CN102917588B - 化合物 - Google Patents

化合物 Download PDF

Info

Publication number
CN102917588B
CN102917588B CN201180025962.7A CN201180025962A CN102917588B CN 102917588 B CN102917588 B CN 102917588B CN 201180025962 A CN201180025962 A CN 201180025962A CN 102917588 B CN102917588 B CN 102917588B
Authority
CN
China
Prior art keywords
dihydro
amine
indoles
ethanoyl
pyrimidine
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201180025962.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN102917588A (zh
Inventor
J.M.阿克森
S.W.格兰特
D.A.赫尔丁
J.R.梅迪纳
S.P.罗默里尔
唐军
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of CN102917588A publication Critical patent/CN102917588A/zh
Application granted granted Critical
Publication of CN102917588B publication Critical patent/CN102917588B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
    • 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
    • A61P3/08—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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201180025962.7A 2010-03-25 2011-03-23 化合物 Expired - Fee Related CN102917588B (zh)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US31747610P 2010-03-25 2010-03-25
US61/317,476 2010-03-25
US35286310P 2010-06-09 2010-06-09
US61/352,863 2010-06-09
US38148010P 2010-09-10 2010-09-10
US61/381,480 2010-09-10
US38815110P 2010-09-30 2010-09-30
US61/388,151 2010-09-30
US41906810P 2010-12-02 2010-12-02
US61/419,068 2010-12-02
PCT/US2011/029511 WO2011119663A1 (en) 2010-03-25 2011-03-23 Chemical compounds

Publications (2)

Publication Number Publication Date
CN102917588A CN102917588A (zh) 2013-02-06
CN102917588B true CN102917588B (zh) 2014-10-08

Family

ID=46160738

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180025962.7A Expired - Fee Related CN102917588B (zh) 2010-03-25 2011-03-23 化合物

Country Status (15)

Country Link
US (1) US20120077828A1 (enExample)
EP (1) EP2549868B1 (enExample)
JP (1) JP5876031B2 (enExample)
KR (1) KR101676077B1 (enExample)
CN (1) CN102917588B (enExample)
AR (1) AR080792A1 (enExample)
AU (1) AU2011232516B2 (enExample)
EA (1) EA022325B1 (enExample)
ES (1) ES2530955T3 (enExample)
IL (1) IL222120A (enExample)
MX (1) MX2012011045A (enExample)
SG (1) SG183954A1 (enExample)
TW (1) TW201202241A (enExample)
UY (1) UY33288A (enExample)
WO (1) WO2011119663A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110392579A (zh) * 2017-03-06 2019-10-29 坪田实验室股份有限公司 小鼠近视诱导模型及用于近视预防/抑制的内质网应激抑制剂

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112012024380A2 (pt) 2010-03-25 2015-09-15 Glaxosmithkline Llc compostos químicos
US20140227289A1 (en) * 2011-05-13 2014-08-14 Stephen Michael Cohen Compounds and methods for treating insulin resistance syndrome
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
CN106243113B (zh) 2011-07-19 2018-12-18 默沙东有限责任公司 作为btk抑制剂的选择的咪唑并吡嗪类
JP6496246B2 (ja) * 2012-10-05 2019-04-03 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． アルドステロンシンターゼインヒビター関連用途としてのインドリン化合物
TWI498325B (zh) * 2013-01-18 2015-09-01 Hoffmann La Roche ３－取代吡唑及其用途
EP2989091B1 (en) * 2013-04-04 2017-05-10 Janssen Pharmaceutica NV Novel n-(2,3-dihydro-1h-pyrrolo[2,3-b]pyridin-5-yl)-4- quinazolinamine and n-(2,3-dihydro-1h-indol-5-yl)-4- quinazolinamine derivatives as perk inhibitors
TWI482757B (zh) * 2013-10-07 2015-05-01 Luminescence Technology Corp Ｖｅｇｆ－２／３受體及蛋白質酪胺酸激酶抑制劑及其醫藥用途
WO2015056180A1 (en) * 2013-10-15 2015-04-23 Glaxosmithkline Intellectual Property (No.2) Limited Indoline derivatives as inhibitors of perk
AU2014358868A1 (en) 2013-12-05 2016-06-09 Acerta Pharma B.V. Therapeutic combination of a PI3K inhibitor and a BTK inhibitor
US10272083B2 (en) 2014-01-21 2019-04-30 Acerta Pharma B.V. Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor
EP3116877A1 (en) * 2014-03-11 2017-01-18 Glaxosmithkline Intellectual Property (No. 2) Limited Chemical compounds acting as perk inhibitors
US9937171B2 (en) 2014-04-11 2018-04-10 Acerta Pharma B.V. Methods of blocking the CXCR-4/SDF-1 signaling pathway with inhibitors of bruton's tyrosine kinase
WO2015193740A2 (en) 2014-06-17 2015-12-23 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pi3k inhibitor and/or a jak-2 inhibitor
EP3179991B1 (en) 2014-08-11 2021-10-06 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor and a bcl-2 inhibitor
PT3461821T (pt) * 2014-10-24 2020-08-05 Bristol Myers Squibb Co Compostos de indol carboxamida úteis como inibidores de quinase
CA2967125C (en) 2014-11-14 2022-10-25 Nerviano Medical Sciences S.R.L. 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors
WO2016126026A2 (ko) * 2015-02-04 2016-08-11 서울대학교병원 당뇨병 치료 조성물 및 이의 용도
DK3954690T3 (da) 2015-07-02 2023-06-06 Acerta Pharma Bv Faste former og formuleringer af (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamid
WO2017046739A1 (en) * 2015-09-15 2017-03-23 Glaxosmithkline Intellectual Property (No.2) Limited Imidazolidinone derivatives as inhibitors of perk
TW201722957A (zh) * 2015-09-15 2017-07-01 葛蘭素史克智慧財產（第二）有限公司 化學化合物
PE20181884A1 (es) * 2016-04-07 2018-12-07 Glaxosmithkline Ip Dev Ltd Amidas heterociclicas utiles como moduladores de proteinas
IL297192A (en) * 2016-04-15 2022-12-01 Cancer Research Tech Ltd Heterocyclic compounds as ret kinase inhibitors
US11026945B2 (en) * 2016-04-29 2021-06-08 The Trustees Of The University Of Pennsylvania Protein kinase RNA-like endoplasmic reticulum kinase (PERK) inhibitors for prevention and/or treatment of lung injury and/or inflammation
US10723706B2 (en) 2016-06-13 2020-07-28 Ramot At Tel-Aviv University Ltd. Perk inhibitors and uses thereof in treating diseases associated with aggregation-prone proteins
WO2017220477A1 (en) 2016-06-21 2017-12-28 Nerviano Medical Sciences S.R.L. N-(substituted-phenyl)-sulfonamide derivatives as kinase inhibitors
WO2018015879A1 (en) * 2016-07-20 2018-01-25 Glaxosmithkline Intellectual Property Development Limited Isoquinoline derivatives as perk inhibitors
US11759437B2 (en) 2016-09-22 2023-09-19 The University Of Hong Kong Preventive and therapeutic approach for aberrant cell differentiation and ISR-associated diseases
WO2018138358A1 (en) 2017-01-30 2018-08-02 Université de Liège Perk and ire-1a inhibitors against neurodevelopmental disorders
CN106974910B (zh) * 2017-03-02 2019-11-12 深圳大学 含索拉非尼和gsk2656157的药物组合物及用途
CN106963769B (zh) * 2017-03-03 2019-10-25 深圳大学 含pi3k抑制剂和perk抑制剂的药物组合物及其应用
PT3448859T (pt) * 2017-03-20 2019-10-25 Forma Therapeutics Inc Composições de pirrolopirrole como ativadores de piruvato quinase (pkr).
WO2019021208A1 (en) * 2017-07-27 2019-01-31 Glaxosmithkline Intellectual Property Development Limited USEFUL INDAZOLE DERIVATIVES AS PERK INHIBITORS
CA3080971A1 (en) 2017-11-02 2019-05-09 Calico Life Sciences Llc Modulators of the integrated stress pathway
CN108003163B (zh) * 2017-11-30 2020-11-24 武汉九州钰民医药科技有限公司 用作激酶抑制剂的吡唑并嘧啶类化合物及其应用
CN111100130B (zh) * 2018-10-29 2022-07-15 四川大学 4-氨基吡咯并嘧啶衍生物及其制备方法和用途
CN111213632B (zh) * 2019-11-19 2022-03-01 长春中医药大学 动物药环氧树脂标本制作方法
JP2023528659A (ja) 2020-06-08 2023-07-05 ハリア・セラピューティクス・インコーポレイテッド Ｎｅｋ７キナーゼの阻害剤
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
WO2022212326A1 (en) 2021-03-29 2022-10-06 Halia Therapeutics, Inc. Nek7 inhibitors
PH12023552774A1 (en) 2021-04-05 2024-04-15 Halia Therapeutics Inc Nek7 inhibitors
WO2023034236A1 (en) * 2021-08-31 2023-03-09 Wisconsin Alumni Research Foundation Deuterated inhibitors of rip kinases
GB202407386D0 (en) 2024-05-24 2024-07-10 Apollo Ap45 Ltd 1H-pyrazolo(4,3-D)pyrimidine derivatives

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005110410A2 (en) * 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
JP4163738B2 (ja) * 2004-06-11 2008-10-08 日本たばこ産業株式会社 癌の治療用の５−アミノ−２，４，７−トリオキソ−３，４，７，８−テトラヒドロ−２Ｈ−ピリド’２，３−ｄ！ピリミジン誘導体及び関連化合物
JP2009514899A (ja) * 2005-11-04 2009-04-09 スミスクライン ビーチャム コーポレーション チエノピリジンＢ−Ｒａｆキナーゼ阻害剤
EP2368566A1 (en) * 2006-07-13 2011-09-28 ZymoGenetics, Inc. Interleukin 21 and tyrosine kinase inhibitor combination therapy
WO2009151621A1 (en) * 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
EP2376492B1 (en) * 2008-09-19 2015-04-08 Nerviano Medical Sciences S.r.l. 3,4 DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110392579A (zh) * 2017-03-06 2019-10-29 坪田实验室股份有限公司 小鼠近视诱导模型及用于近视预防/抑制的内质网应激抑制剂
CN110392579B (zh) * 2017-03-06 2022-11-08 坪田实验室股份有限公司 小鼠近视诱导模型及用于近视预防/抑制的内质网应激抑制剂
US12478597B2 (en) 2017-03-06 2025-11-25 Tsubota Laboratory, Inc. Mouse myopia-induced model and endoplasmic reticulum stress suppressant for preventing and suppressing myopia

Also Published As

Publication number Publication date
EA022325B1 (ru) 2015-12-30
TW201202241A (en) 2012-01-16
KR20130018272A (ko) 2013-02-20
US20120077828A1 (en) 2012-03-29
SG183954A1 (en) 2012-10-30
IL222120A (en) 2015-09-24
CN102917588A (zh) 2013-02-06
AU2011232516A8 (en) 2012-12-13
EP2549868A1 (en) 2013-01-30
KR101676077B1 (ko) 2016-11-14
UY33288A (es) 2011-10-31
JP2013534902A (ja) 2013-09-09
EP2549868A4 (en) 2013-08-07
ES2530955T3 (es) 2015-03-09
MX2012011045A (es) 2012-11-16
EP2549868B1 (en) 2015-01-07
AU2011232516A1 (en) 2012-10-04
WO2011119663A8 (en) 2012-10-26
WO2011119663A1 (en) 2011-09-29
AU2011232516B2 (en) 2014-08-07
AR080792A1 (es) 2012-05-09
JP5876031B2 (ja) 2016-03-02
EA201290952A1 (ru) 2013-04-30

Similar Documents

Publication Publication Date Title
CN102917588B (zh) 化合物
US8598156B2 (en) Chemical compounds
CN109563043B (zh) 作为dnmt1的抑制剂的取代的吡啶
CN104955824B (zh) 作为含t790m的egfr突变体的抑制剂的氨基嘧啶化合物
CN105308038B (zh) Zeste增强子同源物2的抑制剂
DK2262807T3 (en) NOVEL tyrosine kinase inhibitors
CN112135824A (zh) 作为免疫调节剂的杂环化合物
TWI476199B (zh) 用於治療疾病之巨環衍生物
TW201922721A (zh) 化學化合物
CN115702025A (zh) 稠合三环kras抑制剂
CN115835908A (zh) 作为fgfr抑制剂的双环杂环
CN105916857B (zh) 吡咯并吡咯酮衍生物及其作为bet抑制剂的用途
CN112165944A (zh) 转录激活蛋白的咪唑并哌嗪抑制剂
TW201524958A (zh) 用作轉染期間重排抑制劑之新穎化合物
WO2015056180A1 (en) Indoline derivatives as inhibitors of perk
CN102858175A (zh) 作为脂肪酸合成酶抑制剂的三唑酮
CN107148419A (zh) Zeste增强子同源物2抑制剂
WO2018015879A1 (en) Isoquinoline derivatives as perk inhibitors
CN115515940A (zh) 用于治疗疾病的受体相互作用蛋白激酶i的抑制剂
CN107921044A (zh) 用于治疗疾病的gls1抑制剂
CN108349989A (zh) 吡喃并二吡啶化合物
CN104284899A (zh) 三环化合物和其应用方法
HK40117941A (zh) 包含抗癌剂和对前列腺素e2受体具有抑制活性的新化合物的用於治疗癌症的药物组合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20141008

Termination date: 20200323

CF01 Termination of patent right due to non-payment of annual fee