618004A1 (de) 1986-05-28 1987-12-03 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonyliso(thio)-harnstoff-derivaten
JPS6434982A (en) 1987-07-30 1989-02-06 Nissan Chemical Ind Ltd Condensed heterocyclic derivative, production thereof and herbicide containing said derivative as active ingredient
US5256625A (en) 1987-08-13 1993-10-26 Monsanto Company Safening imidazolinone herbicides
US5502025A (en) 1987-08-13 1996-03-26 Monsanto Company Safening herbicidal pyrazolylsulfonylureas
US5041454A (en) 1987-09-25 1991-08-20 Janssen Pharmaceutica N.V. Novel substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides
US5201933A (en) 1988-08-01 1993-04-13 Monsanto Company Safening herbicidal benzoic acid derivatives
US5063230A (en) 1988-11-29 1991-11-05 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted saturated and unsaturated indole quinoline and benzazepine carboxamides and their use as pharmacological agents
JP2955634B2 (ja) 1990-04-12 1999-10-04 株式会社リコー 電子写真感光体
KR900016822A (ko) 1990-04-20 1990-11-14 하라 레이노스께 슬라이드 프로젝터
EP0543919B1 (en) 1990-08-13 1996-04-10 G.D. Searle & Co. Use of heterocyclic amino-alcohol compounds in the manufacture of a medicament for treatment of cns diseases
IL100643A (en) 1991-01-25 1996-10-31 Nippon Kayaku Kk History of hydrazine and pesticides containing these histories as an active ingredient
TW198715B (es) 1991-04-19 1993-01-21 Dtsuka Seiyaku Kk
US5194571A (en) 1991-08-19 1993-03-16 Eastman Kodak Company Colored polyester compositions
TW222276B (es) 1992-01-27 1994-04-11 Fujisawa Pharmaceutical Co
EP0555183A1 (de) 1992-02-07 1993-08-11 Ciba-Geigy Ag Schädlingsbekämpfungsmittel
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
GB9307527D0 (en) 1993-04-13 1993-06-02 Fujisawa Pharmaceutical Co New venzamide derivatives,processes for the preparation thereof and pharmaceutical composition comprising the same
GB9307833D0 (en) 1993-04-15 1993-06-02 Glaxo Inc Modulators of cholecystokinin and gastrin
HU222275B1 (hu) 1993-08-19 2003-05-28 Janssen Pharmaceutica N.V. Érszűkítő hatású szubsztituált aril-oxi-alkil-diaminok, ezek előállítási eljárása, valamint hatóanyagként ilyen vegyületeket tartalmazó gyógyszerkészítmények
US5889022A (en) 1993-12-21 1999-03-30 Smithkline Beecham, P.L.C. Indole, indoline and quinoline derivatives with 5HT1D (anti-depressive) activity
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
WO1995030675A1 (en) 1994-05-06 1995-11-16 Smithkline Beecham Plc Biphenylcarboxamides useful as 5-ht1d antagonists
GB9416972D0 (en) 1994-08-23 1994-10-12 Smithkline Beecham Plc Carbon side chain/indole/indolene
EP0702004A2 (de) 1994-09-15 1996-03-20 Ciba-Geigy Ag 2,9-Diamino- und 2-amino-8-carbamoyl-4-hydroxy-alkansäureamid-derivative
GB9420763D0 (en) 1994-10-14 1994-11-30 Glaxo Inc Acetamide derivatives
US5910495A (en) 1994-10-14 1999-06-08 Glaxo Wellcome Inc. Use of 1,5-benzo b!1,4-diazepines to control gastric emptying
US5780464A (en) 1994-10-14 1998-07-14 Glaxo Wellcome Inc. Enteric coated compositions of 1,5-benzodiazepine derivatives having CCK antagonistic or agonistic activity
US5693646A (en) 1994-12-22 1997-12-02 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
GB9508637D0 (en) 1995-04-28 1995-06-14 Fujisawa Pharmaceutical Co New use
US5654316A (en) 1995-06-06 1997-08-05 Schering Corporation Piperidine derivatives as neurokinin antagonists
US5767129A (en) 1995-08-24 1998-06-16 Warner-Lambert Company Substituted quinolines and isoquinolines as calcium channel blockers, their preparation and the use thereof
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
WO1998008818A1 (en) 1996-08-26 1998-03-05 Genetics Institute, Inc. Inhibitors of phospholipase enzymes
DE19638484A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE19638486A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
WO1998035939A1 (fr) 1997-02-18 1998-08-20 Sanwa Kagaku Kenkyusho Co., Ltd. Derives de diamide malonique et utilisation de ces derniers
WO1998050346A2 (en) 1997-04-18 1998-11-12 Smithkline Beecham Plc Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders
US6011031A (en) 1997-05-30 2000-01-04 Dr. Reddy's Research Foundation Azolidinediones useful for the treatment of diabetes, dyslipidemia and hypertension: process for their preparation and pharmaceutical compositions containing them
DE19727117A1 (de) 1997-06-26 1999-01-07 Boehringer Ingelheim Pharma Phenylalkylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JP2001519387A (ja) 1997-09-29 2001-10-23 ブリストル−マイヤーズ スクイブ カンパニー ファルネシルたんぱく転移酵素のインヒビター
BR9812770A (pt) 1997-10-27 2000-12-12 Reddy Research Foundation Compostos bicìclicos, processo para seu preparo e composições farmacêuticas contendo os mesmos
AU1687699A (en) 1997-12-25 1999-07-19 Yamanouchi Pharmaceutical Co., Ltd. Nitrogenous heterocyclic derivatives
US5994379A (en) 1998-02-13 1999-11-30 Merck Frosst Canada, Inc. Bisaryl COX-2 inhibiting compounds, compositions and methods of use
PL342516A1 (en) 1998-02-25 2001-06-18 Genetics Inst Phospholipase a2 inhibitors
US6084098A (en) 1999-02-26 2000-07-04 Neurogen Corporation Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands
EP1068193A1 (en) 1998-02-26 2001-01-17 Neurogen Corporation Benzylpiperazinyl- and benzylpiperidinyl ethanone derivatives, their preparation and their use as dopamine d 4? receptor antagonists
AU5265599A (en) 1998-04-08 1999-11-01 Takeda Chemical Industries Ltd. Amine compounds, their production and their use as somatostatin receptor antagonists or agonists
EP1005464B1 (de) 1998-06-19 2002-04-17 Optische Werke G. Rodenstock Photochrome naphthopyrane
DE19827855A1 (de) 1998-06-23 1999-12-30 Hoechst Schering Agrevo Gmbh Kombinationen aus Herbiziden und Safenern
DE19838011C2 (de) 1998-08-21 2000-01-13 Christoph Syldatk Verfahren zur biotechnischen Herstellung von Fettsäuremethylestern ("Biodiesel") auf Molkebasis
IL142121A0 (en) 1998-09-29 2002-03-10 American Cyanamid Co Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors
US6048873A (en) 1998-10-01 2000-04-11 Allergan Sales, Inc. Tetrahdroquinolin-2-one 6 or 7-yl, tetrahdroquinilin-2-thione 6 or 7-yl pentadienoic acid and related derivatives having retinoid-like biological activity
AU1881900A (en) 1998-12-23 2000-07-31 Aventis Pharma Limited Dihydro-benzo(1,4)oxazines and tetrahydroquinoxalines
EP1106605A4 (en) 1999-06-24 2005-12-07 Toray Industries ANTAGONISTS OF THE ADRENERGIC RECEPTOR-ALPHA1B
WO2001002384A1 (de) 1999-07-02 2001-01-11 Optische Werke G. Rodenstock Spirofluorenopyrane
WO2001032610A1 (fr) 1999-10-29 2001-05-10 Kaken Pharmaceutical Co., Ltd. Derive d'uree, son procede de production, et produit pharmaceutique contenant ce derive d'uree
US7101869B2 (en) 1999-11-30 2006-09-05 Pfizer Inc. 2,4-diaminopyrimidine compounds useful as immunosuppressants
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
US20030216398A1 (en) 2001-04-05 2003-11-20 Mitsuru Kakihana Soluble beta amyloid precursor protein secretion promoters
AU2002257114A1 (en) 2001-04-06 2002-10-21 Schering Corporation Treatment of malaria with farsenyl protein transferase inhibitors
EP1382598A4 (en) 2001-04-26 2005-03-23 Takeda Pharmaceutical NEW HETEROCYCLIC DERIVATIVES
TW200301698A (en) 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
US6720420B2 (en) 2001-12-21 2004-04-13 Johnson & Johnson Vision Care, Inc. Photochromic oxazine compounds and methods for their manufacture
AU2003249534A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 6,6-fused heteroaryl derivatives as matrix metalloproteinase inhibitors
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
CA2510851A1 (en) 2002-12-20 2004-07-08 Warner-Lambert Company Llc Benzoxazines and derivatives thereof as inhibitors of pi3ks
TWI322012B (en) * 2002-12-20 2010-03-21 Organon Nv Tetrahydroquinoline derivatives
WO2004072041A1 (en) 2003-02-12 2004-08-26 Care X S.A. Tetrahydroquinolines as agonists of liver- x receptors
US20040204450A1 (en) 2003-03-28 2004-10-14 Pfizer Inc Quinoline and quinoxaline compounds
CN1795177A (zh) 2003-03-28 2006-06-28 辉瑞产品公司 作为治疗动脉粥样硬化和肥胖症的cetp抑制剂的 1 , 2 , 4 , -取代的1,2,3,4,-四氢-和1,2二氢-喹啉以及1, 2 , 3 , 4-四氢-喹喔啉衍生物
NZ597500A (en) 2003-08-06 2014-08-29 Senomyx Inc Novel flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof
JP2007501800A (ja) 2003-08-07 2007-02-01 アラーガン インコーポレイテッド レチノイドリガンドを用いて悪液質を処置するための方法
EP1515192B1 (en) 2003-09-11 2015-07-15 Ricoh Company, Ltd. Electrophotographic photoconductor, electrophotographic process, electrophotographic apparatus, and process cartridge
DE10343098A1 (de) 2003-09-18 2005-04-14 Bayer Healthcare Ag Tetrahydrochinoxaline und ihre Verwendung
WO2005044192A2 (en) 2003-10-28 2005-05-19 Amgen Inc. Triazole compounds and uses related thereto
WO2005063735A1 (de) 2003-12-20 2005-07-14 Merck Patent Gmbh 2- (hetero) -arylsubstituierte tetrahydrochinolinderivate
MXPA06007654A (es) 2003-12-31 2006-09-04 Warner Lambert Co Derivados de piperidina n-sustituidos.
US8519158B2 (en) 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
EP2522670A1 (en) * 2004-04-07 2012-11-14 Takeda Pharmaceutical Company Limited Heterocyclic CRF receptor antagonists
CA2565200C (en) 2004-05-07 2013-12-24 Exelixis, Inc. Raf modulators and methods of use
US7442693B2 (en) 2004-05-28 2008-10-28 Smithkline Beecham Corporation Diazepine compounds as ligands of the melanocortin 1 and/or 4 receptors
US20050282812A1 (en) 2004-06-18 2005-12-22 JONES Zachary Inhibitors of cholesteryl ester transfer protein
JP2008518003A (ja) 2004-10-29 2008-05-29 アストラゼネカ・アクチエボラーグ 医薬品としての不飽和キノリンもしくはナフタレン誘導体の使用
WO2007134169A2 (en) 2006-05-10 2007-11-22 Nuada, Llc Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
US20090264384A1 (en) 2004-11-01 2009-10-22 Nuada, Inc. Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
US20080319044A1 (en) 2004-11-01 2008-12-25 Nuada, Llc Compounds and Methods of Use Thereof
JP2008518923A (ja) 2004-11-01 2008-06-05 ヌアダ,リミテッド・ライアビリティ・カンパニー 化合物およびその使用方法
AR051780A1 (es) 2004-11-29 2007-02-07 Japan Tobacco Inc Compuestos en anillo fusionados que contienen nitrogeno y utilizacion de los mismos
BRPI0608553A2 (pt) 2005-02-24 2010-01-12 Millennium Pharm Inc antagonistas de receptor de pgd2 para o tratamento de doenças inflamatórias
BRPI0520097A2 (pt) 2005-02-25 2009-08-25 Lilly Co Eli composto ou estereoisÈmeros únicos, misturas de estereoisÈmeros, ou sais farmaceuticamente aceitáveis dos mesmos, composição farmacêutica, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo
WO2006094210A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Tetrahydroquinoxalinone sirtuin modulators
EP1888575A2 (en) 2005-05-09 2008-02-20 Hydra Biosciences, Inc. Compounds for modulating trpv3 function
EP1885704B1 (en) 2005-05-11 2011-09-28 Abbott Laboratories Antagonists of the vanilloid receptor subtype 1 (vr1) and uses thereof
WO2006134939A1 (ja) 2005-06-14 2006-12-21 Nippon Kayaku Kabushiki Kaisha 色素増感光電変換素子
MX2007015679A (es) 2005-06-30 2008-02-21 Amgen Inc Inhibidores de quinasa bis-aril y su uso en el tratamiento de inflamacion, angiogenesis y cancer.
CN101228149B (zh) 2005-07-26 2013-01-02 塞诺菲-安万特股份有限公司 作为Rho-激酶抑制剂的哌啶基取代的异喹啉酮衍生物
LT1937244T (lt) 2005-09-30 2018-11-12 Io Therapeutics, Llc Vėžio gydymas specifiniais rxr agonistais
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
AU2006319235A1 (en) 2005-11-30 2007-06-07 F. Hoffmann-La Roche Ag 5-substituted indole-2-carboxamide derivatives
CA2630314A1 (en) 2005-11-30 2007-06-07 F. Hoffmann-La Roche Ag 1,5-substituted indol-2-yl amide derivatives
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
WO2007073935A1 (en) 2005-12-29 2007-07-05 Lek Pharmaceuticals D.D. Heterocyclic compounds
TWI385161B (zh) 2006-02-02 2013-02-11 Mitsubishi Tanabe Pharma Corp 含氮雜雙環化合物
US20070185055A1 (en) 2006-02-06 2007-08-09 Guang Liang Jiang Method for treating cachexia with retinoid ligands
KR101034961B1 (ko) 2006-02-13 2011-05-17 에프. 호프만-라 로슈 아게 당뇨병의 치료를 위한 헤테로바이사이클릭 설폰아마이드 유도체
DE602007009932D1 (de) 2006-02-16 2010-12-02 Schering Corp Pyrrolidin-derivate als erk-hemmer
JPWO2007129745A1 (ja) 2006-05-09 2009-09-17 第一三共株式会社 ヘテロアリールアミド低級カルボン酸誘導体
CA2651942A1 (en) 2006-05-11 2008-07-03 Janssen Pharmaceutica N.V. 1,2,3,4-tetrahydro-quinoline derivatives as cetp inhibitors
CN101448820A (zh) 2006-05-30 2009-06-03 霍夫曼-拉罗奇有限公司 哌啶基嘧啶衍生物
FR2901794A1 (fr) 2006-06-01 2007-12-07 Oreal Composition pour la coloration des fibres keratiniques comprenant un colorant direct diazoique a motif 2-imidazolium
WO2007146230A2 (en) 2006-06-14 2007-12-21 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
TW200811158A (en) 2006-06-27 2008-03-01 Sanofi Aventis Piperidine or pyrrolidine urea derivatives, their preparation and their therapeutic application
PE20080344A1 (es) 2006-06-27 2008-06-09 Sanofi Aventis Compuestos 8-azabiciclo[3.2.1]oct-8-il-1,2,3,4-tetrahidroquinolina sustituidos como inhibidores 11b-hsd1
ES2448494T3 (es) 2006-07-13 2014-03-14 Achillion Pharmaceuticals, Inc. Péptidos de 4-amino-4-oxobutanoilo en calidad de inhibidores de la replicación viral
GB0618168D0 (en) 2006-09-15 2006-10-25 Babraham Inst Compounds
US20080186971A1 (en) 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
KR100999592B1 (ko) 2007-02-15 2010-12-08 주식회사 엘지화학 새로운 시클로펜타디에닐 리간드를 갖는 4족 전이금속화합물, 이의 제조방법 및 이를 이용한 올레핀계 중합체의제조방법
TW200848021A (en) 2007-03-06 2008-12-16 Wyeth Corp Sulfonylated heterocycles useful for modulation of the progesterone receptor
GB0706072D0 (en) 2007-03-28 2007-05-09 Sterix Ltd Compound
US20090012045A1 (en) 2007-06-26 2009-01-08 Rigel Pharmaceuticals, Inc. Methods of Treating Cell Proliferative Disorders
EP2172453A4 (en) 2007-06-27 2010-12-22 Taisho Pharmaceutical Co Ltd COMPOUND HAVING 11 ß-HSD1 INHIBITION ACTIVITY
WO2009020140A1 (ja) 2007-08-06 2009-02-12 Dainippon Sumitomo Pharma Co., Ltd. アダマンチルウレア誘導体
WO2009022746A1 (ja) 2007-08-10 2009-02-19 Nippon Soda Co., Ltd. 含窒素複素環化合物および有害生物防除剤
US9493419B2 (en) 2007-08-21 2016-11-15 The Hong Kong Polytechnic University Quinoline derivatives as anti-cancer agents
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
US8288377B2 (en) 2007-09-21 2012-10-16 Janssen Pharmaceutica N.V. Inhibitors of the interaction between MDM2 and p53
US20100280024A1 (en) 2007-10-15 2010-11-04 Jigar Desai Renin inhibitors
JP2009114107A (ja) 2007-11-06 2009-05-28 Daiichi Sankyo Co Ltd ヘテロアリールアミド低級カルボン酸誘導体を含有する医薬組成物
US8119656B2 (en) 2007-12-07 2012-02-21 The Board Of Regents Of The University Of Texas System Inhibitors of the influenza virus non-structural 1 protein
CN101990537A (zh) 2008-02-07 2011-03-23 雅培制药有限公司 作为阳性别构调节剂的酰胺衍生物和其使用方法
JP2011528369A (ja) 2008-07-16 2011-11-17 シェーリング コーポレイション 二環式ヘテロ環誘導体およびそれらの使用方法
BRPI0919648A2 (pt) 2008-10-29 2015-12-08 Hoffmann La Roche novos derivados de fenil amida ou piridil amida e seu uso como agonistas de gpbar1
TW201030007A (en) 2009-02-06 2010-08-16 Gruenenthal Gmbh Substituted spiro-amides as b1r modulators
AU2010226829A1 (en) 2009-03-18 2011-09-15 Schering Corporation Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
US8791090B2 (en) 2009-03-31 2014-07-29 Kowa Company, Ltd. Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient
CN102459271B (zh) 2009-04-15 2014-07-02 Jw制药公司 回折模拟物的新化合物及其制备方法和用途
GB0909672D0 (en) 2009-06-04 2009-07-22 Xention Discovery Ltd Compounds
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
US9360482B2 (en) * 2009-11-05 2016-06-07 Glaxosmithkline Llc Process for the identification of a compound which inhibits the binding of the second bromodomain of each of human BRD-2, BRD-3, and BRD-4
US8420647B2 (en) 2010-01-21 2013-04-16 Hoffmann-La Roche Inc. 4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds
ES2674745T3 (es) 2010-02-11 2018-07-03 Bristol-Myers Squibb Company Macrociclos como inhibidores del factor XIa
US8299117B2 (en) 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
WO2012064744A2 (en) 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
WO2012137224A1 (en) 2011-04-05 2012-10-11 University Of Delhi Coumarin compounds for the treatment of mycobacterial infections
MX2013011926A (es) 2011-04-14 2013-11-01 Novartis Ag Derivados de glicosido y usos de los mismos.
GB201106750D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
CN103619817A (zh) 2011-04-28 2014-03-05 百时美施贵宝公司 新颖的二环含氮杂芳基tgr5受体调节剂
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
CN102816175B (zh) 2011-06-09 2015-12-16 上海汇伦生命科技有限公司 一种杂环并吡啶酮类化合物,其中间体、制备方法和用途
AU2012269643A1 (en) 2011-06-16 2014-02-06 AB Pharma Ltd. Macrocyclic heterocyclic compound for inhibiting hepatitis C virus and preparation and use thereof
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
WO2013012723A1 (en) 2011-07-13 2013-01-24 Novartis Ag Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors
WO2013036676A1 (en) 2011-09-06 2013-03-14 New York Blood Center, Inc. Hiv inhibitors
US9403800B2 (en) 2012-01-24 2016-08-02 Chemregen, Inc. Compounds for inhibition of cancer cell proliferation
WO2013152687A1 (zh) 2012-04-11 2013-10-17 中国科学院理化技术研究所 一种近红外荧光染料的制备及应用
KR20150007300A (ko) 2012-05-08 2015-01-20 머크 샤프 앤드 돔 코포레이션 Ror감마 활성의 억제를 위한 테트라히드로나프티리딘 및 관련 비시클릭 화합물 및 질환의 치료
EP3409666A3 (en) 2012-06-07 2019-01-02 Georgia State University Research Foundation, Inc. Seca inhibitors and methods of making and using thereof
CA2900335C (en) 2012-10-22 2021-10-26 City Of Hope Synthetic analogs of epipolythiodioxopiperazines and uses thereof
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US20160256458A1 (en) 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
EP3071205B1 (en) 2013-11-18 2020-02-05 Forma Therapeutics, Inc. Benzopiperazine compositions as bet bromodomain inhibitors
ES2860695T3 (es) * 2013-11-18 2021-10-05 Forma Therapeutics Inc Composiciones de tetrahidroquinolina como inhibidores de bromodominio BET
US20160256448A1 (en) 2013-11-18 2016-09-08 Forma Therapeutics, Inc. Tetrahydroquinoline compositions as bet bromodomain inhibitors

Also Published As

Publication number Publication date
MX2019015068A (es) 2020-02-13
HUE053645T2 (hu) 2021-07-28
CA2930414C (en) 2020-02-11
KR102007796B1 (ko) 2019-08-07
US20160257692A1 (en) 2016-09-08
TWI742513B (zh) 2021-10-11
MX2016006438A (es) 2016-10-21
PL3071203T3 (pl) 2021-08-23
IL245582A0 (en) 2016-06-30
BR122020006707B1 (pt) 2021-03-16
US10611750B2 (en) 2020-04-07
KR20160086940A (ko) 2016-07-20
JP2019189641A (ja) 2019-10-31
TW202015682A (zh) 2020-05-01
US20190127347A1 (en) 2019-05-02
BR112016011024B1 (pt) 2020-09-01
US9388161B2 (en) 2016-07-12
SI3071203T1 (sl) 2021-07-30
JP6553632B2 (ja) 2019-07-31
CN105934246A (zh) 2016-09-07
CY1124394T1 (el) 2022-07-22
WO2015074064A3 (en) 2015-07-09
US20180215766A1 (en) 2018-08-02
US20150232445A1 (en) 2015-08-20
CA2930414A1 (en) 2015-05-21
TW201609657A (zh) 2016-03-16
IL276456A (en) 2020-09-30
EP3071203A2 (en) 2016-09-28
US11111229B2 (en) 2021-09-07
NZ720004A (en) 2020-03-27
ES2860695T3 (es) 2021-10-05
US20200369642A1 (en) 2020-11-26
US20230061891A1 (en) 2023-03-02
IL245582B (en) 2020-08-31
ZA201603278B (en) 2021-08-25
JP2016540831A (ja) 2016-12-28
JP6845897B2 (ja) 2021-03-24
CN110627770A (zh) 2019-12-31
RU2727169C2 (ru) 2020-07-21
HRP20210431T1 (hr) 2021-05-14
RS61519B1 (sr) 2021-03-31
EP3799872A1 (en) 2021-04-07
RU2016124176A (ru) 2017-12-22
DK3071203T3 (da) 2021-03-15
IL276456B (en) 2021-04-29
BR112016011024A2 (pt) 2017-08-08
AU2014348191B2 (en) 2019-03-28
TWI684588B (zh) 2020-02-11
EP3071203B1 (en) 2020-12-23
LT3071203T (lt) 2021-05-25
AU2014348191A1 (en) 2016-06-02
BR122019007990B1 (pt) 2021-05-04
EP3071203A4 (en) 2017-10-04
US10336722B2 (en) 2019-07-02
PT3071203T (pt) 2021-03-11
WO2015074064A2 (en) 2015-05-21
CN105934246B (zh) 2019-10-22

Similar Documents

Publication Publication Date Title
MX2019015068A (es) Compuestos de tetrahidroquinolina como inhibidores del bromodominio extra terminal y bromo ( bet ) y el uso de los mismos en el tratamiento de cancer.
PH12017501817A1 (en) Heterocyclic compounds as lsd1 inhibitors
MX2015017045A (es) Inhibidores de bromodominio biciclicos novedosos.
IL246252A0 (en) Diaminopyrimidyl derivative compounds, their compositions and methods of treatment
HK1212207A1 (en) Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
EA201890239A2 (ru) Фумараты как пролекарства и их применение при лечении различных заболеваний
NZ743274A (en) Substituted tricyclic compounds as fgfr inhibitors
MX2016004570A (es) Uso de inhibidores del bromodominio de cbp/ep300 para la inmunoterapia del cáncer.
EP3049070A4 (en) Compositions and methods for treatment and prophylaxis of gastrointestinal diseases
PH12016501160A1 (en) Isochromene derivatives as phosphoinositide 3-kinases inhibitors
MX2020001756A (es) Compuestos deuterados del inhibidor vmat y el uso de dichos compuestos.
MX2016006975A (es) Compuestos, composicion farmaceutica y metodos para su uso en el tratamiento de enfermedades inflamatorias.
IN2013MU03641A (es)
HK1220621A1 (zh) 用於治療口腔乾燥和用於牙齒治療的組合物
SG10201900954SA (en) Heterocycles as Modulators of Kinase Activity
PH12015502746A1 (en) Prodrug derivatives of substituted triazolopyridines
EA201500737A1 (ru) Пиразолилкарбоксамиды ii в качестве ингибиторов crac каналов
EA201500736A1 (ru) Пиразолилкарбоксамиды i в качестве ингибиторов crac каналов
EP2994156A4 (en) Compounds, compositions and methods for the treatment of diseases through inhibiting tgf- activity
PH12015502703A1 (en) Pharmaceutical compositions
EA201690938A1 (ru) Соединения для лечения диабета и осложнений, возникающих из-за этого заболевания
IN2013MU02732A (es)
IN2013MU02279A (es)

Legal Events

Date Code Title Description
FG Grant or registration