MD4658B1 - Inhibitori ai kinazei inductoare de apoptoză - Google Patents

Inhibitori ai kinazei inductoare de apoptoză Download PDF

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Publication number
MD4658B1
MD4658B1 MD20160069A MD20160069A MD4658B1 MD 4658 B1 MD4658 B1 MD 4658B1 MD 20160069 A MD20160069 A MD 20160069A MD 20160069 A MD20160069 A MD 20160069A MD 4658 B1 MD4658 B1 MD 4658B1
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MD
Moldova
Prior art keywords
diseases
regulating kinase
signal
apotosis
kinase inhibitors
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MD20160069A
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English (en)
Russian (ru)
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MD20160069A2 (ro
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Gregory Notte
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Gilead Sciences Inc
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Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of MD20160069A2 publication Critical patent/MD20160069A2/ro
Publication of MD4658B1 publication Critical patent/MD4658B1/ro

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    • C07ORGANIC CHEMISTRY
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    • 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
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    • 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
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • 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 or sparfloxacin
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    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
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    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic 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
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Invenţia se referă la derivaţi de piridin-2-carboxamidă, având activitate de inhibare a kinazei reglatoare a semnalului de apoptoză (ASK1), deci sunt astfel utili în tratarea stărilor mediate de ASK1, inclusiv a tulburărilor autoimune, bolilor inflamatorii, bolilor cardiovasculare, diabetului, nefropatiei diabetice, bolilor cardio-renale, inclusiv a bolii de rinichi, bolilor fibrotice, bolilor respiratorii, BPOC, fibrozei pulmonare idiopatice, leziunilor pulmonare acute, bolilor hepatice acute şi cronice, precum şi a bolilor neuro-degenerative.
MD20160069A 2013-12-20 2014-12-15 Inhibitori ai kinazei inductoare de apoptoză MD4658B1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361918784P 2013-12-20 2013-12-20
PCT/US2014/070362 WO2015095059A1 (en) 2013-12-20 2014-12-15 Apoptosis signal-regulating kinase inhibitors

Publications (2)

Publication Number Publication Date
MD20160069A2 MD20160069A2 (ro) 2016-11-30
MD4658B1 true MD4658B1 (ro) 2019-11-30

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MD20160069A MD4658B1 (ro) 2013-12-20 2014-12-15 Inhibitori ai kinazei inductoare de apoptoză

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US (2) US9908875B2 (ro)
EP (1) EP3083615B1 (ro)
JP (3) JP2016540029A (ro)
KR (1) KR20160098463A (ro)
CN (1) CN105980382A (ro)
AP (1) AP2016009248A0 (ro)
AU (1) AU2014366235B2 (ro)
CA (1) CA2934454C (ro)
CL (1) CL2016001538A1 (ro)
CR (1) CR20160268A (ro)
CU (1) CU20160095A7 (ro)
DO (1) DOP2016000136A (ro)
EA (1) EA201690973A1 (ro)
ES (1) ES2731703T3 (ro)
HK (1) HK1226073A1 (ro)
IL (1) IL245807A0 (ro)
MD (1) MD4658B1 (ro)
MX (1) MX2016008254A (ro)
NZ (1) NZ720660A (ro)
PE (1) PE20160859A1 (ro)
PH (1) PH12016501149A1 (ro)
SG (1) SG11201604473VA (ro)
WO (1) WO2015095059A1 (ro)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI625121B (zh) 2009-07-13 2018-06-01 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
CA2802743C (en) * 2010-07-02 2019-05-07 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibitors
UY35212A (es) 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis
EP3152198B1 (en) * 2014-06-09 2019-02-27 Takeda Pharmaceutical Company Limited Radiolabeled compounds
WO2018090869A1 (zh) * 2016-11-16 2018-05-24 广东东阳光药业有限公司 酰胺衍生物及其在药物中的应用
WO2018094964A1 (zh) * 2016-11-25 2018-05-31 武汉大学 一种以凋亡信号调节激酶1n端二聚化为靶点筛选用于治疗脂肪性肝炎药物的方法
US20180325931A1 (en) 2017-01-21 2018-11-15 Ningbo Zhiming Biotechnology Co., Ltd. Use of paeoniflorin-6'-o-benzenesulfonate in treatment of sjögren's syndrome
CN109071538B (zh) * 2017-01-22 2020-03-17 福建广生堂药业股份有限公司 作为ask1抑制剂的吡啶衍生物及其制备方法和应用
WO2018157856A1 (zh) * 2017-03-03 2018-09-07 江苏豪森药业集团有限公司 酰胺类衍生物抑制剂及其制备方法和应用
US10683279B2 (en) 2017-05-12 2020-06-16 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10450301B2 (en) 2017-05-25 2019-10-22 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10246439B2 (en) 2017-05-25 2019-04-02 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US10253018B2 (en) 2017-05-25 2019-04-09 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2019046186A1 (en) 2017-08-28 2019-03-07 Enanta Pharmaceuticals, Inc. INHIBITORS OF KINASE 1 REGULATING THE APOPTOTIC SIGNAL CONTAINING TETRAZOLES AND METHODS OF USE THEREOF
CN111518080A (zh) * 2017-10-12 2020-08-11 深圳市塔吉瑞生物医药有限公司 一种1,2,4-三氮唑类化合物
EP3735404B1 (en) 2018-01-02 2023-11-29 Seal Rock Therapeutics, Inc. Ask1 inhibitor compounds and uses thereof
CN110407806B (zh) * 2018-04-28 2021-08-17 深圳微芯生物科技股份有限公司 甲酰胺类化合物、其制备方法及其应用
IL278368B2 (en) 2018-05-02 2024-06-01 Enanta Pharm Inc Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2019213239A1 (en) 2018-05-02 2019-11-07 Enanta Pharmaceuticals Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
ES3032286T3 (en) * 2018-06-27 2025-07-16 Biogen Ma Inc Ask1 inhibiting agents
US10968199B2 (en) 2018-08-22 2021-04-06 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US11345699B2 (en) 2018-11-19 2022-05-31 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020198214A1 (en) 2019-03-25 2020-10-01 Enanta Pharmaceuticals, Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2802743C (en) * 2010-07-02 2019-05-07 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibitors
UY35212A (es) * 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis

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US9169243B2 (en) 2015-10-27
PH12016501149A1 (en) 2016-08-22
EA201690973A1 (ru) 2016-11-30
MD20160069A2 (ro) 2016-11-30
EP3083615A1 (en) 2016-10-26
IL245807A0 (en) 2016-08-02
CA2934454C (en) 2019-03-26
CA2934454A1 (en) 2015-06-25
DOP2016000136A (es) 2016-06-30
AU2014366235B2 (en) 2017-04-13
NZ720660A (en) 2018-01-26
WO2015095059A1 (en) 2015-06-25
MX2016008254A (es) 2016-10-14
HK1224284A1 (en) 2017-08-18
SG11201604473VA (en) 2016-07-28
JP2019077719A (ja) 2019-05-23
AP2016009248A0 (en) 2016-05-31
KR20160098463A (ko) 2016-08-18
HK1226073A1 (zh) 2017-09-22
CN105980382A (zh) 2016-09-28
CL2016001538A1 (es) 2016-10-28
CR20160268A (es) 2016-08-16
AU2014366235A1 (en) 2016-06-16
US9908875B2 (en) 2018-03-06
ES2731703T3 (es) 2019-11-18
US20150175597A1 (en) 2015-06-25
PE20160859A1 (es) 2016-09-18
EP3083615B1 (en) 2019-04-17
JP2016540029A (ja) 2016-12-22
US20160318922A1 (en) 2016-11-03
JP6509968B2 (ja) 2019-05-08
JP2017193592A (ja) 2017-10-26
CU20160095A7 (es) 2016-11-29

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