IN2012CH01573A - - Google Patents

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Publication number
IN2012CH01573A
IN2012CH01573A IN1573CH2012A IN2012CH01573A IN 2012CH01573 A IN2012CH01573 A IN 2012CH01573A IN 1573CH2012 A IN1573CH2012 A IN 1573CH2012A IN 2012CH01573 A IN2012CH01573 A IN 2012CH01573A
Authority
IN
India
Prior art keywords
compounds
bruton
btk
formula
tyrosine kinase
Prior art date
Application number
Inventor
Mahesh Thakkar
Summon Koul
Debnath Bhuniya
Kasim Mookhtiar
Original Assignee
Advinus Therapeutics Ltd
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 Advinus Therapeutics Ltd filed Critical Advinus Therapeutics Ltd
Priority to CN201380019452.8A priority Critical patent/CN104662018B/en
Priority to JP2015506355A priority patent/JP6182593B2/en
Priority to CA2869954A priority patent/CA2869954C/en
Priority to AU2013250726A priority patent/AU2013250726B2/en
Priority to PCT/IN2013/000259 priority patent/WO2013157022A1/en
Priority to IN1573CH2012 priority patent/IN2012CH01573A/en
Priority to EP13737672.9A priority patent/EP2838898B1/en
Priority to US14/509,793 priority patent/US9233983B2/en
Priority to ZA2014/07341A priority patent/ZA201407341B/en
Priority to IL235146A priority patent/IL235146A/en
Publication of IN2012CH01573A publication Critical patent/IN2012CH01573A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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    • 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
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    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present disclosure provides hetero-biclyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton’s tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I).These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton’s tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
IN1573CH2012 2012-04-20 2013-04-18 IN2012CH01573A (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
CN201380019452.8A CN104662018B (en) 2012-04-20 2013-04-18 Substituted Heterobicyclic compounds, composition and its medical applications
JP2015506355A JP6182593B2 (en) 2012-04-20 2013-04-18 Substituted heterobicyclic compounds, compositions and medicaments and uses thereof
CA2869954A CA2869954C (en) 2012-04-20 2013-04-18 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof in medical conditions related to modulation of bruton's tyrosine kinase activity
AU2013250726A AU2013250726B2 (en) 2012-04-20 2013-04-18 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
PCT/IN2013/000259 WO2013157022A1 (en) 2012-04-20 2013-04-18 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
IN1573CH2012 IN2012CH01573A (en) 2012-04-20 2013-04-18
EP13737672.9A EP2838898B1 (en) 2012-04-20 2013-04-18 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
US14/509,793 US9233983B2 (en) 2012-04-20 2014-10-08 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
ZA2014/07341A ZA201407341B (en) 2012-04-20 2014-10-09 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
IL235146A IL235146A (en) 2012-04-20 2014-10-19 Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IN1573CH2012 IN2012CH01573A (en) 2012-04-20 2013-04-18

Publications (1)

Publication Number Publication Date
IN2012CH01573A true IN2012CH01573A (en) 2015-07-10

Family

ID=48794150

Family Applications (1)

Application Number Title Priority Date Filing Date
IN1573CH2012 IN2012CH01573A (en) 2012-04-20 2013-04-18

Country Status (10)

Country Link
US (1) US9233983B2 (en)
EP (1) EP2838898B1 (en)
JP (1) JP6182593B2 (en)
CN (1) CN104662018B (en)
AU (1) AU2013250726B2 (en)
CA (1) CA2869954C (en)
IL (1) IL235146A (en)
IN (1) IN2012CH01573A (en)
WO (1) WO2013157022A1 (en)
ZA (1) ZA201407341B (en)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2571361A4 (en) 2010-05-19 2013-11-13 Univ North Carolina PYRAZOLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER
US9273056B2 (en) 2011-10-03 2016-03-01 The University Of North Carolina At Chapel Hill Pyrrolopyrimidine compounds for the treatment of cancer
US9567326B2 (en) 2012-05-22 2017-02-14 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
JP6348492B2 (en) 2012-08-10 2018-06-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Heteroaromatic compounds as breton-type tyrosine kinase (BTK) inhibitors
WO2014062774A1 (en) 2012-10-17 2014-04-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
WO2014085225A1 (en) 2012-11-27 2014-06-05 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
MX2015012899A (en) * 2013-03-14 2016-06-02 Abbvie Inc Pyrrolo[2,3-b]pyridine cdk9 kinase inhibitors.
CN104211703B (en) * 2013-05-30 2018-04-03 南京勇山生物科技有限公司 A kind of fused heterocyclic compound as Bu Ludun kinase inhibitors
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
WO2015157127A1 (en) 2014-04-11 2015-10-15 The University Of North Carolina At Chapel Hill Therapuetic uses of selected pyrimidine compounds with anti-mer tyrosine kinase activity
CN105294571B (en) * 2014-07-03 2019-04-23 浙江九洲药业股份有限公司 A kind of Ibrutinib intermediate and its preparation method and use
MX381819B (en) 2014-08-04 2025-03-13 Nuevolution As OPTIONALLY CONDENSED HETEROCYCLIC PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF INFLAMMATORY, METABOLIC, ONCOLOGICAL AND AUTOIMMUNE DISEASES.
KR102523111B1 (en) 2014-10-06 2023-04-18 메르크 파텐트 게엠베하 Heteroaryl compounds as btk inhibitors and uses thereof
US10272070B2 (en) 2014-10-14 2019-04-30 The Board of Trustees of the Leland Stanford Junio r University Method for treating neurodegenerative diseases
LT3461821T (en) 2014-10-24 2020-08-10 Bristol-Myers Squibb Company INDOL CARBOXAMIDE COMPOUNDS FOR USE AS KINASE INHIBITORS
EP3042903B1 (en) * 2015-01-06 2019-08-14 Impetis Biosciences Ltd. Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
CN107847765B (en) 2015-06-18 2021-05-04 89生物有限公司 1,4-Substituted piperidine derivatives
MX379846B (en) 2015-06-18 2025-03-11 89Bio Ltd SUBSTITUTED 4-BENZYL AND 4-BENZOYL PIPERIDINE DERIVATIVES.
GB201517216D0 (en) * 2015-09-29 2015-11-11 Cancer Res Technology Ltd And Astex Therapeutics Ltd Pharmaceutical compounds
GB201517217D0 (en) * 2015-09-29 2015-11-11 Astex Therapeutics Ltd And Cancer Res Technology Ltd Pharmaceutical compounds
KR20180094989A (en) 2015-12-15 2018-08-24 더 보드 오브 트러스티스 오브 더 리랜드 스탠포드 주니어 유니버시티 A method for preventing and / or treating aging-related cognitive disorders and neuroinflammation
EP3402789B1 (en) * 2016-01-13 2020-03-18 Boehringer Ingelheim International Gmbh Isoquinolones as btk inhibitors
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
KR102426043B1 (en) 2016-04-15 2022-07-27 블루프린트 메디신즈 코포레이션 Inhibitors of activin receptor-like kinases
CA2969295A1 (en) 2016-06-06 2017-12-06 Pfizer Inc. Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor
CA3034239A1 (en) * 2016-08-16 2018-02-22 Merck Patent Gmbh 2-oxo-imidazopyridines as reversible btk inhibitors and uses thereof
KR102565546B1 (en) 2016-11-25 2023-08-10 카나 바이오사이언스, 인코포레이션 Novel oxoisoquinoline derivatives
CN106883235B (en) * 2016-12-29 2019-04-30 天津国际生物医药联合研究院 The preparation and application of furodiazole compound
EP3556761B1 (en) * 2017-02-08 2021-03-03 The National Institutes Of Pharmaceutical Research Pyrrolo-aromatic heterocyclic compound, preparation method therefor, and medical use thereof
CN108794480A (en) * 2017-04-28 2018-11-13 天津药物研究院有限公司 Azolopyrimidines, preparation method and use
CN111566102B (en) 2017-10-18 2023-09-08 缆图药品公司 Substituted pyrrolopyridines as activin receptor-like kinase inhibitors
KR102708147B1 (en) * 2017-12-13 2024-09-19 루핀 리미티드 Substituted bicyclic heterocyclic compounds as PRMT5 inhibitors
CN109293638B (en) * 2018-03-27 2020-08-14 大连理工大学 An enhanced fluorescence sensor targeting receptor tyrosine kinase and its application in cell membrane fluorescence imaging
CN108707154A (en) * 2018-07-10 2018-10-26 刘凤娟 A kind of drug solvent for the treatment of cancer closes object and preparation method thereof
US12195432B2 (en) 2018-08-06 2025-01-14 The Board Of Trustees Of The Leland Stanford Junior University 2-arylbenzimidazoles as Ppargc1a activators for treating neurodegenerative diseases
EP3847170B1 (en) * 2018-09-06 2022-06-22 F. Hoffmann-La Roche AG Novel cyclic amidine compounds for the treatment of autoimmune disease
CN109180643A (en) * 2018-10-04 2019-01-11 南京先进生物材料与过程装备研究院有限公司 Phthalazines ketone compound crystal form A and preparation method thereof
CN109485636A (en) * 2018-10-04 2019-03-19 南京先进生物材料与过程装备研究院有限公司 A kind of hydrochloride of novel B TK kinase inhibitor and preparation method thereof and purposes
CN109180642A (en) * 2018-10-04 2019-01-11 南京先进生物材料与过程装备研究院有限公司 Phthalazines ketone BTK inhibitor and its application
CN109336864A (en) * 2018-10-04 2019-02-15 南京先进生物材料与过程装备研究院有限公司 Phthalazines ketone compound crystal form N and preparation method thereof
CN109369619A (en) * 2018-10-04 2019-02-22 南京先进生物材料与过程装备研究院有限公司 Phthalazines ketone compound crystal form B and preparation method thereof
CN109293635A (en) * 2018-10-04 2019-02-01 南京先进生物材料与过程装备研究院有限公司 A kind of P crystal form of novel B TK kinase inhibitor and preparation method thereof
CN109180644A (en) * 2018-10-04 2019-01-11 南京先进生物材料与过程装备研究院有限公司 A kind of mesylate of novel B TK kinase inhibitor and preparation method thereof and purposes
CN109336863A (en) * 2018-10-04 2019-02-15 南京先进生物材料与过程装备研究院有限公司 A kind of novel phthalazines ketone BTK inhibitor, preparation and its application
HUE064493T2 (en) * 2019-06-10 2024-03-28 Lupin Ltd Prmt5 inhibitors
CN110305140B (en) * 2019-07-30 2020-08-04 上海勋和医药科技有限公司 Dihydropyrrolopyrimidines selective JAK2 inhibitors
CA3160522A1 (en) 2019-12-20 2021-06-24 Sanne Schroder Glad Compounds active towards nuclear receptors
WO2021120890A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
MX2022012259A (en) 2020-03-31 2022-12-08 Nuevolution As COMPOUNDS ACTIVE AGAINST NUCLEAR RECEPTORS.
MX2022012260A (en) 2020-03-31 2022-11-30 Nuevolution As COMPOUNDS ACTIVE AGAINST NUCLEAR RECEPTORS.
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
CN116854709A (en) * 2022-03-28 2023-10-10 药雅科技(上海)有限公司 Bruton's tyrosine kinase reversible inhibitors and their applications

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
EP2258371A1 (en) * 2001-08-10 2010-12-08 Novartis AG Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia
EP1446115B1 (en) 2001-11-13 2008-02-27 Merck Frosst Canada Ltd. Cyanoalkylamino derivatives as protease inhibitors
US20060183746A1 (en) * 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
CN101124227A (en) * 2004-11-10 2008-02-13 Cgi制药有限公司 Imidazo[1,2-a]pyrazin-8-ylamines useful as modulators of kinase activity
US7456195B2 (en) 2005-06-24 2008-11-25 Bristol-Myers Squibb Company Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
US8071609B2 (en) * 2005-08-11 2011-12-06 Ariad Pharmaceuticals, Inc. Unsaturated heterocyclic derivatives
ATE528302T1 (en) 2005-08-29 2011-10-15 Vertex Pharma 3,5-DISUBSTITUTED PYRID-2-ONES USEFUL AS INHIBITORS OF THE TEC FAMILY OF NON-RECEPTOR TYROSINE KINASES
US20070129364A1 (en) 2005-12-07 2007-06-07 Han-Qing Dong Pyrrolopyridine kinase inhibiting compounds
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
DK2242749T3 (en) 2008-02-05 2013-06-17 Hoffmann La Roche NEW PYRIDINONES AND PYRIDAZINONES
JP5638961B2 (en) 2008-03-13 2014-12-10 ザ ジェネラル ホスピタル コーポレイション Inhibitors of BMP signaling pathway
CA2725754C (en) 2008-06-11 2017-05-23 Hazel Joan Dyke Diazacarbazoles and methods of use
ES2420854T3 (en) 2008-07-02 2013-08-27 F. Hoffmann-La Roche Ag New phenylpyrazinones as kinase inhibitors
CA2728559A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
JP2011527677A (en) 2008-07-08 2011-11-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Pyrrolidinyl and piperidinyl compounds useful as NHE-1 inhibitors
UY31984A (en) 2008-07-16 2010-02-26 Boehringer Ingelheim Int DERIVATIVES OF N-substituted 1- (3,4-difluorobenzyl) -6-oxo-1,6-dihydropyrimidin-5-carboxamides and 2- (3,4-difluorobenzyl) -3-oxo-2,3-dihydro- N-substituted 1H-pyrazol-4-carboxamides.
EP2307418B1 (en) 2008-07-18 2014-03-12 F.Hoffmann-La Roche Ag Novel phenylimidazopyrazines
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
WO2010068788A1 (en) 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Heterocyclic amides as btk inhibitors
WO2010068810A2 (en) 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
WO2010068806A1 (en) * 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Amide derivatives as btk inhibitors in the treatment of allergic, autoimmune and inflammatory disorders as well as cancer
BRPI0922565A2 (en) 2008-12-19 2015-12-15 Bristol Myers Squibb Co carbazole carboxamide compounds useful as kinase inhibitors
US8299077B2 (en) 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
SG175287A1 (en) 2009-04-24 2011-11-28 Hoffmann La Roche Inhibitors of bruton's tyrosine kinase
CN102458402B (en) 2009-06-12 2013-10-02 百时美施贵宝公司 Nicotinamide compounds useful as kinase modulators
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
EP3461824B1 (en) * 2009-09-04 2021-08-25 Biogen MA Inc. Bruton's tyrosine kinase inhibitors
US7718662B1 (en) 2009-10-12 2010-05-18 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase
PE20121519A1 (en) 2010-01-27 2012-12-02 Boehringer Ingelheim Int PIRAZOLE COMPOUNDS AS ANTAGONISTS OF CRTH2
US9307625B2 (en) * 2011-04-05 2016-04-05 Eth Zurich Droplet dispensing device and light source comprising such a droplet dispensing device
MX2014000338A (en) * 2011-07-08 2014-05-01 Novartis Ag Novel pyrrolo pyrimidine derivatives.
CA2841801A1 (en) 2011-08-17 2013-02-21 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase

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