CN104703979B - 杂环化合物及其应用 - Google Patents

杂环化合物及其应用 Download PDF

Info

Publication number
CN104703979B
CN104703979B CN201380030485.2A CN201380030485A CN104703979B CN 104703979 B CN104703979 B CN 104703979B CN 201380030485 A CN201380030485 A CN 201380030485A CN 104703979 B CN104703979 B CN 104703979B
Authority
CN
China
Prior art keywords
alkyl
group
compound
heteroaryl
disease
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
CN201380030485.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN104703979A (zh
Inventor
阿尔弗雷多·C·卡斯特罗
K·常
凯瑟琳·A·埃文斯
S·加纳达南奈尔
A·莱斯卡博
李连生
刘涛
刘异
任平达
丹尼尔·A·斯奈德
马丁·R·特伦布莱
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.)
Tver Treatment Co.
Original Assignee
Infinity Pharmaceuticals Inc
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 Infinity Pharmaceuticals Inc filed Critical Infinity Pharmaceuticals Inc
Publication of CN104703979A publication Critical patent/CN104703979A/zh
Application granted granted Critical
Publication of CN104703979B publication Critical patent/CN104703979B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • 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
    • A61P17/06—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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
CN201380030485.2A 2012-04-10 2013-04-03 杂环化合物及其应用 Active CN104703979B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261622259P 2012-04-10 2012-04-10
US61/622,259 2012-04-10
US201261713404P 2012-10-12 2012-10-12
US61/713,404 2012-10-12
PCT/US2013/035069 WO2013154878A1 (en) 2012-04-10 2013-04-03 Heterocyclic compounds and uses thereof

Publications (2)

Publication Number Publication Date
CN104703979A CN104703979A (zh) 2015-06-10
CN104703979B true CN104703979B (zh) 2018-11-27

Family

ID=48142967

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380030485.2A Active CN104703979B (zh) 2012-04-10 2013-04-03 杂环化合物及其应用

Country Status (8)

Country Link
US (3) US8940742B2 (enExample)
EP (1) EP2836487B1 (enExample)
JP (1) JP6309505B2 (enExample)
CN (1) CN104703979B (enExample)
AU (1) AU2013205238B2 (enExample)
CA (1) CA2870087C (enExample)
HK (1) HK1207069A1 (enExample)
WO (1) WO2013154878A1 (enExample)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3219705T3 (da) 2005-12-28 2020-04-14 Vertex Pharma Farmaceutiske sammensætninger af den amorfe form af n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinolin-3-carboxamid
CA2711558C (en) 2008-01-04 2016-12-13 Intellikine, Inc. Phosphatidyl inositol-3 kinase inhibiting compounds
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
AU2012205669B2 (en) 2011-01-10 2015-08-20 Infinity Pharmaceuticals Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
JP2014517079A (ja) 2011-06-22 2014-07-17 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
EP2751093A1 (en) 2011-08-29 2014-07-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8940742B2 (en) * 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
US9365760B2 (en) * 2013-01-17 2016-06-14 Jx Nippon Oil & Energy Corporation Refrigerating machine oil and working fluid composition for refrigerating machine
WO2014143241A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
JP6799201B2 (ja) 2013-07-31 2020-12-16 アヴァリン ファーマ インク． エアロゾルチロシンキナーゼ阻害剤の化合物、及びその使用
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20160685A1 (es) * 2013-10-04 2016-07-23 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
EA201691169A1 (ru) 2013-12-05 2016-09-30 Асерта Фарма Б.В. Терапевтическая комбинация ингибитора pi3k и ингибитора btk
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
RU2016134406A (ru) 2014-01-24 2018-03-01 Лэм Терапьютикс, Инк. Композиции апилимода и способы их применения
SG10201808053XA (en) * 2014-03-19 2018-10-30 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
UY36060A (es) 2014-04-02 2015-10-30 Bayer Pharma AG Compuestos de azol sustituidos con amida
CN107074863B (zh) 2014-06-05 2019-12-03 沃泰克斯药物股份有限公司 Atr激酶抑制剂的制备方法及其不同的固体形式
PL3157566T3 (pl) 2014-06-17 2019-10-31 Vertex Pharma Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr
SG11201610770PA (en) 2014-07-04 2017-01-27 Lupin Ltd Quinolizinone derivatives as pi3k inhibitors
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
RS62713B1 (sr) 2014-08-11 2022-01-31 Acerta Pharma Bv Terapeutske kombinacije btk inhibitora i bcl-2 inhibitora
US20170224819A1 (en) 2014-08-11 2017-08-10 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a CDK 4/6 Inhibitor
HRP20220738T1 (hr) 2014-08-11 2022-08-19 Acerta Pharma B.V. Terapijske kombinacije inhibitora btk, inhibitora pd-1 i/ili inhibitora pd-l1
US9708348B2 (en) * 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
CN107250113B (zh) 2014-10-07 2019-03-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调节蛋白的调节剂的共晶
US10206910B2 (en) 2014-11-07 2019-02-19 Lam Therapeutics, Inc. Apilimod for use in the treatment of renal cancer
PT3215157T (pt) 2014-11-07 2019-07-12 Ai Therapeutics Inc Apilimod para utilização no tratamento de melanoma
JP6861154B2 (ja) 2014-12-03 2021-04-21 ヤンセン ファーマシューティカ エヌ．ベー． 放射標識されたｍＧｌｕＲ２ ＰＥＴリガンド
JP6689856B2 (ja) 2014-12-03 2020-04-28 ヤンセン ファーマシューティカ エヌ．ベー． ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
KR102678021B1 (ko) 2015-09-30 2024-06-26 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물
TWI744256B (zh) * 2015-11-06 2021-11-01 美商英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
LT3389727T (lt) 2015-12-18 2020-10-12 Janssen Pharmaceutica Nv Radioaktyviai pažymėti mglur2/3 pet ligandai
JP6929285B2 (ja) 2015-12-18 2021-09-01 ヤンセン ファーマシューティカ エヌ．ベー． 放射性標識ｍＧｌｕＲ２／３ＰＥＴリガンド
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
TW201734003A (zh) 2016-01-05 2017-10-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之吡啶及嘧啶化合物
MX2018009870A (es) * 2016-02-15 2018-11-29 Cemm Forschungszentrum Fuer Molekulare Medizin Gmbh Inhibidores de taf1 para la terapia del cancer.
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AR108875A1 (es) 2016-06-24 2018-10-03 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
CA3066939A1 (en) 2017-06-21 2018-12-27 SHY Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
GB201710851D0 (en) * 2017-07-06 2017-08-23 Galápagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
WO2019028395A1 (en) * 2017-08-03 2019-02-07 Fronthera U.S. Pharmaceuticals Llc PI3 KINASE INHIBITORS AND USES THEREOF
US10751339B2 (en) 2018-01-20 2020-08-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
AU2019223014B2 (en) 2018-02-21 2024-10-17 Orphai Therapeutics Inc. Combination therapy with apilimod and glutamatergic agents
US12589097B2 (en) 2018-02-21 2026-03-31 OrphAl Therapeutics Inc. Apilimod compositions and methods of use
MD3762368T2 (ro) 2018-03-08 2022-07-31 Incyte Corp Compuși diol aminopirazină ca inhibitori ai PI3K-Y
CN112292374B (zh) * 2018-05-31 2023-01-03 信达生物制药(苏州)有限公司 一种新型磷酸肌醇3-激酶抑制剂及其制备方法和用途
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
WO2020119592A1 (zh) * 2018-12-12 2020-06-18 信达生物制药(苏州)有限公司 一种新颖的三并环结构化合物及其制备方法和用途
EP3898609A1 (en) 2018-12-19 2021-10-27 Shy Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
CN110698418B (zh) * 2019-09-11 2022-07-01 广西师范大学 一种3-芳胺基喹喔啉-2-甲酰胺类衍生物及其制备方法和应用
JP2023529867A (ja) 2020-06-05 2023-07-12 キネート バイオファーマ インク． 線維芽細胞増殖因子受容体キナーゼの阻害剤
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
WO2022006470A1 (en) 2020-07-01 2022-01-06 Vanderbilt University Methods of treatment for a kidney disease
BR112023000047A2 (pt) 2020-07-02 2023-03-14 Incyte Corp Compostos de ureia tricíclicos como inibidores da v617f da jak2
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
CA3207819A1 (en) 2021-02-19 2022-08-25 Anjali Pandey Tyk2 inhibitors and uses thereof
JP2024508794A (ja) 2021-02-19 2024-02-28 スドー バイオサイエンシーズ リミテッド Ｔｙｋ２阻害剤およびその使用
JP2024507253A (ja) 2021-02-19 2024-02-16 スドー バイオサイエンシーズ リミテッド Ｔｙｋ２阻害剤およびその使用
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
CN113173940B (zh) * 2021-04-26 2022-08-09 湖南大学 一种双生物活性因子级联激活的抗黑色素瘤前药的合成与应用
KR20240163688A (ko) 2022-03-17 2024-11-19 인사이트 코포레이션 Jak2 v617f 억제제로서의 삼환계 우레아 화합물
JP2025514198A (ja) * 2022-04-25 2025-05-02 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン 二重機能免疫調節化合物、製剤、及びその使用
WO2024163752A1 (en) * 2023-02-02 2024-08-08 Synnovation Therapeutics, Inc. HETEROCYCLIC COMPOUNDS AS PI3Kα INHIBITORS
KR102912267B1 (ko) 2023-04-20 2026-01-15 한국화학연구원 신규한 헤테로고리 화합물 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 포함하는 바이러스성 질환의 예방 또는 치료용 약학적 조성물
WO2024217587A1 (zh) * 2023-04-21 2024-10-24 南京正大天晴制药有限公司 具有axl抑制活性的取代吡嗪化合物
CN116606298A (zh) * 2023-05-26 2023-08-18 康化（上海）新药研发有限公司 2,3-二氢-[1,4]二噁烷并[2,3-b]吡啶-8-羧酸的合成方法
EP4553080A1 (en) 2023-11-07 2025-05-14 Ustav Organicke Chemie a Biochemie AV CR, v.v.i. Nucleoside derivatives as antiviral agents against coronaviruses

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090312319A1 (en) * 2008-01-04 2009-12-17 Intellikine Certain chemical entities, compositions and methods

Family Cites Families (665)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB812366A (en) 1955-08-18 1959-04-22 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the preparation thereof
GB937725A (en) 1960-05-11 1963-09-25 Ciba Ltd Pyrazolo[3:4-d]pyrimidines
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
DE2139107A1 (de) 1971-08-04 1973-02-15 Merck Patent Gmbh Heterocyclisch substituierte adenosinverbindungen
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
IT1153216B (it) 1981-10-16 1987-01-14 Schering Ag Procedimento per la preparazione di composti cianoeterociclici
DE3244594A1 (de) 1982-12-02 1984-06-07 Hoechst Ag, 6230 Frankfurt 1-phenylisochinolinderivate und verfahren zu ihrer herstellung, diese verbindung enthaltende pharmazeutische praeparate und deren anwendung
DE3406533A1 (de) 1984-02-23 1985-08-29 Boehringer Mannheim Gmbh, 6800 Mannheim Verwendung von adenosin-derivaten als antiallergica und arzneimittel, die diese enthalten
US5310731A (en) 1984-06-28 1994-05-10 Whitby Research, Inc. N-6 substituted-5'-(N-substitutedcarboxamido)adenosines as cardiac vasodilators and antihypertensive agents
KR890002631B1 (ko) 1984-10-04 1989-07-21 몬산토 캄파니 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물
US4795627A (en) 1984-10-18 1989-01-03 University Of Pittsburgh Tritium labelled N-mustard type compounds and a process for their production
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US4656159A (en) 1984-10-31 1987-04-07 Georgetown University Galactose-C-6 nitrogen mustard compounds and their uses
JPS61109797A (ja) 1984-11-01 1986-05-28 Yuki Gosei Yakuhin Kogyo Kk 標識化ヌクレオチドおよび標識化ポリヌクレオチド
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4886499A (en) 1986-12-18 1989-12-12 Hoffmann-La Roche Inc. Portable injection appliance
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
GB8707053D0 (en) 1987-03-25 1987-04-29 Ici Plc Anti-tumour agents
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
WO1990003370A1 (en) 1988-09-28 1990-04-05 Microprobe Corporation DERIVATIVES OF PYRAZOLO[3,4-d]PYRIMIDINE
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
WO1993019767A1 (en) 1992-04-07 1993-10-14 The Regents Of The University Of Michigan Cd28 pathway immunoregulation
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5442039A (en) 1989-07-17 1995-08-15 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5763596A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. C-4' modified adenosine kinase inhibitors
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. Orally active adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5674998A (en) 1989-09-15 1997-10-07 Gensia Inc. C-4' modified adenosine kinase inhibitors
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
GB9009542D0 (en) 1990-04-27 1990-06-20 Beecham Group Plc Novel compounds
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
GB9113137D0 (en) 1990-07-13 1991-08-07 Ici Plc Thioxo heterocycles
US5563257A (en) 1990-08-20 1996-10-08 Boehringer Mannheim Gmbh Phospholipid derivatives of nucleosides
DE4026265A1 (de) 1990-08-20 1992-02-27 Boehringer Mannheim Gmbh Neue phospholipid-derivate von nucleosiden, deren herstellung sowie deren verwendung als antivirale arzneimittel
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
CA2092305C (en) 1990-09-25 2003-02-11 Alfred P. Spada Compounds having antihypertensive and anti-ischemic properties
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
GB9103839D0 (en) 1991-02-23 1991-04-10 Smithkline Beecham Plc Pharmaceuticals
CA2102780C (en) 1991-05-10 2007-01-09 Alfred P. Spada Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5272158A (en) 1991-10-29 1993-12-21 Merck & Co., Inc. Fibrinogen receptor antagonists
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
MX9300141A (es) 1992-01-13 1994-07-29 Smithkline Beecham Corp Compuestos de imidazol novedosos, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
DE4204031A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue lipidphosphonsaeure-nucleosid-konjugate sowie deren verwendung als antivirale arzneimittel
DE4204032A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue liponucleotide, deren herstellunmg sowie deren verwendung als antivirale arzneimittel
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
JPH05239036A (ja) 1992-02-27 1993-09-17 Nissan Chem Ind Ltd 含窒素複素環化合物の製造方法
WO1993018035A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
JP2737518B2 (ja) 1992-03-16 1998-04-08 富士通株式会社 赤外線検知器の冷却構造
US5294612A (en) 1992-03-30 1994-03-15 Sterling Winthrop Inc. 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
AU4115693A (en) 1992-04-24 1993-11-29 Sri International In vivo homologous sequence targeting in eukaryotic cells
DE69328440T3 (de) 1992-06-19 2009-05-07 Honeywell, Inc., Minneapolis Infrarot kamera mit thermoelektrischer temperaturstabilisierung
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US6057305A (en) 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
TW444018B (en) 1992-12-17 2001-07-01 Pfizer Pyrazolopyrimidines
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
IL108523A0 (en) 1993-02-03 1994-05-30 Gensia Inc Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain
AU673055B2 (en) 1993-02-03 1996-10-24 Gensia, Inc. Adenosine kinase inhibitors comprising lyxofuranosyl derivatives
GB9308957D0 (en) 1993-04-30 1993-06-16 Cancer Res Campaign Tech Novel produgs
WO1994029436A1 (en) 1993-06-04 1994-12-22 The United States Of America Represented By The Secretary Of The Navy Methods for selectively stimulating proliferation of t cells
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
US5504103A (en) 1993-08-25 1996-04-02 Eli Lilly And Company Inhibition of phosphatidylinositol 3-kinase with 17 β-hydroxywortmannin and analogs thereof
US5525503A (en) 1993-09-28 1996-06-11 Dana-Farber Cancer Institute, Inc. Signal transduction via CD28
DE4333761A1 (de) 1993-10-04 1995-04-06 Luitpold Pharma Gmbh Heterocyclische Carbamate, Verfahren zu ihrer Herstellung und Arzneimittel
WO1995012588A1 (en) 1993-11-05 1995-05-11 Biochem Pharma Inc. Antineoplastic heteronaphthoquinones
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
US6632789B1 (en) 1994-04-29 2003-10-14 The United States Of America As Represented By The Secretary Of The Navy Methods for modulating T cell responses by manipulating intracellular signal transduction
DE4418690A1 (de) 1994-05-28 1996-01-11 Boehringer Mannheim Gmbh Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5756502A (en) 1994-08-08 1998-05-26 Warner-Lambert Company Quinazolinone derivatives as cholyecystokinin (CCK) ligands
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
JP4249804B2 (ja) 1995-04-03 2009-04-08 ノバルティス・アクチエンゲゼルシャフト ピラゾール誘導体およびその製造法
US6312894B1 (en) 1995-04-03 2001-11-06 Epoch Pharmaceuticals, Inc. Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
US5977061A (en) 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
JPH08295667A (ja) 1995-04-27 1996-11-12 Takeda Chem Ind Ltd 複素環化合物、その製造法および剤
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
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
CN1192696A (zh) 1995-06-07 1998-09-09 G·D·瑟尔公司 用于充血性心力衰竭治疗的螺甾内酯与血管紧张素ⅱ拮抗药组合疗法
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
WO1996040256A1 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angiotensin ii antagonist and spironolactone
ES2167571T3 (es) 1995-06-07 2002-05-16 Searle & Co Terapia de combinacion de antagonista de aldosterona epoxi-esteroideo y antagonista de angiotensina ii para el tratamiento del fallo cardiaco congestivo.
WO1997001331A2 (en) 1995-06-27 1997-01-16 Takeda Chemical Industries, Ltd. Method of producing sustained-release preparation
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
WO1997010221A1 (en) 1995-09-15 1997-03-20 Torrey Pines Institute For Molecular Studies Synthesis of quinazolinone libraries
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US5763885A (en) 1995-12-19 1998-06-09 Loral Infrared & Imaging Systems, Inc. Method and apparatus for thermal gradient stabilization of microbolometer focal plane arrays
JPH09143163A (ja) 1995-11-29 1997-06-03 Fuji Photo Film Co Ltd 含窒素ヘテロ芳香族アミド類の製造方法
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
US5747235A (en) 1996-01-26 1998-05-05 Eastman Kodak Company Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
US5763608A (en) 1996-02-05 1998-06-09 Hoechst Celanese Corporation Process for preparing pyrimidine derivatives
US5914488A (en) 1996-03-05 1999-06-22 Mitsubishi Denki Kabushiki Kaisha Infrared detector
US5872136A (en) 1996-04-03 1999-02-16 Merck & Co., Inc. Arylheteroaryl inhibitors of farnesyl-protein transferase
EP0891361A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
WO1997048694A1 (en) 1996-06-20 1997-12-24 Board Of Regents, The University Of Texas System Compounds and methods for providing pharmacologically active preparations and uses thereof
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
FR2750862B1 (fr) 1996-07-12 1998-10-16 Dupin Jean Pierre Utilisation d'heterocycles diazotes fusionnes avec un systeme aromatique ou heteroaromatique pour le traitement des maladies thrombo-emboliques
CA2260898C (en) 1996-07-18 2002-05-14 Pfizer Limited Phosphinate based inhibitors of matrix metalloproteases
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
US5990169A (en) 1996-10-23 1999-11-23 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6342514B1 (en) 1996-10-23 2002-01-29 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5919808A (en) 1996-10-23 1999-07-06 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5994358A (en) 1996-10-23 1999-11-30 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6251901B1 (en) 1996-10-23 2001-06-26 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US5965573A (en) 1996-10-23 1999-10-12 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
US6153631A (en) 1996-10-23 2000-11-28 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
ES2221019T3 (es) 1996-10-31 2004-12-16 Takeda Chemical Industries, Ltd. Preparacion de liberacion mantenida.
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
US5977134A (en) 1996-12-05 1999-11-02 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP4094066B2 (ja) 1996-12-06 2008-06-04 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 インターロイキン−１β変換酵素のインヒビター
ZA9711385B (en) 1996-12-20 1999-06-18 Takeda Chemical Industries Ltd Method of producing a sustained-release preparation
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE69730151T2 (de) 1997-01-06 2005-08-04 Pfizer Inc. Cyclische sulfonderivate
JPH10206995A (ja) 1997-01-21 1998-08-07 Konica Corp ハロゲン化銀写真感光材料
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
AU721748B2 (en) 1997-02-03 2000-07-13 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
WO1998035048A2 (en) 1997-02-07 1998-08-13 Princeton University Engineered protein kinases which can utilize modified nucleotide triphosphate substrates
WO1998034918A1 (en) 1997-02-11 1998-08-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
TR199902301T2 (xx) 1997-03-19 1999-12-21 Basf Aktiengesellschaft Pirilo $2,3D]pirimidinler ve onlar�n kullan�m�.
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
WO1998052611A1 (en) 1997-05-23 1998-11-26 Nippon Shinyaku Co., Ltd. Medicinal composition for prevention or treatment of hepatopathy
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
US6207697B1 (en) 1997-09-09 2001-03-27 Dupont Pharmaceuticals Company Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor Xa
DE69839887D1 (de) 1997-10-02 2008-09-25 Eisai R&D Man Co Ltd Kondensierte pyridinderivate
US6649631B1 (en) 1997-10-23 2003-11-18 The Board Of Regents Of The University Of Texas System Compositions and methods for treating bone deficit conditions
CA2309350C (en) 1997-11-12 2007-04-03 Mitsubishi Chemical Corporation Purine derivatives and medicaments comprising the same as active ingredient
US6040321A (en) * 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6184377B1 (en) 1997-12-15 2001-02-06 Sepracor Inc. Compositions containing N-amino- and N-hydroxy-quinazolinones and methods for preparing libraries thereof
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US6191170B1 (en) 1998-01-13 2001-02-20 Tularik Inc. Benzenesulfonamides and benzamides as therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
EP0945441A3 (de) 1998-03-27 2002-07-17 Degussa AG Verfahren zur Herstellung von cyclischen 4-Oxoamidinen
US7715989B2 (en) 1998-04-03 2010-05-11 Elitech Holding B.V. Systems and methods for predicting oligonucleotide melting temperature (TmS)
US6127121A (en) 1998-04-03 2000-10-03 Epoch Pharmaceuticals, Inc. Oligonucleotides containing pyrazolo[3,4-D]pyrimidines for hybridization and mismatch discrimination
US6432970B2 (en) 1998-04-09 2002-08-13 Johns Hopkins University School Of Medicine Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
HK1039325B (en) 1998-09-18 2006-02-24 Abbott Gmbh & Co. Kg 4-aminopyrrolopyrimidines as kinase inhibitors
HK1043128B (zh) 1998-12-19 2007-01-19 詹森药业有限公司 抗组胺的螺环化合物
DK1140938T3 (da) 1999-01-11 2003-12-22 Univ Princeton Højaffinitetsinhibitorer for målvalidering og anvendelser heraf
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6596497B1 (en) 1999-03-17 2003-07-22 New York Blood Center, Inc. Screening of antiviral compounds targeted to the HIV-1 gp41 core structure
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
SE515856C2 (sv) 1999-05-19 2001-10-22 Ericsson Telefon Ab L M Bärare för elektronikkomponenter
MXPA01012442A (es) 1999-06-03 2004-09-10 Abbott Gmbh & Co Kg Compuestos de benzotiazinona y benzoxazinona.
US6387894B1 (en) 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
JP4831906B2 (ja) 1999-08-27 2011-12-07 ケモセントリックス， インコーポレイテッド Ｃｘｃｒ３機能を調節するための複素環式化合物および方法
DE19940860A1 (de) 1999-08-27 2001-03-01 Bayer Ag Selektive Herbizide auf Basis eines substituierten Phenylsulfonyl aminocarbonyltriazolinons und Safenern II
DE19940859A1 (de) 1999-08-27 2001-03-01 Bayer Ag Selektive Herbizide auf Basis eines substituierten Phenylsulfonylaminocarbonyltriazolinons und Safenern
US20050080138A1 (en) 1999-09-16 2005-04-14 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
ATE286033T1 (de) 1999-09-16 2005-01-15 Curis Inc Vermittler von igel signalwegen, deren zusammenstellungen und verwendungen
US20070021493A1 (en) 1999-09-16 2007-01-25 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
KR20020088406A (ko) 1999-09-17 2002-11-27 애보트 게엠베하 운트 콤파니 카게 치료제로서의 피라졸로피리미딘
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
ATE277044T1 (de) 1999-10-06 2004-10-15 Boehringer Ingelheim Pharma Heterocyclische verbindungen verwendbar als tyrosinkinase inhibitoren
CA2386190C (en) 1999-10-13 2009-04-14 Johns Hopkins University School Of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
WO2001026644A2 (en) 1999-10-14 2001-04-19 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US6472153B1 (en) 1999-10-26 2002-10-29 Epoch Biosciences, Inc. Hybridization-triggered fluorescent detection of nucleic acids
US7230000B1 (en) 1999-10-27 2007-06-12 Cytokinetics, Incorporated Methods and compositions utilizing quinazolinones
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US7671200B2 (en) 1999-10-27 2010-03-02 Cytokinetics, Inc. Quinazolinone KSP inhibitors
US6660845B1 (en) 1999-11-23 2003-12-09 Epoch Biosciences, Inc. Non-aggregating, non-quenching oligomers comprising nucleotide analogues; methods of synthesis and use thereof
IL133809A0 (en) 1999-12-30 2001-04-30 Yeda Res & Dev Steroidal alkaloids and pharmaceutical compositions comprising them
GB0002032D0 (en) 2000-01-28 2000-03-22 Zeneca Ltd Chemical compounds
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
JP2001250689A (ja) 2000-03-07 2001-09-14 Toray Ind Inc 発光素子
WO2001072712A1 (en) 2000-03-24 2001-10-04 Cor Therapeutics, Inc. ISOQUINOLONE INHIBITORS OF FACTOR Xa
US7115653B2 (en) 2000-03-30 2006-10-03 Curis, Inc. Small organic molecule regulators of cell proliferation
WO2001074344A2 (en) 2000-03-30 2001-10-11 Curis, Inc. Small organic molecule regulators of cell proliferation
US6683192B2 (en) 2000-03-30 2004-01-27 Curis, Inc. Small organic molecule regulators of cell proliferation
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. Small organic molecule regulators of cell proliferation
US20050070578A1 (en) 2000-03-30 2005-03-31 Baxter Anthony David Small organic molecule regulators of cell proliferation
US6683108B1 (en) 2000-03-30 2004-01-27 Curis, Inc. Agonists of hedgehog signaling pathways and uses related thereto
US20020127625A1 (en) 2000-03-31 2002-09-12 Forskarpatent Is Syd Ab Methods of diagnosing immune related diseases
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
DK2223922T3 (en) 2000-04-25 2016-06-06 Icos Corp Inhibitors of HUMANPHOSPHATIDYL-inositol 3-KINASEDELTA
AU6513701A (en) 2000-05-30 2001-12-11 Advanced Res & Tech Inst Compositions and methods for identifying agents which modulate pten function andpi-3 kinase pathways
BR0112030A (pt) 2000-06-27 2003-04-29 Genelabs Tech Inc Novos compostos que possuem atividade antibacteriana, antifúngica ou antitumor
US6534691B2 (en) 2000-07-18 2003-03-18 E. I. Du Pont De Nemours And Company Manufacturing process for α-olefins
JP4854909B2 (ja) 2000-09-20 2012-01-18 メルク・シャープ・エンド・ドーム・コーポレイション イソキノリノン系カリウムチャンネル阻害剤
CA2425663C (en) 2000-10-11 2009-12-29 Applera Corporation Fluorescent nucleobase conjugates having anionic linkers
US20020173524A1 (en) 2000-10-11 2002-11-21 Tularik Inc. Modulation of CCR4 function
JP2002131859A (ja) 2000-10-19 2002-05-09 Konica Corp 撮影用赤外感光性ハロゲン化銀写真感光材料及び赤外感光性ハロゲン化銀乳剤
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
NZ526622A (en) 2000-12-11 2006-07-28 Amgen Sf Llc CXCR3 antagonists
ES2275621T3 (es) 2000-12-21 2007-06-16 Glaxo Group Limited Antibioticos macrolidos.
ATE524441T1 (de) 2000-12-28 2011-09-15 Daiichi Seiyaku Co Vla-4-inhibitoren
SI1355916T1 (sl) 2001-01-22 2007-04-30 Merck & Co Inc Nukleozidni derivati kot inhibitorji RNA-odvisne RNA virusne polimeraze
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
GB0102239D0 (en) 2001-01-29 2001-03-14 Cancer Res Ventures Ltd Methods of chemical synthisis
GB2373186A (en) 2001-02-23 2002-09-18 Astrazeneca Ab Pharmaceutical combinations of a CCR3 antagonist and a compound which is usefulreatment of asthma, allergic disease or inflammation
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
DE10118698A1 (de) 2001-04-17 2002-11-07 Jerini Ag Verfahren zur Immobilisierung und damit hergestellte Anordnungen von Verbindungen auf einer planaren Oberfläche
ATE364685T1 (de) 2001-04-25 2007-07-15 Cornell Res Foundation Inc Anlagen und verfahren für zellkulturen auf pharmacokinetischer basis
WO2002088025A1 (en) 2001-04-26 2002-11-07 New York University Method for dissolving carbon nanotubes
US7405235B2 (en) 2001-05-04 2008-07-29 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
DE60218458T2 (de) 2001-05-08 2007-11-15 Kudos Pharmaceuticals Ltd. Isochinolinon derivate als parp inhibitoren
WO2002094264A1 (en) 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
US6794379B2 (en) 2001-06-06 2004-09-21 Tularik Inc. CXCR3 antagonists
AU2002312370A1 (en) 2001-06-13 2002-12-23 Roland W. Burli Antipathogenic benzamide compounds
WO2002100832A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
US6825228B2 (en) 2001-06-13 2004-11-30 Genesoft Pharmaceuticals, Inc. Benzothiophene compounds having antiinfective activity
EP1463742A4 (en) 2001-06-21 2006-05-10 Ariad Pharma Inc NEW PYRAZOLO AND PYRROLO PYRIMIDINES AND THEIR USES
US20030220338A1 (en) 2001-07-16 2003-11-27 Watkins Will J. Fungal efflux pump inhibitors
US6596723B1 (en) 2001-07-16 2003-07-22 Essential Therapeutics, Inc. Fungal efflux pump inhibitors
US6689782B2 (en) 2001-07-16 2004-02-10 Essential Therapeutics, Inc. Fungal efflux pump inhibitors
AU2002322585A1 (en) 2001-07-20 2003-03-03 Adipogenix, Inc. Fat accumulation-modulating compounds
NZ530580A (en) 2001-07-27 2007-02-23 Curis Inc Mediators of hedgehog signaling pathways, compositions and uses related thereto
AU2002355732B2 (en) 2001-08-01 2006-11-09 Merck Sharp & Dohme Corp. Benzimidazo[4,5-f]isoquinolinone derivatives
AU2002327422A1 (en) 2001-08-03 2003-03-18 Abbott Laboratories Method of identifying inhibitors of lck
DK3042894T1 (da) 2001-08-10 2016-11-07 Shionogi & Co Antiviralt middel
JP2003073357A (ja) 2001-09-03 2003-03-12 Mitsubishi Pharma Corp アミド化合物を含有するＲｈｏキナーゼ阻害剤
CA2459583A1 (en) 2001-09-05 2003-03-13 Minerva Biotechnologies Corporation Compositions and methods of treatment of cancer
WO2004043335A2 (en) 2001-09-13 2004-05-27 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
US7269663B2 (en) 2001-09-28 2007-09-11 Intel Corporation Tagging packets with a lookup key to facilitate usage of a unified packet forwarding cache
TWI330183B (enExample) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
MXPA04004178A (es) 2001-11-01 2004-09-06 Janssen Pharmaceutica Nv Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta.
US7053216B2 (en) 2001-11-19 2006-05-30 Iconix Pharmaceuticals, Inc. Modulators of Rho C activity
WO2003043995A1 (en) 2001-11-20 2003-05-30 Cytokinetics, Inc. Process for the racemization of chiral quinazolinones
US6596718B1 (en) * 2001-11-27 2003-07-22 Hoffmann-La Roche Inc. 7-Morpholin-4yl-benzothiazole amide derivatives
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
ATE424388T1 (de) 2001-12-06 2009-03-15 Merck & Co Inc Mitotische kinesinhemmer
WO2003049679A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
JP4085237B2 (ja) 2001-12-21 2008-05-14 日本電気株式会社 携帯電話の利用契約システムと通信方法
AU2002351412B2 (en) 2001-12-21 2010-05-20 Exelixis Patent Company Llc Modulators of LXR
US7064218B2 (en) 2001-12-26 2006-06-20 Genelabs Technologies, Inc. Aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
US7414036B2 (en) 2002-01-25 2008-08-19 Muscagen Limited Compounds useful as A3 adenosine receptor agonists
AU2003213092A1 (en) 2002-02-15 2003-09-09 Smithkline Beecham Corporation Syntheses of quinazolinones
US20040043959A1 (en) 2002-03-04 2004-03-04 Bloom Laura A. Combination therapies for treating methylthioadenosine phosphorylase deficient cells
EP1521746B1 (en) 2002-03-07 2011-04-27 X-Ceptor Therapeutics, Inc. Quinazolinone modulators of nuclear receptors
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
US20030180924A1 (en) 2002-03-22 2003-09-25 Desimone Robert W. Formulation of certain pyrazolo [3,4,-d] pyrimidines as kinase modulators
CA2480468C (en) 2002-03-26 2012-03-13 Biofrontera Discovery Gmbh Fredericamycin derivatives
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
US6900219B2 (en) 2002-04-04 2005-05-31 Cv Therapeutics, Inc. ABCA-1 elevating compounds
DE10217046A1 (de) 2002-04-17 2003-11-06 Bioleads Gmbh Fredericamycin-Derivate
AU2003231032B2 (en) 2002-04-22 2008-07-10 Johns Hopkins University School Of Medicine Modulators of hedgehog signaling pathways, compositions and uses related thereto
MXPA04010550A (es) 2002-04-26 2005-01-25 Pfizer Prod Inc Inhibidores de metaloproteinasa de pirimidina-2,4,6-triona.
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
JP2005530785A (ja) 2002-05-09 2005-10-13 サイトキネティクス・インコーポレーテッド 化合物、組成物、及び方法
EP1503993A4 (en) 2002-05-09 2006-05-03 Cytokinetics Inc COMPOUNDS, METHODS AND COMPOSITIONS
TW200407143A (en) 2002-05-21 2004-05-16 Bristol Myers Squibb Co Pyrrolotriazinone compounds and their use to treat diseases
CA2485343A1 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1513820A4 (en) 2002-05-23 2006-09-13 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
EP1556357A4 (en) 2002-06-14 2006-09-13 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
US7265111B2 (en) 2002-06-27 2007-09-04 Sanofi-Aventis Deutschland Gmbh Adenosine analogues and their use as pharmaceutical agents
KR101124245B1 (ko) 2002-06-27 2012-07-02 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
DE10230917A1 (de) 2002-07-09 2004-02-05 Bioleads Gmbh Fredericamycin-Derivate
EA011807B1 (ru) * 2002-07-10 2009-06-30 Лаборатуар Сероно Са Азолидинонвинильные производные конденсированного бензола
AU2003249244A1 (en) 2002-07-15 2004-02-02 Combinatorx, Incorporated Methods for the treatment of neoplasms
JP2006503008A (ja) 2002-08-13 2006-01-26 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー マトリクスメタロプロテイナーゼ阻害物質としての４−ヒドロキシキノリン誘導体
JP4646626B2 (ja) 2002-08-16 2011-03-09 アストラゼネカ アクチボラグ ホスホイノシチド３−キナーゼβの阻害
AU2003262747A1 (en) 2002-08-21 2004-03-11 Cytokinetics, Inc. Compounds, compositions, and methods
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
AU2003265853A1 (en) 2002-08-29 2004-03-19 Curis, Inc. Hedgehog antagonists, methods and uses related thereto
GB0220319D0 (en) 2002-09-02 2002-10-09 Cancer Res Campaign Tech Enzyme activated self-immolative nitrogen mustard drugs
AU2003266668A1 (en) 2002-09-30 2004-04-23 Banyu Pharmaceutical Co., Ltd. 2-aminobenzimidazole derivative
US20040132732A1 (en) 2002-10-21 2004-07-08 Wei Han Quinazolinones and derivatives thereof as factor Xa inhibitors
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Ｊｎｋ阻害剤
CN1281590C (zh) 2002-11-27 2006-10-25 南京凯衡科贸有限公司 具有抑制血管生成活性的六员氨基酰胺类衍生物
EP1572660B1 (en) 2002-12-20 2011-01-26 X-Ceptor Therapeutics, Inc. Isoquinolinone derivatives and their use as therapeutic agents
US7071355B2 (en) 2002-12-23 2006-07-04 4 Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
US7365094B2 (en) 2002-12-23 2008-04-29 4Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
FR2850022B1 (fr) 2003-01-22 2006-09-08 Centre Nat Rech Scient Nouvelle utilisation de la mifepristone et de ses derives comme modulateurs de la voie de signalisation des proteines hedgehog et ses applications
WO2004069145A2 (en) 2003-02-07 2004-08-19 Dr. Reddy's Laboratories Ltd. Anticancer compounds, process for their preparation and pharmaceutical compositions containing them
US20060135790A1 (en) 2003-03-06 2006-06-22 Hyett David J Process for the preparation of an alpha-amino carbonyl compound
AR050920A1 (es) 2003-03-07 2006-12-06 Astrazeneca Ab Enantiomeros de heterociclos fusionados seleccionados y usos de los mismos
CA2518465A1 (en) 2003-03-25 2004-10-14 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
GB0306907D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Boireductively-activated prodrugs
US7217794B2 (en) 2003-04-02 2007-05-15 Daiamed, Inc. Compounds and methods for treatment of thrombosis
WO2004092123A2 (en) 2003-04-10 2004-10-28 Microbia, Inc. Inhibitors of fungal invasion
US7652061B2 (en) 2003-05-20 2010-01-26 Novartis A.G. N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
US7022850B2 (en) 2003-05-22 2006-04-04 Bristol-Myers Squibb Co. Bicyclicpyrimidones and their use to treat diseases
US7345046B2 (en) 2003-05-30 2008-03-18 Chiron Corporation Heteroaryl-fused pyrimidinyl compounds as anticancer agents
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
EP1637523A4 (en) 2003-06-18 2009-01-07 Ube Industries PROCESS FOR PRODUCING A PYRIMIDIN-4-ONE COMPOUND
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
CA2572324A1 (en) 2003-07-02 2005-01-13 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 and a ligand to an alpha-2-delta receptor
JP2009513523A (ja) 2003-07-08 2009-04-02 ノバルティス アクチエンゲゼルシャフト ベンゼンスルホニルアミノ化合物およびそれらを含む医薬組成物
WO2005013800A2 (en) 2003-07-15 2005-02-17 The Johns Hopkins University Elevated hedgehog pathway activity in digestive system tumors, and methods of treating digestive system tumors having elevated hedgehog pathway activity
JP2005035933A (ja) 2003-07-15 2005-02-10 Takeda Chem Ind Ltd 含窒素縮合複素環化合物の製造方法
GB0317951D0 (en) 2003-07-31 2003-09-03 Trigen Ltd Compounds
US7501538B2 (en) 2003-08-08 2009-03-10 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
US20050043239A1 (en) 2003-08-14 2005-02-24 Jason Douangpanya Methods of inhibiting immune responses stimulated by an endogenous factor
US20050054614A1 (en) 2003-08-14 2005-03-10 Diacovo Thomas G. Methods of inhibiting leukocyte accumulation
MXPA06001758A (es) 2003-08-15 2006-08-11 Irm Llc Anilino purinas sustituidas en la posicion 6 utiles como inhibidores de rtk.
US7390820B2 (en) 2003-08-25 2008-06-24 Amgen Inc. Substituted quinolinone derivatives and methods of use
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
GB0322409D0 (en) 2003-09-25 2003-10-29 Astrazeneca Ab Quinazoline derivatives
US8067608B2 (en) 2003-09-29 2011-11-29 The Johns Hopkins University Hedgehog pathway antagonists
WO2005032343A2 (en) 2003-10-01 2005-04-14 The Johns Hopkins University Hedgehog signaling in prostate regeneration neoplasia and metastasis
US6994605B2 (en) 2003-10-14 2006-02-07 S. R. Mickelberg Company, Inc. Vibratory amusement device for producing concentric illuminated rings
US20080057071A1 (en) 2003-10-20 2008-03-06 Watkins David N Use Of Hedgehog Pathway Inhibitors In Small-Cell Lung Cancer
EP1687002A4 (en) 2003-11-10 2008-07-23 Synta Pharmaceuticals Corp CONDENSED HETEROCYCLIC COMPOUNDS
CA2545725A1 (en) 2003-11-14 2005-06-02 Merck Sharp & Dohme Limited Bicyclic pyrimidin-4-(3h)-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (vr1)
JP2007511596A (ja) 2003-11-17 2007-05-10 ファイザー・プロダクツ・インク 癌の治療において有用なピロロピリミジン化合物
WO2005054202A1 (en) 2003-11-25 2005-06-16 Eli Lilly And Company 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b)
WO2005051922A1 (en) 2003-11-25 2005-06-09 Chiron Corporation Quinazolinone compounds as anticancer agents
JP2007513154A (ja) 2003-12-08 2007-05-24 サイトキネティクス・インコーポレーテッド 化合物、組成物及び方法
WO2005063258A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
US20050152940A1 (en) 2003-12-23 2005-07-14 Medtronic Vascular, Inc. Medical devices to treat or inhibit restenosis
AU2004309420B2 (en) 2003-12-23 2008-10-30 Novartis Ag Bicyclic heterocyclic p-38 kinase inhibitors
JPWO2005061707A1 (ja) 2003-12-24 2007-07-12 協和醗酵工業株式会社 癌細胞のＥｇ５阻害剤に対する感受性を判定する方法
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
US20050214310A1 (en) 2004-01-23 2005-09-29 Seattle Genetics, Inc. Melphalan prodrugs
CA2553724A1 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
UA83416C2 (en) 2004-02-13 2008-07-10 Баниу Фармасьютикал Ко., Лтд. Fused ring 4-oxopyrimidine derivative
US7117807B2 (en) 2004-02-17 2006-10-10 University Of Florida Research Foundation, Inc. Dynamically modifiable polymer coatings and devices
US7650848B2 (en) 2004-02-17 2010-01-26 University Of Florida Research Foundation, Inc. Surface topographies for non-toxic bioadhesion control
US9016221B2 (en) 2004-02-17 2015-04-28 University Of Florida Research Foundation, Inc. Surface topographies for non-toxic bioadhesion control
US20050187418A1 (en) 2004-02-19 2005-08-25 Small Brooke L. Olefin oligomerization
US20070049593A1 (en) 2004-02-24 2007-03-01 Japan Tobacco Inc. Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
WO2005080394A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
JP2007523938A (ja) 2004-02-27 2007-08-23 エフ．ホフマン−ラ　ロシュ　アーゲー ピラゾールの縮合誘導体
HRP20090495T1 (hr) 2004-04-02 2009-10-31 Osi Pharmaceuticals Heterobiciklički inhibitori protein kinaze supstituirani 6,6-bicikličkim prstenom
KR20070005736A (ko) 2004-04-30 2007-01-10 제넨테크, 인크. 헤지호그 신호전달 경로의 퀴녹살린 억제제
CN1976907A (zh) 2004-04-30 2007-06-06 武田药品工业株式会社 杂环酰胺化合物及其作为mmp－13抑制剂的用途
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
WO2005112935A1 (en) 2004-05-13 2005-12-01 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
EP1761540B1 (en) 2004-05-13 2016-09-28 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
CA2567883A1 (en) 2004-05-25 2005-12-15 Icos Corporation Methods for treating and/or preventing aberrant proliferation of hematopoietic cells
GB0412467D0 (en) 2004-06-04 2004-07-07 Astrazeneca Ab Chemical compounds
WO2005120511A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
US20050282834A1 (en) 2004-06-09 2005-12-22 Fady Malik Compositions, devices and methods for treating cardiovascular disease
US7375102B2 (en) 2004-06-28 2008-05-20 Amgen Sf, Llc Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-D]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use
US7939538B2 (en) 2004-06-28 2011-05-10 Amgen Inc. Compounds, compositions and methods for prevention and treatment of inflammatory and immunoregulatory disorders and diseases
WO2006023381A1 (en) 2004-08-16 2006-03-02 Taigen Biotechnology Pyrimidinone compounds
US20060041128A1 (en) 2004-08-18 2006-02-23 Astrazeneca Ab Selected fused heterocyclics and uses thereof
BRPI0514390A (pt) 2004-08-18 2008-06-10 Astrazeneca Ab enanciÈmero de um composto ou um sal farmacêuticamente aceitável ou um éster hidrolisável in vivo do mesmo, uso do mesmo, métodos para o tratamento de cáncer, para produzir um efeito inibidor de eg5 em um animal de sangue quente e para tratar doenças, e, composição farmacêutica
ES2578728T3 (es) 2004-08-27 2016-07-29 Infinity Pharmaceuticals, Inc. Proceso para la preparación de compuestos análogos de ciclopamina
WO2006026597A2 (en) 2004-08-30 2006-03-09 Smithkline Beecham Corporation Novel compositions and methods of treatment
MX2007002434A (es) 2004-08-31 2007-05-04 Astrazeneca Ab Derivados de quinazolinona y su uso como inhibidores de b-raf.
KR20200019263A (ko) 2004-09-02 2020-02-21 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038865A1 (en) 2004-10-01 2006-04-13 Betagenon Ab Nucleotide derivatives for the treatment of type 2 diabetes and other disorders
MX2007005125A (es) 2004-10-28 2007-07-04 Irm Llc Compuestos y composiciones como moduladores de la senda de hedgehog.
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
AU2005301957B2 (en) 2004-11-03 2012-02-23 Department Of Health And Human Services Novobiocin analogues as anticancer agents
US7622451B2 (en) 2004-11-03 2009-11-24 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
US8212011B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
EP1831225A2 (en) 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
JP2008520741A (ja) 2004-11-23 2008-06-19 ピーティーシー セラピューティクス， インコーポレイテッド 翻訳制御によるｖｅｇｆ生成を阻害するための活性因子としてのテトラヒドロカルバゾール
US20060156485A1 (en) 2005-01-14 2006-07-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CN101106998A (zh) 2005-01-19 2008-01-16 默克公司 有丝分裂驱动蛋白抑制剂
CA2595130A1 (en) 2005-01-19 2006-07-27 Paul J. Coleman Mitotic kinesin inhibitors
US20070161644A1 (en) 2005-01-25 2007-07-12 Stockwell Brent R Erastin analogs and uses thereof
NZ560320A (en) 2005-01-25 2011-02-25 Prolexys Pharmaceuticals Inc Quinoxaline derivatives as antitumor agents
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
WO2006089106A2 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
US7579348B2 (en) 2005-02-25 2009-08-25 Pgxhealth, Llc Derivatives of 8-substituted xanthines
US20090124654A1 (en) 2005-03-01 2009-05-14 Mjalli Adnan M M Aryl and Heteroaryl Compounds, Compositions, Methods of Use
US7872050B2 (en) 2005-03-14 2011-01-18 Yaupon Therapeutics Inc. Stabilized compositions of volatile alkylating agents and methods of using thereof
JP2006265107A (ja) 2005-03-22 2006-10-05 Kyowa Hakko Kogyo Co Ltd 緑内障治療剤
GB0506147D0 (en) 2005-03-24 2005-05-04 Merck Sharp & Dohme Therapeutic agents
EP1869037B1 (en) 2005-03-25 2011-07-27 Tibotec Pharmaceuticals Heterobicylic inhibitors of hvc
CN101189234B (zh) 2005-03-25 2011-08-17 泰博特克药品有限公司 Hcv的杂二环抑制剂
EP1865775A1 (en) 2005-04-06 2007-12-19 Irm, Llc Diarylamine-containing compounds and compositions, and their use as modulators of steroid hormone nuclear receptors
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
JP2008538771A (ja) 2005-04-25 2008-11-06 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー， アカデミー オブ サイエンシズ オブ ザ チェコ リパブリック テロメラーゼのプロセッシビティーを向上させるための化合物の使用
WO2006121522A2 (en) 2005-05-10 2006-11-16 Angiotech International Ag Implantable sensors and pumps, anti-scarring agents, and therapeutic compositions
US20090280153A1 (en) 2005-05-10 2009-11-12 Angiotech International Ag electrical devices, anti-scarring agents, and therapeutic compositions
WO2006135479A2 (en) 2005-05-10 2006-12-21 Angiotech International Ag Anti-scarring agents, therapeutic compositions, and use thereof
GB0509573D0 (en) 2005-05-11 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
US20090298856A1 (en) 2005-05-11 2009-12-03 Rebecca Elizabeth Brown 2,3 Substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilliod-1receptor (VR1)
DE102005024017A1 (de) 2005-05-25 2006-11-30 Merck Patent Gmbh Chinazolinone
CN100526315C (zh) 2005-06-16 2009-08-12 浙江医药股份有限公司新昌制药厂 N2-喹啉或异喹啉取代的嘌呤衍生物及其制备方法和其用途
ZA200800309B (en) 2005-06-22 2009-10-28 Chemocentryx Inc Azaindazole compounds and methods of use
JP2008546843A (ja) 2005-06-27 2008-12-25 アムゲン インコーポレイティッド 抗炎症性アリールニトリル化合物
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
BRPI0615524A2 (pt) 2005-07-11 2010-04-06 Devgen Nv derivados da amida como inibidores da quinase
WO2007006547A1 (en) 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
WO2007015877A2 (en) 2005-07-20 2007-02-08 Kalypsys, Inc. Inhibitors of p38 kinase and methods of treating inflammatory disorders
US20070017915A1 (en) 2005-07-22 2007-01-25 Weder Donald E Collapsible and/or erectable substantially egg-shaped container
GB0516723D0 (en) 2005-08-15 2005-09-21 Novartis Ag Organic compounds
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
WO2007023110A2 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
EP1940805A4 (en) 2005-08-26 2009-11-11 Methylgene Inc BENZODIAZEPIN AND BENZOPIPERAZINANALOGA AS INHIBITORS OF HISTONDEACETYLASE
EP1919873A1 (de) 2005-09-01 2008-05-14 BioAgency AG Fredericamycin-derivate
CA2624220A1 (en) 2005-09-29 2007-04-12 Wyeth 1- (1h- indol- 1-yl) -3- (methylamino) -1- phenylpropan-2-ol derivatives and related compounds as modulators of the monoamine reuptake for the treatment of vasomotor symptoms (vms)
EP2298770A1 (en) 2005-11-03 2011-03-23 ChemBridge Corporation Heterocyclic compounds as TrkA modulators
EP1954283A2 (en) 2005-11-04 2008-08-13 Hydra Biosciences, Inc. Compounds for modulating trpv3 function
US20090156611A1 (en) 2005-11-11 2009-06-18 Licentia Ltd. Mammalian hedgehog signaling modulators
WO2007059157A1 (en) 2005-11-14 2007-05-24 Genentech, Inc. Bisamide inhibitors of hedgehog signaling
ES2436877T3 (es) 2005-11-17 2014-01-07 OSI Pharmaceuticals, LLC Intermedios para la preparación de inhibidores de mTOR bicíclicos condensados
CA2629192A1 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Indole orexin receptor antagonists
US20070265231A1 (en) 2005-11-30 2007-11-15 Michael Hofmann Hydrazide Compounds for Combating Animal Pests
US20090221488A1 (en) 2005-12-08 2009-09-03 Wood Kenneth W Certain Compositions and Methods of Treatment
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
US20080299113A1 (en) 2005-12-19 2008-12-04 Arnold Lee D Combined treatment with and composition of 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitor and anti-cancer agents
TW200811185A (en) 2005-12-22 2008-03-01 Prolexys Pharmaceuticals Inc Fused pyrimidones and thiopyrimidones, and uses thereof
WO2007076055A2 (en) 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
TW200801008A (en) 2005-12-29 2008-01-01 Abbott Lab Protein kinase inhibitors
AR059197A1 (es) 2006-01-25 2008-03-19 Smithkline Beecham Corp Derivados de indazolo piridina para el tratamiento de hiv
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
MX2008011220A (es) 2006-03-07 2008-09-11 Array Biopharma Inc Compuestos de pirazol heterobiciclicos y metodos de uso.
TW200800997A (en) 2006-03-22 2008-01-01 Astrazeneca Ab Chemical compounds
HRP20160990T1 (hr) 2006-03-24 2016-10-07 Biogen Hemophilia Inc. Pc5 kao enzim obrade faktor ix propeptida
EP2007373A4 (en) 2006-03-29 2012-12-19 Foldrx Pharmaceuticals Inc INHIBITION OF ALPHA SYNUCLEINE TOXICITY
EA200870409A1 (ru) 2006-04-04 2009-04-28 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Антагонисты киназы pi3
EP2007736A1 (en) 2006-04-05 2008-12-31 AstraZeneca AB Substituted quinazolines with anti-cancer activity
JP2009532450A (ja) 2006-04-05 2009-09-10 アストラゼネカ アクチボラグ 化合物
RU2008144805A (ru) 2006-04-14 2010-05-20 Новартис АГ (CH) Применение биарилкарбоксамидов в лечении заболеваний, связанных с hedgehog-путем
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
CN101421253A (zh) 2006-04-18 2009-04-29 阿斯利康(瑞典)有限公司 喹唑啉-4-酮衍生物、其制备方法及含有它们的药用组合物
EP2016070B1 (en) * 2006-04-20 2016-01-13 Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
ATE549337T1 (de) 2006-04-21 2012-03-15 Novartis Ag Purinderivate zur verwendung als adenosin-a2a- rezeptoragonisten
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
US20090082370A1 (en) 2006-04-25 2009-03-26 Neil Thomas Thompson Pharmaceutical Combinations of PK Inhibitors and Other Active Agents
WO2007125315A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
DE102006020327A1 (de) 2006-04-27 2007-12-27 Bayer Healthcare Ag Heterocyclisch substituierte, anellierte Pyrazol-Derivate und ihre Verwendung
UA93548C2 (uk) 2006-05-05 2011-02-25 Айерем Елелсі Сполуки та композиції як модулятори хеджхогівського сигнального шляху
KR100722686B1 (ko) 2006-05-09 2007-05-30 주식회사 비에스이 부가적인 백 챔버를 갖고 기판에 음향홀이 형성된 실리콘콘덴서 마이크로폰
US20090306126A1 (en) 2006-05-22 2009-12-10 Astrazeneca Ab Indole Derivatives
GB0610242D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
ES2358043T3 (es) 2006-05-24 2011-05-05 Guardant S.R.L. Anestésico local alcalinizado, en bolsa.
GB0610317D0 (en) 2006-05-24 2006-07-05 Medical Res Council Antiparasitic compounds and compositions
US20080004253A1 (en) 2006-06-30 2008-01-03 Bryan James Branstetter Thiazolopyrimidine modulators of TRPV1
AU2007275682B2 (en) 2006-07-20 2012-05-17 Amgen Inc. Substituted pyridone compounds and methods of use
WO2008013987A2 (en) 2006-07-27 2008-01-31 Prolexys Pharmaceuticals, Inc. N-alkyl substituted piperazinylmethylquinazolinones and azepanylmethylquinazolinones
EP2044222A4 (en) 2006-07-27 2010-03-03 HSPA1A AS A MARKER FOR SENSITIVITY AGAINST KSP HEMMER
RU2009106722A (ru) 2006-07-28 2010-09-10 Новартис АГ (CH) 2,4-замещенные хиназолины в качестве ингибиторов липидной киназы
EP2061764B1 (en) 2006-08-22 2014-07-02 Technion Research & Development Foundation LTD. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
JP2010501593A (ja) 2006-08-24 2010-01-21 セレネックス， インコーポレイテッド イソキノリン、キナゾリンおよびフタラジン誘導体
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
US7956064B2 (en) 2006-09-01 2011-06-07 Cylene Pharmaceuticals, Inc. Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
US8492405B2 (en) 2006-10-18 2013-07-23 Takeda Pharmaceutical Company Limited Glucokinase-activating fused heterocyclic compounds and methods of treating diabetes and obesity
WO2008070357A2 (en) 2006-10-31 2008-06-12 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services Smoothened polypeptides and methods of use
RU2333211C1 (ru) 2006-11-01 2008-09-10 Институт физиологически активных веществ Российской Академии наук N,n`-замещенные 3, 7-диазабицикло[3.3.1]нонаны, обладающие фармакологической активностью, фармацевтические композиции на их основе и способ их применения
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JP5313909B2 (ja) 2006-11-13 2013-10-09 アイコス コーポレイション 炎症性疾患および癌の処置のためのチエノピリミジノン
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
KR20090080530A (ko) 2006-11-20 2009-07-24 노파르티스 아게 2-메틸-2-[4-(3-메틸-2-옥소-8-퀴놀린-3-일-2,3-디히드로-이미다조[4,5-ｃ]퀴놀린-1-일)-페닐]-프로피오니트릴의 염 및 결정 형태
MX2009005264A (es) 2006-12-06 2009-05-28 Boehringer Ingelheim Int Mimeticos de glucocorticoides, metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos.
EP2103619A4 (en) 2006-12-14 2011-11-23 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOLDERIVATE
CA2672940A1 (en) 2006-12-20 2008-07-10 Schering Corporation Novel jnk inhibitors
ES2385759T3 (es) 2006-12-22 2012-07-31 Industrial Research Limited Análogos azetidina de inhibidores de nucleosidasa y fosforilasa
TWI433674B (zh) 2006-12-28 2014-04-11 Infinity Discovery Inc 環杷明（ｃｙｃｌｏｐａｍｉｎｅ）類似物類
US8389544B2 (en) 2007-01-17 2013-03-05 The Hong Kong University Of Science And Technology Isoquinolone compounds as subtype-selective agonists for melatonin receptors MT1 and MT2
WO2008091555A2 (en) 2007-01-22 2008-07-31 Gtx, Inc. Nuclear receptor binding agents
US20130116277A1 (en) 2007-01-22 2013-05-09 James T. Dalton Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors
MX2009007944A (es) 2007-01-26 2009-08-07 Irm Llc Compuestos y composiciones de purina como inhibidores de quinasa para el tratamiento de enfermedades relacionadas con plasmodium.
CL2008000252A1 (es) 2007-01-29 2008-03-14 Xenon Pharmaceuticals Inc Compuestos derivados de quinazolinona o pirimidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades mediadas por los canales de calcio, tales como dolor, depresion, enfermedades cardiovasculares, respir
JP2010520310A (ja) 2007-03-07 2010-06-10 インフィニティ・ディスカバリー・インコーポレイテッド シクロパミンラクタム類似体及びその使用方法
WO2008109184A1 (en) 2007-03-07 2008-09-12 Infinity Pharmaceuticals, Inc. Heterocyclic cyclopamine analogs and methods of use thereof
CN101686952A (zh) 2007-03-12 2010-03-31 Vm生物医药公司 新型钙离子通道调节剂
KR20090130051A (ko) 2007-03-14 2009-12-17 엑셀리시스, 인코포레이티드 헤지호그 경로의 억제제
EP2137162B1 (en) 2007-03-15 2018-08-01 Novartis AG Organic compounds and their uses
RS54706B1 (sr) 2007-03-23 2016-08-31 Amgen Inc. Heterociklična jedinjenja i njihove upotrebe
MX2009010050A (es) 2007-03-23 2009-10-12 Amgen Inc Derivados de quinolina o quinoxalina 3-sustituidos y su uso como inhibidores de fosfotidilinositol 3-cinasa (p13k).
AU2008231384B2 (en) 2007-03-23 2011-09-15 Amgen Inc. Heterocyclic compounds and their use
US7867983B2 (en) 2007-03-29 2011-01-11 The University Of Connecticut Methods to protect skeletal muscle against injury
EP1977765A1 (en) 2007-04-03 2008-10-08 Diatos Peptide prodrugs
CN101636397B (zh) 2007-04-13 2012-06-13 中国人民解放军军事医学科学院毒物药物研究所 脲类化合物、其制备方法及其医药用途
KR20100015546A (ko) 2007-04-13 2010-02-12 사노피-아벤티스 Ｎ-아미노인돌의 전이 금속 촉매된 합성
US20090054517A1 (en) 2007-04-20 2009-02-26 Lubahn Dennis B Phytoestrogens As Regulators Of Hedgehog Signaling And Methods Of Their Use In Cancer Treatment
JP2010163361A (ja) 2007-04-27 2010-07-29 Dainippon Sumitomo Pharma Co Ltd キノリン誘導体
CA2685753A1 (en) 2007-05-09 2008-11-20 Neuromed Pharmaceuticals Ltd. Bicyclic pyrimidine derivatives as calcium channel blockers
US7960353B2 (en) 2007-05-10 2011-06-14 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
EA200901546A1 (ru) 2007-05-17 2010-04-30 Кортекс Фармасеутикалс, Инк. Дизамещенные амиды для усиления глутаматергических синаптических ответов
WO2008147852A1 (en) 2007-05-22 2008-12-04 Taigen Biotechnology Co., Ltd. Kinesin inhibitors
EP2148678A4 (en) 2007-05-23 2010-08-04 Siga Technologies Inc ANTIVIRAL DRUGS FOR THE TREATMENT AND PREVENTION OF DENGUE INFECTION
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
CN101801937A (zh) 2007-06-22 2010-08-11 艾科尔公司 喹唑啉酮化合物及其使用方法
US20110217300A1 (en) 2007-06-22 2011-09-08 Arqule, Inc. Quinazolinone Compounds and Methods of Use Thereof
CN104383553A (zh) 2007-06-25 2015-03-04 恩多塞特公司 含有亲水性间隔区接头的共轭物
WO2009002553A1 (en) 2007-06-25 2008-12-31 Prolexys Pharmaceuticals, Inc. Methods of treating multiple myeloma and resistant cancers
AU2008267443A1 (en) 2007-06-26 2008-12-31 Sanofi-Aventis A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
EP2170274A1 (en) 2007-07-02 2010-04-07 Technion Research and Development Foundation, Ltd. Compositions, articles and methods comprising tspo ligands for preventing or reducing tobacco-associated damage
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
RU2010106878A (ru) 2007-07-31 2011-09-10 Шеринг Корпорейшн (US) Комбинация антимитотического агента и ингибитора аврора киназы как средство для лечения рака
WO2009018811A1 (de) 2007-08-06 2009-02-12 Schebo Biotech Ag Neue pharmazeutika, verfahren zu ihrer herstellung und ihre verwendung in der medizinischen therapie
WO2009021163A2 (en) 2007-08-08 2009-02-12 University Of Rochester Enhancing gene transfer
EP2190466A4 (en) 2007-08-10 2011-12-21 Burnham Inst Medical Research Tissue-specific alkaline phosphatase (TNAP) activators and their use
MX2010001784A (es) 2007-08-13 2010-03-15 Metabasis Therapeutics Inc Activadores novedosos de la glucocinasa.
WO2009029617A1 (en) 2007-08-27 2009-03-05 Kalypsys, Inc. Diarylamine-substituted quinolones useful as inducible nitric oxide synthase inhibitors
CN104586832B (zh) 2007-09-10 2018-02-16 北京强新生物科技有限公司 用于癌症治疗的组合物和方法
WO2009044707A1 (ja) 2007-10-03 2009-04-09 Riken ニトロトリアゾール誘導体、およびそれを用いる化合物の製造方法
KR20100089082A (ko) 2007-10-15 2010-08-11 아스트라제네카 아베 조합 059
GEP20125635B (en) 2007-11-13 2012-09-10 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
CA2705405A1 (en) 2007-11-22 2009-05-28 Boehringer Ingelheim International Gmbh New compounds
WO2009078981A2 (en) 2007-12-13 2009-06-25 Sri International Ppar-delta ligands and methods of their use
EP2070932A1 (en) 2007-12-13 2009-06-17 4Sc Ag Pyrazolotriazines
CA2709203A1 (en) 2007-12-13 2009-06-18 Siena Biotech S.P.A. Hedgehog pathway antagonists and therapeutic applications thereof
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2231641B1 (en) 2007-12-21 2016-06-01 UCB Biopharma SPRL Quinoxaline and quinoline derivatives as kinase inhibitors
US7960397B2 (en) 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
US7894450B2 (en) 2007-12-31 2011-02-22 Nortel Network, Ltd. Implementation of VPNs over a link state protocol controlled ethernet network
CA2711558C (en) 2008-01-04 2016-12-13 Intellikine, Inc. Phosphatidyl inositol-3 kinase inhibiting compounds
AU2009204084A1 (en) 2008-01-09 2009-07-16 Trovis Pharmaceuticals Llc Intrathecal treatment of neuropathic pain with A2AR agonists
KR20100103455A (ko) 2008-01-10 2010-09-27 아사히 가라스 가부시키가이샤 유리, 발광 장치용 피복재 및 발광 장치
NZ586399A (en) 2008-01-24 2011-12-22 Ucb Pharma Sa Compounds comprising a cyclobutoxy group
CA2710929A1 (en) 2008-01-28 2009-08-06 Schering Corporation Imidazopyrazines as protein kinase inhibitors
US20110098267A1 (en) 2008-02-07 2011-04-28 Synta Pharmaceuticals Corporation Topical formulations for the treatment of psoriasis
KR20100117105A (ko) 2008-02-07 2010-11-02 질레드 팔로 알토 인코포레이티드 Ａｂｃａ-1 상승 화합물 및 이의 용도
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
WO2009114826A2 (en) 2008-03-13 2009-09-17 Angiodynamics, Inc. Treatment systems and methods for renal-related diseases
CN101531638B (zh) 2008-03-13 2011-12-28 中国科学院广州生物医药与健康研究院 用作雌激素相关受体调节剂的化合物及其应用
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン， エルエルシー キナーゼ阻害剤および使用方法
JP2011515401A (ja) 2008-03-20 2011-05-19 アムジエン・インコーポレーテツド オーロラキナーゼモジュレーターおよび使用方法
AU2009228765B2 (en) 2008-03-24 2012-05-31 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
RU2506267C2 (ru) * 2008-03-31 2014-02-10 Дженентек, Инк. Бензопирановые и бензоксепиновые ингибиторы рi3k и их применение
GB0808282D0 (en) 2008-05-07 2008-06-11 Medical Res Council Compounds for use in stabilizing p53 mutants
US8148408B2 (en) 2008-05-09 2012-04-03 Abbott Laboratories Selective substituted pyridine ligands for neuronal nicotinic receptors
US8158624B2 (en) 2008-05-30 2012-04-17 Genetech, Inc. Purine PI3K inhibitor compounds and methods of use
KR20110040818A (ko) 2008-06-10 2011-04-20 노파르티스 아게 상피 나트륨 채널 차단제로서의 피라진 유도체
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
AU2009268611B2 (en) 2008-07-08 2015-04-09 Intellikine, Llc Kinase inhibitors and methods of use
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
UY31984A (es) 2008-07-16 2010-02-26 Boehringer Ingelheim Int DERIVADOS DE 1-(3,4-difluorobencil)-6-oxo-1,6-dihidropirimidin-5-carboxamidas N-sustituidas y de 2-(3,4-difluorobencil)-3-oxo-2,3-dihidro-1H-pirazol-4-carboxamidas N-sustituidas.
US20110118286A1 (en) 2008-07-16 2011-05-19 Santhosh Francis Neelamkavil Bicyclic heterocycle derivatives and their use as gpcr modulators
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
AU2009282480B2 (en) 2008-08-11 2015-05-07 Children's Medical Center Corporation Halofuginone analogs for inhibition of tRNA synthetases and uses thereof
US20100099871A1 (en) 2008-08-15 2010-04-22 Miller Dwight W Anti-psychotic compounds and pharmaceutical compositions thereof
CA2738313A1 (en) 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン， エルエルシー 複素環キナーゼ阻害剤
WO2010051391A1 (en) 2008-10-31 2010-05-06 Facet Biotech Corporation Use of anti-cs1 antibodies for treatment of rare lymphomas
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
WO2010056758A1 (en) 2008-11-12 2010-05-20 Yangbo Feng Quinazoline derivatives as kinase inhibitors
US20110269779A1 (en) 2008-11-18 2011-11-03 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
EP2365810A2 (en) 2008-12-04 2011-09-21 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Phosphatidylinositol-3-kinase p110 delta-targeted drugs in the treatment of cns disorders
CN106336400A (zh) 2008-12-08 2017-01-18 萌蒂制药国际有限公司 酪氨酸激酶蛋白受体拮抗剂
DK2379525T3 (en) 2008-12-19 2015-10-19 Boehringer Ingelheim Int Cyclic pyrimidin-4-carboxamides, as CCR2 receptor antagonists for the treatment of inflammation, asthma and COPD
WO2010083218A1 (en) 2009-01-13 2010-07-22 Van Andel Research Institute Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids
EP2396315B1 (en) 2009-02-13 2016-08-31 UCB Biopharma SPRL Quinoline derivatives as pi3k kinase inhibitors
US8569316B2 (en) 2009-02-17 2013-10-29 Boehringer Ingelheim International Gmbh Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases
US9341627B2 (en) 2009-02-20 2016-05-17 Sunyoung Kim Protein structural biomarkers to guide targeted chemotherapies
US8591943B2 (en) 2009-04-09 2013-11-26 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors
WO2010127208A1 (en) 2009-04-30 2010-11-04 Forest Laboratories Holdings Limited Inhibitors of acetyl-coa carboxylase
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
GB0908957D0 (en) 2009-05-22 2009-07-01 Ucb Pharma Sa Therapeutic agents
EP2451811A1 (en) 2009-05-27 2012-05-16 F. Hoffmann-La Roche AG Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
SG175708A1 (en) 2009-05-27 2011-12-29 Genentech Inc Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
EP2438041A4 (en) 2009-06-01 2012-11-21 Merck Sharp & Dohme PYRAZINE-carboxamide-orexin receptor Antagonist
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
CN101602768B (zh) 2009-07-17 2012-05-30 河南省农科院农副产品加工研究所 一种芝麻素和芝麻林素的提纯方法
EP2286808A1 (en) 2009-08-18 2011-02-23 Rheinische Friedrich-Wilhelms Universität Cytohesin inhibitors
TWI481601B (zh) 2009-08-21 2015-04-21 Otsuka Pharma Co Ltd 含氮化合物及藥學組成物
CA2770475C (en) 2009-08-27 2017-06-27 Merck Sharp & Dohme Corp. Novel pyrrolidine derived beta 3 adrenergic receptor agonists
US20130005802A1 (en) 2009-09-21 2013-01-03 Wei Chen Treatment of wnt/frizzled-related diseases
WO2011038163A1 (en) 2009-09-23 2011-03-31 Medivation Technologies, Inc. Pyrido[3,4-b]indoles and methods of use
NZ599342A (en) 2009-09-25 2014-04-30 Vertex Pharma Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
CN102741253A (zh) 2009-09-29 2012-10-17 艾科睿控股公司 PI3K(δ)选择性抑制剂
US8106146B2 (en) 2009-10-06 2012-01-31 Medtronic, Inc. Therapeutic polymers and methods of generation
US9095596B2 (en) 2009-10-15 2015-08-04 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
GB0918249D0 (en) 2009-10-19 2009-12-02 Respivert Ltd Compounds
EP2947073B1 (en) 2009-10-22 2019-04-03 Fibrotech Therapeutics Pty Ltd Fused ring analogues of anti-fibrotic agents
WO2011058109A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors
EP2499144B1 (en) 2009-11-12 2013-10-23 UCB Pharma, S.A. Quinoline and quinoxaline derivatives as kinase inhibitors
ES2520345T3 (es) 2009-11-12 2014-11-11 Ucb Pharma, S.A. Derivados de quinolina y quinoxalina en calidad de inhibidores de quinasa
MX2012006953A (es) 2009-12-18 2012-10-09 Amgen Inc Compuestos heterociclicos y sus usos.
EP3309152B1 (en) 2009-12-22 2020-09-09 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
DE102010013716A1 (de) 2010-03-31 2011-10-06 Rheinische Friedrich-Wilhelms-Universität Bonn Körperschaft des öffentlichen Rechts Verwendung von Cytohesin-Inhibitoren
AU2011239537A1 (en) * 2010-04-16 2012-11-15 Curis, Inc. Treatment of cancers having K-ras mutations
EP3699915A1 (en) 2010-04-29 2020-08-26 The Regents of The University of California Pathway recognition algorithm using data integration on genomic models (paradigm)
AU2011255218B2 (en) * 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
WO2011150201A2 (en) 2010-05-27 2011-12-01 Ambit Biosciences Corporation Azolyl amide compounds and methods of use thereof
WO2012009097A1 (en) 2010-06-17 2012-01-19 Cytokinetics, Inc. Methods of treating lung disease
RU2013114710A (ru) 2010-09-03 2014-10-10 Байер Интеллектуэль Проперти Гмбх Замещенные конденсированные пиримидиноны и дигидропиримидиноны
AR082799A1 (es) 2010-09-08 2013-01-09 Ucb Pharma Sa Derivados de quinolina y quinoxalina como inhibidores de quinasa
WO2012037204A1 (en) 2010-09-14 2012-03-22 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
EP2619209A1 (en) 2010-09-24 2013-07-31 Gilead Calistoga LLC Atropisomers of pi3k-inhibiting compounds
WO2012054332A1 (en) 2010-10-18 2012-04-26 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
UY33337A (es) 2010-10-18 2011-10-31 Respivert Ltd DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS
WO2012061696A1 (en) 2010-11-04 2012-05-10 Amgen Inc. 5 -cyano-4, 6 -diaminopyrimidine or 6 -aminopurine derivatives as pi3k- delta inhibitors
JP2013545749A (ja) 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環化合物及びその使用
WO2012065057A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
WO2012065019A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
CA2820362C (en) 2010-12-08 2020-03-24 The United States Of America, As Represented By The Secretary, Departmt Of Health And Human Services Substituted pyrazolopyrimidines as glucocerebrosidase activators
GB201021104D0 (en) 2010-12-13 2011-01-26 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
AU2012205669B2 (en) 2011-01-10 2015-08-20 Infinity Pharmaceuticals Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
JP2012184225A (ja) 2011-02-18 2012-09-27 Otsuka Pharmaceut Co Ltd 医薬組成物
CN103443105A (zh) 2011-02-18 2013-12-11 沃泰克斯药物股份有限公司 作为离子通道调节剂的苯并二氢吡喃-螺环哌啶酰胺
EP2678342B1 (en) 2011-02-25 2015-01-07 Takeda Pharmaceutical Company Limited N-substituted oxazinopteridines and oxazinopteridinones
JP5569437B2 (ja) 2011-03-09 2014-08-13 コニカミノルタ株式会社 光学フィルム及びそれを用いた偏光板、液晶表示装置
WO2012143796A2 (en) 2011-04-21 2012-10-26 Institut Pasteur Korea Anti-inflammation compounds
AU2012253653A1 (en) 2011-05-10 2013-05-02 Gilead Sciences, Inc. Fused heterocyclic compounds as sodium channel modulators
JP2013010734A (ja) 2011-06-03 2013-01-17 Sumitomo Chemical Co Ltd Ｎ−置換ラクタム化合物の製造方法
US9845327B2 (en) 2011-06-22 2017-12-19 The General Hospital Corporation Treatment of proteinopathies
US8716297B2 (en) 2011-07-15 2014-05-06 Abbvie Inc. Chemical entities to be used for Wee1 inhibition for the treatment of cancer
JP6027610B2 (ja) 2011-07-19 2016-11-16 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環式化合物及びその使用
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP2751093A1 (en) 2011-08-29 2014-07-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
SG11201401082XA (en) 2011-09-30 2014-04-28 Kineta Inc Anti-viral compounds
JP2015027951A (ja) 2011-11-02 2015-02-12 日本農薬株式会社 フタルアミド誘導体及び該誘導体を含有する農園芸用殺虫剤並びにその使用方法
JP6189874B2 (ja) 2012-03-13 2017-08-30 レスピバート・リミテツド 新規製薬学的製剤
KR101781922B1 (ko) 2012-04-10 2017-09-26 안지 파마슈티컬 코퍼레이션 리미티드 히스톤 탈아세틸효소(hdacs) 억제제
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2013188432A2 (en) 2012-06-11 2013-12-19 New York University Asymmetric catalysts
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
IN2015MN00405A (enExample) 2012-08-30 2015-09-04 Univ Tokyo
US20140120060A1 (en) 2012-11-01 2014-05-01 Infinity Pharmaceuticals, Inc. Treatment of rheumatoid arthritis and asthma using pi3 kinase inhibitors
US20140120083A1 (en) 2012-11-01 2014-05-01 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
WO2014110114A1 (en) 2013-01-10 2014-07-17 Nimbus Iris, Inc. Irak inhibitors and uses thereof
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
AU2014324873B2 (en) 2013-09-25 2018-11-08 Vertex Pharmaceuticals Incorporated A selective inhibitor of phosphatidylinositol 3-kinase-gamma
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20160685A1 (es) 2013-10-04 2016-07-23 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090312319A1 (en) * 2008-01-04 2009-12-17 Intellikine Certain chemical entities, compositions and methods

Also Published As

Publication number Publication date
CA2870087C (en) 2021-02-02
JP6309505B2 (ja) 2018-04-11
HK1207069A1 (en) 2016-01-22
EP2836487A1 (en) 2015-02-18
WO2013154878A1 (en) 2013-10-17
US20130267521A1 (en) 2013-10-10
CA2870087A1 (en) 2013-10-17
US20150105385A1 (en) 2015-04-16
JP2015512940A (ja) 2015-04-30
EP2836487B1 (en) 2018-10-31
CN104703979A (zh) 2015-06-10
US8940742B2 (en) 2015-01-27
US20160207940A1 (en) 2016-07-21
AU2013205238A1 (en) 2013-10-24
US9255108B2 (en) 2016-02-09
AU2013205238B2 (en) 2015-12-10

Similar Documents

Publication Publication Date Title
JP6309505B2 (ja) 複素環式化合物及びその使用
JP6027610B2 (ja) 複素環式化合物及びその使用
TWI565709B (zh) 雜環化合物及其用途
JP6029668B2 (ja) 複素環式化合物及びその使用
TWI657085B (zh) 雜環化合物及其用途
US9751888B2 (en) Heterocyclic compounds and uses thereof
CN103298474A (zh) 杂环化合物及其用途
TW201700475A (zh) 製備異喹啉酮之方法及異喹啉酮之固體形式
CN109912599A (zh) 化学实体、组合物和方法

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
CB03 Change of inventor or designer information

Inventor after: Alfredo C. Castro

Inventor after: Snyder Daniel A.

Inventor after: Martin R Tremblay

Inventor after: K.Chang

Inventor after: Evans Catherine A.

Inventor after: S Ghana Da Nannaier

Inventor after: A Lay Eivind Skabo

Inventor after: Li Liansheng

Inventor after: Liu Tao

Inventor after: Liu Yi

Inventor after: Ren Pingda

Inventor before: Alfredo C. Castro

Inventor before: Snyder Daniel A.

Inventor before: Martin R Tremblay

Inventor before: K.Chang

Inventor before: Evans Catherine A.

Inventor before: S Ghana Da Nannaier

Inventor before: A Lay Eivind Skabo

Inventor before: Raw Lee of beam

Inventor before: Liu Tao

Inventor before: Liu Yi

Inventor before: Ren Pingda

COR Change of bibliographic data
GR01 Patent grant
GR01 Patent grant
TR01 Transfer of patent right

Effective date of registration: 20251023

Address after: New York State, USA

Patentee after: Tver Treatment Co.

Country or region after: U.S.A.

Address before: Massachusetts, USA

Patentee before: INFINITY PHARMACEUTICALS, Inc.

Country or region before: U.S.A.

TR01 Transfer of patent right