CA2766882C - Therapeutic compounds and compositions - Google Patents

Therapeutic compounds and compositions Download PDF

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Publication number
CA2766882C
CA2766882C CA2766882A CA2766882A CA2766882C CA 2766882 C CA2766882 C CA 2766882C CA 2766882 A CA2766882 A CA 2766882A CA 2766882 A CA2766882 A CA 2766882A CA 2766882 C CA2766882 C CA 2766882C
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Canada
Prior art keywords
compound
alkyl
pharmaceutically acceptable
acceptable salt
aryl
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CA2766882A
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English (en)
French (fr)
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CA2766882A1 (en
Inventor
Jeffrey O. Saunders
Francesco G. Salituro
Shunqi Yan
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Agios Pharmaceuticals Inc
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Agios Pharmaceuticals Inc
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Application filed by Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Priority to CA2944788A priority Critical patent/CA2944788C/en
Publication of CA2766882A1 publication Critical patent/CA2766882A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20Nitrogen atoms
    • C07D241/22Benzenesulfonamido pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/36Sulfur atoms
    • CCHEMISTRY; METALLURGY
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    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38Nitrogen atoms
    • C07D215/40Nitrogen atoms attached in position 8
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/64Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D319/00Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/101,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/141,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/161,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18Ethylenedioxybenzenes, not substituted on the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
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    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/582Recycling of unreacted starting or intermediate materials

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA2766882A 2009-06-29 2010-06-29 Therapeutic compounds and compositions Active CA2766882C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2944788A CA2944788C (en) 2009-06-29 2010-06-29 Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US22143009P 2009-06-29 2009-06-29
US61/221,430 2009-06-29
US29236010P 2010-01-05 2010-01-05
US61/292,360 2010-01-05
PCT/US2010/040486 WO2011002817A1 (en) 2009-06-29 2010-06-29 Therapeutic compounds and compositions

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2944788A Division CA2944788C (en) 2009-06-29 2010-06-29 Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same

Publications (2)

Publication Number Publication Date
CA2766882A1 CA2766882A1 (en) 2011-01-06
CA2766882C true CA2766882C (en) 2016-11-22

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ID=43381412

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2944788A Active CA2944788C (en) 2009-06-29 2010-06-29 Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same
CA2766882A Active CA2766882C (en) 2009-06-29 2010-06-29 Therapeutic compounds and compositions

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CA2944788A Active CA2944788C (en) 2009-06-29 2010-06-29 Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same

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US (8) US8785450B2 (enExample)
EP (3) EP3241554B1 (enExample)
JP (2) JP5856052B2 (enExample)
KR (2) KR101712035B1 (enExample)
CN (2) CN102481300B (enExample)
AR (1) AR077292A1 (enExample)
AU (1) AU2010266386C1 (enExample)
BR (1) BRPI1011587B1 (enExample)
CA (2) CA2944788C (enExample)
CL (1) CL2011003350A1 (enExample)
CO (1) CO6480955A2 (enExample)
CR (2) CR20170071A (enExample)
CY (2) CY1119443T1 (enExample)
DK (1) DK2448582T3 (enExample)
EC (1) ECSP11011567A (enExample)
ES (1) ES2632954T3 (enExample)
FI (1) FIC20230017I1 (enExample)
FR (1) FR23C1017I2 (enExample)
HR (1) HRP20170955T1 (enExample)
HU (2) HUE032969T2 (enExample)
IL (1) IL217277A (enExample)
IN (1) IN2012DN00471A (enExample)
LT (2) LT2448582T (enExample)
LU (1) LUC00306I2 (enExample)
MX (1) MX2012000256A (enExample)
MY (1) MY191825A (enExample)
NI (1) NI201200003A (enExample)
NL (1) NL301230I2 (enExample)
NO (1) NO2023017I1 (enExample)
NZ (2) NZ622505A (enExample)
PE (1) PE20120693A1 (enExample)
PL (1) PL2448582T3 (enExample)
PT (1) PT2448582T (enExample)
RU (1) RU2561132C2 (enExample)
SG (3) SG10201811480WA (enExample)
SI (1) SI2448582T1 (enExample)
SM (1) SMT201700309T1 (enExample)
TW (4) TWI691493B (enExample)
UA (1) UA107667C2 (enExample)
WO (1) WO2011002817A1 (enExample)
ZA (1) ZA201200054B (enExample)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108524505A (zh) 2009-03-13 2018-09-14 安吉奥斯医药品有限公司 用于细胞增殖相关病症的方法和组合物
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
CA2760929C (en) 2009-05-04 2018-01-02 Agios Pharmaceuticals, Inc. Pkm2 activators for use in the treatment of cancer
PT2448582T (pt) * 2009-06-29 2017-07-10 Agios Pharmaceuticals Inc Compostos e composições terapêuticas
PL2448938T3 (pl) 2009-06-29 2014-11-28 Incyte Holdings Corp Pirymidynony jako inhibitory PI3K
CA2766873C (en) 2009-06-29 2018-08-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
ES2594402T3 (es) 2009-10-21 2016-12-20 Agios Pharmaceuticals, Inc. Métodos y composiciones para trastornos relacionados con la proliferación celular
EP2525790B1 (en) 2009-10-21 2020-05-27 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
EP2509600B1 (en) * 2009-12-09 2017-08-02 Agios Pharmaceuticals, Inc. Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
CA2796311A1 (en) 2010-04-14 2011-10-20 Incyte Corporation Fused derivatives as pi3k.delta. inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
WO2012056319A1 (en) 2010-10-27 2012-05-03 Dynamix Pharmaceuticals Ltd. Sulfonamides for the modulation of pkm2
FR2967674B1 (fr) 2010-11-23 2012-12-14 Pf Medicament Derives d'heteroarylsulfonamides, leur preparation et leur application en therapeutique humaine
US9221792B2 (en) 2010-12-17 2015-12-29 Agios Pharmaceuticals, Inc N-(4-(azetidine-1-carbonyl) phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase M2 (PMK2) modulators
CA2822070C (en) 2010-12-20 2019-09-17 Incyte Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
ES2569712T3 (es) 2010-12-21 2016-05-12 Agios Pharmaceuticals, Inc. Activadores de PKM2 bicíclicos
TWI549947B (zh) * 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
US9181231B2 (en) 2011-05-03 2015-11-10 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia
WO2012151448A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
US9404081B2 (en) 2011-05-03 2016-08-02 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
SG194697A1 (en) * 2011-05-03 2013-12-30 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
PH12021552978A1 (en) 2011-09-02 2022-08-22 Incyte Holdings Corp Heterocyclylamines as pi3k inhibitors
US20140249150A1 (en) * 2011-10-13 2014-09-04 Agios Pharmaceuticals, Inc Activators of pyruvate kinase m2 and methods of treating disease
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
BR112014020773A2 (pt) * 2012-02-22 2020-10-27 Sanford-Burnham Medical Research Institute compostos de sulfonamida e seus usos como inibidores tnap
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US9605521B2 (en) 2012-09-14 2017-03-28 Weatherford Technology Holdings, Llc Gas lift valve with mixed bellows and floating constant volume fluid chamber
NZ706999A (en) 2012-10-15 2018-12-21 Agios Pharmaceuticals Inc Inhibitors of mutant isocitrate dehydrogenase and therapeutical uses thereof
WO2014071512A1 (en) * 2012-11-06 2014-05-15 Universite Laval Combination therapy and methods for the treatment of respiratory diseases
CN103808929A (zh) * 2012-11-08 2014-05-21 中国科学院上海生命科学研究院 一种gbss1比酶活测定方法
NZ707778A (en) * 2012-11-08 2019-03-29 Agios Pharmaceuticals Inc Therapeutic compounds and compositions and their use as pkm2 modulators
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
US10376510B2 (en) 2013-07-11 2019-08-13 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
CN112159391A (zh) 2014-03-14 2021-01-01 阿吉奥斯制药公司 治疗活性化合物的药物组合物
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
GB201419579D0 (en) * 2014-11-03 2014-12-17 Iomet Pharma Ltd Pharmaceutical compound
WO2016115463A1 (en) * 2015-01-15 2016-07-21 Whitehead Institute For Biomedical Research Inhibitors of phosphoglycerate dehydrogenase (phgdh) and uses thereof
LT3262046T (lt) 2015-02-27 2021-01-11 Incyte Corporation Pi3k inhibitoriaus druskos ir jų gamybos būdai
CN104803923B (zh) * 2015-04-22 2017-09-05 江苏恩华药业股份有限公司 一种1‑(2‑嘧啶)哌嗪盐酸盐的制备方法
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
SI3307271T1 (sl) * 2015-06-11 2023-11-30 Agios Pharmaceuticals, Inc. Postopki za uporabo aktivatorjev piruvat kinaze
EP3362065B1 (en) 2015-10-15 2024-04-03 Les Laboratoires Servier Combination therapy comprising ivosidenib, cytarabine and daunorubicin or idarubicin for treating acute myelogenous leukemia
HUE057263T2 (hu) 2015-10-15 2022-04-28 Servier Lab Kombinációs terápia rosszindulató betegségek kezelésére
ES2788856T3 (es) 2017-03-20 2020-10-23 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)
PE20200724A1 (es) 2017-08-15 2020-07-21 Agios Pharmaceuticals Inc Activadores de piruvato quinasas para usar en el tratamiento de trastornos en la sangre
WO2019099651A1 (en) * 2017-11-16 2019-05-23 Agios Pharmaceuticals, Inc. Methods of using deuterated pyruvate kinase activators
KR102682430B1 (ko) 2017-11-22 2024-07-08 아지오스 파마슈티컬스 아이엔씨. N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의 결정 형태
CN108440505A (zh) * 2018-03-30 2018-08-24 中南大学 依他匹隆的全合成方法
CA3101323A1 (en) 2018-06-01 2019-12-05 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders
JP7359783B2 (ja) 2018-06-05 2023-10-11 クリネティックス ファーマシューティカルズ,インク. メラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
US20220081412A1 (en) * 2018-12-20 2022-03-17 The Regents Of The University Of Michigan Quinolinyl-pyrazine-carboxamide compounds and uses thereof
AU2020221837A1 (en) 2019-02-13 2021-09-02 Agios Pharmaceuticals, Inc. Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as PKM2 derivatives for the treatment of cancer, obesity and diabetes related disorders
AU2020280045A1 (en) * 2019-05-22 2021-12-23 Agios Pharmaceuticals, Inc. Crystalline salt forms of N-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
US11878049B1 (en) * 2019-06-14 2024-01-23 Agios Pharmaceuticals, Inc. Mitapivat therapy and modulators of cytochrome P450
MA57202B1 (fr) 2019-09-19 2025-09-30 Novo Nordisk Health Care Ag Compositions d'activation de la pyruvate kinase r (pkr)
EP4054583A4 (en) 2019-11-07 2023-10-25 Crinetics Pharmaceuticals, Inc. MELANOCORTIN SUBTYPE 2 RECEPTOR (MC2R) ANTAGONISTS AND THEIR USES
EP4077307B1 (en) 2019-12-18 2025-03-12 Crinetics Pharmaceuticals, Inc. Gem-disubstituted piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
WO2021133563A1 (en) 2019-12-23 2021-07-01 Crinetics Pharmaceuticals, Inc. Spirocyclic piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
WO2021154987A1 (en) 2020-01-28 2021-08-05 Teva Pharmaceuticals International Gmbh Solid state forms of mitapivat and process for preparation thereof
AU2021347349A1 (en) 2020-09-25 2023-06-08 Agios Pharmaceuticals, Inc. Pharmaceutical formulation
WO2022197798A1 (en) 2021-03-19 2022-09-22 Crinetics Pharmaceuticals, Inc. Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of disease
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
WO2023154036A1 (en) 2022-02-08 2023-08-17 Agios Pharmaceuticals, Inc. Methods for titrating mitapivat
WO2022231627A1 (en) 2021-04-30 2022-11-03 Agios Pharmaceuticals, Inc. Methods for titrating mitapivat for use in treating thalassemia
TW202308630A (zh) 2021-04-30 2023-03-01 美商阿吉歐斯製藥公司 用於滴定米塔皮瓦的方法
JP2024543345A (ja) 2021-11-16 2024-11-21 アジオス ファーマシューティカルズ, インコーポレイテッド Mds関連貧血及び他の状態を処置するための化合物
AU2022391025A1 (en) 2021-11-19 2024-06-06 The Brigham And Women's Hospital, Inc. Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof
EP4455136A4 (en) 2021-12-21 2025-11-05 Scinnohub Pharmaceutical Co Ltd COMPOUND CONTAINING A BIS(AZANYLYLIDENE)SULFONYL STRUCTURE AND ITS USE IN MEDICINE
WO2024084501A1 (en) 2022-10-17 2024-04-25 Mylan Laboratories Limited Crystalline polymorphs of mitapivat and mitapivat hemisulfate
DE202022106287U1 (de) 2022-11-09 2022-11-21 Ahmad Salawi Eine Methode zur Synthese und biologischen Bewertung von neuen Sulfonamid-Analoga
ES2975743A1 (es) * 2022-11-22 2024-07-12 Moehs Iberica Sl Metodo de preparacion de mitapivat, intermedios de sintesis de mitapivat y metodos de preparacion de los mismos
AU2024271540A1 (en) * 2023-05-18 2025-11-27 Concarlo Therapeutics, Inc. Small molecule inhibitors of p27
CN121175042A (zh) 2023-05-26 2025-12-19 赛诺哈勃药业(成都)有限公司 含二氮杂亚基磺酰结构化合物的药物组合物在治疗贫血相关疾病中的用途
CN119638695B (zh) * 2025-02-17 2025-06-06 上海健康医学院 一种菲啰啉取代甲基胍类化合物及其制备和应用

Family Cites Families (266)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2390529A (en) 1942-02-03 1945-12-11 Ernst A H Friedheim Hydrazino-1,3,5-triazino derivatives of substituted phenylarsenic compounds
BE516129A (enExample) * 1949-07-23
GB935538A (en) * 1959-04-06 1963-08-28 Stop Motion Devices Corp Stop-motion head for use on knitting machines
GB1274436A (en) 1970-06-09 1972-05-17 Wolfen Filmfab Veb Process for the sensitization of photographic silver chloride and silver chlorobromide emulsions that may contain colour couplers
BE754242A (fr) 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3867383A (en) 1971-03-29 1975-02-18 Ciba Geigy Corp Monoanthranilatoanilino-s-triazines
CH606334A5 (enExample) 1974-06-21 1978-10-31 Ciba Geigy Ag
US3998828A (en) * 1975-01-31 1976-12-21 Pfizer Inc. 4-[2-(1,3-Dialkyl-1,2,3,4-tetra-hydropyrimidine-2,4-dione-5-carboxamido)ethyl]-1-piperidine sulfonamide
US4235871A (en) * 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
DE2928485A1 (de) 1979-07-14 1981-01-29 Bayer Ag Verwendung von harnstoffderivaten als arzneimittel bei der behandlung von fettstoffwechselstoerungen
DE2948434A1 (de) * 1979-12-01 1981-06-11 Hoechst Ag, 6000 Frankfurt 1-piperidinsulfonylharnstoffe und verfahren zu ihrer herstellung
JPS58186682A (ja) 1982-04-27 1983-10-31 日本化薬株式会社 セルロ−ス又はセルロ−ス含有繊維材料の染色法
US4474599A (en) 1982-07-14 1984-10-02 The Dow Chemical Company 1-(Pyridyl)-1H-1,2,3-triazole derivatives, and use as herbicidal agents
US4501728A (en) * 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
GB8325370D0 (en) 1983-09-22 1983-10-26 Fujisawa Pharmaceutical Co Benzoxazoline and benzothiazoline derivatives
US4593102A (en) * 1984-04-10 1986-06-03 A. H. Robins Company, Inc. N-[(amino)alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulfur linked substitution in the 2, 3 or 4-position
US4643759A (en) 1984-07-13 1987-02-17 E. I. Du Pont De Nemours And Company Herbicidal sulfonamides
IT1196195B (it) 1984-07-20 1988-11-10 Minnesota Mining & Mfg Copulanti formatori di colorante cian ed elementi e procedimenti fotografici
US5019369A (en) * 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
JPS61129129A (ja) 1984-11-28 1986-06-17 Kureha Chem Ind Co Ltd 抗腫瘍剤
FI855180A7 (fi) 1985-01-18 1986-07-19 Nissan Chemical Ind Ltd Pyratsolisulfonamidijohdannainen, menetelmä sen valmistamiseksi ja sitä sisältävä rikkaruohomyrkky.
DE3512630A1 (de) 1985-04-06 1986-10-23 Hoechst Ag, 6230 Frankfurt Verfahren zum faerben oder bedrucken von cellulosefasern oder cellulosemischfasern
EP0246749A3 (en) 1986-05-17 1988-08-31 AgrEvo UK Limited Triazole herbicides
JPS6339875A (ja) 1986-08-05 1988-02-20 Nissin Food Prod Co Ltd ピリミジン誘導体
US4837028A (en) * 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
US4775762A (en) * 1987-05-11 1988-10-04 The Dow Chemical Company Novel (1H-1,2,3-triazol-1-yl)pyridines
US5962490A (en) * 1987-09-25 1999-10-05 Texas Biotechnology Corporation Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
DE3813886A1 (de) 1988-04-20 1989-11-02 Schering Ag 1-triazinyl-1h-1,2,4-triazol-3- sulfonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als mittel mit herbizider, fungizider und pflanzenwachstumsregulierender wirkung
DE3813885A1 (de) 1988-04-20 1989-11-02 Schering Ag 1-chlorpyrimidinyl-1h-1,2,4-triazol-3-sulfonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als mittel mit herbizider, fungizider und pflanzenwachstumsregulierender wirkung
US5220028A (en) * 1988-10-27 1993-06-15 Nissan Chemical Industries, Ltd. Halogeno-4-methylpyrazoles
US5041443A (en) 1989-02-21 1991-08-20 Dainippon Pharmaceutical Co., Ltd. Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof
ES2058630T3 (es) 1989-03-03 1994-11-01 Dainippon Pharmaceutical Co Derivados de 2-(1-piperazinil)-4-fenilcicloalcanopiridinas, procedimientos de preparacion y composiciones farmaceuticas que los contienen.
KR910021381A (ko) * 1990-02-20 1991-12-20 모리 히데오 4-3급 부틸이미다졸 유도체, 및 이의 제조방법 및 용도
CA2036148A1 (en) * 1990-06-29 1991-12-30 Hiroki Tomioka A 1-phenylimidazole derivative and its production and use
JPH0499768A (ja) 1990-08-17 1992-03-31 Dainippon Pharmaceut Co Ltd 4―(4―フェニルピリジン―2―イル)ピペラジン―1―オキシド誘導体
SK69293A3 (en) 1990-12-31 1993-10-06 Monsanto Co Safening pesticidal interactions in crops
US5252590A (en) * 1991-06-28 1993-10-12 Sumitomo Chemical Company, Limited 1-pyridylimidazole derivative
IT1252567B (it) 1991-12-20 1995-06-19 Italfarmaco Spa Derivati di 5-isochinolinsolfonammidi inibitori delle protein-chinasi
WO1993017009A1 (fr) 1992-02-28 1993-09-02 Zenyaku Kogyo Kabushiki Kaisha DERIVE DE s-TRIAZINE ET REMEDE CONTRE DES MALADIES DEPENDENTES DE L'×STROGENE LE CONTENANT COMME INGREDIENT ACTIF
JPH0625177A (ja) 1992-07-09 1994-02-01 Nissan Chem Ind Ltd ピラゾール誘導体及び除草剤
JP3409165B2 (ja) * 1993-04-28 2003-05-26 株式会社林原生物化学研究所 養毛剤とその製造方法
JP3719612B2 (ja) 1993-06-14 2005-11-24 塩野義製薬株式会社 ヘテロ環を含有する尿素誘導体
JP3545461B2 (ja) 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
IL115420A0 (en) * 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
CN1164232A (zh) * 1994-09-26 1997-11-05 曾尼卡有限公司 作为抗血栓形成剂或抗凝血剂的氨基杂环衍生物
RU2126001C1 (ru) * 1995-01-10 1999-02-10 Самдзин Фармасьютикал Ко., Лтд Производные пиперазина и фармацевтическая композиция на их основе
CA2210889C (en) 1995-01-20 2007-08-28 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
WO1998021191A1 (en) 1995-05-16 1998-05-22 Nissan Chemical Industries, Ltd. Cyanoethylmelamine derivatives and process for producing the same
FR2735127B1 (fr) 1995-06-09 1997-08-22 Pf Medicament Nouvelles piperazines heteroaromatiques utiles comme medicaments.
ES2100129B1 (es) 1995-10-11 1998-02-16 Medichem Sa Nuevos compuestos aminopiridinicos policiclicos inhibidores de acetilcolinesterasa, procedimiento para su preparacion y su utilizacion.
DE19541146A1 (de) 1995-10-25 1997-04-30 Schering Ag Imidazolderivate und deren Verwendung als Stickstoffmonoxid-Synthase-Inhibitoren
GB9602166D0 (en) * 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
WO1997028128A1 (en) * 1996-02-02 1997-08-07 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
FR2744449B1 (fr) 1996-02-02 1998-04-24 Pf Medicament Nouvelles piperazines aromatiques derivees de cycloazanes substitues, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments
US5807876A (en) 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
JPH09291034A (ja) 1996-02-27 1997-11-11 Yoshitomi Pharmaceut Ind Ltd 縮合ピリジン化合物およびその医薬としての用途
US6262113B1 (en) 1996-03-20 2001-07-17 Smithkline Beecham Corporation IL-8 receptor antagonists
AU722662B2 (en) * 1996-05-20 2000-08-10 Darwin Discovery Limited Quinoline sulfonamides as TNF inhibitors and as PDE-IV inhibitors
US5843485A (en) * 1996-06-28 1998-12-01 Incoe Corporation Valve-gate bushing for gas-assisted injection molding
PT912559E (pt) 1996-07-13 2003-03-31 Glaxo Group Ltd Compostos heterociclicos fundidos como inibidores de proteina tirosina quinase
DE19629335A1 (de) 1996-07-20 1998-01-22 Golden Records Ass Internation Karte aus Kunststoff
US5984882A (en) 1996-08-19 1999-11-16 Angiosonics Inc. Methods for prevention and treatment of cancer and other proliferative diseases with ultrasonic energy
US6020357A (en) * 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
DE19702988A1 (de) * 1997-01-28 1998-07-30 Hoechst Ag Isoxazol- und Crotonsäureamidderivate und deren Verwendung als Arzneimittel und Diagnostika
CA2280515A1 (en) * 1997-03-11 1998-09-17 E.I. Du Pont De Nemours And Company Heteroaryl azole herbicides
US7863444B2 (en) * 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
US6399358B1 (en) 1997-03-31 2002-06-04 Thomas Jefferson University Human gene encoding human chondroitin 6-sulfotransferase
EP0986551B1 (en) * 1997-05-30 2006-08-02 Takeda Pharmaceutical Company Limited Sulfonamide derivatives, their production and use
JPH1158073A (ja) 1997-08-12 1999-03-02 Ishikawajima Harima Heavy Ind Co Ltd 吊ピース溶接装置
JPH11158073A (ja) 1997-09-26 1999-06-15 Takeda Chem Ind Ltd アデノシンa3拮抗剤
DE19743435A1 (de) 1997-10-01 1999-04-08 Merck Patent Gmbh Benzamidinderivate
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
DE69830513T2 (de) 1997-12-22 2006-03-16 Bayer Pharmaceuticals Corp., West Haven HEMMUNG DER p38 KINASE UNTER VERWENDUNG VON SYMMETRISCHEN UND ASYMMETRISCHEN DIPHENYLHARNSTOFFEN
US6106849A (en) * 1998-01-21 2000-08-22 Dragoco Gerberding & Co. Ag Water soluble dry foam personal care product
GB9805520D0 (en) 1998-03-17 1998-05-13 Zeneca Ltd Chemical compounds
US6214879B1 (en) 1998-03-24 2001-04-10 Virginia Commonwealth University Allosteric inhibitors of pyruvate kinase
GB9811427D0 (en) * 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds
JP2002523451A (ja) * 1998-09-01 2002-07-30 ブリストル−マイヤーズ スクイブ カンパニー カリウムチャネル抑制剤および方法
DE19841985A1 (de) 1998-09-03 2000-03-09 Schering Ag Dialkylsulfonsäure- und Dialkylcarbonsäure-Derivate
DE69928414T2 (de) 1998-09-18 2006-08-03 Abbott Gmbh & Co. Kg 4-aminopyrrolopyrimidine als kinaseinhibitoren
UY25842A1 (es) 1998-12-16 2001-04-30 Smithkline Beecham Corp Antagonistas de receptores de il-8
US6211182B1 (en) 1999-03-08 2001-04-03 Schering Corporation Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
US6274620B1 (en) 1999-06-07 2001-08-14 Biochem Pharma Inc. Thiophene integrin inhibitors
US6492408B1 (en) 1999-07-21 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
ES2252058T3 (es) 1999-08-27 2006-05-16 Sugen, Inc. Mimicos de fosfato y metodos de tratamiento empleando inhibidores de fosfatasa.
NZ517828A (en) 1999-09-17 2003-10-31 Millennium Pharm Inc Inhibitors having activity against mammalian factor Xa
HK1052497B (zh) 1999-09-17 2007-03-02 千禧药品公司 苯甲酸胺和相关的因子xa抑制剂
ES2254385T3 (es) 2000-02-29 2006-06-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
US20010037689A1 (en) * 2000-03-08 2001-11-08 Krouth Terrance F. Hydraulic actuator piston measurement apparatus and method
US6515013B2 (en) 2000-07-13 2003-02-04 Abbott Laboratories 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
CA2415606A1 (en) 2000-07-20 2002-01-31 Neurogen Corporation Capsaicin receptor ligands
FR2817349B1 (fr) * 2000-11-28 2003-06-20 Centre Nat Rech Scient Nouveau procede de criblage de modulateurs de la transcription bacterienne
JP2002193710A (ja) 2000-12-25 2002-07-10 Kumiai Chem Ind Co Ltd ピリミジン又はトリアジン誘導体及び農園芸用殺菌剤
US6525091B2 (en) 2001-03-07 2003-02-25 Telik, Inc. Substituted diarylureas as stimulators for Fas-mediated apoptosis
DE10164711A1 (de) * 2001-03-13 2002-10-17 Schebo Biotech Ag Verwendung von Zuckerphosphaten, Zuckerphosphatanalogen, Aminosäuren und/oder Aminosäureanalogen zur Modulation des Glycolyse-Enzym-Komplexes, des Malat Aspartat Shuttles und/oder der Transaminasen
JP2004534017A (ja) * 2001-04-27 2004-11-11 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 Baceのインヒビター
US20040198979A1 (en) * 2001-05-07 2004-10-07 Dashyant Dhanak Sulfonamides
ES2312595T3 (es) 2001-05-23 2009-03-01 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. Piruvato-quinasa como nueva molecula diana.
US6967212B2 (en) * 2001-05-30 2005-11-22 Bristol-Myers Squibb Company Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
BR0210291A (pt) 2001-06-11 2004-07-13 Biovitrum Ab Compostos de sulfonamida substituìdos, processo para sua preparação e seu uso como medicamento para o tratamento de distúrbios do sistema nervoso central, obesidade e diabetes do tipo ii
DE10128331A1 (de) * 2001-06-12 2002-12-19 Aventis Pharma Gmbh Anthranilsäureamide mit Heteroarylsulfonyl-Seitenkette, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltende pharmazeutische Zubereitungen
JP4083397B2 (ja) * 2001-06-18 2008-04-30 株式会社ルネサステクノロジ 半導体集積回路装置
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
WO2003016300A1 (en) * 2001-08-15 2003-02-27 E. I. Du Pont De Nemours And Company Ortho-substituted aryl amides for controlling invertebrate pests
WO2003016289A1 (en) 2001-08-17 2003-02-27 Ciba Specialty Chemicals Holding Inc. Triazine derivatives and their use as sunscreens
JP4753336B2 (ja) 2001-09-04 2011-08-24 日本化薬株式会社 新規アリル化合物及びその製法
JP2003081937A (ja) 2001-09-07 2003-03-19 Bayer Ag ベンゼンスルホンアミド誘導体
AU2002361577A1 (en) 2001-10-30 2003-05-12 Merck And Co., Inc. Tyrosine kinase inhibitors
US6878196B2 (en) 2002-01-15 2005-04-12 Fuji Photo Film Co., Ltd. Ink, ink jet recording method and azo compound
EP1472248A1 (en) 2002-01-17 2004-11-03 Eli Lilly And Company Modulators of acetylcholine receptors
EP1474145B1 (en) * 2002-02-04 2008-04-23 F. Hoffmann-La Roche Ag Quinoline derivatives as npy antagonists
US20040180889A1 (en) 2002-03-01 2004-09-16 Pintex Pharmaceuticals, Inc. Pin1-modulating compounds and methods of use thereof
US7205304B2 (en) 2002-03-13 2007-04-17 Janssen Pharmaceutica N.V. Sulfonyl-Derivatives as novel inhibitors of histone deacetylase
ATE425152T1 (de) * 2002-03-13 2009-03-15 Janssen Pharmaceutica Nv Aminocarbonylderivate als histone-deacetylase- inhibitoren
US7452888B2 (en) * 2002-03-27 2008-11-18 Glaxo Group Limited Quinoline derivatives and their use as 5-ht6 ligands
EP1501514B1 (en) 2002-05-03 2012-12-19 Exelixis, Inc. Protein kinase modulators and methods of use
GB0215775D0 (en) 2002-07-06 2002-08-14 Astex Technology Ltd Pharmaceutical compounds
US20040067234A1 (en) 2002-07-11 2004-04-08 Paz Einat Isocitrate dehydrogenase and uses thereof
EP2256108B1 (en) 2002-07-18 2016-03-23 Janssen Pharmaceutica NV Substituted triazine kinase inhibitors
AU2003261415C1 (en) 2002-08-09 2010-01-14 Merck Sharp & Dohme Corp. Tyrosine kinase inhibitors
JP2004107220A (ja) 2002-09-13 2004-04-08 Mitsubishi Pharma Corp TNF−α産生抑制剤
KR20050059294A (ko) 2002-10-24 2005-06-17 스테릭스 리미티드 11-베타-하이드록시 스테로이드 데하이드로게나제 형태 1및 형태 2의 억제제
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
EP1575580A4 (en) 2002-12-02 2009-06-10 Arqule Inc METHOD FOR TREATING CARCINOMA
EP1590364B1 (en) 2002-12-16 2011-10-05 Genmab A/S Human monoclonal antibodies against interleukin 8 (il-8)
JP2006515883A (ja) 2003-01-10 2006-06-08 スレッシュオールド ファーマシューティカルズ, インコーポレイテッド 2−デオキシグルコースによる癌の処置
US7358262B2 (en) 2003-01-29 2008-04-15 Whitehead Institute For Biomedical Research Identification of genotype-selective anti-tumor agents
WO2004074438A2 (en) * 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
WO2004073619A2 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
AU2004213124A1 (en) 2003-02-19 2004-09-02 F. Hoffmann-La Roche Ag Sulfonamide substituted xanthine derivatives for use as PEPCK inhibitors
US20070032418A1 (en) * 2003-02-25 2007-02-08 Ambion, Inc Small-molecule inhibitors of angiogenin and rnases and in vivo and in vitro methods of using same
JP4969238B2 (ja) * 2003-03-27 2012-07-04 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
CN1829704A (zh) * 2003-03-28 2006-09-06 詹森药业有限公司 用作cck2调节剂的苯并[1,2,5]噻二唑化合物
ATE482747T1 (de) 2003-04-11 2010-10-15 High Point Pharmaceuticals Llc Neue amide derivate und deren pharmazeutische verwendungen
EP1635832A2 (en) 2003-06-06 2006-03-22 Merck & Co., Inc. Combination therapy for the treatment of diabetes
ES2222827B1 (es) * 2003-07-30 2006-03-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 5-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
US6818631B1 (en) * 2003-08-15 2004-11-16 Nippon Soda Co. Ltd. Fungicidal pyrimidine derivatives
EP1689722A2 (en) 2003-10-10 2006-08-16 Bayer Pharmaceuticals Corporation 4-aminopyrimidine derivatives for treatment of hyperproliferative disorders
US20080051414A1 (en) * 2003-10-14 2008-02-28 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
JP4099768B2 (ja) 2003-11-10 2008-06-11 富士電機デバイステクノロジー株式会社 電子写真感光体および該電子写真感光体に起因する干渉縞有無の判定方法
US20070196395A1 (en) 2003-12-12 2007-08-23 Mackerell Alexander Immunomodulatory compounds that target and inhibit the py'binding site of tyrosene kinase p56 lck sh2 domain
TW200522944A (en) * 2003-12-23 2005-07-16 Lilly Co Eli CB1 modulator compounds
US20050245508A1 (en) 2003-12-24 2005-11-03 Scios, Inc. Treatment of malignant gliomas with TGF-beta inhibitors
US20050170316A1 (en) 2004-01-29 2005-08-04 Russell Bruce M. Toothbrush for detecting the presence of plaque
WO2005074946A1 (en) * 2004-02-10 2005-08-18 Adenobio N.V. Stable and active complexes of adenosine and adenosine phosphates with aminoalcohols for the treatment of pulmonary artery hypertension, cardiac failure and other diseases
JP2007523202A (ja) * 2004-02-24 2007-08-16 ビオアクソン・テラプティーク・インコーポレーテッド 4置換ピペリジン誘導体
US7588779B2 (en) 2004-05-28 2009-09-15 Andrx Labs, Llc Pharmaceutical formulation containing a biguanide and an angiotensin antagonist
GB0412526D0 (en) 2004-06-05 2004-07-14 Leuven K U Res & Dev Type 2 diabetes
ATE529106T1 (de) * 2004-06-24 2011-11-15 Univ Temple Alpha-, beta-ungesättigte sulfone, sulfonoxide, sulfonimide, sulfinimide, acylsulfonamide und acylsulfinamide und therapeutische verwendungen damit
TW200606152A (en) 2004-07-02 2006-02-16 Tanabe Seiyaku Co Piperidine compound and process for preparing the same
FR2872704B1 (fr) * 2004-07-12 2007-11-02 Laurent Schwartz Pluritherapie contre le cancer
TW200626155A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
CA2581623A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyridine compounds, process for their preparation and compositions containing them
JP2008514590A (ja) 2004-09-24 2008-05-08 アストラゼネカ・アクチエボラーグ ベンゾイミダゾール誘導体、それを含む組成物、その製造方法及びその使用
WO2006038594A1 (ja) * 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. N型カルシウムチャネル阻害薬
WO2006043950A1 (en) 2004-10-20 2006-04-27 Smithkline Beecham Corporation Il-8 receptor antagonists
WO2006052546A2 (en) * 2004-11-04 2006-05-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
SE0402762D0 (sv) 2004-11-11 2004-11-11 Astrazeneca Ab Indazole sulphonamide derivatives
WO2006055880A2 (en) * 2004-11-16 2006-05-26 Genzyme Corporation Diagnostic pkm2 methods and compositions
US20080194681A1 (en) * 2004-12-09 2008-08-14 Kalypsys, Inc. Novel Inhibitors of Histone Deacetylase for the Treatment of Disease
US20100160324A1 (en) 2004-12-30 2010-06-24 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
WO2006077821A1 (ja) 2005-01-19 2006-07-27 Dainippon Sumitomo Pharma Co., Ltd. アルドステロン受容体調節剤としての芳香族スルホン化合物
KR20070107061A (ko) 2005-01-25 2007-11-06 아스트라제네카 아베 화학적 화합물
JP4058106B2 (ja) * 2005-02-18 2008-03-05 アストラゼネカ アクチボラグ 抗菌性のピペリジン誘導体
NZ563186A (en) 2005-05-03 2011-09-30 Ranbaxy Lab Ltd Antimicrobial agents
EP1891028A1 (de) 2005-05-18 2008-02-27 Forschungsverbund Berlin e.V. Nicht-peptidische inhibitoren der akap-pka-wechselwirkung
EP1899486A4 (en) 2005-06-08 2009-07-22 Millennium Pharm Inc METHOD FOR IDENTIFYING, ASSESSING AND TREATING PATIENTS IN CANCER THERAPY
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
WO2007004959A1 (en) * 2005-07-05 2007-01-11 Astrazeneca Ab New compounds, process for their preparation, intermediates, pharmaceutical compositions and their use in the treatment of 5-ht6 mediated disorders such as alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and parkinson's disease
US20080214495A1 (en) 2005-07-08 2008-09-04 Astrazeneca Ab Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa
US8071597B2 (en) * 2005-08-26 2011-12-06 Merck Serono Sa Pyrazine compounds and uses as PI3K inhibitors
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
FI20055644A0 (fi) * 2005-12-02 2005-12-02 Nokia Corp Ryhmäviestintä
WO2007075524A2 (en) * 2005-12-22 2007-07-05 Merck & Co., Inc. Substituted piperidines as calcium channel blockers
AU2007243131A1 (en) 2006-01-20 2007-11-08 Smithkline Beecham Corporation Use of sulfonamide derivatives in the treatment of disorders of the metabolism and the nervous system
JP2007238458A (ja) 2006-03-06 2007-09-20 D Western Therapeutics Institute Inc 新規なイソキノリン誘導体及びこれを含有する医薬
WO2007108742A1 (en) * 2006-03-17 2007-09-27 Astrazeneca Ab Novel tetralins as 5-ht6 modulators
US7524848B2 (en) * 2006-03-23 2009-04-28 Amgen Inc. Diaza heterocyclic amide compounds and their uses
MX2008012482A (es) 2006-03-31 2008-10-10 Abbott Lab Compuestos de indazol.
TW200815426A (en) 2006-06-28 2008-04-01 Astrazeneca Ab New pyridine analogues II 333
AU2007281911B2 (en) 2006-08-04 2014-02-06 Beth Israel Deaconess Medical Center Inhibitors of pyruvate kinase and methods of treating disease
EP2056828A4 (en) 2006-08-21 2010-06-23 Merck Sharp & Dohme SULFONYLATED PIPERAZINES AS CANNABINOID-1 RECEPTOR MODULATORS
EP2059809B1 (en) 2006-08-30 2014-07-23 Metanomics GmbH Means and method for diagnosing hemolytic anemia
EP2050745B1 (en) 2006-09-01 2012-03-21 Otsuka AgriTechno Co., Ltd N-pyridylpiperidine compound, method for producing the same, and pest control agent
US8752584B2 (en) 2006-10-12 2014-06-17 Fluid Automation Systems S.A. Rocker valve mechanism and rocker valve
KR20090066297A (ko) 2006-10-16 2009-06-23 화이자 프로덕츠 인크. 치료용 피라졸릴 티에노피리딘
US7906555B2 (en) 2006-10-26 2011-03-15 Arizona Board Of Regents On Behalf Of The University Of Arizona Aquaporin modulators and methods of using them for the treatment of edema and fluid imbalance
HUP0600810A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
EP2121662A1 (en) 2006-12-04 2009-11-25 Neurocrine Biosciences, Inc. Substituted pyrimidines as adenosine receptor antagonists
ES2409090T3 (es) 2006-12-08 2013-06-24 Millennium Pharmaceuticals, Inc. Formulaciones de dosis unitaria y métodos para el tratamiento de trombosis con un inhibidor oral del factor Xa
CA2672893C (en) 2006-12-15 2016-02-23 Abraxis Bioscience, Inc. Triazine derivatives and their therapeutical applications
WO2008130718A1 (en) * 2007-04-23 2008-10-30 Atherogenics, Inc. Sulfonamide containing compounds for treatment of inflammatory disorders
CN101679321B (zh) 2007-04-30 2012-10-03 普罗米蒂克生物科学公司 三嗪衍生物、含所述衍生物的组合物以及所述衍生物在制备用于治疗癌症和自身免疫性疾病药物中的应用
AU2008262291A1 (en) 2007-06-11 2008-12-18 Miikana Therapeutics, Inc. Substituted pyrazole compounds
EP2183239B1 (en) 2007-07-18 2012-08-22 Janssen Pharmaceutica, N.V. Sulfonamides as trpm8 modulators
NZ583450A (en) 2007-07-20 2012-05-25 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
TW200906818A (en) 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
WO2009025781A1 (en) 2007-08-16 2009-02-26 Beth Israel Deaconess Medical Center Activators of pyruvate kinase m2 and methods of treating disease
AR068764A1 (es) 2007-10-10 2009-12-02 Takeda Pharmaceutical N-piperazin amidas y su uso en medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de faah.
EP2053045A1 (en) 2007-10-26 2009-04-29 Syngenta Participations AG Novel imidazole derivatives
US20110224252A1 (en) * 2007-10-26 2011-09-15 Syngenta Crop Protection, Inc. Novel imidazole derivatives
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP5277685B2 (ja) 2008-03-26 2013-08-28 富士ゼロックス株式会社 電子写真感光体、画像形成装置、プロセスカートリッジ及び画像形成方法
GB0805477D0 (en) 2008-03-26 2008-04-30 Univ Nottingham Pyrimidines triazines and their use as pharmaceutical agents
US20090281089A1 (en) 2008-04-11 2009-11-12 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
CN101575408B (zh) 2008-05-09 2013-10-30 Mca技术有限公司 用作阻燃剂和光稳定剂的聚三嗪基化合物
FR2932483A1 (fr) 2008-06-13 2009-12-18 Cytomics Systems Composes utiles pour le traitement des cancers.
TW201028381A (en) 2008-07-14 2010-08-01 Shionogi & Co Pyridine derivative having ttk inhibition activity
GB0815781D0 (en) 2008-08-29 2008-10-08 Xention Ltd Novel potassium channel blockers
WO2010028179A1 (en) 2008-09-03 2010-03-11 Dr. Reddy's Laboratories Ltd. Heterocyclic compounds as gata modulators
DK2546365T3 (en) 2008-09-03 2017-01-16 Univ Johns Hopkins Genetic changes of isocitrate dehydrogenase and other genes in malignant glioma
JP2010079130A (ja) 2008-09-29 2010-04-08 Fuji Xerox Co Ltd 電子写真感光体、プロセスカートリッジ、及び画像形成装置
WO2010042867A2 (en) 2008-10-09 2010-04-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
WO2010059239A2 (en) 2008-11-21 2010-05-27 Millennium Pharmaceuticals, Inc Lactate salt of 4-(6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders
JP2010181540A (ja) 2009-02-04 2010-08-19 Fuji Xerox Co Ltd 電子写真感光体、プロセスカートリッジ、及び画像形成装置
ES2453474T3 (es) 2009-02-06 2014-04-07 Nippon Shinyaku Co., Ltd. Derivados de aminopirazina y medicamento correspondiente
CN108524505A (zh) 2009-03-13 2018-09-14 安吉奥斯医药品有限公司 用于细胞增殖相关病症的方法和组合物
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
CA2760929C (en) 2009-05-04 2018-01-02 Agios Pharmaceuticals, Inc. Pkm2 activators for use in the treatment of cancer
WO2010130638A1 (en) 2009-05-14 2010-11-18 Evotec Ag Sulfonamide compounds, pharmaceutical compositions and uses thereof
CN102573485B (zh) 2009-06-08 2014-11-26 加利福尼亚资本权益有限责任公司 三嗪衍生物及其治疗应用
JP2012529518A (ja) 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー ヘッジホッグシグナル伝達のピリジル−トリアジン阻害剤
US20120202818A1 (en) 2009-06-09 2012-08-09 California Capital Equity, Llc Ureidophenyl substituted triazine derivatives and their therapeutical applications
CA2766873C (en) 2009-06-29 2018-08-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
PT2448582T (pt) 2009-06-29 2017-07-10 Agios Pharmaceuticals Inc Compostos e composições terapêuticas
CA2773561A1 (en) 2009-09-14 2011-03-17 Phusis Therapeutics Inc. Pharmaceutical compositions and formulations including inhibitors of the pleckstrin homology domain and methods for using same
JP5473851B2 (ja) 2009-09-30 2014-04-16 富士フイルム株式会社 高分子フィルム、位相差フィルム、偏光板及び液晶表示装置
US8652534B2 (en) 2009-10-14 2014-02-18 Berry Pharmaceuticals, LLC Compositions and methods for treatment of mammalian skin
EP2525790B1 (en) 2009-10-21 2020-05-27 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
ES2594402T3 (es) 2009-10-21 2016-12-20 Agios Pharmaceuticals, Inc. Métodos y composiciones para trastornos relacionados con la proliferación celular
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
EP2509600B1 (en) 2009-12-09 2017-08-02 Agios Pharmaceuticals, Inc. Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation
JP2013522171A (ja) 2010-03-01 2013-06-13 ミレクシス, インコーポレイテッド 化合物およびその治療用途
JP5761173B2 (ja) * 2010-03-04 2015-08-12 味の素株式会社 糖尿病又は肥満症の予防又は治療剤
EP2553116A4 (en) 2010-04-01 2013-10-23 Agios Pharmaceuticals Inc METHOD FOR IDENTIFYING A CANDIDATE COMPOUND
EP2563761A1 (en) 2010-04-29 2013-03-06 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
WO2011143160A2 (en) 2010-05-10 2011-11-17 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
SG186885A1 (en) * 2010-06-04 2013-02-28 Albany Molecular Res Inc Glycine transporter-1 inhibitors, methods of making them, and uses thereof
MX342951B (es) 2010-07-16 2016-10-18 Agios Pharmaceuticals Inc * Composiciones terapeuticamente activas y su metodo de uso.
WO2012054005A1 (en) 2010-10-20 2012-04-26 Yota Devices Ipr Ltd Mobile device with input arrangement
NZ609490A (en) 2010-10-21 2015-06-26 Biomarin Pharm Inc Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt
FR2967674B1 (fr) 2010-11-23 2012-12-14 Pf Medicament Derives d'heteroarylsulfonamides, leur preparation et leur application en therapeutique humaine
SG10201601507YA (en) 2010-11-29 2016-04-28 Galleon Pharmaceuticals Inc Novel compounds as respiratory stimulants for treatment of breathing control disorders or diseases
US9221792B2 (en) 2010-12-17 2015-12-29 Agios Pharmaceuticals, Inc N-(4-(azetidine-1-carbonyl) phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase M2 (PMK2) modulators
ES2569712T3 (es) 2010-12-21 2016-05-12 Agios Pharmaceuticals, Inc. Activadores de PKM2 bicíclicos
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
EP2671402B1 (en) 2011-02-04 2017-01-18 Nec Corporation Radio communication system, base station apparatus, radio resource control method, and non-transitory computer readable medium
SG194697A1 (en) 2011-05-03 2013-12-30 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
US9404081B2 (en) 2011-05-03 2016-08-02 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之4-芳基-n-苯基-1,3,5-三氮雜苯-2-胺
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
US20140249150A1 (en) 2011-10-13 2014-09-04 Agios Pharmaceuticals, Inc Activators of pyruvate kinase m2 and methods of treating disease
CN102659765B (zh) 2011-12-31 2014-09-10 沈阳药科大学 嘧啶及三嗪类化合物的制备方法和应用
SI2800743T1 (en) 2012-01-06 2018-08-31 Agios Pharmaceuticals, Inc. Therapeutically active compounds and methods for their use
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
CA2860858A1 (en) 2012-01-19 2013-07-25 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
EP2634259A1 (en) 2012-03-01 2013-09-04 Deutsches Krebsforschungszentrum Means and methods for the determination of (D)-2-hydroxyglutarate (D2HG)
CN104169260A (zh) 2012-03-09 2014-11-26 卡尔那生物科学株式会社 新三嗪衍生物
WO2014015422A1 (en) 2012-07-27 2014-01-30 Ontario Institute For Cancer Research Cellulose-based nanoparticles for drug delivery
NZ706999A (en) 2012-10-15 2018-12-21 Agios Pharmaceuticals Inc Inhibitors of mutant isocitrate dehydrogenase and therapeutical uses thereof
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
SI3307271T1 (sl) 2015-06-11 2023-11-30 Agios Pharmaceuticals, Inc. Postopki za uporabo aktivatorjev piruvat kinaze
KR102682430B1 (ko) * 2017-11-22 2024-07-08 아지오스 파마슈티컬스 아이엔씨. N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의 결정 형태

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