JP2010528027A - Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体 - Google Patents

Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体 Download PDF

Info

Publication number
JP2010528027A
JP2010528027A JP2010509463A JP2010509463A JP2010528027A JP 2010528027 A JP2010528027 A JP 2010528027A JP 2010509463 A JP2010509463 A JP 2010509463A JP 2010509463 A JP2010509463 A JP 2010509463A JP 2010528027 A JP2010528027 A JP 2010528027A
Authority
JP
Japan
Prior art keywords
pyridinyl
substituted
quinolinyl
cancer
group
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.)
Pending
Application number
JP2010509463A
Other languages
English (en)
Japanese (ja)
Inventor
ニコラス・ディ・アダムス
アミタ・エム・チョーダリ
カーラ・エイ・ドナテリ
スティーブン・デイビッド・ナイト
ケネス・アレン・ニューランダー
シンシア・エイ・パリッシュ
ランス・リジャース
マーサ・エイ・サーポング
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.)
GlaxoSmithKline LLC
Original Assignee
GlaxoSmithKline LLC
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 GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of JP2010528027A publication Critical patent/JP2010528027A/ja
Pending legal-status Critical Current

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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—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 sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
    • C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
    • C07D285/22—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D285/24—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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 two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
JP2010509463A 2007-05-18 2008-05-16 Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体 Pending JP2010528027A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US93876107P 2007-05-18 2007-05-18
PCT/US2008/063821 WO2008144464A1 (en) 2007-05-18 2008-05-16 Quinoline derivatives as p13 kinase inhibitors

Publications (1)

Publication Number Publication Date
JP2010528027A true JP2010528027A (ja) 2010-08-19

Family

ID=40088996

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2010509463A Pending JP2010528027A (ja) 2007-05-18 2008-05-16 Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体
JP2010509462A Expired - Fee Related JP4814396B2 (ja) 2007-05-18 2008-05-16 Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体
JP2011059612A Pending JP2011126913A (ja) 2007-05-18 2011-03-17 Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2010509462A Expired - Fee Related JP4814396B2 (ja) 2007-05-18 2008-05-16 Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体
JP2011059612A Pending JP2011126913A (ja) 2007-05-18 2011-03-17 Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体

Country Status (31)

Country Link
US (6) US8138347B2 (enExample)
EP (3) EP2192902A4 (enExample)
JP (3) JP2010528027A (enExample)
KR (1) KR101458660B1 (enExample)
CN (1) CN101754759B (enExample)
AR (1) AR066614A1 (enExample)
AU (1) AU2008254915B2 (enExample)
BR (1) BRPI0811761A2 (enExample)
CA (1) CA2686016C (enExample)
CL (1) CL2008001457A1 (enExample)
CO (1) CO6241101A2 (enExample)
CR (1) CR11165A (enExample)
CY (1) CY1114070T1 (enExample)
DK (1) DK2162131T3 (enExample)
EA (1) EA019540B1 (enExample)
ES (2) ES2404557T3 (enExample)
HR (1) HRP20130252T1 (enExample)
IL (1) IL202018A (enExample)
JO (1) JO2891B1 (enExample)
MA (1) MA31443B1 (enExample)
MX (2) MX342959B (enExample)
MY (1) MY158843A (enExample)
NZ (1) NZ580979A (enExample)
PE (1) PE20090717A1 (enExample)
PL (1) PL2162131T3 (enExample)
PT (1) PT2162131E (enExample)
SI (1) SI2162131T1 (enExample)
TW (1) TWI410417B (enExample)
UA (1) UA104408C2 (enExample)
WO (2) WO2008144463A1 (enExample)
ZA (1) ZA200907777B (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013543008A (ja) * 2010-11-19 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド Ｂｒａｆ阻害剤による治療方法
JP2014506601A (ja) * 2011-02-23 2014-03-17 インテリカイン， エルエルシー 複素環化合物およびその使用
JP2019528275A (ja) * 2016-08-16 2019-10-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 可逆性ｂｔｋ阻害剤としてのオキソ−イミダゾピリジン及びその使用
JP2020503321A (ja) * 2016-12-26 2020-01-30 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物

Families Citing this family (257)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
EP2183232B1 (en) 2007-08-02 2013-03-06 Amgen, Inc Pi3 kinase modulators and methods of use
US20100311736A1 (en) * 2007-10-22 2010-12-09 Glaxosmithkline Llc Pyridosulfonamide derivatives as p13 kinase inhibitors
EP2231661A1 (en) 2007-12-19 2010-09-29 Amgen, Inc. Inhibitors of pi3 kinase
MX315904B (es) 2008-05-30 2013-11-29 Amgen Inc Inhibidores de fosfoinosituro-3 cinasa.
WO2009157196A1 (ja) * 2008-06-25 2009-12-30 武田薬品工業株式会社 アミド化合物
KR20110058866A (ko) 2008-09-02 2011-06-01 노파르티스 아게 비시클릭 키나제 억제제
EP2370424A1 (en) 2008-11-10 2011-10-05 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2010059549A1 (en) * 2008-11-18 2010-05-27 Glaxosmithkline Llc Prolyl hydroxylase inhibitors
EP2376485B1 (en) 2008-12-19 2017-12-06 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
SG172353A1 (en) * 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
RU2505540C2 (ru) 2008-12-23 2014-01-27 Эббви Инк. Антивирусные соединения
EP2387564A1 (en) 2009-01-15 2011-11-23 Rutgers, The State University of New Jersey Benzo ýc¨phenanthridines as antimicrobial agents
AU2010231162B2 (en) 2009-04-02 2014-12-11 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Imidazo [2, 1-b] [ 1, 3, 4 ] thiadiazole derivatives
US9278922B2 (en) 2009-04-15 2016-03-08 Abbvie Inc. Anti-viral compounds
WO2010127307A1 (en) 2009-04-30 2010-11-04 Rutgers, The State University Of New Jersey Antimicrobial agents
DK2429995T3 (da) 2009-05-15 2014-04-22 Novartis Ag Arylpyridiner som aldosteronsyntaseinhibitorer
WO2010135568A1 (en) 2009-05-22 2010-11-25 Exelixis, Inc. Benzoxazepines as inhibitors of mtor and their use to treat cancer
US8765940B2 (en) * 2009-06-25 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
NZ598220A (en) 2009-08-17 2014-02-28 Intellikine Llc Heterocyclic compounds and uses thereof
WO2011021678A1 (ja) * 2009-08-21 2011-02-24 武田薬品工業株式会社 縮合複素環化合物
LT2473487T (lt) 2009-09-03 2017-01-10 Bristol-Myers Squibb Company Chinazolinai kaip kalio jonų kanalų inhibitoriai
PH12012500491A1 (en) * 2009-09-09 2018-03-21 Celgene Avilomics Res Inc P13 kinase inhibitors and uses thereof
SG179172A1 (en) 2009-09-16 2012-04-27 Avila Therapeutics Inc Protein kinase conjugates and inhibitors
MX2012003779A (es) * 2009-09-28 2012-06-01 Glaxosmithkline Llc Combinacion.
CN102665720A (zh) * 2009-10-12 2012-09-12 葛兰素史密斯克莱有限责任公司 组合
WO2011051958A1 (en) 2009-10-30 2011-05-05 E.I. Du Pont De Nemours And Company Fungicidal pyrazolones
BR112012015721A2 (pt) 2009-12-30 2017-09-26 Avila Therapeutics Inc modificação covalente de proteínas dirigida por ligante
US9630956B2 (en) 2010-05-12 2017-04-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526539A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用なピラジン
JP2013526538A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
CN102947272A (zh) 2010-05-12 2013-02-27 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的2-氨基吡啶衍生物
US9062008B2 (en) 2010-05-12 2015-06-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011143425A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011156626A1 (en) 2010-06-09 2011-12-15 Rutgers, The State University Of New Jersey Antimicrobial agents
CA2803802A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
WO2011163610A2 (en) * 2010-06-25 2011-12-29 Rutgers, The State University Of New Jersey Antimicrobial agents
DK2597955T3 (en) * 2010-07-30 2016-03-14 Onco Therapy Science Inc QUINOLINE DERIVATIVES AND MILK INHIBITORS CONTAINING THESE
JP2013536192A (ja) * 2010-08-09 2013-09-19 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 組み合わせ
WO2012068096A2 (en) 2010-11-15 2012-05-24 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
EP2640367A2 (en) 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
US20130317037A1 (en) * 2010-11-16 2013-11-28 Glaxosmithkline Intellectual Property Development Limited Method of administration and treatment
EP2643316A2 (en) 2010-11-24 2013-10-02 Exelixis, Inc. Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture
ES2609578T3 (es) 2011-03-04 2017-04-21 Glaxosmithkline Intellectual Property Development Limited Amino-quinolinas como inhibidores de quinasa
US9051305B2 (en) 2011-03-08 2015-06-09 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
CN102718745A (zh) * 2011-03-30 2012-10-10 中国科学院上海药物研究所 新型胺基吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
JP2014513104A (ja) * 2011-04-29 2014-05-29 エクセリクシス， インク． Ｐｉ３ｋ／ｍｔｏｒのピリドピリミジノン阻害剤を用いたリンパ腫の治療方法
WO2012178124A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
BR112014007721B1 (pt) 2011-09-30 2022-11-01 Vertex Pharmaceuticals Incorporated Processos para preparar compostos úteis como inibidores de atr quinase
KR102056586B1 (ko) 2011-09-30 2019-12-18 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 억제제를 이용한 췌장암 및 비소세포 폐암의 치료
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CA2850564A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
AU2012331289B2 (en) 2011-11-04 2017-07-13 F. Hoffmann-La Roche Ag New aryl-quinoline derivatives
WO2013071085A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776422A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2790705B1 (en) 2011-12-15 2017-12-06 Novartis AG Use of inhibitors of the activity or function of pi3k
US9822108B2 (en) 2012-01-13 2017-11-21 Rutgers, The State University Of New Jersey Antimicrobial agents
CN104093408A (zh) * 2012-02-06 2014-10-08 葛兰素史克知识产权第二有限公司 用于治疗纤维化疾病的pi3k抑制剂
EP2812003A1 (en) * 2012-02-06 2014-12-17 Glaxosmithkline Intellectual Property (No. 2) Limited Pi3k inhibitors for treating cough
EP2828245A1 (en) 2012-03-21 2015-01-28 Rutgers, The State University of New Jersey Antimicrobial agents
AU2013243291B2 (en) 2012-04-05 2018-02-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase and combination therapies thereof
EP2863920B1 (en) 2012-06-20 2023-03-22 Eutropics Pharmaceuticals, Inc. Quinoline derivatives for use in the tratment of breast cancer
AR092529A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
AR092530A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de amino-quinolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
CN103497177B (zh) * 2012-09-29 2017-03-22 天津滨江药物研发有限公司 作为c‑Met抑制剂的氨基芳香杂环类化合物及其制备方法
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN103788071A (zh) * 2012-11-01 2014-05-14 中国人民解放军第二军医大学 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
US20160038503A1 (en) 2012-11-21 2016-02-11 David Richard Methods and compositions useful for treating diseases involving bcl-2 family proteins with isoquinoline and quinoline derivatives
LT3486245T (lt) 2012-12-07 2021-08-25 Vertex Pharmaceuticals Incorporated 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius
TWI630203B (zh) 2013-02-21 2018-07-21 葛蘭素史克智慧財產發展有限公司 做為激酶抑制劑的喹唑啉類
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
CN104098542A (zh) * 2013-04-11 2014-10-15 苏州朗信医药科技有限公司 一种6-溴代-4-(4-吡嗪基)喹啉的制备方法
US10732182B2 (en) 2013-08-01 2020-08-04 Eutropics Pharmaceuticals, Inc. Method for predicting cancer sensitivity
CN104418858B (zh) 2013-08-30 2018-12-11 浙江医药股份有限公司新昌制药厂 2,6-二含氮取代的嘌呤衍生物及其制备方法和其药物组合物与应用
BR112016003229A8 (pt) 2013-09-22 2020-02-04 Calitor Sciences Llc composto, composição farmacêutica, e, uso de um composto ou de uma composição farmacêutica
CN104557955B (zh) * 2013-10-23 2017-05-03 上海汇伦生命科技有限公司 作为PI3K/mTOR抑制剂的三环类化合物，其制备方法和用途
AU2014342269B2 (en) 2013-10-30 2020-02-27 Eutropics Pharmaceuticals, Inc. Methods for determining chemosensitivity and chemotoxicity
US9458150B2 (en) 2013-11-08 2016-10-04 Rutgers, The State University Of New Jersey Antimicrobial agents
KR102398473B1 (ko) * 2013-11-27 2022-05-16 시그널켐 라이프사이언시즈 코포레이션 Tam 패밀리 키나제 억제제로서의 아미노피리딘 유도체
CA2932757C (en) 2013-12-06 2023-10-31 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
US9340540B2 (en) 2014-02-28 2016-05-17 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
CN104922116B (zh) * 2014-03-23 2020-08-11 上海诗丹德生物技术有限公司 甲基丙烯酰基苯并咪唑酮衍生物的用途
NO2714752T3 (enExample) * 2014-05-08 2018-04-21
AU2015271030B2 (en) 2014-06-05 2019-05-16 Vertex Pharmaceuticals Incorporated Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof
LT3157566T (lt) 2014-06-17 2019-08-12 Vertex Pharmaceuticals Incorporated Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį
EP3159342B1 (en) 2014-06-17 2020-08-05 Cisen Pharmaceutical Co., Ltd. Pyridino[1,2-a]pyrimidone analogue used as mtor/pi3k inhibitor
CN106715456B (zh) 2014-08-12 2023-08-29 莫纳什大学 定向淋巴的前药
CN105330699B (zh) * 2014-08-13 2018-12-04 山东汇睿迪生物技术有限公司 一种含磷吡啶并[2,3-d]嘧啶-7-酮类化合物或其药学上可接受的盐、药物组合物及其应用
PT3180329T (pt) 2014-08-15 2020-06-08 Janssen Pharmaceuticals Inc Triazóis como inibidores do recetor nr2b
DK3180315T3 (da) 2014-08-15 2020-04-06 Janssen Pharmaceuticals Inc Pyrazoler
ES2870449T3 (es) 2014-10-29 2021-10-27 Bicyclerd Ltd Ligandos peptídicos bicíclicos específicos de MT1-MMP
TWI744225B (zh) 2015-02-27 2021-11-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶２（ｔｙｋ２）抑制劑及其用途
FR3033499A1 (fr) 2015-03-11 2016-09-16 Centre Leon-Berard Composition pour le traitement des tumeurs neuroendocrines pancreatiques
CN104961725B (zh) * 2015-06-18 2017-04-19 浙江大学 4‑α,β不饱和酰胺基喹啉类化合物及制备和应用
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
SI3319963T1 (sl) * 2015-07-09 2020-02-28 Janssen Pharmaceutica Nv Substituirani 4-azaindoli in njihova uporaba kot modulatorji receptorja GLUN2B
CN108137514A (zh) * 2015-07-30 2018-06-08 百时美施贵宝公司 芳基取代的二环杂芳基化合物
WO2017027768A1 (en) * 2015-08-13 2017-02-16 The Broad Institute, Inc. Compositions and methods for treating tuberculosis
EP4327809A3 (en) 2015-09-02 2024-04-17 Takeda Pharmaceutical Company Limited Tyk2 inhibitors and uses thereof
CN114031658A (zh) 2015-09-08 2022-02-11 莫纳什大学 定向淋巴的前药
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
GB201516504D0 (en) 2015-09-17 2015-11-04 Astrazeneca Ab Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer
WO2017059357A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
RS64114B1 (sr) 2015-10-23 2023-04-28 Navitor Pharm Inc Modulatori interakcije sestrin-gator2 i nјihova upotreba
US11370792B2 (en) 2015-12-14 2022-06-28 Raze Therapeutics, Inc. Caffeine inhibitors of MTHFD2 and uses thereof
WO2017101829A1 (zh) * 2015-12-16 2017-06-22 辰欣药业股份有限公司 吡啶并[1,2-a]嘧啶酮类似物的晶型及其制备方法和中间体
EP3414233A1 (en) 2016-02-10 2018-12-19 Janssen Pharmaceutica NV Substituted 1,2,3-triazoles as nr2b-selective nmda modulators
WO2017147316A1 (en) 2016-02-25 2017-08-31 Taxis Pharmaceuticals, Inc. Synthetic processes and intermediates
EP4234552A3 (en) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
EP3884939B1 (en) 2016-03-09 2023-10-25 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
WO2017177230A1 (en) 2016-04-08 2017-10-12 X4 Pharmaceuticals, Inc. Methods for treating cancer
EP3471726A4 (en) 2016-06-21 2019-10-09 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
JP7054529B2 (ja) 2016-06-21 2022-04-14 エックス４ ファーマシューティカルズ， インコーポレイテッド Ｃｘｃｒ４阻害剤およびその使用
CN109641838A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
US10154992B2 (en) * 2016-07-12 2018-12-18 The Regents Of The University Of California Compounds and methods for treating HIV infection
TW201819376A (zh) 2016-10-06 2018-06-01 比利時商健生藥品公司 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途
TWI825663B (zh) 2016-10-14 2023-12-11 美商林伯士拉克許米公司 Tyk2抑制劑及其用途
EP3528816A4 (en) 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
US10414727B2 (en) 2016-11-08 2019-09-17 Navitor Pharmaceuticals, Inc. Phenyl amino piperidine mTORC inhibitors and uses thereof
CN106580986B (zh) * 2016-11-28 2017-09-15 王保亮 一种治疗少弱精子症的药物组合物
EP3548005A4 (en) 2016-11-29 2020-06-17 Puretech Health LLC Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
US20180153922A1 (en) 2016-12-06 2018-06-07 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease
EP3559018A1 (en) 2016-12-23 2019-10-30 Bicyclerd Limited Peptide derivatives having novel linkage structures
US10624968B2 (en) 2017-01-06 2020-04-21 Bicyclerd Limited Compounds for treating cancer
AR111233A1 (es) 2017-03-08 2019-06-19 Nimbus Lakshmi Inc Inhibidores de tyk2, usos y métodos para la producción de los mismos
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
WO2018183917A1 (en) 2017-03-30 2018-10-04 Taxis Pharmaceuticals, Inc. Synthetic processes and synthetic intermediates
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
JP7179015B2 (ja) 2017-04-26 2022-11-28 ナビター ファーマシューティカルズ， インコーポレイテッド Ｓｅｓｔｒｉｎ－ＧＡＴＯＲ２相互座用のモジュレーターおよびその使用
EP3615550A1 (en) 2017-04-27 2020-03-04 BicycleTx Limited Bicyclic peptide ligands and uses thereof
EP3628044B1 (en) * 2017-05-15 2023-11-22 The Regents of The University of Michigan Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors
US10899798B2 (en) 2017-06-26 2021-01-26 Bicyclerd Limited Bicyclic peptide ligands with detectable moieties and uses thereof
DK3658557T3 (da) 2017-07-28 2024-07-29 Takeda Pharmaceuticals Co Tyk2-inhibitorer og anvendelser deraf
WO2019025811A1 (en) 2017-08-04 2019-02-07 Bicycletx Limited SPECIFIC BICYCLIC PEPTIDE LIGANDS OF CD137
EP3668550A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
AU2018324037A1 (en) 2017-08-29 2020-04-16 Monash University Lymphatic system-directing lipid prodrugs
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
JP7366031B2 (ja) 2017-09-22 2023-10-20 カイメラ セラピューティクス， インコーポレイテッド タンパク質分解剤およびそれらの使用
CN107793404A (zh) * 2017-11-07 2018-03-13 全椒先奇医药科技有限公司 一种治疗缺血性脑损伤药物组合物及其应用
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
WO2019126378A1 (en) 2017-12-19 2019-06-27 Ariya Therapeutics, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
IL301089A (en) 2018-01-29 2023-05-01 Vertex Pharma GCN2 inhibitors and their uses
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
CA3091775A1 (en) 2018-02-23 2019-08-29 Bicycletx Limited Multimeric bicyclic peptide ligands
WO2019169001A1 (en) 2018-02-27 2019-09-06 Artax Biopharma Inc. Chromene derivatives as inhibitors of tcr-nck interaction
PE20251292A1 (es) * 2018-03-08 2025-05-14 Incyte Corp Compuestos diolicos de aminopirazina como inhibidores de pi3k-gamma
EP3774732A4 (en) 2018-04-04 2022-02-09 Janssen Pharmaceutica NV PYRIDINE AND SUBSTITUTED PYRIMIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
HUE058746T2 (hu) 2018-04-24 2022-09-28 Merck Patent Gmbh Antiproliferációs vegyületek és felhasználásuk
ES2969982T3 (es) 2018-04-24 2024-05-23 Vertex Pharma Compuestos de pteridinona y usos de los mismos
EP3807248A4 (en) * 2018-05-29 2021-10-27 Council of Scientific and Industrial Research BICYCLIC TOPOISOMERASE I INHIBITOR COMPOUNDS, THEIR PREPARATION AND USE
EP3575305A1 (fr) * 2018-05-31 2019-12-04 Biocidal Alternative Solutions Procédé de fabrication de composés comprenant un groupe fonctionnel oxazolopyridinones
EP3801069A4 (en) 2018-06-01 2022-03-16 Cornell University MULTIPLE THERAPY FOR DISEASE OR DISORDER ASSOCIATED WITH PI3K
HUE067446T2 (hu) 2018-06-15 2024-10-28 Janssen Pharmaceutica Nv Rapamicin analógok és alkalmazásaik
IL279489B2 (en) 2018-06-22 2025-10-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
KR102595520B1 (ko) * 2018-07-05 2023-10-30 엘지디스플레이 주식회사 헤테로아릴기를 가진 벤즈아졸 유도체 및 이를 포함하는 유기전계발광소자
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
JP2022500499A (ja) 2018-09-07 2022-01-04 ピク セラピューティクス， インコーポレイテッド Ｅｉｆ４ｅ阻害剤およびその使用
JP7619951B2 (ja) 2018-10-15 2025-01-22 武田薬品工業株式会社 Ｔｙｋ２阻害剤およびその使用
WO2020084305A1 (en) 2018-10-23 2020-04-30 Bicycletx Limited Bicyclic peptide ligands and uses thereof
EP3870158A4 (en) 2018-10-24 2022-08-10 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
CN113271938A (zh) 2018-11-30 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
PH12021500026A1 (en) 2018-11-30 2022-05-11 Kymera Therapeutics Inc Irak degraders and uses thereof
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
JP2022514618A (ja) 2018-12-21 2022-02-14 バイスクルテクス・リミテッド Ｐｄ－ｌ１に特異的な二環式ペプチドリガンド
CN113348021B (zh) 2019-01-23 2025-07-11 武田药品工业株式会社 Tyk2抑制剂和其用途
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
JP2022528887A (ja) 2019-04-02 2022-06-16 バイスクルテクス・リミテッド バイシクルトキシンコンジュゲートおよびその使用
US11485750B1 (en) 2019-04-05 2022-11-01 Kymera Therapeutics, Inc. STAT degraders and uses thereof
EP3976027B1 (en) * 2019-05-30 2025-11-05 Merck Sharp & Dohme LLC Quinoline derivatives as factor xi activation inhibitors
BR112021024224A2 (pt) 2019-05-31 2022-04-26 Ikena Oncology Inc Inibidores de tead e usos dos mesmos
US12521438B2 (en) 2019-06-10 2026-01-13 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
EP3983073A1 (en) 2019-06-14 2022-04-20 Janssen Pharmaceutica NV Substituted pyrazolo[4,3-b]pyridines and their use as glun2b receptor modulators
PH12021552839A1 (en) 2019-06-14 2022-10-03 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators
EP3983413A1 (en) 2019-06-14 2022-04-20 Janssen Pharmaceutica NV Substituted pyrazolo-pyrazines and their use as glun2b receptor modulators
CA3142998A1 (en) 2019-06-14 2020-12-17 Janssen Pharmaceutica Nv Pyrazine carbamates and their use as glun2b receptor modulators
PE20220386A1 (es) 2019-06-14 2022-03-18 Janssen Pharmaceutica Nv Amidas de pirazolo-piridina sustituidas y su uso como moduladores del receptor glun2b
AU2020293584A1 (en) 2019-06-14 2022-01-20 Janssen Pharmaceutica Nv Pyridine carbamates and their use as GluN2B receptor modulators
SG11202112405VA (en) 2019-06-14 2021-12-30 Janssen Pharmaceutica Nv Substituted heteroaromatic pyrazolo-pyridines and their use as glun2b receptor modulators
TWI860386B (zh) 2019-07-30 2024-11-01 英商拜西可泰克斯有限公司 異質雙環肽複合物
EP4028385A4 (en) 2019-09-11 2023-11-08 Vincere Biosciences, Inc. USP30 INHIBITORS AND USES THEREOF
PH12022550605A1 (en) 2019-09-13 2023-09-25 Nimbus Saturn Inc Hpk1 antagonists and uses thereof
MX2022005215A (es) 2019-11-01 2022-06-08 Navitor Pharm Inc Metodos de tratamiento que usan un modulador de la diana mecanicista del complejo 1 de rapamicina (mtorc1).
IL293549A (en) 2019-12-05 2022-08-01 Anakuria Therapeutics Inc Rapamycin analogs and uses thereof
EP4076520A4 (en) 2019-12-17 2024-03-27 Kymera Therapeutics, Inc. IRAQ DEGRADATION AGENTS AND THEIR USES
US11591332B2 (en) 2019-12-17 2023-02-28 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
CN115297931A (zh) 2019-12-23 2022-11-04 凯麦拉医疗公司 Smarca降解剂和其用途
US20210268115A1 (en) 2020-02-05 2021-09-02 Puretech Lyt, Inc. Lipid prodrugs of neurosteroids
CN115515685B (zh) 2020-03-03 2025-04-08 皮克医疗公司 Eif4e抑制剂及其用途
MX2022011602A (es) 2020-03-19 2023-01-04 Kymera Therapeutics Inc Degradadores de la proteína de homólogo de ratón de minuto 2 (mdm2) y usos de los mismos.
WO2021202731A1 (en) 2020-03-31 2021-10-07 Chemocentryx, Inc. Compositions and methods for treating inflammatory bowel disease using ccr9 inhibitor and anti-il-23 blocking antibodies
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
CA3186504A1 (en) 2020-08-17 2022-02-24 Stephen J. Blakemore Bicycle conjugates specific for nectin-4 and uses thereof
TW202233612A (zh) 2020-10-23 2022-09-01 美商林伯士科羅索公司 Ctps1抑制劑及其用途
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
KR20230131189A (ko) 2020-12-02 2023-09-12 이케나 온콜로지, 인코포레이티드 Tead 억제제 및 이의 용도
KR20230143632A (ko) 2020-12-30 2023-10-12 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
AU2022216810A1 (en) 2021-02-02 2023-08-24 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
MX2023009059A (es) 2021-02-02 2023-09-15 Liminal Biosciences Ltd Antagonistas de gpr84 y usos de estos.
EP4291235A4 (en) 2021-02-12 2025-01-08 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND USES THEREOF
US11773103B2 (en) 2021-02-15 2023-10-03 Kymera Therapeutics, Inc. IRAK4 degraders and uses thereof
IL304907A (en) 2021-02-15 2023-10-01 Kymera Therapeutics Inc Irak4 degraders and uses thereof
EP4295850A4 (en) 2021-02-16 2025-03-05 Ribotech Co., Ltd. COMPOUND FOR INHIBITING NONSENSE-MEDIATED mRNA DEGRADATION
US11926625B2 (en) 2021-03-05 2024-03-12 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
KR20230158659A (ko) * 2021-03-18 2023-11-21 쑤저우 궈쾅 팜테크 코포레이션 리미티드 Ctla-4 소분자 분해제 및 그 응용
EP4313989A4 (en) 2021-03-29 2025-03-05 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND USES THEREOF
BR112023020781A2 (pt) 2021-04-09 2023-12-19 Nimbus Clio Inc Moduladores de cbl-b e usos dos mesmos
AU2022258968A1 (en) 2021-04-16 2023-10-19 Ikena Oncology, Inc. Mek inhibitors and uses thereof
TW202309030A (zh) 2021-05-07 2023-03-01 美商凱麥拉醫療公司 Cdk2降解劑及其用途
CN115353512B (zh) * 2021-07-30 2025-07-08 上海翊石医药科技有限公司 一种杂环脲类化合物及其制备方法和用途
CN113416181B (zh) * 2021-08-02 2022-05-03 四川大学 喹唑啉类衍生物及其用途
WO2023028238A1 (en) 2021-08-25 2023-03-02 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス， インコーポレイテッド ｅＩＦ４Ｅ阻害剤及びその使用
WO2023046182A1 (zh) * 2021-09-27 2023-03-30 广州嘉越医药科技有限公司 一种吡啶并[1,2-a]嘧啶酮类化合物的应用
EP4422635A4 (en) 2021-10-29 2025-11-26 Kymera Therapeutics Inc IRAQ4 DEGRADATION AGENTS AND THEIR SYNTHESIS
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
EP4472967A2 (en) 2022-01-31 2024-12-11 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
EP4532470A1 (en) 2022-05-25 2025-04-09 Ikena Oncology, Inc. Mek inhibitors and uses thereof
CN117402146A (zh) * 2022-07-13 2024-01-16 武汉人福创新药物研发中心有限公司 杂环并苯环类化合物及其制备方法和用途
TW202416972A (zh) 2022-08-02 2024-05-01 英商利米那生物科技有限公司 經取代之吡啶酮gpr84拮抗劑及其用途
TW202415650A (zh) 2022-08-02 2024-04-16 英商利米那生物科技有限公司 芳基-三唑基及相關gpr84拮抗劑及其用途
EP4565568A1 (en) 2022-08-02 2025-06-11 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
CN120457127A (zh) * 2022-10-20 2025-08-08 麦克尼斯迪克治疗有限公司 用于调节egfr和pi3k的化合物
US20240208961A1 (en) 2022-11-22 2024-06-27 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
CN116239594B (zh) * 2023-03-05 2023-09-22 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) 6-(咪唑并[1,2-a]吡啶-6-基)喹唑啉衍生物及用途
EP4620470A3 (en) 2023-06-23 2025-10-08 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2025045915A1 (en) * 2023-08-29 2025-03-06 Institut National de la Santé et de la Recherche Médicale Methods for inducing muscle hypertrophy
WO2025062372A1 (en) 2023-09-21 2025-03-27 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
CN118126038B (zh) * 2024-05-08 2024-07-12 烟台大学 吡唑并吡啶类衍生物及其制备方法和应用

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE533691C (de) * 1929-06-10 1931-09-23 I G Farbenindustrie Akt Ges Verfahren zur Darstellung von Chinolin- und Acridinverbindungen, die im Kern eine Benzthiazolyl-, Benzoxazolyl- oder Benzimidazolylgruppe und eine primaere, sekundaere oder tertiaere Aminogruppe enthalten
WO2001083456A1 (en) * 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
JP2004508357A (ja) * 2000-09-06 2004-03-18 エフ．ホフマン−ラ　ロシュ　アーゲー キノリンおよびキナゾリン誘導体
JP2004535404A (ja) * 2001-05-24 2004-11-25 イーライ・リリー・アンド・カンパニー 医薬物質としての新規ピロール誘導体
JP2006519846A (ja) * 2003-03-10 2006-08-31 シェーリング　コーポレイション 複素環式キナーゼインヒビター：使用および合成の方法
WO2007022241A2 (en) * 2005-08-17 2007-02-22 Schering Corporation Novel high affinity quinoline-based kinase ligands
JP2009528385A (ja) * 2006-03-02 2009-08-06 スミスクライン・ビーチャム・コーポレイション Ｐｉ３キナーゼ阻害剤として用いるためのチアゾロン
JP2009533467A (ja) * 2006-04-11 2009-09-17 スミスクライン・ビーチャム・コーポレイション Ｐｉ３キナーゼ阻害剤としてのチアゾリジンジオン誘導体
JP2009544664A (ja) * 2006-07-28 2009-12-17 ノバルティス アクチエンゲゼルシャフト 脂質キナーゼ阻害剤としての２，４−置換キナゾリン
JP2010526823A (ja) * 2007-05-10 2010-08-05 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのキノキサリン誘導体
JP2010528026A (ja) * 2007-05-18 2010-08-19 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559235A (en) 1991-10-29 1996-09-24 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
US5342947A (en) 1992-10-09 1994-08-30 Glaxo Inc. Preparation of water soluble camptothecin derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5491237A (en) 1994-05-03 1996-02-13 Glaxo Wellcome Inc. Intermediates in pharmaceutical camptothecin preparation
US5965589A (en) * 1994-08-10 1999-10-12 Takeda Chemical Industries, Ltd. Thiazolidinedione derivatives, their production and use
US5925656A (en) 1995-04-10 1999-07-20 Dr. Reddy's Research Foundation Compounds having antidiabetic, hypolipidemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
ATE231136T1 (de) 1996-04-09 2003-02-15 Reddys Lab Ltd Dr Thiazolidinedionderivate mit antidiabetischen, hypolipidämischen und antihypertensiven eigenschaften, verfahren zu deren herstellung und pharmazeutischen zusammenstellungen, die sie enthalten
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
ES2193590T3 (es) 1997-11-28 2003-11-01 Lg Chemical Ltd Derivados de imidazol que tienen actividad inhibitoria frente a la farnesil transferasa y procedimiento para la preparacion de los mismos.
WO1999059586A1 (en) 1998-05-19 1999-11-25 Regents Of The University Of California Thiazolidine and oxazolidine derivatives for the treatment of acute myocardial infarction and inhibition of cardiomyocyte apoptosis
US7343348B2 (en) * 2000-05-19 2008-03-11 First American Residential Group, Inc. System for performing real-estate transactions over a computer network using participant templates
US6452014B1 (en) 2000-12-22 2002-09-17 Geron Corporation Telomerase inhibitors and methods of their use
JP2005506290A (ja) * 2001-03-07 2005-03-03 マキシア・ファーマシューティカルズ・インコーポレイテッド 癌および他の増殖性疾患を処置するための複素環式誘導体
TWI223807B (en) * 2001-03-28 2004-11-11 Bayer Ag Optical data carrier comprising a merocyanine dye as light-absorbent compound in the information layer
WO2002092076A1 (en) 2001-05-16 2002-11-21 Cytovia, Inc. Substituted coumarins and quinolines as caspases activators
AUPR688101A0 (en) 2001-08-08 2001-08-30 Luminis Pty Limited Protein domains and their ligands
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
AR038703A1 (es) * 2002-02-28 2005-01-26 Novartis Ag Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
US20050019825A9 (en) 2002-03-15 2005-01-27 Qing Dong Common ligand mimics: pseudothiohydantoins
EP1501509A4 (en) 2002-04-30 2009-07-15 Merck & Co Inc ARYL-LINK-ARYL-SUBSTITUTED THIAZOLIDIN-DION- AND OXAZOLIDIN-DION AS SODIUM CHANNEL BLOCKER
US20040092561A1 (en) 2002-11-07 2004-05-13 Thomas Ruckle Azolidinone-vinyl fused -benzene derivatives
BR0312752A (pt) 2002-07-10 2005-04-26 Applied Research Systems Derivados de benzeno fundido de azolidinona-vinil
AU2003255529B2 (en) 2002-07-10 2008-11-20 Laboratoires Serono Sa Use of compounds for increasing spermatozoa motility
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
AU2003291024A1 (en) * 2002-11-13 2004-06-03 Rigel Pharmaceuticals, Inc. Rhodanine derivatives and pharmaceutical compositions containing them
HUP0203985A3 (en) 2002-11-18 2005-04-28 Gene Res Lab Inc New York N Use of a pharmaceutical composition for alleviating side effect
GB0302882D0 (en) 2003-02-07 2003-03-12 Univ Cardiff Improvements in or relating to agents for the treatment of cardiovascular dysfunction and weight loss
US20070037848A1 (en) 2003-04-03 2007-02-15 Masters Colin L Treatment of neurological conditions
SG160211A1 (en) * 2003-04-03 2010-04-29 Semafore Pharmaceuticals Inc Pi-3 kinase inhibitor prodrugs
US20060106077A1 (en) 2003-07-18 2006-05-18 Pintex Pharmaceuticals, Inc. Pin1-Modulating compounds and methods of use thereof
ES2328146T3 (es) 2003-07-28 2009-11-10 Merck Serono Sa 2-imino-4-(tio)oxo-5-policiclovinilazolinas para su uso como inhibidores de p13 quinasas.
EP1654380A4 (en) 2003-08-14 2009-09-09 Insight Biopharmaceuticals Ltd METHODS AND PHARMACEUTICAL COMPOSITIONS FOR MODULATING HEPARANASE ACTIVATION AND USES THEREOF
US7432377B2 (en) 2004-01-16 2008-10-07 Wyeth Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof
WO2005085277A1 (en) * 2004-02-06 2005-09-15 Concepcion Gisela P Cyclic hexapeptides, process and use thereof
WO2005085227A1 (en) 2004-03-02 2005-09-15 Smithkline Beecham Corporation Inhibitors of akt activity
US20060074102A1 (en) 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
AU2005259511A1 (en) 2004-07-01 2006-01-12 F. Hoffmann-La Roche Ag Quinoline thiazolinones with CDK1 antiproliferative activity
JP2008508304A (ja) 2004-07-27 2008-03-21 エスジーエックス ファーマシューティカルズ、インコーポレイテッド 縮合環ヘテロ環キナーゼ調節因子
US20060249289A1 (en) 2005-05-05 2006-11-09 Halliburton Energy Services, Inc. Set-delayed cement compositions comprising hydrated lime and silica and methods of cementing in subterranean formations
GB0509224D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
US20070004763A1 (en) 2005-06-10 2007-01-04 Nand Baindur Aminoquinoline and aminoquinazoline kinase modulators
US7449571B2 (en) 2005-06-14 2008-11-11 Board Of Regents Of The University Of Nebraska Halogenated aminoquinolines and oligonucleotides containing the same
WO2007005668A2 (en) 2005-06-30 2007-01-11 Amgen Inc. Bis-aryl kinase inhibitors and their use in the treatment of inflammation, angiogenesis and cancer
US7667043B2 (en) 2006-03-20 2010-02-23 E.I. Du Pont De Nemours And Company Molecular structures with controllable electron conducting properties
WO2007139496A1 (en) 2006-05-30 2007-12-06 Clanotech Ab Quinoline derivatives acting as tyrosine kinase inhibitors

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE533691C (de) * 1929-06-10 1931-09-23 I G Farbenindustrie Akt Ges Verfahren zur Darstellung von Chinolin- und Acridinverbindungen, die im Kern eine Benzthiazolyl-, Benzoxazolyl- oder Benzimidazolylgruppe und eine primaere, sekundaere oder tertiaere Aminogruppe enthalten
WO2001083456A1 (en) * 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
JP2004508357A (ja) * 2000-09-06 2004-03-18 エフ．ホフマン−ラ　ロシュ　アーゲー キノリンおよびキナゾリン誘導体
JP2004535404A (ja) * 2001-05-24 2004-11-25 イーライ・リリー・アンド・カンパニー 医薬物質としての新規ピロール誘導体
JP2006519846A (ja) * 2003-03-10 2006-08-31 シェーリング　コーポレイション 複素環式キナーゼインヒビター：使用および合成の方法
WO2007022241A2 (en) * 2005-08-17 2007-02-22 Schering Corporation Novel high affinity quinoline-based kinase ligands
JP2009528385A (ja) * 2006-03-02 2009-08-06 スミスクライン・ビーチャム・コーポレイション Ｐｉ３キナーゼ阻害剤として用いるためのチアゾロン
JP2009533467A (ja) * 2006-04-11 2009-09-17 スミスクライン・ビーチャム・コーポレイション Ｐｉ３キナーゼ阻害剤としてのチアゾリジンジオン誘導体
JP2009544664A (ja) * 2006-07-28 2009-12-17 ノバルティス アクチエンゲゼルシャフト 脂質キナーゼ阻害剤としての２，４−置換キナゾリン
JP2010526823A (ja) * 2007-05-10 2010-08-05 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのキノキサリン誘導体
JP2010528026A (ja) * 2007-05-18 2010-08-19 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JPN7013001886; Ｔｈｅ　Ｊｏｕｒｎａｌ　ｏｆ　Ｂｉｏｌｏｇｉｃａｌ　Ｃｈｅｍｉｓｔｒｙ ２６９（７）, 1994, ５２４１-５２４８ *

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013543008A (ja) * 2010-11-19 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド Ｂｒａｆ阻害剤による治療方法
JP2014506601A (ja) * 2011-02-23 2014-03-17 インテリカイン， エルエルシー 複素環化合物およびその使用
JP2019528275A (ja) * 2016-08-16 2019-10-10 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 可逆性ｂｔｋ阻害剤としてのオキソ−イミダゾピリジン及びその使用
JP2020503321A (ja) * 2016-12-26 2020-01-30 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物
JP7077323B2 (ja) 2016-12-26 2022-05-30 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物
JP2022119852A (ja) * 2016-12-26 2022-08-17 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物
JP2022119853A (ja) * 2016-12-26 2022-08-17 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物
US11534443B2 (en) 2016-12-26 2022-12-27 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Quinazoline compounds, preparation method, use, and pharmaceutical composition thereof
JP7384536B2 (ja) 2016-12-26 2023-11-21 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物
JP7384535B2 (ja) 2016-12-26 2023-11-21 中国医学科学院薬物研究所 キナゾリン化合物並びにその調製方法、使用及び医薬組成物
US12508264B2 (en) 2016-12-26 2025-12-30 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Quinazoline compounds, preparation method, use, and pharmaceutical composition thereof
US12508263B2 (en) 2016-12-26 2025-12-30 Institute Of Materia Medica, Chinese Academy Of Medical Sciences Quinazoline compounds, preparation method, use, and pharmaceutical composition thereof

Also Published As

Publication number Publication date
ES2404557T3 (es) 2013-05-28
PT2162131E (pt) 2013-04-23
CN101754759A (zh) 2010-06-23
US20120165321A1 (en) 2012-06-28
EP2192902A1 (en) 2010-06-09
US20140296224A1 (en) 2014-10-02
EP2162131B1 (en) 2013-03-06
ZA200907777B (en) 2010-07-28
EP2596793B1 (en) 2015-07-08
IL202018A0 (en) 2010-06-16
JP2010528026A (ja) 2010-08-19
CR11165A (es) 2010-03-01
EA200971072A1 (ru) 2010-06-30
CA2686016A1 (en) 2008-11-27
EP2596793A1 (en) 2013-05-29
US20100168100A1 (en) 2010-07-01
MX342959B (es) 2016-10-18
EP2162131A1 (en) 2010-03-17
JP4814396B2 (ja) 2011-11-16
WO2008144464A1 (en) 2008-11-27
US8404837B2 (en) 2013-03-26
CA2686016C (en) 2015-04-21
TWI410417B (zh) 2013-10-01
PE20090717A1 (es) 2009-07-18
CL2008001457A1 (es) 2008-11-21
TW200911784A (en) 2009-03-16
DK2162131T3 (da) 2013-05-27
HRP20130252T1 (hr) 2013-04-30
UA104408C2 (uk) 2014-02-10
ES2547256T3 (es) 2015-10-02
KR101458660B1 (ko) 2014-11-06
MX2009012479A (es) 2009-12-02
JO2891B1 (en) 2015-09-15
EP2192902A4 (en) 2010-11-03
SI2162131T1 (sl) 2013-07-31
AU2008254915B2 (en) 2012-02-09
CO6241101A2 (es) 2011-01-20
MY158843A (en) 2016-11-15
IL202018A (en) 2016-03-31
US20140100234A1 (en) 2014-04-10
US20080300239A1 (en) 2008-12-04
WO2008144463A1 (en) 2008-11-27
US8633187B2 (en) 2014-01-21
AR066614A1 (es) 2009-09-02
PL2162131T3 (pl) 2013-07-31
HK1137938A1 (en) 2010-08-13
EA019540B1 (ru) 2014-04-30
AU2008254915A1 (en) 2008-11-27
US20100152112A1 (en) 2010-06-17
CY1114070T1 (el) 2016-07-27
CN101754759B (zh) 2013-10-09
US8138347B2 (en) 2012-03-20
EP2162131A4 (en) 2010-11-03
KR20100017852A (ko) 2010-02-16
US8785433B2 (en) 2014-07-22
MA31443B1 (fr) 2010-06-01
JP2011126913A (ja) 2011-06-30
NZ580979A (en) 2012-01-12
BRPI0811761A2 (pt) 2014-11-11

Similar Documents

Publication Publication Date Title
JP4814396B2 (ja) Ｐｉ３キナーゼ阻害物質としてのキノリン誘導体
JP2011500823A (ja) Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体
JP2010526823A (ja) Ｐｉ３キナーゼ阻害物質としてのキノキサリン誘導体
US20090215818A1 (en) Thiozolidinedione derivatives as pi3 kinase inhibitors
EP2167092A2 (en) Quinazoline derivatives as pi3 kinase inhibitors
EP2154965A1 (en) Naphthyridine, derivatives as p13 kinase inhibitors
JP2010535804A (ja) Ｐｉ３キナーゼ阻害薬としてのキノキサリン誘導体
JP2010539239A (ja) Ｐｉ３キナーゼ阻害剤としてのピリドピリミジン誘導体
HK1181657A (en) Quinoline derivatives as pi3 kinase inhibitors
AU2012202710A1 (en) Quinoline derivatives as P13 kinase inhibitors

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20110516

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20120309

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20130516

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130528

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20131022