CN103732597B - 三环杂环化合物和jak抑制剂 - Google Patents

三环杂环化合物和jak抑制剂 Download PDF

Info

Publication number
CN103732597B
CN103732597B CN201280039516.6A CN201280039516A CN103732597B CN 103732597 B CN103732597 B CN 103732597B CN 201280039516 A CN201280039516 A CN 201280039516A CN 103732597 B CN103732597 B CN 103732597B
Authority
CN
China
Prior art keywords
group
alkyl
unsubstituted
phenyl
aromatic heterocyclic
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
CN201280039516.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN103732597A (zh
Inventor
林圭史
渡边恒夫
外山公二
加门淳司
南昌孝
宇仁巳由纪
奈须麻莉子
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.)
Misao Kusano
Original Assignee
Nissan Chemical 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 Nissan Chemical Corp filed Critical Nissan Chemical Corp
Priority to CN201510345134.1A priority Critical patent/CN105001226B/zh
Publication of CN103732597A publication Critical patent/CN103732597A/zh
Application granted granted Critical
Publication of CN103732597B publication Critical patent/CN103732597B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems

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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201280039516.6A 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂 Expired - Fee Related CN103732597B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510345134.1A CN105001226B (zh) 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
JP2011-177289 2011-08-12
JP2011177270 2011-08-12
JP2011177289 2011-08-12
JP2011-177270 2011-08-12
JP2012097073 2012-04-20
JP2012-097073 2012-04-20
JP2012103516 2012-04-27
JP2012-103516 2012-04-27
JP2012-103517 2012-04-27
JP2012103517 2012-04-27
PCT/JP2012/070876 WO2013024895A1 (en) 2011-08-12 2012-08-10 Tricyclic heterocyclic compounds and jak inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510345134.1A Division CN105001226B (zh) 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂

Publications (2)

Publication Number Publication Date
CN103732597A CN103732597A (zh) 2014-04-16
CN103732597B true CN103732597B (zh) 2016-08-17

Family

ID=46826883

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201280039516.6A Expired - Fee Related CN103732597B (zh) 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂
CN201510345134.1A Expired - Fee Related CN105001226B (zh) 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201510345134.1A Expired - Fee Related CN105001226B (zh) 2011-08-12 2012-08-10 三环杂环化合物和jak抑制剂

Country Status (17)

Country Link
US (2) US9216999B2 (https=)
EP (2) EP3112370A1 (https=)
JP (2) JP6123804B2 (https=)
KR (1) KR102021159B1 (https=)
CN (2) CN103732597B (https=)
AU (1) AU2012295802B2 (https=)
BR (1) BR112014002472A2 (https=)
CA (1) CA2841458C (https=)
IL (2) IL230812A0 (https=)
IN (1) IN2014MN00228A (https=)
MX (1) MX365311B (https=)
MY (2) MY166970A (https=)
PH (1) PH12013502670A1 (https=)
RU (1) RU2632870C2 (https=)
TW (1) TWI601727B (https=)
UA (1) UA114606C2 (https=)
WO (1) WO2013024895A1 (https=)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7960139B2 (en) 2007-03-23 2011-06-14 Academia Sinica Alkynyl sugar analogs for the labeling and visualization of glycoconjugates in cells
ES2442024T3 (es) 2008-07-15 2014-02-07 Academia Sinica Matrices de glucano sobre portaobjetos de vidrio revestidos con aluminio de tipo PTFE y métodos relacionados
US11377485B2 (en) 2009-12-02 2022-07-05 Academia Sinica Methods for modifying human antibodies by glycan engineering
US10087236B2 (en) 2009-12-02 2018-10-02 Academia Sinica Methods for modifying human antibodies by glycan engineering
US10338069B2 (en) 2010-04-12 2019-07-02 Academia Sinica Glycan arrays for high throughput screening of viruses
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
AU2012295802B2 (en) 2011-08-12 2017-03-30 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and JAK inhibitors
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014031498A1 (en) 2012-08-18 2014-02-27 Academia Sinica Cell-permeable probes for identification and imaging of sialidases
AU2013305827A1 (en) 2012-08-21 2015-03-05 Academia Sinica Benzocyclooctyne compounds and uses thereof
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
JP6248948B2 (ja) * 2013-02-08 2017-12-20 日産化学工業株式会社 3環性ピロロピリジン化合物及びjak阻害剤
US9447026B2 (en) 2013-03-14 2016-09-20 Kalyra Pharmaceuticals, Inc. Bicyclic analgesic compounds
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
EP3013365B1 (en) 2013-06-26 2019-06-05 Academia Sinica Rm2 antigens and use thereof
EP3013347B1 (en) 2013-06-27 2019-12-11 Academia Sinica Glycan conjugates and use thereof
JP6486368B2 (ja) 2013-09-06 2019-03-20 アカデミア シニカAcademia Sinica 改変されたグリコシル基を含む糖脂質を用いたヒトiNKT細胞の活性化
CA2932039A1 (en) 2013-12-12 2015-06-18 Kalyra Pharmaceuticals, Inc. Bicyclic alkyl compounds and synthesis
AU2015206370A1 (en) 2014-01-16 2016-07-07 Academia Sinica Compositions and methods for treatment and detection of cancers
US10150818B2 (en) 2014-01-16 2018-12-11 Academia Sinica Compositions and methods for treatment and detection of cancers
CN113336653A (zh) 2014-03-07 2021-09-03 里科瑞尔姆Ip控股有限责任公司 螺桨烷衍生物及合成
CN106415244B (zh) * 2014-03-27 2020-04-24 中央研究院 反应性标记化合物及其用途
EP2924026A1 (en) * 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
BR112016023299A8 (pt) * 2014-05-14 2021-06-29 Nissan Chemical Ind Ltd composto tricíclico e inibidor de jak, agente preventivo, terapêutico ou de melhoria para doenças contra as quais inibição de jak é eficaz e para artrite reumatoide, medicamento e utilização desses compostos
CN106661099A (zh) 2014-05-27 2017-05-10 中央研究院 抗her2醣抗体及其用途
US10118969B2 (en) 2014-05-27 2018-11-06 Academia Sinica Compositions and methods relating to universal glycoforms for enhanced antibody efficacy
JP7093612B2 (ja) 2014-05-27 2022-06-30 アカデミア シニカ Bacteroides由来のフコシダーゼおよびそれを使用する方法
CA2950415A1 (en) 2014-05-27 2015-12-03 Academia Sinica Anti-cd20 glycoantibodies and uses thereof
WO2015184001A1 (en) 2014-05-28 2015-12-03 Academia Sinica Anti-tnf-alpha glycoantibodies and uses thereof
TWI745275B (zh) 2014-09-08 2021-11-11 中央研究院 使用醣脂激活人類iNKT細胞
US10308609B2 (en) 2014-09-17 2019-06-04 Zeno Royalties & Milestones, LLC Bicyclic compounds
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9975965B2 (en) 2015-01-16 2018-05-22 Academia Sinica Compositions and methods for treatment and detection of cancers
US10495645B2 (en) 2015-01-16 2019-12-03 Academia Sinica Cancer markers and methods of use thereof
JP6779887B2 (ja) 2015-01-24 2020-11-04 アカデミア シニカAcademia Sinica 新規なグリカンコンジュゲートおよびその使用方法
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
EP3426693A4 (en) 2016-03-08 2019-11-13 Academia Sinica PROCESS FOR MODULAR SYNTHESIS OF N-GLYCANES AND ARRANGEMENTS THEREOF
CA3034057A1 (en) 2016-08-22 2018-03-01 CHO Pharma Inc. Antibodies, binding fragments, and methods of use
MX390005B (es) 2016-10-03 2025-03-20 Hangzhou Highlightll Pharmaceutical Co Ltd Inhibidores selectivos de jak1 novedosos y usos de los mismos.
US11242327B2 (en) 2017-05-15 2022-02-08 Recurium Ip Holdings, Llc Analgesic compounds
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3656806B1 (en) 2017-07-20 2024-08-21 Mitsubishi Chemical Corporation Sheet molding compound, fiber-reinforced composite material, and method for producing fiber-reinforced composite material
KR102821964B1 (ko) 2017-11-03 2025-06-19 어클라리스 쎄라퓨틱스, 인코포레이티드 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법
WO2019090143A1 (en) 2017-11-03 2019-05-09 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrimidine-5-carboxylate analogs and methods of making the same
KR102034538B1 (ko) * 2017-11-28 2019-10-21 주식회사한국파마 Jak 저해제 화합물, 및 이의 제조방법
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
CN119080779A (zh) 2018-08-10 2024-12-06 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CA3138544A1 (en) 2019-05-02 2020-11-05 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as jak inhibitors
EP3969458A4 (en) 2019-05-13 2023-05-17 Borah, Inc. CHEMICAL COMPOUNDS
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
KR102228442B1 (ko) * 2019-08-14 2021-03-16 (주)호모미미쿠스 도식을 이용한 아이디에이션 플랫폼 장치 및 방법
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
IL298316A (en) * 2020-05-20 2023-01-01 Bayer Ag Process for preparing butyl-(5s)-5-({2-[4-(butoxycarbonyl)phenyl]ethyl}[2-(2-{[3-chloro-4'-(trifluoromethyl)[biphenyl]-4-yl) methoxy}phenyl)ethyl]amino)-8,7,6,5-tetrahydroquinoline-2-carboxylate
IL300557A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK1 inhibitor
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
CN114591351B (zh) * 2020-12-03 2023-12-05 成都科岭源医药技术有限公司 一种多环化合物及其制备方法和用途
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
EP4456896A1 (en) 2021-12-29 2024-11-06 Bayer Aktiengesellschaft Treatment of cardiopulmonary disorders
KR20240144177A (ko) 2021-12-29 2024-10-02 바이엘 악티엔게젤샤프트 (5s)-{[2-(4-카르복시페닐)에틸][2-(2-{[3-클로로-4'-(트리플루오로메틸)비페닐-4-일]메톡시}페닐)에틸]아미노}-5,6,7,8-테트라히드로퀴놀린-2-카르복실산및 약학적 활성 화합물로서 사용하기 위한 이의 결정질 형태를 제조하는 방법
AU2023235233A1 (en) 2022-03-14 2024-09-12 Slap Pharmaceuticals Llc Multicyclic compounds
CN116554057B (zh) * 2023-05-05 2023-12-15 杭州安道药业有限公司 降低促红细胞生长素(epo)生成的化合物及其用途
CN117586285B (zh) * 2024-01-19 2024-04-05 英矽智能科技(上海)有限公司 三并环类化合物

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101351466A (zh) * 2005-12-28 2009-01-21 安斯泰来制药株式会社 Janus激酶3的杂环抑制剂
CN101437822A (zh) * 2006-05-11 2009-05-20 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
WO2010044885A2 (en) * 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
WO2010119875A1 (ja) * 2009-04-14 2010-10-21 アステラス製薬株式会社 縮合ピロロピリジン誘導体
WO2011068899A1 (en) * 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds
CN102118968A (zh) * 2008-06-10 2011-07-06 雅培制药有限公司 新的三环化合物
WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
WO2012085176A1 (en) * 2010-12-23 2012-06-28 F. Hoffmann-La Roche Ag Tricyclic pyrazinone compounds, compositions and methods of use thereof as janus kinase inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60037345T2 (de) 1999-12-10 2008-11-13 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-Verbindungen
DE602006010553D1 (de) * 2005-06-29 2009-12-31 Nxp Bv Synchronisationsschema mit adaptiver referenzfrequenzkorrektur
WO2007007919A2 (en) * 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
AR064879A1 (es) 2007-01-12 2009-04-29 Astellas Pharma Inc Compuesto de piridina condensado
US8361962B2 (en) * 2009-07-27 2013-01-29 Roche Palo Alto Llc Tricyclic inhibitors of JAK
ES2426407T3 (es) 2009-10-15 2013-10-23 Pfizer Inc. Compuestos de pirrolo[2,3-d]pirimidina
RU2711869C3 (ru) 2009-12-01 2022-02-02 Эббви Инк. Имидазопирролопиразиновые производные, полезные для лечения заболеваний, вызванных аномальной активностью протеинкиназ Jak1, Jak3 или Syk
WO2011075334A1 (en) 2009-12-18 2011-06-23 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
CN201663335U (zh) * 2010-01-04 2010-12-01 飞利浦(中国)投资有限公司 一种插接站及包含该插接站的多媒体系统
CN102399233B (zh) * 2010-09-15 2014-08-13 山东轩竹医药科技有限公司 PI3K和mTOR双重抑制剂类化合物
WO2012149280A2 (en) * 2011-04-29 2012-11-01 Abbott Laboratories Novel tricyclic compounds
WO2013007765A1 (en) * 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
AU2012295802B2 (en) * 2011-08-12 2017-03-30 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and JAK inhibitors

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101351466A (zh) * 2005-12-28 2009-01-21 安斯泰来制药株式会社 Janus激酶3的杂环抑制剂
CN101437822A (zh) * 2006-05-11 2009-05-20 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
CN102118968A (zh) * 2008-06-10 2011-07-06 雅培制药有限公司 新的三环化合物
WO2010044885A2 (en) * 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
WO2010119875A1 (ja) * 2009-04-14 2010-10-21 アステラス製薬株式会社 縮合ピロロピリジン誘導体
WO2011068899A1 (en) * 2009-12-01 2011-06-09 Abbott Laboratories Novel tricyclic compounds
WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
WO2012085176A1 (en) * 2010-12-23 2012-06-28 F. Hoffmann-La Roche Ag Tricyclic pyrazinone compounds, compositions and methods of use thereof as janus kinase inhibitors

Also Published As

Publication number Publication date
US20160102102A1 (en) 2016-04-14
EP3112370A1 (en) 2017-01-04
UA114606C2 (uk) 2017-07-10
CA2841458A1 (en) 2013-02-21
WO2013024895A1 (en) 2013-02-21
JP2014525397A (ja) 2014-09-29
AU2012295802A1 (en) 2014-02-27
RU2014109363A (ru) 2015-09-20
BR112014002472A2 (pt) 2017-04-11
IN2014MN00228A (https=) 2015-09-25
TW201321380A (zh) 2013-06-01
TWI601727B (zh) 2017-10-11
JP6123804B2 (ja) 2017-05-10
JP2017141254A (ja) 2017-08-17
CA2841458C (en) 2019-07-16
CN105001226B (zh) 2017-09-08
US9216999B2 (en) 2015-12-22
US9556187B2 (en) 2017-01-31
KR20140059195A (ko) 2014-05-15
IL245309B (en) 2018-08-30
AU2012295802B2 (en) 2017-03-30
NZ709835A (en) 2016-03-31
IL245309A0 (en) 2016-06-30
EP2742049A1 (en) 2014-06-18
MX2014001687A (es) 2014-05-27
RU2632870C2 (ru) 2017-10-11
CN103732597A (zh) 2014-04-16
CN105001226A (zh) 2015-10-28
IL230812A0 (en) 2014-03-31
MY176647A (en) 2020-08-19
MX365311B (es) 2019-05-29
JP6432624B2 (ja) 2018-12-05
NZ620037A (en) 2015-09-25
US20140200344A1 (en) 2014-07-17
MY166970A (en) 2018-07-26
KR102021159B1 (ko) 2019-09-11
PH12013502670A1 (en) 2016-07-29

Similar Documents

Publication Publication Date Title
CN103732597B (zh) 三环杂环化合物和jak抑制剂
CN113840603B (zh) 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用
JP5567137B2 (ja) Jak2阻害剤、ならびに骨髄増殖性疾患および癌の治療のためのそれらの使用
CN102791714B (zh) N-(咪唑并嘧啶-7-基)-杂芳基酰胺衍生物及其作为pde10a抑制剂的用途
KR20210018915A (ko) Erk 억제제 및 이의 용도
CN109153651A (zh) 酰胺基-取代的环己烷衍生物
MX2012010050A (es) Inhibidores de pirrolopirazina cinasa.
US20250002507A1 (en) 7,8-dihydro-5h-1,6-naphthyridine derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor m4 for treating neurological and psychiatric disorders
EP3292127A1 (en) Tricyclic piperidine compounds
JP7611900B2 (ja) 縮合複素環化合物
KR20150036763A (ko) 축환 복소환 화합물
TW202446381A (zh) 作為α5-GABAA受體調節劑的雜環化合物
AU2024373566A1 (en) Ripk1 inhibitors and methods of use
HK40066114A (zh) 三唑并哒嗪类衍生物、其制备方法、药物组合物和用途
HK40066114B (zh) 三唑并哒嗪类衍生物、其制备方法、药物组合物和用途
NZ620037B2 (en) Tricyclic heterocyclic compounds and jak inhibitors
NZ709835B2 (en) Tricyclic heterocyclic compounds and jak inhibitors
HK1232539A1 (en) Tricyclic heterocyclic compounds and jak inhibitors

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
CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: Tokyo, Japan

Patentee after: Misao Kusano

Address before: Tokyo, Japan

Patentee before: Nissan Chemical Industries Co., Ltd.

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

Granted publication date: 20160817

Termination date: 20190810