JP5927201B2 - Ask1阻害ピロロピリミジン誘導体 - Google Patents

Ask1阻害ピロロピリミジン誘導体 Download PDF

Info

Publication number
JP5927201B2
JP5927201B2 JP2013543883A JP2013543883A JP5927201B2 JP 5927201 B2 JP5927201 B2 JP 5927201B2 JP 2013543883 A JP2013543883 A JP 2013543883A JP 2013543883 A JP2013543883 A JP 2013543883A JP 5927201 B2 JP5927201 B2 JP 5927201B2
Authority
JP
Japan
Prior art keywords
pyrrolo
pyrimidin
piperidinyl
methyl
benzamide
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
JP2013543883A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014505037A (ja
JP2014505037A5 (enExample
Inventor
アール.ウイトトイ ダビド
アール.ウイトトイ ダビド
ノルトン ダビド
ノルトン ダビド
パウル トイエルネイ ジャソン
パウル トイエルネイ ジャソン
ロルトヒオイル グヒスライネ
ロルトヒオイル グヒスライネ
シメ マイリ
シメ マイリ
ロウイセ プヒルポトト カレン
ロウイセ プヒルポトト カレン
Original Assignee
カルチャン リミテッド
カルチャン リミテッド
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 カルチャン リミテッド, カルチャン リミテッド filed Critical カルチャン リミテッド
Publication of JP2014505037A publication Critical patent/JP2014505037A/ja
Publication of JP2014505037A5 publication Critical patent/JP2014505037A5/ja
Application granted granted Critical
Publication of JP5927201B2 publication Critical patent/JP5927201B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P17/06—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
    • A61P19/08—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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P37/08—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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
JP2013543883A 2010-12-16 2011-12-15 Ask1阻害ピロロピリミジン誘導体 Expired - Fee Related JP5927201B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42386510P 2010-12-16 2010-12-16
US61/423,865 2010-12-16
PCT/GB2011/052484 WO2012080735A1 (en) 2010-12-16 2011-12-15 Ask1 inhibiting pyrrolopyrimidine derivatives

Publications (3)

Publication Number Publication Date
JP2014505037A JP2014505037A (ja) 2014-02-27
JP2014505037A5 JP2014505037A5 (enExample) 2016-01-07
JP5927201B2 true JP5927201B2 (ja) 2016-06-01

Family

ID=45444639

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013543883A Expired - Fee Related JP5927201B2 (ja) 2010-12-16 2011-12-15 Ask1阻害ピロロピリミジン誘導体

Country Status (6)

Country Link
US (3) US9045485B2 (enExample)
EP (1) EP2651417B1 (enExample)
JP (1) JP5927201B2 (enExample)
ES (1) ES2617339T3 (enExample)
PL (1) PL2651417T3 (enExample)
WO (1) WO2012080735A1 (enExample)

Families Citing this family (32)

* 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
PL2651417T3 (pl) * 2010-12-16 2017-08-31 Calchan Limited Pochodne pirolopirymidyny hamujące ASK1
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
JP6318156B2 (ja) * 2012-09-06 2018-04-25 プレキシコン インコーポレーテッドPlexxikon Inc. キナーゼをモジュレートするための化合物および方法、ならびにその指標
CN104119342A (zh) * 2013-04-25 2014-10-29 苏州科捷生物医药有限公司 一种制备高纯度4-氯-5-甲基-7H-吡咯[2,3-d]嘧啶的方法
WO2015187499A1 (en) * 2014-06-03 2015-12-10 Gilead Sciences, Inc. Use of an ask1 inhibitor for the treatment of liver disease, optionally in combination with a loxl2 inhibitor
TW201618781A (zh) 2014-08-13 2016-06-01 吉李德科學股份有限公司 治療肺高血壓之方法
BR112017004589A2 (pt) * 2014-09-10 2018-01-23 Epizyme Inc composto, composição farmacêutica, método para tratar um paciente, uso de um composto, kit, e método para tratar um distúrbio mediado por proteína smyd
US10238636B2 (en) 2014-09-24 2019-03-26 Gilead Sciences, Inc. Methods of treating liver disease
US9586933B2 (en) 2014-12-23 2017-03-07 Gilead Sciences, Inc. Processes for preparing ASK1 inhibitors
MA41252A (fr) 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1
ES2886840T3 (es) 2016-08-31 2021-12-21 Eisai R&D Man Co Ltd Compuesto de pirazolo[1,5-a]pirimidina
JOP20190221A1 (ar) 2017-04-05 2019-09-23 Seal Rock Therapeutics Inc مركبات مثبطات كيناز منظم لإشارات الاستماتة 1 (ask1) واستخداماتها
PL3621615T3 (pl) 2017-05-12 2024-03-25 Enanta Pharmaceuticals, Inc. Inhibitory regulujące sygnał apoptozy kinazy 1 i sposoby ich stosowania
WO2018218042A1 (en) 2017-05-25 2018-11-29 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
WO2018218044A2 (en) 2017-05-25 2018-11-29 Enanta Pharmaceuticals Inc Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
GB201711234D0 (en) * 2017-07-12 2017-08-23 Galapagos Nv Pyrrolopyrimidine and pyrrolopyridine derivatives
CN107556318B (zh) * 2017-08-22 2020-08-11 山东大学 一种含哌啶的吡咯并嘧啶类化合物及其制备方法与应用
US10597382B2 (en) 2017-08-28 2020-03-24 Enanta Pharmaceuticals, Inc. Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
US11434249B1 (en) 2018-01-02 2022-09-06 Seal Rock Therapeutics, Inc. ASK1 inhibitor compounds and uses thereof
KR102723164B1 (ko) 2018-02-26 2024-10-30 에자이 알앤드디 매니지먼트 가부시키가이샤 피라졸로[1,5-a]피리미딘 화합물의 염 및 이의 결정
WO2019213239A1 (en) 2018-05-02 2019-11-07 Enanta Pharmaceuticals Inc. Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
IL278368B2 (en) 2018-05-02 2024-06-01 Enanta Pharm Inc Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020017569A1 (ja) * 2018-07-17 2020-01-23 日本ケミファ株式会社 T型カルシウムチャネル阻害剤
US10968199B2 (en) 2018-08-22 2021-04-06 Enanta Pharmaceuticals, Inc. Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
WO2020106707A1 (en) 2018-11-19 2020-05-28 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
JP2022081710A (ja) * 2019-03-29 2022-06-01 ユーティアイ リミテッド パートナーシップ 関節リウマチを治療するためのt型カルシウムチャネル阻害剤の使用
US20220226299A1 (en) * 2019-03-29 2022-07-21 Nippon Chemiphar Co., Ltd. Use of t-type calcium channel blocker for treating pruritus
CN111303155A (zh) * 2020-03-13 2020-06-19 深圳大学 靶向pak1抑制剂及其在抗肿瘤治疗药物中的应用
WO2023246876A1 (zh) * 2022-06-24 2023-12-28 上海科技大学 甲酰胺类衍生物的医药用途、甲酰胺类衍生物、包含其的药物组合物

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU641183B2 (en) 1989-09-19 1993-09-16 Teijin Limited Pyrrolo(2,3-d)pyrimidine derivative, process for preparing the same, and pharmaceutical preparation comprising the derivative as active ingredient
HUP0103836A3 (en) 1998-06-02 2003-05-28 Osi Pharmaceuticals Inc Uniond Pyrrolo[2,3d]pyrimidine compositions and their use
US6878716B1 (en) 1998-06-02 2005-04-12 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptor and uses thereof
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
AU781137B2 (en) * 1999-10-25 2005-05-05 Altana Pharma Ag Tetrahydrothiopy ranphthalazinone derivatives as PDE4 inhibitors
US6680322B2 (en) 1999-12-02 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US7160890B2 (en) 1999-12-02 2007-01-09 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
ES2269217T3 (es) 1999-12-02 2007-04-01 Osi Pharmaceuticals, Inc. Compuestos especificos para los receptores a1, a2a y a3 de adenosina y sus usos.
CA2464934A1 (en) 2001-10-31 2003-05-08 Bayer Healthcare Ag Pyrimido [4,5-b] indole derivatives
US20040138238A1 (en) 2002-08-08 2004-07-15 Dhanoa Dale S. Substituted aminopyrimidine compounds as neurokinin antagonists
WO2004048565A1 (ja) 2002-11-22 2004-06-10 Takeda Pharmaceutical Company Limited アポトーシス関連蛋白質およびその用途
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
WO2007125321A2 (en) * 2006-04-25 2007-11-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
JP2009534456A (ja) 2006-04-25 2009-09-24 アステックス、セラピューティックス、リミテッド 医薬化合物
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
EP2058309A4 (en) * 2006-08-04 2010-12-22 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
JP2010513458A (ja) * 2006-12-19 2010-04-30 ファイザー・プロダクツ・インク H−pgdsの阻害剤としてのニコチンアミド誘導体、およびプロスタグランジンd2の仲介による疾患を治療するためのその使用
AR064415A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de pirrolo-piperidinas y purinas,composiciones farmaceuticas que los contienen y usos en trastornos y/o enfermedades mediadas por pka y pkb.
AR064416A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
CA2679198C (en) * 2007-02-26 2011-07-12 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
WO2008117796A1 (ja) 2007-03-28 2008-10-02 Dainippon Sumitomo Pharma Co., Ltd. 新規ムチリン誘導体
CA2691448A1 (en) 2007-08-31 2009-03-05 Dominique Swinnen Triazolopyridine compounds and their use as ask inhibitors
BRPI0818533B8 (pt) 2007-10-11 2021-05-25 Astrazeneca Ab composto, composição farmacêutica, uso de um composto, e, processo para a preparação de um composto
WO2009123986A1 (en) 2008-03-31 2009-10-08 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
EP2297153B1 (en) 2008-04-21 2015-05-27 Lexicon Pharmaceuticals, Inc. Limk2 inhibitors, compositions comprising them, and methods of their use
WO2010008843A1 (en) 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
CA2728559A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
CN102159556A (zh) 2008-08-15 2011-08-17 得克萨斯大学评议会 1,4-苯并嗪化合物及其衍生物作为治疗药物用于治疗神经变性病状
PT2385832E (pt) 2009-01-08 2015-11-02 Curis Inc Inibidores de fosfoinoritide 3-quinase com uma fração de ligação ao zinco
US8987309B2 (en) 2009-04-17 2015-03-24 The Translational Genomics Research Institute Compounds, pharmaceutical compositions and methods of use of 2-aryl pyridylazoles
JP5690823B2 (ja) 2009-07-08 2015-03-25 レオ ファーマ アクティーゼルスカブ Jak受容体およびタンパク質チロシンキナーゼ阻害薬としての複素環化合物
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
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
WO2011041293A1 (en) 2009-09-30 2011-04-07 Takeda Pharmaceutical Company Limited Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors
SI2531501T1 (sl) 2010-02-03 2014-04-30 Takeda Pharmaceutical Company Limited Inhibitorji kinaze-1, ki regulirajo signal apoptoze
WO2011097594A2 (en) 2010-02-08 2011-08-11 Kinagen, Inc. Therapeutic methods and compositions involving allosteric kinase inhibition
EP2550266B1 (en) 2010-03-24 2018-05-09 Amitech Therapeutics Solutions, Inc. Heterocyclic compounds useful for kinase inhibition
US8440665B2 (en) 2010-07-02 2013-05-14 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibitors
JP5525612B2 (ja) 2010-07-23 2014-06-18 国立大学法人 東京大学 含窒素複素環誘導体
BR112013003864B1 (pt) 2010-08-20 2021-08-31 Hutchison Medipharma Limited Compostos de pirrolpirimidina, composição e uso dos mesmos
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
CN102372717B (zh) 2010-08-20 2014-06-18 和记黄埔医药(上海)有限公司 吡咯并嘧啶类化合物及其用途
US8937077B2 (en) 2010-10-22 2015-01-20 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
US9273028B2 (en) 2010-10-29 2016-03-01 Biogen Ma Inc. Heterocyclic tyrosine kinase inhibitors
PL2651417T3 (pl) * 2010-12-16 2017-08-31 Calchan Limited Pochodne pirolopirymidyny hamujące ASK1
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
EA025186B1 (ru) 2012-06-29 2016-11-30 Пфайзер Инк. НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2
JP6318156B2 (ja) 2012-09-06 2018-04-25 プレキシコン インコーポレーテッドPlexxikon Inc. キナーゼをモジュレートするための化合物および方法、ならびにその指標
WO2014043272A1 (en) 2012-09-12 2014-03-20 Trius Therapeutics Inc. Tricyclic gyrase inhibitors for use as antibacterial agents
UY35212A (es) 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis

Also Published As

Publication number Publication date
US20170210748A1 (en) 2017-07-27
EP2651417B1 (en) 2016-11-30
JP2014505037A (ja) 2014-02-27
PL2651417T3 (pl) 2017-08-31
US9585886B2 (en) 2017-03-07
US9045485B2 (en) 2015-06-02
US20140038957A1 (en) 2014-02-06
US20160067251A1 (en) 2016-03-10
EP2651417A1 (en) 2013-10-23
ES2617339T3 (es) 2017-06-16
WO2012080735A1 (en) 2012-06-21

Similar Documents

Publication Publication Date Title
JP2014505037A (ja) Ask1阻害ピロロピリミジン誘導体
CN110312719B (zh) 作为jak家族激酶抑制剂的咪唑并吡咯并吡啶
ES2866152T3 (es) Derivados de tirosina amida como inhibidores de la Rho-quinasa
CN121925411A (zh) 作为sos1抑制剂的新型酞嗪衍生物化合物及其用途
US20080039450A1 (en) Compounds
JP7130873B2 (ja) バニン阻害剤としてのヘテロ芳香族化合物
CN111448199A (zh) 具有抗乙型肝炎病毒(hbv)活性的新的高活性的氨基-噻唑取代的吲哚-2-甲酰胺
CN111212834A (zh) 作为变构shp2抑制剂的吡啶、吡嗪和三嗪化合物
TW202031659A (zh) 具抗b型肝炎病毒(hbv)活性之新穎6,7-二氫-4h-吡唑并[1,5-a]吡嗪吲哚-2-羧醯胺
TWI826509B (zh) 作為vanin抑制劑之雜芳族化合物
JP7195436B2 (ja) バニン阻害剤としての複素芳香族化合物
US10947218B2 (en) Aminopyridine derivatives and their use as selective ALK-2 inhibitors
CN111566103A (zh) 作为激酶抑制剂的氨基咪唑并吡嗪
TW202031661A (zh) 對抗b型肝炎病毒(hbv)之新穎6,7-二氫-4h-吡唑并[1,5-a]吡吲哚-2-甲醯胺活性劑
CN105611930A (zh) 作为非凋亡调控性细胞死亡抑制剂的螺环喹喔啉衍生物
CN114262322A (zh) 一类细胞程序性坏死抑制剂及其制备方法和用途
TW201910312A (zh) 環狀胺衍生物及其醫藥用途
WO2024089155A1 (en) Heterocyclic compounds as sting antagonists
WO2023072301A1 (zh) 吡唑[3,4-d]嘧啶-3-酮类化合物及其医药用途
CA3188786A1 (en) Novel vdac1 inhibitors
JP2023513488A (ja) Irak4阻害剤として有用な三環ヘテロアリール化合物
TW202106678A (zh) 抗b型肝炎病毒(hbv)之新穎草醯基哌嗪活性劑
JP2022541819A (ja) Irak4阻害剤として有用なチエノピリジニルおよびチアゾロピリジニル化合物
JP7682154B2 (ja) Irak4阻害剤として有用な二環ヘテロ環式化合物
WO2025228900A1 (en) Arylamide substituted indazoles and the use thereof as medicament

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141209

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20141209

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150806

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150818

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151110

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20151110

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20160204

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20160204

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20160329

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160425

R150 Certificate of patent or registration of utility model

Ref document number: 5927201

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R154 Certificate of patent or utility model (reissue)

Free format text: JAPANESE INTERMEDIATE CODE: R154

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313114

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees