AU2013205238B2 - Heterocyclic compounds and uses thereof - Google Patents

Heterocyclic compounds and uses thereof Download PDF

Info

Publication number
AU2013205238B2
AU2013205238B2 AU2013205238A AU2013205238A AU2013205238B2 AU 2013205238 B2 AU2013205238 B2 AU 2013205238B2 AU 2013205238 A AU2013205238 A AU 2013205238A AU 2013205238 A AU2013205238 A AU 2013205238A AU 2013205238 B2 AU2013205238 B2 AU 2013205238B2
Authority
AU
Australia
Prior art keywords
compound
alkyl
substituted
heteroaryl
aryl
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
AU2013205238A
Other languages
English (en)
Other versions
AU2013205238A1 (en
Inventor
Alfredo C. Castro
Katrina Chan
Catherine A. Evans
Somarajannair Janardanannair
Andre Lescarbeau
Liansheng Li
Tao Liu
Yi Liu
Pingda Ren
Daniel A. Snyder
Martin R. Tremblay
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.)
Infinity Pharmaceuticals Inc
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
Assigned to INFINITY PHARMACEUTICALS INC. reassignment INFINITY PHARMACEUTICALS INC. Request for Assignment Assignors: INFINITY PHARMACEUTICALS, INC., INTELLIKINE LLC
Publication of AU2013205238A1 publication Critical patent/AU2013205238A1/en
Application granted granted Critical
Publication of AU2013205238B2 publication Critical patent/AU2013205238B2/en
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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
AU2013205238A 2012-04-10 2013-04-03 Heterocyclic compounds and uses thereof Active AU2013205238B2 (en)

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
AU2013205238A1 AU2013205238A1 (en) 2013-10-24
AU2013205238B2 true AU2013205238B2 (en) 2015-12-10

Family

ID=48142967

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013205238A Active AU2013205238B2 (en) 2012-04-10 2013-04-03 Heterocyclic compounds and uses thereof

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 (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS55940B1 (sr) 2005-12-28 2017-09-29 Vertex Pharma Čvrsti oblici n-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksohinolin-3-karboksamida
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
CN104926815B (zh) 2008-01-04 2017-11-03 英特利凯恩有限责任公司 某些化学实体、组合物和方法
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
MX2014002542A (es) 2011-08-29 2014-07-09 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
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
FI4190786T3 (fi) 2012-12-07 2025-05-23 Vertex Pharma Atr-kinaasin estäjinä käyttökelpoisia yhdisteitä
KR101987631B1 (ko) * 2013-01-17 2019-06-12 제이엑스티지 에네루기 가부시키가이샤 냉동기유 및 냉동기용 작동 유체 조성물
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2970286A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
WO2014143242A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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
US20150044288A1 (en) 2013-07-31 2015-02-12 Windward Pharma, Inc. Aerosol tyrosine kinase inhibitor compounds and uses thereof
JP6466924B2 (ja) * 2013-10-04 2019-02-06 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
WO2015051241A1 (en) * 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
BR112016012794A2 (pt) 2013-12-05 2017-08-08 Acerta Pharma Bv Combinação terapêutica de um inibidor de pi3k e um inibidor de btk
EP3077397B1 (en) 2013-12-06 2019-09-18 Vertex Pharmaceuticals Inc. 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
BR112016017112A2 (pt) 2014-01-24 2017-08-08 Ai Therapeutics Inc Composições de apilimod e métodos de uso das mesmas
CN113620958A (zh) * 2014-03-19 2021-11-09 无限药品股份有限公司 用于治疗PI3K-γ介导的障碍的杂环化合物
UY36060A (es) 2014-04-02 2015-10-30 Bayer Pharma AG Compuestos de azol sustituidos con amida
HRP20200186T1 (hr) 2014-06-05 2020-05-29 Vertex Pharmaceuticals Inc. Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici
JP6936007B2 (ja) 2014-06-17 2021-09-15 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 Ｃｈｋ１阻害剤とａｔｒ阻害剤との組み合わせを使用してがんを処置する方法
EA201692557A1 (ru) 2014-07-04 2017-05-31 Люпин Лимитед Хинолизиноновые производные в качестве ингибиторов pi3k
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
PL3179992T3 (pl) 2014-08-11 2022-08-16 Acerta Pharma B.V. Kombinacje terapeutyczne inhibitora BTK, inhibitora PD-1 i/lub inhibitora PD-L1
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、及／或ｃｄｋ４／６抑制劑的治療組合物
HRP20211813T1 (hr) 2014-08-11 2022-03-04 Acerta Pharma B.V. Terapeutske kombinacije inhibitora btk i inhibitora bcl-2
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP3204358B1 (en) 2014-10-07 2018-09-19 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
PL3215158T3 (pl) 2014-11-07 2019-11-29 Ai Therapeutics Inc Apilimod do zastosowania do leczenia raka nerki
CN107206090A (zh) 2014-11-07 2017-09-26 拉姆医疗公司 阿匹莫德在结肠直肠癌治疗中的用途
AU2015357169B2 (en) 2014-12-03 2021-03-04 Janssen Pharmaceutica Nv Radiolabelled mGluR2 PET ligands
ES2727379T3 (es) 2014-12-03 2019-10-15 Janssen Pharmaceutica Nv Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona y su uso como moduladores alostéricos negativos de receptores de mGlu2
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
KR102787845B1 (ko) 2015-09-14 2025-03-31 트웰브 테라퓨틱스, 아이엔씨. 이소퀴놀리논의 고체형, 그의 제조 방법, 이를 포함하는 조성물 및 이를 사용하는 방법
EP3355926B1 (en) 2015-09-30 2025-12-24 Vertex Pharmaceuticals Inc. Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using
LT3371190T (lt) * 2015-11-06 2022-08-10 Incyte Corporation Heterocikliniai junginiai, kaip pi3k-gama inhibitoriai
AU2016374571B2 (en) 2015-12-18 2021-05-06 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
CA3003962A1 (en) 2015-12-18 2017-06-22 Janssen Pharmaceutica Nv Radiolabelled mglur2/3 pet ligands
CN109311868B (zh) 2015-12-22 2022-04-01 尚医治疗有限责任公司 用于治疗癌症和炎性疾病的化合物
ES2995198T3 (en) 2016-01-05 2025-02-07 Incyte Corp Pyridine compounds as pi3k-gamma inhibitors
EP3416947A1 (en) * 2016-02-15 2018-12-26 CeMM - Forschungszentrum für Molekulare Medizin GmbH Taf1 inhibitors for the therapy of cancer
US10759806B2 (en) 2016-03-17 2020-09-01 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
TW201803871A (zh) 2016-06-24 2018-02-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
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
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
BR112019027640A2 (pt) 2017-06-21 2020-07-07 SHY Therapeutics LLC composto, método para testar a capacidade de um ou mais compostos, método para inibir a função de ras, método para inibir a função de rho, método para inibir a função de rac, composição farmacêutica
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
KR102737185B1 (ko) 2018-01-20 2024-12-05 선샤인 레이크 파르마 컴퍼니 리미티드 치환된 아미노피리미딘 화합물 및 이의 사용 방법
CN111801098A (zh) 2018-02-21 2020-10-20 人工智能治疗公司 使用阿匹莫德和谷氨酸能剂的组合疗法
TWI827583B (zh) 2018-03-08 2024-01-01 美商英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之胺基吡嗪二醇化合物
WO2019228404A1 (zh) * 2018-05-31 2019-12-05 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
WO2020010003A1 (en) 2018-07-02 2020-01-09 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
US12391705B2 (en) 2018-12-19 2025-08-19 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
IL298760A (en) 2020-06-05 2023-02-01 Kinnate Biopharma Inc Fibroblast growth factor receptor kinase inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine 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
ES3035284T3 (en) 2020-07-02 2025-09-01 Incyte Corp Tricyclic urea compounds as jak2 v617f inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
KR20230159421A (ko) 2021-02-19 2023-11-21 수도 바이오사이언시즈 리미티드 Tyk2 억제제 및 이의 용도
MX2023009682A (es) 2021-02-19 2023-10-30 Sudo Biosciences Ltd Inhibidores de tyk2 y sus usos.
CA3211748A1 (en) 2021-02-25 2022-09-01 Incyte Corporation Spirocyclic lactams as jak2 v617f inhibitors
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
PE20251706A1 (es) 2022-03-17 2025-07-02 Incyte Corp Compuestos de urea triciclica como inhibidores de v617f de jak2
CN119301107A (zh) * 2022-04-25 2025-01-10 密歇根大学董事会 双重功能免疫调节化合物、其制剂及用途
WO2024163752A1 (en) * 2023-02-02 2024-08-08 Synnovation Therapeutics, Inc. HETEROCYCLIC COMPOUNDS AS PI3Kα INHIBITORS
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

Family Cites Families (666)

* 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
ES8702440A1 (es) 1984-10-04 1986-12-16 Monsanto Co Un procedimiento para la preparacion de una composicion de polipeptido inyectable sustancialmente no acuosa.
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
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
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
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule 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
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.
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5442039A (en) 1989-07-17 1995-08-15 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
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. Orally active adenosine kinase inhibitors
US5674998A (en) 1989-09-15 1997-10-07 Gensia Inc. C-4' modified adenosine kinase inhibitors
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active 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
DE4026265A1 (de) 1990-08-20 1992-02-27 Boehringer Mannheim Gmbh Neue phospholipid-derivate von nucleosiden, deren herstellung sowie deren verwendung als antivirale arzneimittel
US5563257A (en) 1990-08-20 1996-10-08 Boehringer Mannheim Gmbh Phospholipid derivatives of nucleosides
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
WO1992005177A1 (en) 1990-09-25 1992-04-02 Rhone-Poulenc Rorer International (Holdings) Inc. 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
CA2133075A1 (en) 1992-04-07 1993-10-14 Craig B. Thompson CD28 Pathway Immunoregulation
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
DE69333955D1 (de) 1992-04-24 2006-02-02 Stanford Res Inst Int Targeting homologer sequenzen in eukaryotenzellen
KR100271083B1 (ko) 1992-06-19 2000-11-01 데이비드 에스. 호이리스 열전 온도 안정화를 갖는 적외선 카메라(Infrared Camera with Thermoelectric Temperature Stabilization)
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
CA2154681A1 (en) 1993-02-03 1994-08-18 Mark David Erion Adenosine kinase inhibitors comprising lyxofuranosyl derivatives
GB9308957D0 (en) 1993-04-30 1993-06-16 Cancer Res Campaign Tech Novel produgs
JPH08511166A (ja) 1993-06-04 1996-11-26 アメリカ合衆国 Ｔ細胞の増殖を選択的に刺激する方法
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
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
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
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
ATE195123T1 (de) 1995-04-03 2000-08-15 Novartis Erfind Verwalt Gmbh Pyrazolderivate und verfahren zu deren herstellung
US6312894B1 (en) 1995-04-03 2001-11-06 Epoch Pharmaceuticals, Inc. Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders
PT821671E (pt) 1995-04-20 2001-04-30 Pfizer Derivados do acido arilsulfonil hidroxamico como inibidores de mmp e tnf
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
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
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
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
DE69617235T2 (de) 1995-06-07 2002-07-25 G.D. Searle & Co., Chicago Epoxysteroide aldosteronantagonist und angiotensin ii rezeptor antagonist kombinationstherapie zur behandlung von congestivem herzversagen
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
ATE216261T1 (de) 1995-06-07 2002-05-15 Searle & Co Kombinationstherapie zur behandlung des kongestiven herzversagens mit spironolacton und angiotensin ii-antagonist
AU5982296A (en) 1995-06-07 1996-12-30 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angi otensin ii antagonist and spironolactone
ATE268591T1 (de) 1995-06-27 2004-06-15 Takeda Chemical Industries Ltd Verfahren zur herstellung von zubereitungen mit verzögerter freisetzung
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
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. 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
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
US5763608A (en) 1996-02-05 1998-06-09 Hoechst Celanese Corporation Process for preparing pyrimidine derivatives
GB2310952B (en) 1996-03-05 1998-08-19 Mitsubishi Electric Corp Infrared detector
US5872136A (en) 1996-04-03 1999-02-16 Merck & Co., Inc. Arylheteroaryl inhibitors of farnesyl-protein transferase
AU706150B2 (en) 1996-04-03 1999-06-10 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
BR9711805A (pt) 1996-06-20 2002-01-15 Regents The Univesity Of Texas Compostos e métodos para providenciar preparações farmacologicamente ativas e uso dos mesmos
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
YU1899A (sh) 1996-07-18 2000-03-21 Pfizer Inc. Inhibitori matričnih metaloproteaza na bazi fosfinata
JP2000501423A (ja) 1996-08-23 2000-02-08 ファイザー インク． アリールスルホニルアミノヒドロキサム酸誘導体
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
US5965573A (en) 1996-10-23 1999-10-12 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
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
US5990169A (en) 1996-10-23 1999-11-23 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
US6153631A (en) 1996-10-23 2000-11-28 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
US5919808A (en) 1996-10-23 1999-07-06 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
ATE272394T1 (de) 1996-10-31 2004-08-15 Takeda Chemical Industries Ltd Zubereitung mit verzögerter freisetzung
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
AU7624798A (en) 1996-12-06 1998-06-29 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1 beta converting enzyme
AU7871298A (en) 1996-12-20 1998-07-17 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
EP0950059B1 (en) 1997-01-06 2004-08-04 Pfizer Inc. Cyclic sulfone derivatives
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
SK283963B6 (sk) 1997-02-03 2004-06-08 Pfizer Products Inc. Deriváty arylsulfonylaminohydroxamovej kyseliny, farmaceutický prostriedok, spôsob inhibície matričných metaloproteináz alebo produkcie faktora nekrózy nádorov
ATE271130T1 (de) 1997-02-07 2004-07-15 Univ Princeton Veränderte proteinkinasen, die modifizierte nukleotidtriphosphat substrate verwenden können
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
ID22809A (id) 1997-02-11 1999-12-09 Pfizer Turunan-turunan asam arilsulfonil hidroksamat
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
PT970084E (pt) 1997-03-19 2003-10-31 Abbott Gmbh & Co Kg Pirrolo¬2,3d|pirimidinas e sua utilizacao como inibidores da tirosina-cinase
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
AU9309898A (en) 1997-09-09 1999-03-29 Du Pont Pharmaceuticals Company Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor xa
US6340759B1 (en) 1997-10-02 2002-01-22 Eisai Co., Ltd. Fused pyridine derivatives
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
US6040321A (en) * 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
CA2309350C (en) 1997-11-12 2007-04-03 Mitsubishi Chemical Corporation Purine derivatives and medicaments comprising the same as active ingredient
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
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
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
DE69928414T2 (de) 1998-09-18 2006-08-03 Abbott Gmbh & Co. Kg 4-aminopyrrolopyrimidine als kinaseinhibitoren
PT1144411E (pt) 1998-12-19 2005-09-30 Janssen Pharmaceutica Nv Compostos espiro anti-histaminicos
AU779008C (en) 1999-01-11 2005-06-30 Princeton University High affinity inhibitors for target validation and uses thereof
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
WO2000075139A2 (en) 1999-06-03 2000-12-14 Basf Aktiengesellschaft Benzothiazinone and benzoxazinone compounds
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
DE19940859A1 (de) 1999-08-27 2001-03-01 Bayer Ag Selektive Herbizide auf Basis eines substituierten Phenylsulfonylaminocarbonyltriazolinons und Safenern
DE19940860A1 (de) 1999-08-27 2001-03-01 Bayer Ag Selektive Herbizide auf Basis eines substituierten Phenylsulfonyl aminocarbonyltriazolinons und Safenern II
US6559160B1 (en) 1999-08-27 2003-05-06 Chemocentryx, Inc. Compounds and methods for modulating cxcr3 function
US20070021493A1 (en) 1999-09-16 2007-01-25 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US20050080138A1 (en) 1999-09-16 2005-04-14 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US6545005B1 (en) 1999-09-16 2003-04-08 Curtis, 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
CA2385747A1 (en) 1999-09-17 2001-03-22 Gavin C. Hirst Pyrazolopyrimidines as therapeutic agents
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
JP5036112B2 (ja) 1999-10-06 2012-09-26 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド チロシンキナーゼのインヒビターとして有益な複素環化合物
CA2386190C (en) 1999-10-13 2009-04-14 Johns Hopkins University School Of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
IL148972A0 (en) 1999-10-14 2002-11-10 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
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US7230000B1 (en) 1999-10-27 2007-06-12 Cytokinetics, Incorporated 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
AU2001249399A1 (en) 2000-03-24 2001-10-08 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
US6683192B2 (en) 2000-03-30 2004-01-27 Curis, Inc. Small organic molecule regulators of cell proliferation
JP4808895B2 (ja) 2000-03-30 2011-11-02 キュリス，インコーポレイテッド 細胞増殖の小型有機分子レギュレーター
US20050070578A1 (en) 2000-03-30 2005-03-31 Baxter Anthony David Small organic molecule regulators of cell proliferation
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. 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
IL152275A0 (en) 2000-04-25 2003-05-29 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
EP1289472A4 (en) 2000-05-30 2004-09-08 Advanced Res & Tech Inst COMPOSITIONS AND METHODS FOR IDENTIFYING SUBSTANCES THAT MODULE THE PTEN FUNCTION AND THE PI-3 KINASE WAYS
RU2003101969A (ru) 2000-06-27 2004-07-10 Дженелэбс Текнолоджиз, Инк. (Us) Новые соединения, обладающие антибактериальной, противогрибковой и противоопухолевой активностью
US6534691B2 (en) 2000-07-18 2003-03-18 E. I. Du Pont De Nemours And Company Manufacturing process for α-olefins
DE60132606T2 (de) 2000-09-20 2009-02-19 Merck & Co., Inc. Isochinolinone als kalium-kanal-inhibitoren
CA2425663C (en) 2000-10-11 2009-12-29 Applera Corporation Fluorescent nucleobase conjugates having anionic linkers
EP1578341A2 (en) 2000-10-11 2005-09-28 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
EP1343505A1 (en) 2000-12-11 2003-09-17 Tularik Inc. Cxcr3 antagonists
HUP0302526A2 (hu) 2000-12-21 2003-11-28 Glaxo Group Limited Makrolid vegyületek, eljárás az előállításukra, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
RU2290403C2 (ru) 2000-12-28 2006-12-27 Дайити Фармасьютикал Ко., Лтд. Ингибиторы vla-4
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
EP1355916B1 (en) 2001-01-22 2007-01-10 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
DK1392814T3 (da) 2001-04-25 2007-09-24 Cornell Res Foundation Inc Indretninger og fremgangsmåder til farmakokinetisk baseret cellekultursystem
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
EP1397350B1 (en) 2001-05-08 2007-02-28 Kudos Pharmaceuticals Limited Isoquinolinone derivatives as parp inhibitors
US7144903B2 (en) 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
US6794379B2 (en) 2001-06-06 2004-09-21 Tularik Inc. CXCR3 antagonists
WO2002100852A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Benzothiophene compounds having antiinfective activity
JP2005505507A (ja) 2001-06-13 2005-02-24 ジーンソフト ファーマシューティカルズ インコーポレイテッド 抗感染活性を有するイソキノリン化合物
US20030236198A1 (en) 2001-06-13 2003-12-25 Genesoft, Inc. Antipathogenic benzamide compounds
US20030114467A1 (en) 2001-06-21 2003-06-19 Shakespeare William C. Novel pyrazolo- and pyrrolo-pyrimidines and uses thereof
US6689782B2 (en) 2001-07-16 2004-02-10 Essential Therapeutics, Inc. Fungal efflux pump inhibitors
US6596723B1 (en) 2001-07-16 2003-07-22 Essential Therapeutics, Inc. Fungal efflux pump inhibitors
US20030220338A1 (en) 2001-07-16 2003-11-27 Watkins Will J. Fungal efflux pump inhibitors
WO2003007888A2 (en) 2001-07-20 2003-01-30 Adipogenix, Inc. Fat accumulation-modulating compounds
MXPA04000803A (es) 2001-07-27 2004-05-21 Curis Inc Mediadores de rutas de senalizacion de hedgehog, composiciones y usos relacionados a los mismos.
DE60216115T2 (de) 2001-08-01 2007-05-31 Merck & Co., Inc. BENZIMIDAZO 4,5-föISOCHINOLINON-DERIVATE
WO2003020880A2 (en) 2001-08-03 2003-03-13 Abbott Laboratories Method of identifying inhibitors of lck
ES2572030T3 (es) 2001-08-10 2017-07-19 Shionogi & Co., Ltd. Agente antiviral
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
DE60236605D1 (de) 2001-09-05 2010-07-15 Minerva Biotechnologies Corp Zusammensetzungen und deren verwendung zur behandlung von krebs
WO2004043335A2 (en) 2001-09-13 2004-05-27 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
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
IL161662A0 (en) 2001-11-01 2004-09-27 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors)
WO2003043961A2 (en) 2001-11-19 2003-05-30 Iconix Pharmaceuticals, Inc. Modulators of rho c activity
AU2002346471A1 (en) 2001-11-20 2003-06-10 Cytokinetics, Inc. Process for the racemization of chiral quinazolinones
BR0214455A (pt) 2001-11-27 2004-11-03 Hoffmann La Roche Derivados benzotiazol
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
US7262187B2 (en) 2001-12-06 2007-08-28 Merck & Co., Inc. Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor
DE60231439D1 (de) 2001-12-06 2009-04-16 Merck & Co Inc Mitotische kinesinhemmer
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
ES2421511T3 (es) 2001-12-21 2013-09-03 X Ceptor Therapeutics Inc Moduladores de 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
CA2475879A1 (en) 2002-02-15 2003-08-28 Cytokinetics, Inc. Synthesis of quinazolinones
US20040043959A1 (en) 2002-03-04 2004-03-04 Bloom Laura A. Combination therapies for treating methylthioadenosine phosphorylase deficient cells
US20080070864A1 (en) 2002-03-07 2008-03-20 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
JP4663986B2 (ja) 2002-03-26 2011-04-06 ツェントファーム・ゲーエムベーハー フレデリカマイシン−誘導体
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
EP1513534A2 (en) 2002-04-04 2005-03-16 Cv Therapeutics, Inc. Compounds for increasing abca-1 expression useful for treating coronary artery disease and atherosclerosis
DE10217046A1 (de) 2002-04-17 2003-11-06 Bioleads Gmbh Fredericamycin-Derivate
ATE404200T1 (de) 2002-04-22 2008-08-15 Univ Johns Hopkins Med Modulatoren von hedgehog signalpfaden, zusammensetzungen und verwandte verwendungen
WO2003090751A1 (en) 2002-04-26 2003-11-06 Pfizer Products Inc. Pyrimidine-2, 4, 6-trione metallo-proteinase inhibitors
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
US7166595B2 (en) 2002-05-09 2007-01-23 Cytokinetics, Inc. Compounds, methods and compositions
WO2003097053A1 (en) 2002-05-09 2003-11-27 Cytokinetics, Inc. Compounds, compositions, and methods
TW200407143A (en) 2002-05-21 2004-05-16 Bristol Myers Squibb Co Pyrrolotriazinone compounds and their use to treat diseases
AU2003265242A1 (en) 2002-05-23 2003-12-22 Cytokinetics, Inc. Compounds, compositions, and methods
US20050203110A1 (en) 2002-05-23 2005-09-15 Coleman Paul J. Mitotic kinesin inhibitors
WO2003106426A1 (en) 2002-06-14 2003-12-24 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
PL215132B1 (pl) 2002-06-27 2013-10-31 Novo Nordisk As Pochodna arylokarbonylowa jako srodek terapeutyczny, jej zastosowanie i kompozycja farmaceutyczna ja zawierajaca
DE10230917A1 (de) 2002-07-09 2004-02-05 Bioleads Gmbh Fredericamycin-Derivate
AU2003255528B2 (en) * 2002-07-10 2009-07-16 Merck Serono Sa Azolidinone-vinyl fused-benzene derivatives
AU2003249244A1 (en) 2002-07-15 2004-02-02 Combinatorx, Incorporated Methods for the treatment of neoplasms
AU2003249532A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors
NZ538420A (en) 2002-08-16 2007-06-29 Kinacia Pty Ltd Inhibition of phosphoinositide 3-kinase beta
EP1539180A4 (en) 2002-08-21 2006-08-30 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
WO2004020599A2 (en) 2002-08-29 2004-03-11 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
EP1553947A4 (en) 2002-10-21 2006-11-29 Bristol Myers Squibb Co 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
US7265131B2 (en) 2002-12-20 2007-09-04 Exelixis, Inc. Isoquinolinone derivatives and their use as therapeutic 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
WO2004056746A1 (en) 2002-12-23 2004-07-08 4Sc Ag Cycloalkene dicarboxylic acid compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
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
CN1756735A (zh) 2003-03-06 2006-04-05 帝斯曼知识产权资产管理有限公司 α－氨羰基化合物的制备方法
AR050920A1 (es) 2003-03-07 2006-12-06 Astrazeneca Ab Enantiomeros de heterociclos fusionados seleccionados y usos de los mismos
JP4887139B2 (ja) 2003-03-25 2012-02-29 武田薬品工業株式会社 ジペプチジルペプチダーゼインヒビター
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
DE602004022819D1 (de) 2003-06-06 2009-10-08 Vertex Pharma Von atp-bindende kassette transportern
US20060270849A1 (en) 2003-06-18 2006-11-30 Shigeyoshi Nishino Process for producing 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
WO2005002585A1 (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
WO2005005421A1 (en) 2003-07-08 2005-01-20 Novartis Ag Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds
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
US20080118493A1 (en) 2003-07-15 2008-05-22 Beachy Philip A Elevated Hedgehog Pathway Activity In Digestive System Tumors, And Methods Of Treating Digestive Sytem Tumors Having Elevated Hedgehog Pathway Activity
GB0317951D0 (en) 2003-07-31 2003-09-03 Trigen Ltd Compounds
WO2005014534A1 (en) 2003-08-08 2005-02-17 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
WO2005016349A1 (en) 2003-08-14 2005-02-24 Icos Corporation Methods of inhibiting leukocyte accumulation
WO2005016528A2 (en) 2003-08-15 2005-02-24 Irm Llc 6-substituted anilino purines as rtk inhibitors
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
US20080095761A1 (en) 2003-10-01 2008-04-24 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
CA2545340A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
WO2005049613A1 (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)
WO2005047289A1 (en) 2003-11-17 2005-05-26 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
CN1886384A (zh) 2003-11-25 2006-12-27 希龙公司 喹唑酮化合物作为抗癌药剂
EP1689719A1 (en) 2003-11-25 2006-08-16 Eli Lilly And Company 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b)
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
AU2004308974A1 (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
CA2548326A1 (en) 2003-12-23 2005-07-14 Novartis Ag Bicyclic heterocyclic p-38 kinase inhibitors
WO2005061707A1 (ja) 2003-12-24 2005-07-07 Kyowa Hakko Kogyo Co., Ltd. 癌細胞のEg5阻害剤に対する感受性を判定する方法
WO2005067901A2 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
WO2005070457A1 (en) 2004-01-23 2005-08-04 Seattle Genetics, Inc. Melphalan prodrugs
JP2007520559A (ja) 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
AU2005212092B2 (en) 2004-02-13 2011-01-20 Msd K.K. Fused-ring 4-oxopyrimidine derivative
US9016221B2 (en) 2004-02-17 2015-04-28 University Of Florida Research Foundation, Inc. Surface topographies for non-toxic bioadhesion control
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
US20050187418A1 (en) 2004-02-19 2005-08-25 Small Brooke L. Olefin oligomerization
CN1980929A (zh) 2004-02-24 2007-06-13 比奥阿克松医疗技术股份有限公司 4－取代哌啶衍生物
US20070049593A1 (en) 2004-02-24 2007-03-01 Japan Tobacco Inc. Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
CA2557575A1 (en) 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Fused derivatives of pyrazole
MXPA06011423A (es) 2004-04-02 2007-01-23 Osi Pharm Inc Inhibidores de proteina cinasa heterobiciclica sustituida en el anillo 6,6-biciclico.
RU2006142305A (ru) 2004-04-30 2008-06-10 Такеда Фармасьютикал Компани Лимитед (Jp) Гетероциклическое амидное соединение и его применение в качестве ингибитора ммр-3
AU2005325267B2 (en) 2004-04-30 2010-11-04 Curis Inc. Quinoxaline inhibitors of the hedgehog signalling pathway
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
ES2605792T3 (es) 2004-05-13 2017-03-16 Icos Corporation Quinazolinona usada como inhibidor de la fosfatidilinositol 3-quinasa delta humana
CA2730540A1 (en) 2004-05-13 2005-12-01 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
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
JP2008501707A (ja) 2004-06-04 2008-01-24 アイコス、コーポレーション マスト細胞障害を処置するための方法
US20050282834A1 (en) 2004-06-09 2005-12-22 Fady Malik Compositions, devices and methods for treating cardiovascular disease
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
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
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
MX2007001953A (es) 2004-08-18 2007-05-09 Astrazeneca Ab Enantiomeros de pirimidonas fusionadas seleccionadas y usos en el tratamiento y prevencion del cancer.
EP2316832B1 (en) 2004-08-27 2017-03-08 Infinity Pharmaceuticals, Inc. Cyclopamine analogues and methods of use thereof
US20070207996A1 (en) 2004-08-30 2007-09-06 Auger Kurt R Novel Compositions And Methods Of Treatment
AU2005278959A1 (en) 2004-08-31 2006-03-09 Astrazeneca Ab Quinazolinone derivatives and their use as B-Raf inhibitors
EP1789390B1 (en) 2004-09-02 2011-11-09 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
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
RU2007119637A (ru) 2004-10-28 2008-12-10 Айрм Ллк (Bm) Соединения и композиции в качестве модуляторов hedgehog-пути
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
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
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
WO2006068760A2 (en) 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
EP1828195A2 (en) 2004-11-23 2007-09-05 PTC Therapeutics, Inc. Substituted phenols as active agents inhibiting vegf production
US20060156485A1 (en) 2005-01-14 2006-07-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CA2595130A1 (en) 2005-01-19 2006-07-27 Paul J. Coleman Mitotic kinesin inhibitors
US20090124641A1 (en) 2005-01-19 2009-05-14 Coleman Paul J Mitotic Kinesin Inhibitors
US20070161644A1 (en) 2005-01-25 2007-07-12 Stockwell Brent R Erastin analogs and uses thereof
US8518959B2 (en) 2005-01-25 2013-08-27 Prolexys Pharmaceuticals, Inc. Quinoxaline derivatives as antitumor agents
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
AU2006214190A1 (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
ES2369282T3 (es) 2005-03-25 2011-11-29 Tibotec Pharmaceuticals Inhibidores heterobicíclicos de vhc.
KR20070122194A (ko) 2005-03-25 2007-12-28 티보텍 파마슈티칼즈 리미티드 Ｈｃｖ의 헤테로비사이클릭 저해제
CN101184395A (zh) 2005-04-06 2008-05-21 Irm责任有限公司 包含二芳基胺的化合物和组合物及其作为类固醇激素核受体调节剂的用途
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
EP1879657A2 (en) 2005-04-25 2008-01-23 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Use of compounds to enhance processivity of telomerase
WO2006135479A2 (en) 2005-05-10 2006-12-21 Angiotech International Ag Anti-scarring agents, therapeutic compositions, and use thereof
US20090280153A1 (en) 2005-05-10 2009-11-12 Angiotech International Ag electrical devices, anti-scarring agents, and therapeutic compositions
WO2006121522A2 (en) 2005-05-10 2006-11-16 Angiotech International Ag Implantable sensors and pumps, anti-scarring agents, and therapeutic compositions
AU2006244027A1 (en) 2005-05-11 2006-11-16 Merck Sharp & Dohme Limited 2,3-substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilloid-1 receptor (VR1)
GB0509573D0 (en) 2005-05-11 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
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
JP5275794B2 (ja) 2005-06-22 2013-08-28 ケモセントリックス，インコーポレイティド アザインダゾール化合物および使用方法
US7799795B2 (en) 2005-06-27 2010-09-21 Amgen Inc. Aryl nitrile compounds and compositions and their uses in treating inflammatory and related disorders
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
WO2007006546A1 (en) 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
BRPI0615522A2 (pt) 2005-07-11 2012-04-10 Devgen Nv derivados da amida como inibidores da quinase
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
MX2008002385A (es) 2005-08-25 2008-03-18 Hoffmann La Roche Inhibidores de proteinas cinasas activads por mitogenos p38 y metodos para utilizarlos.
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
CN101296910A (zh) 2005-08-26 2008-10-29 梅特希尔基因公司 组蛋白脱乙酰酶的苯并二氮杂卓和苯并哌嗪类似物抑制剂
WO2007025534A1 (de) 2005-09-01 2007-03-08 Bioagency Ag Fredericamycin-derivate
AU2006297414A1 (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)
US8629147B2 (en) 2005-11-03 2014-01-14 Chembridge Corporation Heterocyclic compounds useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
WO2007056124A2 (en) 2005-11-04 2007-05-18 Hydra Biosciences, Inc. Compounds for modulating trpv3 function
WO2007054623A2 (en) 2005-11-11 2007-05-18 Licentia Oy Mammalian hedgehog signaling inhiabitors
DK1957461T3 (en) 2005-11-14 2016-12-19 Genentech Inc Bisamidhæmmere the hedgehog-signalling
DK1951724T3 (da) 2005-11-17 2011-08-15 Osi Pharmaceuticals Llc Sammensmeltede bicykliske mTOR-inhibitorer
US20090088452A1 (en) 2005-11-22 2009-04-02 Coleman Paul J Indole Orexin Receptor Antagonists
US20070265231A1 (en) 2005-11-30 2007-11-15 Michael Hofmann Hydrazide Compounds for Combating Animal Pests
EP1956908A2 (en) 2005-12-08 2008-08-20 Cytokinetics, Inc. Certain compositions and methods of treatment
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
EP1979002A2 (en) 2005-12-19 2008-10-15 OSI Pharmaceuticals, Inc. Combination of igfr inhibitor and anti-cancer agent
WO2007076085A2 (en) 2005-12-22 2007-07-05 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
ES2545907T3 (es) 2005-12-29 2015-09-16 Abbvie Inc. Inhibidores de proteína quinasa
PE20070946A1 (es) 2006-01-25 2007-10-16 Smithkline Beecham Corp COMPUESTOS DERIVADOS DE IMIDAZO[1,2-a]PIRIDINA COMO MODULADORES DEL RECEPTOR DE QUIMIOQUINA (CXCR4)
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
JP2009529047A (ja) 2006-03-07 2009-08-13 アレイ バイオファーマ、インコーポレイテッド ヘテロ二環系ピラゾール化合物およびその使用
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
EA200870385A1 (ru) 2006-03-29 2009-04-28 Фолдркс Фармасьютикалз, Инк. Ингибирование токсичности альфа-синуклеина
WO2008127226A2 (en) 2006-04-04 2008-10-23 The Regents Of The University Of California P13 kinase antagonists
JP2009532450A (ja) 2006-04-05 2009-09-10 アストラゼネカ アクチボラグ 化合物
CN101415689A (zh) 2006-04-05 2009-04-22 阿斯利康(瑞典)有限公司 具有抗癌活性的经取代的喹唑啉
BRPI0710723A2 (pt) 2006-04-14 2012-01-31 Novartis Ag uso de biarilcarboxamidas no tratamento de distúrbio relacionados à série de reação hedgehog
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
PE20080074A1 (es) * 2006-04-20 2008-02-11 Janssen Pharmaceutica Nv Derivados de amida como agentes inhibidores de la quinasa c-fms
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
HRP20120494T1 (hr) 2006-04-21 2012-08-31 Novartis Ag Derivati purina za uporabu kao agonista adenozin a2a receptora
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
EP2016077A2 (en) 2006-04-25 2009-01-21 Astex Therapeutics Limited Pharmaceutical compounds
WO2007125310A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
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
JP2009537621A (ja) 2006-05-22 2009-10-29 アストラゼネカ アクチボラグ インドール誘導体
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
JP2009544329A (ja) 2006-07-27 2009-12-17 スミスクライン・ビーチャム・コーポレイション ＫＳＰ阻害剤に対する感受性マーカーとしてのＨＳＰＡ１ａ
JP2009544664A (ja) 2006-07-28 2009-12-17 ノバルティス アクチエンゲゼルシャフト 脂質キナーゼ阻害剤としての２，４−置換キナゾリン
CA2661307C (en) 2006-08-22 2016-07-19 Technion Research And Development Foundation Ltd. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
WO2008024977A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Isoquinoline, quinazoline and phthalazine derivatives
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
EP2061765B1 (en) 2006-09-01 2014-10-22 Senhwa Biosciences, Inc. 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
EP2078036A2 (en) 2006-10-31 2009-07-15 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
CA2669399A1 (en) 2006-11-13 2008-05-29 Eli Lilly & Co. Thienopyrimidinones for treatment of inflammatory disorders and cancers
CN102993202A (zh) 2006-11-20 2013-03-27 诺瓦提斯公司 2-甲基-2-[4-(3-甲基-2-氧代-8-喹啉-3-基-2,3-二氢-咪唑并[4,5-c]喹啉-1-基)-苯基]-丙腈的盐和晶型
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
KR20090097908A (ko) 2006-12-06 2009-09-16 베링거 인겔하임 인터내셔날 게엠베하 글루코코르티코이드 모사물, 이의 제조 방법, 이의 약제학적 조성물 및 용도
AU2007332493A1 (en) 2006-12-14 2008-06-19 Daiichi Sankyo Company, Limited Imidazothiazole derivatives
JP5178738B2 (ja) 2006-12-20 2013-04-10 メルク・シャープ・アンド・ドーム・コーポレーション 新規なｊｎｋ阻害剤
KR20090101278A (ko) 2006-12-22 2009-09-24 인더스트리얼 리서치 리미티드 누클레오시다제 및 포스포릴라제 억제제의 아제티딘 유사체
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
US20130116277A1 (en) 2007-01-22 2013-05-09 James T. Dalton Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors
KR101763674B1 (ko) 2007-01-22 2017-08-01 지티엑스, 인코포레이티드 핵 수용체에 결합하는 물질
CN101622001A (zh) 2007-01-26 2010-01-06 Irm责任有限公司 作为激酶抑制剂用于治疗疟原虫相关疾病的嘌呤化合物和组合物
TW200836743A (en) 2007-01-29 2008-09-16 Xenon Pharmaceuticals Inc Quinazolinone and fused pyrimidinone compounds and their use in treating sodium channel-mediated diseases or conditions
KR20090117957A (ko) 2007-03-07 2009-11-16 인피니티 디스커버리, 인코포레이티드 헤테로시클릭 시클로파민 유사체 및 그의 사용 방법
US7964590B2 (en) 2007-03-07 2011-06-21 Infinity Discovery, Inc. Cyclopamine lactam analogs and methods of use thereof
US20090306625A1 (en) 2007-03-09 2009-12-10 Angiodynamics, Inc. Treatment systems and methods for renal-related diseases
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
EP2527330A1 (en) 2007-03-14 2012-11-28 Exelixis, Inc. Inhibitors of the hedgehog pathway
NZ579402A (en) 2007-03-15 2012-03-30 Novartis Ag Organic compounds for diagnosis and treatment of pathologies relating to the Hedgehog pathway
SI2139882T1 (sl) 2007-03-23 2014-03-31 Amgen Inc. 3-substituirani kinolinski ali kinoksalinski derivati in njihoba uporaba kot inhibitorji fosfatidilinozitol 3-kinaze (pi3k)
NZ579834A (en) 2007-03-23 2012-03-30 Amgen Inc Heterocyclic compounds as selective inhibitors of PI3K activity
CA2680783C (en) 2007-03-23 2012-04-24 Amgen Inc. Heterocyclic compounds and their uses
WO2008156513A2 (en) 2007-03-29 2008-12-24 University Of Connecticut Methods to protect skeletal muscle against injury
EP1977765A1 (en) 2007-04-03 2008-10-08 Diatos Peptide prodrugs
WO2008125014A1 (fr) 2007-04-13 2008-10-23 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. Composés d'urée, leurs procédés de préparation et leurs utilisations pharmaceutiques
MX2009010536A (es) 2007-04-13 2009-10-22 Sanofi Aventis Una sintesis de n-aminoindoles catalizada por un metal de transicion.
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
WO2008138126A1 (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
TW200911768A (en) 2007-05-17 2009-03-16 Cortex Pharma Inc Di-substituted amides for enhancing glutamatergic synaptic responses
TW200902016A (en) 2007-05-22 2009-01-16 Taigen Biotechnology Co Ltd Kinesin inhibitors
CN101743008A (zh) 2007-05-23 2010-06-16 西佳技术公司 用于治疗或预防登革热感染的抗病毒药
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
US20110217300A1 (en) 2007-06-22 2011-09-08 Arqule, Inc. Quinazolinone Compounds and Methods of Use Thereof
AU2008268613A1 (en) 2007-06-22 2008-12-31 Arqule, Inc. Quinazolinone compounds and methods of use thereof
WO2009002553A1 (en) 2007-06-25 2008-12-31 Prolexys Pharmaceuticals, Inc. Methods of treating multiple myeloma and resistant cancers
JP5690589B2 (ja) 2007-06-25 2015-03-25 エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． 親水性スペーサーリンカーを含有する結合体
JP5492769B2 (ja) 2007-06-26 2014-05-14 サノフイ 縮環されたベンゾイミダゾール及びアザベンゾイミダゾールの位置選択的金属触媒合成
US8685962B2 (en) 2007-07-02 2014-04-01 Technion Research & Development Foundation Limited 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
WO2009017701A2 (en) 2007-07-31 2009-02-05 Schering Corporation Anti-mitotic agent and aurora kinase inhibitor combination as anti-cancer treatment
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
WO2009042294A2 (en) 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
WO2009023718A2 (en) 2007-08-13 2009-02-19 Metabasis Therapeutics, Inc. Novel activators of glucokinase
WO2009029617A1 (en) 2007-08-27 2009-03-05 Kalypsys, Inc. Diarylamine-substituted quinolones useful as inducible nitric oxide synthase inhibitors
WO2009036099A1 (en) 2007-09-10 2009-03-19 Boston Biomedical, Inc. A novel group of stat3 pathway inhibitors and cancer stem cell pathway inhibitors
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
AU2008313504A1 (en) 2007-10-15 2009-04-23 Astrazeneca Ab Combination 059
US20110021541A1 (en) 2007-11-13 2011-01-27 White Stephen L Inhibitors of human phosphatidyl-inositol 3-kinase delta
CA2705405A1 (en) 2007-11-22 2009-05-28 Boehringer Ingelheim International Gmbh New compounds
WO2009074300A2 (en) 2007-12-13 2009-06-18 Siena Biotech S.P.A. Hedgehog pathway antagonists and therapeutic applications thereof
EP2070932A1 (en) 2007-12-13 2009-06-17 4Sc Ag Pyrazolotriazines
AU2008338963A1 (en) 2007-12-13 2009-06-25 Sri International PPAR-delta ligands and methods of their use
ES2587738T3 (es) 2007-12-21 2016-10-26 Ucb Biopharma Sprl Derivados de quinoxalina y quinolina como inhibidores de quinasa
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
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
CN104926815B (zh) 2008-01-04 2017-11-03 英特利凯恩有限责任公司 某些化学实体、组合物和方法
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
BRPI0907248A2 (pt) 2008-01-09 2019-02-26 Pgxhealth, Llc tratamento intratecal de dor neuropática com agonistas a2ar
WO2009088086A1 (ja) 2008-01-10 2009-07-16 Asahi Glass Company, Limited ガラス、発光装置用の被覆材および発光装置
CN101925606A (zh) 2008-01-24 2010-12-22 Ucb医药有限公司 包含环丁氧基的化合物
CA2710929A1 (en) 2008-01-28 2009-08-06 Schering Corporation Imidazopyrazines as protein kinase inhibitors
EP2244709A4 (en) 2008-02-07 2012-02-29 Synta Pharmaceuticals Corp 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
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
WO2009114870A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Kinase inhibitors and methods of use
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
EP2288611B1 (en) 2008-03-20 2013-05-15 Amgen Inc. Aurora kinase modulators and method of use
EP2268612B1 (en) 2008-03-24 2014-08-20 Novartis AG Arylsulfonamide-based matrix metalloprotease inhibitors
AR071112A1 (es) * 2008-03-31 2010-05-26 Genentech Inc Derivados de benzopirano y benzoxepina inhibidores de quinasaspi3k, utiles como agentes anticancer,y composiciones farmaceuticas que los contienen.
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
JP2011521968A (ja) 2008-05-30 2011-07-28 ジェネンテック， インコーポレイテッド プリンｐｉ３ｋ阻害剤化合物および使用方法
US8236808B2 (en) 2008-06-10 2012-08-07 Novartis Ag Pyrazine derivatives as ENAC blockers
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
EP2313414B1 (en) 2008-07-08 2015-11-04 Intellikine, LLC Kinase inhibitors and methods of use
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
US9284297B2 (en) 2008-08-11 2016-03-15 President And Fellows Of Harvard College 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
AU2009298877A1 (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
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
WO2010056758A1 (en) 2008-11-12 2010-05-20 Yangbo Feng Quinazoline derivatives as kinase inhibitors
WO2010059593A1 (en) 2008-11-18 2010-05-27 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
KR101805754B1 (ko) 2008-12-08 2017-12-07 먼디파머 인터내셔널 코포레이션 리미티드 단백질 수용체 티로신 키나아제 억제제의 조성물
EP2379525B1 (en) 2008-12-19 2015-07-29 Boehringer Ingelheim International GmbH Cyclic pyrimidin-4-carboxamides as ccr2 receptor antagonists for 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
ES2598358T3 (es) 2009-02-13 2017-01-27 Ucb Pharma, S.A. Derivados de quinolina como inhibidores de PI3K quinasa
US8569316B2 (en) 2009-02-17 2013-10-29 Boehringer Ingelheim International Gmbh Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases
WO2010096680A2 (en) 2009-02-20 2010-08-26 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College 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
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
GB0908957D0 (en) 2009-05-22 2009-07-01 Ucb Pharma Sa Therapeutic agents
CN102459272B (zh) 2009-05-27 2014-08-06 健泰科生物技术公司 对P110δ具有选择性的为PI3K抑制剂的二环嘧啶化合物和使用方法
WO2010136491A1 (en) 2009-05-27 2010-12-02 F. Hoffmann-La Roche Ag Bicyclic indole-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
BR112012004333A2 (pt) 2009-08-27 2015-09-08 Merck Sharp & Dohme composto, composição farmacêutica, e, método para o tratamento ou a prevenção de uma doença ou um distúrbio.
US20130005802A1 (en) 2009-09-21 2013-01-03 Wei Chen Treatment of wnt/frizzled-related diseases
JP5791612B2 (ja) 2009-09-23 2015-10-07 メディベイション テクノロジーズ， インコーポレイテッド ピリド［３，４−ｂ］インドールおよび使用方法
KR20120096474A (ko) 2009-09-25 2012-08-30 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피리미딘 유도체의 제조 방법
KR20120081164A (ko) 2009-09-29 2012-07-18 엑스커버리 홀딩 컴퍼니 엘엘씨 Ｐｉ3ｋ(델타) 선택적 억제제
US8106146B2 (en) 2009-10-06 2012-01-31 Medtronic, Inc. Therapeutic polymers and methods of generation
WO2011047129A1 (en) 2009-10-15 2011-04-21 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
CN105153188B (zh) 2009-10-22 2018-06-01 法博太科制药有限公司 抗纤维化剂的稠环类似物
WO2011058109A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors
WO2011058108A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Quinoline and quinoxaline derivatives as kinase inhibitors
EP2499144B1 (en) 2009-11-12 2013-10-23 UCB Pharma, S.A. Quinoline and quinoxaline derivatives as kinase inhibitors
MX2012006953A (es) 2009-12-18 2012-10-09 Amgen Inc Compuestos heterociclicos y sus usos.
US20120040950A1 (en) 2009-12-22 2012-02-16 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
EP2557923A4 (en) * 2010-04-16 2013-10-23 Curis Inc TREATMENT OF CANCER DISORDERS WITH K-RAS MUTATIONS
CN110322924A (zh) 2010-04-29 2019-10-11 加利福尼亚大学董事会 利用关于基因组模型的数据集成的途径识别方法(paradigm)
JP5951600B2 (ja) 2010-05-21 2016-07-13 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 キナーゼ調節のための、化合物、組成物および方法
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
WO2012028578A1 (de) 2010-09-03 2012-03-08 Bayer Cropscience Ag Substituierte anellierte pyrimidinone und dihydropyrimidinone
AR082799A1 (es) 2010-09-08 2013-01-09 Ucb Pharma Sa Derivados de quinolina y quinoxalina como inhibidores de quinasa
ES2693257T3 (es) 2010-09-14 2018-12-10 Exelixis, Inc. Inhibidores de PI3K-delta y métodos para su uso y fabricación
JP2013540758A (ja) 2010-09-24 2013-11-07 ギリアード カリストガ エルエルシー Ｐｉ３ｋ阻害化合物のアトロプ異性体
US8765773B2 (en) 2010-10-18 2014-07-01 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
JP2013541591A (ja) 2010-11-04 2013-11-14 アムジエン・インコーポレーテツド 複素環化合物およびそれらの使用
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
WO2012065019A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
WO2012065057A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
SI2649075T1 (sl) 2010-12-08 2018-10-30 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Substituirani pirazolopirimidini kot aktivatorji glukocerebrozidaze
GB201021104D0 (en) 2010-12-13 2011-01-26 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
JP5940562B2 (ja) 2011-02-18 2016-06-29 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 イオンチャネルのモジュレーターとしてのクロマン−スピロ環式ピペリジンアミド
JP2012184225A (ja) 2011-02-18 2012-09-27 Otsuka Pharmaceut Co Ltd 医薬組成物
CN103384672B (zh) 2011-02-25 2016-09-28 武田药品工业株式会社 N-取代的噁嗪并喋啶和噁嗪并喋啶酮
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
KR102104125B1 (ko) 2011-04-21 2020-05-29 재단법인 한국파스퇴르연구소 소염 화합물
ES2785475T3 (es) 2011-05-10 2020-10-07 Gilead Sciences Inc Compuestos heterocíclicos fusionados como moduladores de canales iónicos
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
CA2840224C (en) 2011-06-22 2019-08-13 The General Hospital Corporation Treatment of proteinopathies
EP2731953A1 (en) 2011-07-15 2014-05-21 Abbvie Inc. Tricyclic inhibitors of kinases useful for the treatment of proliferative diseases
HK1198475A1 (en) 2011-07-19 2015-05-08 无限药品股份有限公司 Heterocyclic compounds and uses thereof
WO2013012915A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
MX2014002542A (es) * 2011-08-29 2014-07-09 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos.
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
BR112014007781A2 (pt) 2011-09-30 2017-04-11 Kineta Inc compostos anti-virais
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
KR20140141596A (ko) 2012-03-13 2014-12-10 레스피버트 리미티드 결정질 pi3 키나아제 저해제
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
KR101781922B1 (ko) 2012-04-10 2017-09-26 안지 파마슈티컬 코퍼레이션 리미티드 히스톤 탈아세틸효소(hdacs) 억제제
US9221744B2 (en) 2012-06-11 2015-12-29 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
US9562034B2 (en) 2012-08-30 2017-02-07 The University Of Tokyo Endoparasite control agent
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
US9175007B2 (en) 2013-01-10 2015-11-03 Nimbus Iris, Inc. IRAK inhibitors and uses thereof
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
RU2018142605A (ru) 2013-09-25 2019-02-04 Вертекс Фармасьютикалз Инкорпорейтед Селективный ингибитор фосфатидилинозитол-3-киназы-гамма
JP6466924B2 (ja) 2013-10-04 2019-02-06 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
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof

Also Published As

Publication number Publication date
EP2836487A1 (en) 2015-02-18
US20160207940A1 (en) 2016-07-21
CN104703979A (zh) 2015-06-10
CA2870087C (en) 2021-02-02
JP6309505B2 (ja) 2018-04-11
JP2015512940A (ja) 2015-04-30
US9255108B2 (en) 2016-02-09
WO2013154878A1 (en) 2013-10-17
CN104703979B (zh) 2018-11-27
US20130267521A1 (en) 2013-10-10
HK1207069A1 (en) 2016-01-22
US8940742B2 (en) 2015-01-27
US20150105385A1 (en) 2015-04-16
CA2870087A1 (en) 2013-10-17
EP2836487B1 (en) 2018-10-31
AU2013205238A1 (en) 2013-10-24

Similar Documents

Publication Publication Date Title
AU2013205238B2 (en) Heterocyclic compounds and uses thereof
AU2012284091B2 (en) Heterocyclic compounds and uses thereof
AU2012302197B2 (en) Heterocyclic compounds and uses thereof
US9718815B2 (en) Heterocyclic compounds and uses thereof
AU2014329392B2 (en) Heterocyclic compounds and uses thereof
US9751888B2 (en) Heterocyclic compounds and uses thereof
AU2014329392A1 (en) Heterocyclic compounds and uses thereof
WO2015168079A1 (en) Pyrimidine or pyridine derivatives useful as pi3k inhibitors
NZ621521B2 (en) 1-oxo-isoquinolines and uses thereof

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: INFINITY PHARMACEUTICALS INC.

Free format text: FORMER APPLICANT(S): INFINITY PHARMACEUTICALS, INC.; INTELLIKINE LLC

FGA Letters patent sealed or granted (standard patent)