CR20150420A - Amidas heterocíclicas como inhibidores de cinasas - Google Patents

Amidas heterocíclicas como inhibidores de cinasas

Info

Publication number
CR20150420A
CR20150420A CR20150420A CR20150420A CR20150420A CR 20150420 A CR20150420 A CR 20150420A CR 20150420 A CR20150420 A CR 20150420A CR 20150420 A CR20150420 A CR 20150420A CR 20150420 A CR20150420 A CR 20150420A
Authority
CR
Costa Rica
Prior art keywords
kinases
inhibitors
heterocyclic amides
amides
heterocyclic
Prior art date
Application number
CR20150420A
Other languages
English (en)
Inventor
Deepak Bandyopadhyay
Patrick M Eidam
Peter J Gough
Philip Anthony Harris
Jae U Jeong
Jianxing Kang
Bryan Wayne King
Shah Ami Lakdawala
Lara Kathryn Leister
Jr Robert W Marquis
Attiq Rahman
Joshi M Ramanjulu
Clark A Sehon
Jr Robert Singhaus
Daohua Zhang
Original Assignee
Glaxosmithkline Intellectual Property Dev Limitd
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 Glaxosmithkline Intellectual Property Dev Limitd filed Critical Glaxosmithkline Intellectual Property Dev Limitd
Publication of CR20150420A publication Critical patent/CR20150420A/es

Links

Classifications

    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/16—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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/08—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D281/02—Seven-membered rings
    • C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D281/10—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Abstract

Se desvelan compuestos que tienen la fórmula 5 en el que X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A, L y B son como se definen en el presente documento, y procedimientos de preparación y uso de los 10 mismos.
CR20150420A 2013-02-15 2015-08-14 Amidas heterocíclicas como inhibidores de cinasas CR20150420A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361765664P 2013-02-15 2013-02-15
US201361790044P 2013-03-15 2013-03-15
PCT/IB2014/059004 WO2014125444A1 (en) 2013-02-15 2014-02-14 Heterocyclic amides as kinase inhibitors

Publications (1)

Publication Number Publication Date
CR20150420A true CR20150420A (es) 2015-10-19

Family

ID=50151350

Family Applications (3)

Application Number Title Priority Date Filing Date
CR20190511A CR20190511A (es) 2013-02-15 2014-02-14 AMIDAS HETEROCÍCLICAS COMO INHIBIDORES DE CINASAS (Divisional 2015-0420)
CR20190512A CR20190512A (es) 2013-02-15 2014-02-14 AMIDAS HETEROCÍCLICAS COMO INHIBIDORES DE CINASAS (Divisional 2015-0420)
CR20150420A CR20150420A (es) 2013-02-15 2015-08-14 Amidas heterocíclicas como inhibidores de cinasas

Family Applications Before (2)

Application Number Title Priority Date Filing Date
CR20190511A CR20190511A (es) 2013-02-15 2014-02-14 AMIDAS HETEROCÍCLICAS COMO INHIBIDORES DE CINASAS (Divisional 2015-0420)
CR20190512A CR20190512A (es) 2013-02-15 2014-02-14 AMIDAS HETEROCÍCLICAS COMO INHIBIDORES DE CINASAS (Divisional 2015-0420)

Country Status (37)

Country Link
US (6) US9556152B2 (es)
EP (4) EP3508484B1 (es)
JP (3) JP6321045B2 (es)
KR (2) KR102228764B1 (es)
CN (3) CN106928203B (es)
AU (1) AU2014217453B2 (es)
BR (4) BR122017002946A2 (es)
CA (1) CA2900695C (es)
CL (1) CL2015002279A1 (es)
CR (3) CR20190511A (es)
CY (2) CY1120320T1 (es)
DK (2) DK3342771T3 (es)
DO (3) DOP2015000196A (es)
EA (2) EA028991B1 (es)
ES (3) ES2814556T3 (es)
HK (3) HK1213545A1 (es)
HR (2) HRP20180900T1 (es)
HU (2) HUE053215T2 (es)
IL (3) IL240280B (es)
LT (2) LT3342771T (es)
MA (1) MA44820B1 (es)
MX (1) MX360715B (es)
MY (2) MY178552A (es)
NZ (1) NZ628447A (es)
PE (1) PE20151752A1 (es)
PH (4) PH12015501675A1 (es)
PL (2) PL3342771T3 (es)
PT (2) PT2956452T (es)
RS (2) RS61439B1 (es)
SG (1) SG11201505796TA (es)
SI (2) SI3342771T1 (es)
TR (1) TR201808112T4 (es)
TW (4) TWI648274B (es)
UA (1) UA118259C2 (es)
UY (1) UY35330A (es)
WO (1) WO2014125444A1 (es)
ZA (1) ZA201505267B (es)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI648274B (zh) * 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 （二）
WO2016027253A1 (en) 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
EP3218371B1 (en) * 2014-11-14 2018-09-26 Boehringer Ingelheim International GmbH Aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amides as somatostatin receptor subtype 4 (sstr4) agonists
SG11201704764PA (en) 2014-12-11 2017-07-28 Harvard College Inhibitors of cellular necrosis and related methods
CN107207485A (zh) * 2015-02-13 2017-09-26 葛兰素史密斯克莱知识产权发展有限公司 (S)‑5‑苄基‑N‑(5‑甲基‑4‑氧代‑2,3,4,5‑四氢苯并[b][1,4]氧氮杂环庚三烯‑3‑基)‑4H‑1,2,4‑三唑‑3‑甲酰胺的晶型
BR112017018643B1 (pt) 2015-03-02 2024-02-27 Evotec Se Derivados de tetra-hidrotiazepina bicíclicos úteis, composição farmacêutica compreendendo os mesmos, seu uso, e método in vitro ou ex vivo para a produção de células imunes ativadas
UY36680A (es) * 2015-05-19 2016-12-30 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas como inhibidores de quinasa
KR20180030545A (ko) * 2015-06-22 2018-03-23 다이닛본 스미토모 세이야꾸 가부시끼가이샤 바이사이클릭 헤테로사이클릭 아미드 유도체
NZ737297A (en) 2015-07-02 2024-03-22 Hoffmann La Roche Bicyclic lactams and methods of use thereof
JP7112324B2 (ja) 2015-07-22 2022-08-03 エナンタ ファーマシューティカルズ インコーポレイテッド Ｒｓｖ阻害剤としてのベンゾジアゼピン誘導体
CN108431004B (zh) * 2015-10-23 2021-02-12 武田药品工业株式会社 杂环化合物
US10709692B2 (en) 2015-12-04 2020-07-14 Denali Therapeutics Inc. Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (RIPK1)
US10961258B2 (en) 2015-12-21 2021-03-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
CN108699077B (zh) 2016-01-15 2021-03-02 英安塔制药有限公司 作为rsv抑制剂的杂环化合物
EP3414239A2 (en) * 2016-02-05 2018-12-19 Denali Therapeutics Inc. Inhibitors of receptor-interacting protein kinase 1
WO2017146128A1 (ja) 2016-02-26 2017-08-31 大日本住友製薬株式会社 イミダゾリルアミド誘導体
WO2018007973A2 (en) 2016-07-06 2018-01-11 Glaxosmithkline Intellectual Property Development Limited Process and intermediates for preparing benzoxazepines
JP7349359B2 (ja) * 2016-10-17 2023-09-22 エフ． ホフマン－ラ ロシュ アーゲー 二環式ピリドンラクタム及びその使用方法。
TW201822637A (zh) 2016-11-07 2018-07-01 德商拜耳廠股份有限公司 用於控制動物害蟲的經取代磺醯胺類
TW201831464A (zh) 2016-11-18 2018-09-01 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺
US11071721B2 (en) 2016-12-02 2021-07-27 Genentech, Inc. Bicyclic amide compounds and methods of use thereof
PL3552017T3 (pl) 2016-12-09 2022-08-08 Denali Therapeutics Inc. Związki użyteczne jako inhibitory RIPK1
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
JPWO2018117196A1 (ja) 2016-12-20 2019-10-31 大日本住友製薬株式会社 がん幹細胞を標的とする医薬
US10398706B2 (en) 2017-01-06 2019-09-03 Enanta Pharmaceuticals, Inc. Heteroaryldiazepine derivatives as RSV inhibitors
JP7076459B2 (ja) 2017-02-16 2022-05-27 エナンタ ファーマシューティカルズ インコーポレイテッド ベンゾジアゼピン誘導体の製造プロセス
JP2020509009A (ja) 2017-02-27 2020-03-26 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としての複素環式アミド
JOP20190233A1 (ar) * 2017-04-14 2019-10-02 Biogen Ma Inc نظائر بنزوازيبين بوصفها عوامل مثبطة لتيروزين كيناز بروتون
EP3612223A4 (en) * 2017-04-17 2020-04-22 National Institute Of Biological Sciences, Beijing TREATMENT OF MALE SENESCENCE
KR102638151B1 (ko) * 2017-05-17 2024-02-16 데날리 테라퓨틱스 인크. 키나아제 억제제 및 이의 용도
US10752598B2 (en) 2017-06-07 2020-08-25 Enanta Pharmaceuticals, Inc. Aryldiazepine derivatives as RSV inhibitors
WO2019006291A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
WO2019006295A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
CA3185865A1 (en) 2017-07-14 2019-01-17 F. Hoffmann-La Roche Ag Bicyclic ketone compounds and methods of use thereof
WO2019067864A1 (en) 2017-09-29 2019-04-04 Enanta Pharmaceuticals, Inc. PHARMACEUTICAL AGENTS IN COMBINATION AS INHIBITORS OF RSV
KR20200070297A (ko) 2017-10-11 2020-06-17 에프. 호프만-라 로슈 아게 Rip1 키나아제 억제제로서 사용하기 위한 이환형 화합물
PE20211247A1 (es) 2017-10-31 2021-07-13 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos
WO2019094920A1 (en) 2017-11-13 2019-05-16 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as rsv inhibitors
WO2019094903A1 (en) 2017-11-13 2019-05-16 Enanta Pharmaceuticals, Inc. Processes for the resolution of benzodiazepin-2-one and benzoazepin-2-one derivatives
WO2019123219A1 (en) 2017-12-20 2019-06-27 Glaxosmithkline Intellectual Property Development Limited Crystalline salt form of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide
JP2021509113A (ja) 2017-12-29 2021-03-18 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としての複素環式アミド
US10975094B2 (en) 2018-04-11 2021-04-13 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
CN112074519A (zh) 2018-04-20 2020-12-11 豪夫迈·罗氏有限公司 作为rip1激酶抑制剂用于治疗e.g.肠易激综合征（ibs）的n-[4-氧代-2,3-二氢-1,5-苯并氧氮杂-3-基]-5,6-二氢-4h-吡咯并[1,2-b]吡唑-2-甲酰胺衍生物和有关化合物
CN110407770B (zh) * 2018-04-27 2022-12-30 复旦大学 3-取代-1,5-苯并氮杂䓬类化合物及其药物用途
CA3099037A1 (en) 2018-05-03 2019-11-07 Rigel Pharmaceuticals, Inc. Rip1 inhibitory compounds and methods for making and using the same
PT3788045T (pt) * 2018-05-03 2023-06-26 Rigel Pharmaceuticals Inc Compostos inibidores de rip1 e métodos para fazer e usar os mesmos
WO2019224774A1 (en) 2018-05-23 2019-11-28 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors
WO2019224773A1 (en) 2018-05-23 2019-11-28 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors
CN110642874B (zh) * 2018-06-26 2023-03-28 中国科学院上海有机化学研究所 一类细胞坏死抑制剂及其制备方法和用途
US20210292340A1 (en) * 2018-06-26 2021-09-23 Shanghai Institute Of Organic Chemistry, Chinese Academy Of Sciences Cell necrosis inhibitor, preparation method therefor and use thereof
WO2020044206A1 (en) 2018-08-29 2020-03-05 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors for use in the treatment cancer
CN109134448B (zh) * 2018-10-16 2020-11-27 中南大学湘雅医院 杂环化合物及其盐、制备方法、用途和药物
CN111138448B (zh) * 2018-11-02 2022-08-02 中国科学院上海药物研究所 抑制rip1激酶的杂环酰胺及其用途
WO2020088194A1 (zh) 2018-11-02 2020-05-07 中国科学院上海药物研究所 抑制rip1激酶的杂环酰胺及其用途
EP3908586B1 (en) 2019-01-11 2022-12-21 F. Hoffmann-La Roche AG Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
CA3127701C (en) * 2019-01-25 2023-08-15 Beijing Scitech-Mq Pharmaceuticals Limited Acylamino bridged heterocyclic compound, and composition and application thereof
CN113710276B (zh) 2019-03-18 2024-03-29 英安塔制药有限公司 苯二氮䓬衍生物作为rsv抑制剂
US11179400B2 (en) 2019-04-09 2021-11-23 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
US20220218719A1 (en) 2019-05-17 2022-07-14 Glaxosmithkline Intellectual Property Development Limited Matrix composition comprising (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide
CN114008038B (zh) * 2019-05-31 2023-01-24 南京明德新药研发有限公司 作为rip-1激酶抑制剂的双并环类化合物及其应用
US20210040115A1 (en) * 2019-08-09 2021-02-11 Bisichem Co., Ltd. Fused ring heteroaryl compounds as ripk1 inhibitors
CN114761398A (zh) 2019-09-06 2022-07-15 里格尔药品股份有限公司 杂环rip1激酶抑制剂
TW202122397A (zh) 2019-09-06 2021-06-16 美商雷傑製藥公司 Ｒｉｐ１抑制性化合物及用於製備和使用其之方法
US11718612B2 (en) 2019-09-06 2023-08-08 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase I for the treatment of disease
AU2020353663A1 (en) 2019-09-27 2022-04-07 Board Of Regents, The University Of Texas System Inhibitors of Receptor Interacting Protein Kinase I for the treatment of disease
KR20220101083A (ko) 2019-10-04 2022-07-19 이난타 파마슈티칼스, 인코포레이티드 항바이러스 헤테로사이클릭 화합물
US11505558B1 (en) 2019-10-04 2022-11-22 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
JP7395730B2 (ja) 2019-11-07 2023-12-11 ライジェル ファーマシューティカルズ， インコーポレイテッド ヘテロ環式ｒｉｐ１阻害化合物
WO2021108198A1 (en) 2019-11-26 2021-06-03 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase i for the treatment of disease
UY39032A (es) 2020-01-24 2021-07-30 Enanta Pharm Inc Compuestos heterocíclicos como agentes antivirales
EP4110765A4 (en) * 2020-02-28 2024-03-06 Univ Texas INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASES
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
TW202214617A (zh) 2020-06-02 2022-04-16 法商賽諾菲公司 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途
TWI824259B (zh) 2020-07-01 2023-12-01 美商雷傑製藥公司 Rip1k抑制劑
WO2022010882A1 (en) 2020-07-07 2022-01-13 Enanta Pharmaceuticals, Inc, Dihydroquinoxaline and dihydropyridopyrazine derivatives as rsv inhibitors
EP4200281A1 (en) * 2020-08-18 2023-06-28 Hutchison Medipharma Limited Pyrimidinone compounds and uses thereof
WO2022086840A1 (en) 2020-10-19 2022-04-28 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as anti-viral agents
WO2022171110A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Fused tricyclic compounds as rip1-kinase inhibitors and uses thereof
WO2022171111A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Heteroaryl-fused bicyclic compound as rip1-kinase inhibitors and uses thereof
TW202300490A (zh) * 2021-03-11 2023-01-01 美商雷傑製藥公司 雜環rip1激酶抑制劑
CN113045560B (zh) * 2021-03-30 2022-09-06 港科鹏禾生物(苏州)有限公司 一种酰胺类衍生物及其制备方法和应用
TW202304921A (zh) 2021-04-02 2023-02-01 美商建南德克公司 製造雙環酮化合物之方法
EP4329766A1 (en) * 2021-04-27 2024-03-06 Merck Sharp & Dohme LLC Ripk1 inhibitors and methods of use
CN115246796A (zh) * 2021-04-27 2022-10-28 中国科学院上海有机化学研究所 一种抑制细胞程序性死亡的化合物及其制备方法
IL308349A (en) 2021-08-10 2024-01-01 Abbvie Inc NICOTINAMIDE RIPK1 INHIBITORS
CN115806557A (zh) * 2021-09-14 2023-03-17 中国科学院上海有机化学研究所 抑制细胞程序性死亡的化合物及其制备方法
WO2023068881A1 (ko) * 2021-10-22 2023-04-27 주식회사 보로노이바이오 아릴 또는 헤테로아릴 유도체, 및 이를 유효성분으로 포함하는 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
CN113876778B (zh) * 2021-11-05 2023-04-14 中日友好医院(中日友好临床医学研究所) Kw2449在制备改善类风湿性关节炎药物中的应用
US11897876B2 (en) 2021-11-11 2024-02-13 Genzyme Corporation Isoxazolidines as RIPK1 inhibitors and use thereof
WO2023119210A1 (ko) * 2021-12-24 2023-06-29 제일약품주식회사 Ripk1 저해제로서의 신규한 화합물 및 이를 포함하는 약학적 조성물
CN114736197B (zh) * 2022-06-13 2022-09-13 南京医工医药技术有限公司 咪唑啉酮衍生物及其用途
WO2023240379A1 (zh) * 2022-06-13 2023-12-21 南京医工医药技术有限公司 咪唑啉酮衍生物及其用途
CN117447460A (zh) * 2022-07-13 2024-01-26 南京天印健华医药科技有限公司 作为ripk1抑制剂的杂环化合物
WO2024040155A1 (en) 2022-08-19 2024-02-22 Genzyme Corporation Isoxazolidines as ripk1 inhibitors and use thereof
WO2024044183A1 (en) * 2022-08-22 2024-02-29 Enanta Pharmaceuticals, Inc. Fused heterobicyclic antiviral agents

Family Cites Families (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5239065B2 (es) 1971-11-17 1977-10-03
EP0166357A3 (en) * 1984-06-26 1988-10-26 Merck & Co. Inc. Benzofused lactams and pharmaceutical compositions containing them
US4692522A (en) 1985-04-01 1987-09-08 Merck & Co., Inc. Benzofused lactams useful as cholecystokinin antagonists
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
JP3358069B2 (ja) * 1991-12-24 2002-12-16 武田薬品工業株式会社 三環性複素環類、その製造法及び剤
AU720378B2 (en) 1995-06-07 2000-06-01 Merck & Co., Inc. Novel N-(4-oxo-2,3,4,5-tetrahydro-1H-1, 5-benzodiazepin-3yl)-3-amides
WO1998041510A1 (fr) 1997-03-14 1998-09-24 Shionogi & Co., Ltd. Nouveaux derives du benzolactame et compositions medicamenteuses les contenant
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
FR2781483A1 (fr) * 1998-07-21 2000-01-28 Hoechst Marion Roussel Inc Derives de thioazepinone, procede de preparation et intermediaires de ce procede, application a titre de medicament et compositions pharmaceutiques les renfermant
WO2001002358A2 (en) 1999-07-06 2001-01-11 Vertex Pharmaceuticals Incorporated Cyclized amide derivatives for treating or preventing neuronal damage
WO2001035964A1 (en) 1999-11-18 2001-05-25 Antexpharma, Inc. Substituted 1-benzazepines and derivatives thereof
AU2001253108A1 (en) 2000-04-03 2001-10-15 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta protein production
IL151576A0 (en) 2000-04-03 2003-04-10 Bristol Myers Squibb Pharma Co Cyclic lactams as inhibitors of a-beta protein production
CA2379445C (en) 2000-06-01 2007-08-21 Bristol-Myers Squibb Pharma Company Lactams substituted by cyclic succinates as inhibitors of a.beta. protein production
DE10054279A1 (de) 2000-11-02 2002-05-16 Apotech Res & Dev Ltd Verwendung von Liganden von Todesrezeptoren oder RIP zur Auslösung des Caspase-unabhängigen Zelltods und Verbindungen zur Inhibition des Caspase-unabhängigen Zelltods
JP2004536079A (ja) 2001-05-16 2004-12-02 アンテックスファーマ・インコーポレーテッド 置換１−ベンズアゼピンおよびその誘導体
US7057046B2 (en) * 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
WO2004092410A2 (en) 2003-04-15 2004-10-28 Thiesen Hans-Juergen Method for diagnosing rheumatoid arthritis or osteoarthritis
TW200509910A (en) * 2003-05-02 2005-03-16 Elan Pharm Inc Substituted pyrazole derivatives and related compounds as bradykinin B1 receptor antagonists
WO2005028664A2 (en) 2003-09-17 2005-03-31 University Of Massachusetts Modulation of programmed necrosis
US20060067942A1 (en) 2004-09-24 2006-03-30 Salama Zoser B Pharmaceutical agent comprising amino acids, peptides, proteins and/or fractions and fragments thereof and the use of same in the prophylaxis and treatment of immune system deficiency in humans and animals
EP1640012A1 (de) 2004-09-24 2006-03-29 Salama, Zoser B. nat.rer.Dr. Pharmazeutisches Mittel enthaltend Blutbestandteile 10 kDa und deren Verwendung zur Prophylaxe und Behandlung von Defekten des Immunsystems
JP2009521454A (ja) * 2005-12-20 2009-06-04 プレジデント・アンド・フエローズ・オブ・ハーバード・カレツジ 化合物、スクリーニング、および処置方法
FR2894968B1 (fr) 2005-12-20 2008-02-22 Trophos Sa Nouveaux derives de l'oxime de cholest-4-en-3-one, compositions pharmaceutiques les renfermant, et procede de preparation
FR2899108B1 (fr) 2006-03-31 2012-02-03 Trophos Utilisation de derives du cholest-4-en-3-one pour l'obtention d'un medicament cytoprotecteur
US8007790B2 (en) 2006-04-03 2011-08-30 Stowers Institute For Medical Research Methods for treating polycystic kidney disease (PKD) or other cyst forming diseases
FR2907783A1 (fr) 2006-10-30 2008-05-02 Trophos Sa Nouveaux composes chimiques, leurs procedes de synthese et leur utilisation a titre de medicament, particulierement a titre de medicament cytoprotecteur, neuroprotecteur ou cardioprotecteur
WO2008086043A2 (en) 2007-01-10 2008-07-17 Wyeth Methods and compositions for assessment and treatment of asthma
US20100144715A1 (en) 2007-02-28 2010-06-10 Hoyt Scott B Substituted Benzodiazepinones, Benzoxazepinones and Benzothiazepinones as Sodium Channel Blockers
JP5239065B2 (ja) 2007-04-20 2013-07-17 株式会社大一商会 遊技機
JP5645663B2 (ja) 2007-08-15 2014-12-24 プレジデント アンド フェローズ オブ ハーバード カレッジ ネクロトーシスのヘテロ環式抑制剤
FR2934596B1 (fr) 2008-07-30 2015-04-10 Trophos Nouveaux derives de l'oxime de cholest-4-en-3-one, compositions pharmaceutiques les renfermant, et procede de preparation
WO2010075290A1 (en) 2008-12-22 2010-07-01 President And Fellows Of Harvard College Unsaturated heterocyclic inhibitors of necroptosis
US8257921B1 (en) 2008-12-22 2012-09-04 Schering Corporation NRIP1 regulation of apolipoprotein A1
WO2010075561A1 (en) 2008-12-23 2010-07-01 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
FR2940650B1 (fr) 2008-12-29 2017-01-27 Trophos Nouveaux derives d'oxime du 3,5-seco-4-nor-cholestane, compositions pharmaceutiques les renfermant,et procede de preparation
US7622106B1 (en) 2009-03-06 2009-11-24 Board Of Regents, The University Of Texas System Necrosis assay
KR101155506B1 (ko) 2009-07-08 2012-06-15 고려대학교 산학협력단 활성산소조절 유전자를 이용한 ｔｎｆ-알파 유도 질병의 치료제 및 예방제의 스크리닝 방법
US20130195884A1 (en) 2009-12-31 2013-08-01 Deutsches Krebsforschungszentrum Novel modulators of trail signalling
US20130005726A1 (en) 2010-03-08 2013-01-03 Derek Abbott Compositions and methods for treating inflammatory disorders
WO2011133964A2 (en) 2010-04-23 2011-10-27 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
ES2704862T3 (es) 2010-07-16 2019-03-20 Agios Pharmaceuticals Inc Composiciones terapéuticamente activas y su método de uso
US20120022116A1 (en) 2010-07-20 2012-01-26 Huayun Deng Compositions and methods for the treatment of pathological condition(s) related to gpr35 and/or gpr35-herg complex
WO2012061045A2 (en) 2010-11-01 2012-05-10 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving retinal ganglion cells
US9643977B2 (en) 2011-03-11 2017-05-09 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
WO2013013826A1 (en) 2011-07-27 2013-01-31 Friedrich-Alexander-Universität Erlangen-Nürnberg Necroptosis inhibitors for the treatment of inflammatory diseases of the gastrointestinal tract
US20140251917A1 (en) 2011-09-22 2014-09-11 Marv Enterprises,LLC Method for the treatment of multiple sclerosis
CN102343102A (zh) 2011-10-19 2012-02-08 柳忠辉 激活素受体相互作用蛋白2基因在制备药物中的应用
CA2888805C (en) 2011-10-21 2020-07-14 Massachusetts Eye And Ear Infirmary Methods and compositions for promoting axon regeneration and nerve function
KR101410332B1 (ko) 2012-02-29 2014-06-24 코아스템(주) 중간엽 기질세포 배양용 항산화 조성물 및 이의 용도
ES2446494B1 (es) 2012-03-28 2015-03-16 Consejo Superior De Investigaciones Científicas (Csic) Aplicación terapéutica de necrostatina-1 en esteatohepatitis
WO2014022102A1 (en) 2012-08-01 2014-02-06 Amgen Inc. Methods of using anti-apoptotic compounds to modulate one or more properties of a cell culture
EP2880151B1 (en) 2012-08-06 2020-06-03 Brainstorm Cell Therapeutics Ltd. Methods of generating mesenchymal stem cells which secrete neurotrophic factors
ES2878196T3 (es) 2012-12-26 2021-11-18 Koninklijke Philips Nv Evaluación de la actividad de la vía de señalización celular mediante el uso de una o más combinaciones lineales de expresiones de genes diana
WO2014126127A1 (ja) 2013-02-13 2014-08-21 国立大学法人北海道大学 ネクロプトーシス関連疾患の治療用医薬組成物及びその有効成分のスクリーニング方法
TWI648274B (zh) * 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 （二）
CN105593373A (zh) 2013-02-27 2016-05-18 博德研究所 T细胞平衡基因表达、物质组合物及其使用方法
JP2016514693A (ja) 2013-03-15 2016-05-23 プレジデント アンド フェローズ オブ ハーバード カレッジ ハイブリッド型ネクロトーシス阻害剤
WO2016027253A1 (en) 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
EP3414239A2 (en) 2016-02-05 2018-12-19 Denali Therapeutics Inc. Inhibitors of receptor-interacting protein kinase 1

Also Published As

Publication number Publication date
UY35330A (es) 2014-08-29
TW201819369A (zh) 2018-06-01
TWI648273B (zh) 2019-01-21
CN108774214B (zh) 2021-03-09
CN105121432B (zh) 2018-08-03
KR20150119174A (ko) 2015-10-23
CN105121432A (zh) 2015-12-02
BR112015019627B1 (pt) 2022-08-30
CN108774214A (zh) 2018-11-09
US10292987B2 (en) 2019-05-21
US9624202B2 (en) 2017-04-18
EP3375780A1 (en) 2018-09-19
PE20151752A1 (es) 2015-11-25
US10933070B2 (en) 2021-03-02
PH12018500341A1 (en) 2018-09-10
LT2956452T (lt) 2018-06-11
PT2956452T (pt) 2018-06-01
TW201443042A (zh) 2014-11-16
MY195183A (en) 2023-01-11
CN106928203A (zh) 2017-07-07
TW201819368A (zh) 2018-06-01
ES2672530T3 (es) 2018-06-14
CA2900695A1 (en) 2014-08-21
AU2014217453B2 (en) 2016-04-14
HUE037763T2 (hu) 2018-09-28
NZ628447A (en) 2016-08-26
DOP2018000089A (es) 2018-06-30
IL256500B (en) 2018-11-29
EP2956452B1 (en) 2018-03-21
DOP2018000088A (es) 2018-10-31
BR122017002949A2 (pt) 2019-09-10
CN106928203B (zh) 2020-02-07
DK2956452T3 (en) 2018-06-06
TWI648274B (zh) 2019-01-21
JP2016512488A (ja) 2016-04-28
WO2014125444A1 (en) 2014-08-21
CR20190512A (es) 2020-01-08
SI3342771T1 (sl) 2021-04-30
ES2814556T3 (es) 2021-03-29
LT3342771T (lt) 2021-03-10
UA118259C2 (uk) 2018-12-26
HRP20210252T1 (hr) 2021-04-02
BR122017002951A2 (pt) 2020-01-28
JP2018150372A (ja) 2018-09-27
KR20190018558A (ko) 2019-02-22
SG11201505796TA (en) 2015-08-28
PH12018500342A1 (en) 2018-09-10
JP6352571B1 (ja) 2018-07-04
TWI638815B (zh) 2018-10-21
MX360715B (es) 2018-11-13
CY1120320T1 (el) 2019-07-10
EA031971B1 (ru) 2019-03-29
PL2956452T3 (pl) 2018-08-31
MX2015010572A (es) 2015-11-16
US20180098998A1 (en) 2018-04-12
US20170183332A1 (en) 2017-06-29
CL2015002279A1 (es) 2016-07-08
US20170008878A1 (en) 2017-01-12
ES2855135T3 (es) 2021-09-23
AU2014217453A1 (en) 2015-08-13
EP3508484B1 (en) 2021-04-07
US20190201413A1 (en) 2019-07-04
MY178552A (en) 2020-10-16
CA2900695C (en) 2021-10-12
IL256502B (en) 2018-11-29
HRP20180900T1 (hr) 2018-07-13
EP3508484A1 (en) 2019-07-10
BR112015019627A2 (pt) 2017-07-18
US20150353533A1 (en) 2015-12-10
HK1253099A1 (zh) 2019-06-06
HUE053215T2 (hu) 2021-06-28
EP2956452A1 (en) 2015-12-23
MA44820A1 (fr) 2019-09-30
DOP2015000196A (es) 2016-05-15
ZA201505267B (en) 2017-08-30
TW201819370A (zh) 2018-06-01
EA201591506A1 (ru) 2016-01-29
EP3342771A1 (en) 2018-07-04
IL240280A0 (en) 2015-09-24
EA028991B1 (ru) 2018-01-31
HK1249100A1 (zh) 2018-10-26
PT3342771T (pt) 2021-02-11
CY1123915T1 (el) 2022-05-27
DK3342771T3 (da) 2021-02-08
RS61439B1 (sr) 2021-03-31
TR201808112T4 (tr) 2018-07-23
EP3342771B1 (en) 2020-11-25
EP3375780B1 (en) 2020-06-03
US20190262356A1 (en) 2019-08-29
IL256500A (en) 2018-02-28
IL256502A (en) 2018-02-28
KR102228764B1 (ko) 2021-03-18
SI2956452T1 (en) 2018-06-29
IL240280B (en) 2018-04-30
JP2018111712A (ja) 2018-07-19
PH12018500343A1 (en) 2018-09-10
US10940154B2 (en) 2021-03-09
CR20190511A (es) 2020-01-08
RS57332B1 (sr) 2018-08-31
KR102267977B1 (ko) 2021-06-21
PH12015501675A1 (en) 2015-10-19
TWI637951B (zh) 2018-10-11
BR122017002946A2 (pt) 2019-09-10
PL3342771T3 (pl) 2021-06-14
JP6321045B2 (ja) 2018-05-09
MA44820B1 (fr) 2020-06-30
HK1213545A1 (zh) 2016-07-08
US9556152B2 (en) 2017-01-31
EA201792039A1 (ru) 2018-01-31

Similar Documents

Publication Publication Date Title
CR20150420A (es) Amidas heterocíclicas como inhibidores de cinasas
CO2017011754A2 (es) Amidas heterocíclicas como inhibidores de quinasa
DOP2018000147A (es) Compuestos inhibidores de la quinasa de unión a tank
CR20150436A (es) Nuevos octahidro-pirrolo[3,4-c]-pirrol y -piridina-fenilo
UY37487A (es) Amidas heterocíclicas como inhibidores de quinasa
CR20150462A (es) Inhibidores de erk y sus usos
NI201500119A (es) Compuestos de heteroarilo y sus usos
ECSP15043696A (es) Compuestos de heteroarilo y sus usos
BR112016006319A2 (pt) inibidores de irak e usos dos mesmos
CR20150470A (es) Derivados de triazolona de piridinilo y piridinilo fusionado
UY36330A (es) Compuestos inhibidores de quinasa de unión a tank
EA201691194A1 (ru) Стимуляторы ргц
DOP2015000059A (es) Amino-quinolinas como inhibidores de cinasa
CR20160070A (es) Compuestos de triazolopiridina, composiciones y métodos de uso de los mismos
CL2017002856A1 (es) Compuestos de tioéter como inhibidores de la nitrificación
EA201690716A1 (ru) ПИРИДО[2,3-d]ПИРИМИДИН-4-ОНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ ТАНКИРАЗЫ
ECSP15050110A (es) Derivados de triazina
CR20150352A (es) Nuevas composiciones antifúngicidas
ES1111380Y (es) Máquina para el labrado intercepa de la tierra
CR20160539A (es) Compuestos de 2-cloro-2difluorometoxifenil pirazolopirimidina, composiciones y métodos de uso de los mismos