JP6243062B2 - Ｓｙｋ阻害剤 - Google Patents

Ｓｙｋ阻害剤 Download PDF

Info

Publication number
JP6243062B2
JP6243062B2 JP2016560876A JP2016560876A JP6243062B2 JP 6243062 B2 JP6243062 B2 JP 6243062B2 JP 2016560876 A JP2016560876 A JP 2016560876A JP 2016560876 A JP2016560876 A JP 2016560876A JP 6243062 B2 JP6243062 B2 JP 6243062B2
Authority
JP
Japan
Prior art keywords
pharmaceutically acceptable
crystal
compound
acceptable salt
cancer
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.)
Active
Application number
JP2016560876A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017501229A (ja
Inventor
ピーター エー． ブロムグレン，
ピーター エー． ブロムグレン，
ケビン エス． キュリー，
ケビン エス． キュリー，
ジェフリー イー． クロップフ，
ジェフリー イー． クロップフ，
スン エイチ． リー，
スン エイチ． リー，
ジェニファー アール． ロー，
ジェニファー アール． ロー，
スコット エー． ミッチェル，
スコット エー． ミッチェル，
アーロン シー． シュミット，
アーロン シー． シュミット，
ジン−ミン シオン，
ジン−ミン シオン，
ジアンジュン シュー，
ジアンジュン シュー，
ゾンドン ザオ，
ゾンドン ザオ，
スンダラモーシ スワミナサン，
スンダラモーシ スワミナサン，
Original Assignee
ギリアード サイエンシーズ， インコーポレイテッド
ギリアード サイエンシーズ， インコーポレイテッド
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52350364&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP6243062(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ギリアード サイエンシーズ， インコーポレイテッド, ギリアード サイエンシーズ， インコーポレイテッド filed Critical ギリアード サイエンシーズ， インコーポレイテッド
Publication of JP2017501229A publication Critical patent/JP2017501229A/ja
Application granted granted Critical
Publication of JP6243062B2 publication Critical patent/JP6243062B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P1/16—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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/04—Antipruritics
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P37/02—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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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

Landscapes

  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
JP2016560876A 2013-12-23 2014-12-22 Ｓｙｋ阻害剤 Active JP6243062B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361920407P 2013-12-23 2013-12-23
US61/920,407 2013-12-23
PCT/US2014/071842 WO2015100217A1 (en) 2013-12-23 2014-12-22 Syk inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017172941A Division JP6530792B2 (ja) 2013-12-23 2017-09-08 Ｓｙｋ阻害剤

Publications (2)

Publication Number Publication Date
JP2017501229A JP2017501229A (ja) 2017-01-12
JP6243062B2 true JP6243062B2 (ja) 2017-12-06

Family

ID=52350364

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2016560876A Active JP6243062B2 (ja) 2013-12-23 2014-12-22 Ｓｙｋ阻害剤
JP2017172941A Active JP6530792B2 (ja) 2013-12-23 2017-09-08 Ｓｙｋ阻害剤
JP2019093810A Pending JP2019172680A (ja) 2013-12-23 2019-05-17 Ｓｙｋ阻害剤

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2017172941A Active JP6530792B2 (ja) 2013-12-23 2017-09-08 Ｓｙｋ阻害剤
JP2019093810A Pending JP2019172680A (ja) 2013-12-23 2019-05-17 Ｓｙｋ阻害剤

Country Status (44)

Country Link
US (5) US9968601B2 (OSRAM)
EP (2) EP3342773B9 (OSRAM)
JP (3) JP6243062B2 (OSRAM)
KR (3) KR20200098735A (OSRAM)
CN (2) CN107746405B (OSRAM)
AP (1) AP2016009274A0 (OSRAM)
AR (1) AR098912A1 (OSRAM)
AU (3) AU2014370010B2 (OSRAM)
BR (1) BR112016014643B1 (OSRAM)
CA (1) CA2875877C (OSRAM)
CL (1) CL2016001537A1 (OSRAM)
CR (1) CR20160287A (OSRAM)
CU (1) CU20160097A7 (OSRAM)
CY (1) CY1120104T1 (OSRAM)
DK (2) DK3087075T3 (OSRAM)
DO (1) DOP2016000140A (OSRAM)
EA (2) EA201891553A1 (OSRAM)
ES (2) ES2851335T3 (OSRAM)
GT (1) GT201600123A (OSRAM)
HK (1) HK1251563A1 (OSRAM)
HR (2) HRP20180460T1 (OSRAM)
HU (2) HUE053815T2 (OSRAM)
IL (1) IL245846B (OSRAM)
LT (1) LT3087075T (OSRAM)
MD (1) MD4666C1 (OSRAM)
ME (1) ME03001B (OSRAM)
MX (2) MX392440B (OSRAM)
MY (1) MY199564A (OSRAM)
NO (1) NO3183247T3 (OSRAM)
NZ (1) NZ721175A (OSRAM)
PE (1) PE20160995A1 (OSRAM)
PH (2) PH12016501204B1 (OSRAM)
PL (2) PL3342773T3 (OSRAM)
PT (2) PT3342773T (OSRAM)
RS (1) RS57182B1 (OSRAM)
SG (3) SG10201707432SA (OSRAM)
SI (2) SI3342773T1 (OSRAM)
SM (1) SMT201800193T1 (OSRAM)
SV (1) SV2016005229A (OSRAM)
TW (2) TWI735853B (OSRAM)
UA (2) UA124667C2 (OSRAM)
UY (1) UY35898A (OSRAM)
WO (1) WO2015100217A1 (OSRAM)
ZA (1) ZA201800913B (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018513173A (ja) * 2015-04-21 2018-05-24 ギリアード サイエンシーズ， インコーポレイテッド Ｓｙｋ阻害剤を用いた慢性移植片対宿主病の処置

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010068258A1 (en) 2008-12-08 2010-06-17 Cgi Pharmaceuticals, Inc. Imidazopyrazine syk inhibitors
MX350010B (es) 2010-03-11 2017-08-23 Gilead Connecticut Inc Inhibidores syk de imidazopiridinas.
NZ715776A (en) 2013-07-30 2017-04-28 Gilead Connecticut Inc Polymorph of syk inhibitors
CA2919479C (en) 2013-07-31 2017-08-22 Gilead Sciences, Inc. Syk inhibitors
EP3076976B1 (en) 2013-12-04 2020-09-02 Gilead Sciences, Inc. Methods for treating cancers
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
MX2017000610A (es) 2014-07-14 2017-04-27 Gilead Sciences Inc Metodos combinados para tratar canceres.
TW201617074A (zh) * 2014-07-14 2016-05-16 吉李德科學股份有限公司 Ｓｙｋ（脾酪胺酸激酶）抑制劑
EP3331531A1 (en) * 2015-08-03 2018-06-13 Gilead Sciences, Inc. Combination therapies for treating cancers
US20170173034A1 (en) * 2015-12-17 2017-06-22 Gilead Sciences, Inc. Combination of a jak inhibitor and a syk inhibitor for treating cancers and inflammatory disorders
WO2018053190A1 (en) * 2016-09-14 2018-03-22 Gilead Sciences, Inc. Syk inhibitors
TW201822764A (zh) * 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
US11384082B2 (en) 2017-08-25 2022-07-12 Kronos Bio, Inc. Hydrates of polymorphs of 6-(1H-indazol-6-YL)-N-(4-morpholinophenyl)-2,3-dihydroimidazo[1,2-A]pyrazin-8-amine bisemsylate as Syk inhibitors
BR112020007679A2 (pt) 2017-10-19 2020-10-20 Bayer Animal Health Gmbh uso de pirrolidonas heteroaromáticas fundidas para tratamento e prevenção de doenças em animais.
MY196582A (en) 2018-02-13 2023-04-19 Gilead Sciences Inc PD-1/PD-L1 Inhibitors
WO2019204609A1 (en) 2018-04-19 2019-10-24 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
PE20210004A1 (es) 2018-05-14 2021-01-05 Gilead Sciences Inc Inhibidores de mcl-1
PT3820572T (pt) 2018-07-13 2023-11-10 Gilead Sciences Inc Inibidores pd-1/pd-l1
CN110833549B (zh) * 2018-08-15 2023-05-02 广西梧州制药（集团）股份有限公司 吡唑并嘧啶衍生物在治疗慢性盆腔炎的用途
EP3870566A1 (en) 2018-10-24 2021-09-01 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CN113950479A (zh) 2019-02-22 2022-01-18 克洛诺斯生物股份有限公司 作为syk抑制剂的缩合吡嗪的固体形式
JP2022526713A (ja) 2019-03-21 2022-05-26 オンクセオ がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4157848A4 (en) * 2020-06-01 2024-07-17 Nanjing Ruijie Pharma Co., Ltd. COMPOUNDS AND THEIR USES AS SPLEEN TYROSINE KINASE INHIBITORS
US20230277586A1 (en) * 2020-07-29 2023-09-07 University Of Kentucky Research Foundation Accelerating repair of mucosal injury using gold(iii) compounds
US20230265108A1 (en) * 2020-07-29 2023-08-24 University Of Kentucky Research Foundation Gold(iii) compounds and cancer cell-selective modulation of mitochondrial respiration and metabolism
CN112939983A (zh) * 2021-02-01 2021-06-11 暨明医药科技（苏州）有限公司 一种SYK激酶抑制剂Lanraplenib的合成方法
CN113480543B (zh) * 2021-07-07 2022-05-17 无锡市第二人民医院 2,6,8-多取代咪唑并[1,2-a]吡嗪及其合成方法和应用
WO2024037910A1 (en) * 2022-08-17 2024-02-22 Institut National de la Santé et de la Recherche Médicale Syk inhibitors for use in the treatment of cancer
WO2024102970A1 (en) * 2022-11-11 2024-05-16 Kronos Bio, Inc. Compounds for modulating syk activity and e3 ubiquitin ligase activity
WO2024124063A1 (en) * 2022-12-09 2024-06-13 Kronos Bio, Inc. Crystalline forms of lanraplenib and methods of making and using the same
CN118286149B (zh) * 2024-04-17 2024-12-24 湖南天华医药生物科技有限公司 一种治疗风湿骨痛的组合物及其制备方法及其应用

Family Cites Families (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US5137876A (en) 1990-10-12 1992-08-11 Merck & Co., Inc. Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same
DE4327027A1 (de) 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337611A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
KR20040068613A (ko) 1994-03-25 2004-07-31 이소테크니카 인코포레이티드 중수소화된 화합물 이를 포함하는 고혈압 치료용 조성물
FR2723373B1 (fr) 1994-08-02 1996-09-13 Rhone Poulenc Rorer Sa Forme purifiee de streptogramines, sa preparation et les compositions pharmaceutiques qui la contiennent
JPH11505524A (ja) 1995-05-01 1999-05-21 藤沢薬品工業株式会社 イミダゾ１，２−ａピリジンおよびイミダゾ１，２−ａピリデジン誘導体、および骨吸収阻害剤としてのその用途
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
SE9704404D0 (sv) 1997-11-28 1997-11-28 Astra Ab New compounds
DK1146892T3 (da) 1999-01-25 2003-11-24 Apoxis Sa BAFF, inhibitorer deraf og deres anvendelse i modulationen af B-celle responset
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
EP1175205B1 (en) 1999-11-12 2006-06-14 Abbott Laboratories Solid dispersion comprising ritonavir, fenofibrate or griseofulvin
SK8562002A3 (en) 1999-12-23 2003-10-07 Pfizer Prod Inc Pharmaceutical compositions providing enhanced drug concentrations
JP2001302667A (ja) 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
GB0018473D0 (en) 2000-07-27 2000-09-13 Merck Sharp & Dohme Therapeutic agents
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US6858613B2 (en) 2002-02-19 2005-02-22 Pfizer Inc. Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
EP1509526A2 (en) 2002-04-19 2005-03-02 Cellular Genomics Inc. Imidazo(1,2-a)pyrazin-8-ylamines, method of making, and method of use thereof
EP1506188B1 (en) 2002-05-14 2009-02-25 Xenova Limited Process for the preparation of a hydrate of an anthranilic acid derivative
KR20040012451A (ko) 2002-05-14 2004-02-11 어플라이드 머티어리얼스, 인코포레이티드 포토리소그래픽 레티클을 에칭하는 방법
WO2004022562A1 (en) 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
MXPA05003058A (es) 2002-09-19 2005-05-27 Schering Corp Nuevas imidazopiridinas como inhibidores de cinasa dependientes de ciclina.
KR20060010709A (ko) 2002-09-23 2006-02-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진
WO2004026877A1 (en) 2002-09-23 2004-04-01 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
WO2004072080A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of hsp90 complex activity
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
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
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
WO2005019220A2 (en) 2003-08-11 2005-03-03 Cellular Genomics Inc. Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
US7973161B2 (en) 2003-11-13 2011-07-05 Abbott Laboratories Apoptosis promoters
WO2005085252A1 (en) 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
EA011446B1 (ru) 2004-06-17 2009-02-27 Форест Лэборэтериз, Инк. Препаративные формы оральных лекарственных форм мемантина с модифицированным высвобождением
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
CN101124227A (zh) 2004-11-10 2008-02-13 Cgi制药有限公司 可用作激酶活性调节剂的咪唑并[1,2-a]吡嗪-8-基胺
KR20070119606A (ko) 2004-11-10 2007-12-20 씨지아이 파마슈티칼스, 인크. 특정 이미다조[１,２-ａ]피라진-８-일아민, 그의 제조 방법및 용도
CA2606147C (en) 2005-05-12 2011-07-05 Abbott Laboratories Apoptosis promoters
BRPI0618520A2 (pt) 2005-11-10 2011-09-06 Schering Corp imidazopirazinas como inibidores de proteìna cinase
BRPI0716239A2 (pt) 2006-08-30 2013-08-13 Cellzome Ltd derivados de triazol como inibidores de cinase
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
CA2706445C (en) 2007-11-28 2019-07-23 Irx Therapeutics, Inc. Production of apoptosis-resistant t-lymphocytes for use in cancer therapy
CN101952283B (zh) 2007-12-14 2013-04-17 霍夫曼-拉罗奇有限公司 咪唑并[1，2-a]吡啶和咪唑并[1，2-b]哒嗪衍生物
TW200938542A (en) 2008-02-01 2009-09-16 Irm Llc Compounds and compositions as kinase inhibitors
AR075257A1 (es) 2008-02-01 2011-03-23 Hexima Ltd Sistema de proteccion de plantas contra la infeccion por agentes patogenos
US20090221612A1 (en) 2008-02-13 2009-09-03 Mitchell Scott A Certain substituted amides, method of making, and method of use thereof
US8588172B2 (en) 2008-02-15 2013-11-19 Telefonaktiebolaget L M Ericsson (Pub) Methods and network nodes that simultaneously assign temporary block flows for uplink and downlink communication channels to a mobile station
EP2280711A1 (en) 2008-03-07 2011-02-09 Pfizer Inc. Methods, dosage forms, and kits for administering ziprasidone without food
JP5529852B2 (ja) 2008-05-06 2014-06-25 ジリード コネティカット，インコーポレイティド 置換アミド、その製造法及びＢｔｋインヒビターとしての使用
CA2728016C (en) 2008-06-24 2017-02-28 F. Hoffmann-La Roche Ag Novel substituted pyridin-2-ones and pyridazin-3-ones
PT2300459E (pt) 2008-07-02 2013-07-04 Hoffmann La Roche Novas fenilpirazinonas utilizadas como inibidores de cinase
ES2552681T3 (es) 2008-07-15 2015-12-01 F. Hoffmann-La Roche Ag Nuevas fenil-imidazopiridinas y piridazinas
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
WO2010068258A1 (en) 2008-12-08 2010-06-17 Cgi Pharmaceuticals, Inc. Imidazopyrazine syk inhibitors
LT2716157T (lt) 2008-12-08 2016-09-12 Gilead Connecticut, Inc. Imidazopirazino syk inhibitoriai
US8362013B2 (en) 2009-04-30 2013-01-29 Abbvie Inc. Salt of ABT-263 and solid-state forms thereof
US8546399B2 (en) 2009-05-26 2013-10-01 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
EP2512455B8 (en) 2009-12-18 2014-07-23 FrieslandCampina Nederland Holding B.V. Co-processed tablet excipient composition its preparation and use
SG181857A1 (en) 2009-12-23 2012-07-30 Takeda Pharmaceutical Fused heteroaromatic pyrrolidinones as syk inhibitors
MX350010B (es) 2010-03-11 2017-08-23 Gilead Connecticut Inc Inhibidores syk de imidazopiridinas.
WO2012071336A1 (en) 2010-11-23 2012-05-31 Abbott Laboratories Salts and crystalline forms of an apoptosis-inducing agent
EP2703400A4 (en) 2011-04-27 2014-10-08 Daiichi Sankyo Co Ltd PHENYLPYRROLDERIVAT CRYSTAL
WO2013188856A1 (en) * 2012-06-14 2013-12-19 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
AU2013302617A1 (en) 2012-08-14 2015-02-05 Gilead Calistoga Llc Combination therapies for treating cancer
US20140148430A1 (en) 2012-11-26 2014-05-29 Gilead Connecticut, Inc. Imidazopyridines syk inhibitors
NZ715776A (en) 2013-07-30 2017-04-28 Gilead Connecticut Inc Polymorph of syk inhibitors
JP6153667B2 (ja) 2013-07-30 2017-06-28 ギリアード コネチカット， インコーポレイテッド Ｓｋｙ阻害剤の製剤
CA2919479C (en) 2013-07-31 2017-08-22 Gilead Sciences, Inc. Syk inhibitors
EP3076976B1 (en) 2013-12-04 2020-09-02 Gilead Sciences, Inc. Methods for treating cancers
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
SG11201604482QA (en) 2013-12-23 2016-07-28 Gilead Sciences Inc Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide
MX2017000610A (es) 2014-07-14 2017-04-27 Gilead Sciences Inc Metodos combinados para tratar canceres.
TW201617074A (zh) 2014-07-14 2016-05-16 吉李德科學股份有限公司 Ｓｙｋ（脾酪胺酸激酶）抑制劑
TW201639573A (zh) 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
WO2016172117A1 (en) 2015-04-21 2016-10-27 Gilead Sciences, Inc. Treatment of chronic graft versus host disease with syk inhibitors
WO2018053190A1 (en) 2016-09-14 2018-03-22 Gilead Sciences, Inc. Syk inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
CN113950479A (zh) 2019-02-22 2022-01-18 克洛诺斯生物股份有限公司 作为syk抑制剂的缩合吡嗪的固体形式

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018513173A (ja) * 2015-04-21 2018-05-24 ギリアード サイエンシーズ， インコーポレイテッド Ｓｙｋ阻害剤を用いた慢性移植片対宿主病の処置

Also Published As

Publication number Publication date
IL245846A0 (en) 2016-08-02
US20210060011A1 (en) 2021-03-04
CN107746405A (zh) 2018-03-02
HRP20180460T1 (hr) 2018-06-01
MX392440B (es) 2025-03-24
SG10201912586UA (en) 2020-02-27
CA2875877C (en) 2021-10-26
EA201891553A1 (ru) 2019-04-30
MX2020000404A (es) 2022-05-17
KR20160102041A (ko) 2016-08-26
UA118463C2 (uk) 2019-01-25
PT3342773T (pt) 2021-02-17
HUE037662T2 (hu) 2018-09-28
BR112016014643A2 (OSRAM) 2017-08-08
RS57182B1 (sr) 2018-07-31
NO3183247T3 (OSRAM) 2018-04-28
HRP20210233T1 (hr) 2021-04-02
US9968601B2 (en) 2018-05-15
AU2017228612A1 (en) 2017-10-05
GT201600123A (es) 2017-12-01
US12263163B2 (en) 2025-04-01
CU20160097A7 (es) 2017-02-02
JP2019172680A (ja) 2019-10-10
CA2875877A1 (en) 2015-06-23
LT3087075T (lt) 2018-04-10
AP2016009274A0 (en) 2016-06-30
IL245846B (en) 2018-10-31
US20190388419A1 (en) 2019-12-26
PE20160995A1 (es) 2016-10-23
CR20160287A (es) 2016-09-19
AR098912A1 (es) 2016-06-22
US20160310490A1 (en) 2016-10-27
EP3342773B1 (en) 2020-11-11
KR20180130598A (ko) 2018-12-07
EA201690989A1 (ru) 2016-11-30
DK3342773T3 (da) 2021-02-15
PH12016501204A1 (en) 2016-08-15
SG10201707432SA (en) 2017-10-30
ZA201800913B (en) 2022-07-27
SG11201604491VA (en) 2016-07-28
EA031131B1 (ru) 2018-11-30
US10828299B2 (en) 2020-11-10
EP3087075A1 (en) 2016-11-02
KR20200098735A (ko) 2020-08-20
US20230158023A1 (en) 2023-05-25
US11517570B2 (en) 2022-12-06
JP2018021063A (ja) 2018-02-08
PT3087075T (pt) 2018-04-09
KR101925859B1 (ko) 2018-12-07
AU2019236696A1 (en) 2019-10-17
SI3342773T1 (sl) 2021-04-30
ES2664799T3 (es) 2018-04-23
MD4666B1 (ro) 2019-12-31
DK3087075T3 (en) 2018-03-19
SMT201800193T1 (it) 2018-05-02
TW201940488A (zh) 2019-10-16
US10342794B2 (en) 2019-07-09
US20180325896A1 (en) 2018-11-15
UY35898A (es) 2015-07-31
ME03001B (me) 2018-10-20
PL3087075T3 (pl) 2019-03-29
CY1120104T1 (el) 2018-12-12
HK1251563A1 (zh) 2019-02-01
MD20160078A2 (ro) 2017-01-31
WO2015100217A1 (en) 2015-07-02
EP3342773B9 (en) 2021-06-09
HK1256999A1 (en) 2019-10-11
PH12020551986A1 (en) 2023-12-11
JP6530792B2 (ja) 2019-06-12
KR102146477B1 (ko) 2020-08-21
EP3087075B1 (en) 2018-02-14
DOP2016000140A (es) 2016-06-30
CN105934434B (zh) 2017-12-12
AU2014370010A1 (en) 2016-06-30
MD4666C1 (ro) 2021-01-31
SI3087075T1 (en) 2018-06-29
CN105934434A (zh) 2016-09-07
EP3342773A1 (en) 2018-07-04
AU2017228612B2 (en) 2019-06-27
SV2016005229A (es) 2017-07-28
MX2016008456A (es) 2017-01-11
MX371024B (es) 2020-01-13
NZ721175A (en) 2017-05-26
AU2019236696B2 (en) 2021-07-15
PH12016501204B1 (en) 2023-04-26
ES2851335T3 (es) 2021-09-06
HUE053815T2 (hu) 2021-07-28
TWI735853B (zh) 2021-08-11
BR112016014643B1 (pt) 2022-10-25
MY199564A (en) 2023-11-07
PL3342773T3 (pl) 2021-06-14
UA124667C2 (uk) 2021-10-27
TW201609735A (zh) 2016-03-16
CL2016001537A1 (es) 2016-12-02
JP2017501229A (ja) 2017-01-12
AU2014370010B2 (en) 2017-07-06
TWI662037B (zh) 2019-06-11
CN107746405B (zh) 2020-09-22

Similar Documents

Publication Publication Date Title
JP6243062B2 (ja) Ｓｙｋ阻害剤
JP6292691B2 (ja) Ｓｙｋ阻害剤
HK1256999B (en) Syk inhibitors
HK1225029A1 (en) Syk inhibitors
HK1225029B (en) Syk inhibitors
HK1233495A1 (en) Syk inhibitors
BR122020009305B1 (pt) Forma cristalina de 6-(6-aminopirazin-2-il)-n-(4-(4-(oxetan-3-il)piperazin-1- il)fenil)imidazo[1,2-a]pirazin-8-amina, composição farmacêutica, e, uso de uma forma cristalina
EA040127B1 (ru) Кристаллические формы соединений и их применение для лечения лейкоза

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160728

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160808

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160728

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170608

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170615

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170908

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: 20171012

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20171108

R150 Certificate of patent or registration of utility model

Ref document number: 6243062

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

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

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