ES2632954T3 - Derivados de quinolina-8-sulfonamida que tienen una actividad anticancerosa - Google Patents

Derivados de quinolina-8-sulfonamida que tienen una actividad anticancerosa Download PDF

Info

Publication number
ES2632954T3
ES2632954T3 ES10794668.3T ES10794668T ES2632954T3 ES 2632954 T3 ES2632954 T3 ES 2632954T3 ES 10794668 T ES10794668 T ES 10794668T ES 2632954 T3 ES2632954 T3 ES 2632954T3
Authority
ES
Spain
Prior art keywords
compound
nmr
mhz
alkyl
aspects
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
ES10794668.3T
Other languages
English (en)
Spanish (es)
Inventor
Jeffrey O. Saunders
Francesco G. Salituro
Shunqi Yan
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.)
Agios Pharmaceuticals Inc
Original Assignee
Agios 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43381412&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2632954(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2632954T3 publication Critical patent/ES2632954T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/20—Nitrogen atoms
    • C07D241/22—Benzenesulfonamido pyrazines
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/16—Heterocyclic 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
    • C07D295/18—Heterocyclic 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
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • 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
    • C07D407/00—Heterocyclic 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
    • C07D407/02—Heterocyclic 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
    • C07D407/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • 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
    • 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
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • 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)
ES10794668.3T 2009-06-29 2010-06-29 Derivados de quinolina-8-sulfonamida que tienen una actividad anticancerosa Active ES2632954T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US22143009P 2009-06-29 2009-06-29
US221430P 2009-06-29
US29236010P 2010-01-05 2010-01-05
US292360P 2010-01-05
PCT/US2010/040486 WO2011002817A1 (en) 2009-06-29 2010-06-29 Therapeutic compounds and compositions

Publications (1)

Publication Number Publication Date
ES2632954T3 true ES2632954T3 (es) 2017-09-18

Family

ID=43381412

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10794668.3T Active ES2632954T3 (es) 2009-06-29 2010-06-29 Derivados de quinolina-8-sulfonamida que tienen una actividad anticancerosa

Country Status (41)

Country Link
US (8) US8785450B2 (enExample)
EP (3) EP3708169A1 (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) NZ597379A (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 (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6067226B2 (ja) 2009-03-13 2017-01-25 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 細胞増殖関連疾患のための方法および組成物
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
EP2427441B1 (en) 2009-05-04 2016-12-14 Agios Pharmaceuticals, Inc. Pkm2 activators for use in the treatment of cancer
AR077292A1 (es) * 2009-06-29 2011-08-17 Agios Pharmaceuticals Inc Derivados de piperazin - quinolin sulfonamidas y composiciones farmaceuticas
PE20120493A1 (es) 2009-06-29 2012-05-20 Incyte Corp Pirimidinonas como inhibidores de pi3k
CA2766873C (en) 2009-06-29 2018-08-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2011050211A2 (en) 2009-10-21 2011-04-28 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
JP5967827B2 (ja) * 2009-12-09 2016-08-10 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 Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
AR081823A1 (es) 2010-04-14 2012-10-24 Incyte Corp DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd
WO2011163195A1 (en) 2010-06-21 2011-12-29 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
EP2651898B1 (en) 2010-12-17 2015-12-09 Agios Pharmaceuticals, Inc. Novel n-(4-(azetidine-1-carbonyl)phenyl)-(hetero-)arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
US9328077B2 (en) 2010-12-21 2016-05-03 Agios Pharmaceuticals, Inc Bicyclic PKM2 activators
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
CN103608016A (zh) * 2011-05-03 2014-02-26 安吉奥斯医药品有限公司 丙酮酸激酶激活剂在治疗中的用途
HUE065700T2 (hu) * 2011-05-03 2024-06-28 Agios Pharmaceuticals Inc Piruvát-kináz aktivátorok terápiában történõ alkalmazásra
WO2012151440A1 (en) 2011-05-03 2012-11-08 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
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
KR20230038593A (ko) 2011-09-02 2023-03-20 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
WO2013056153A1 (en) * 2011-10-13 2013-04-18 Kung Charles 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
EP2817292B1 (en) 2012-02-22 2019-12-18 Sanford-Burnham Medical Research Institute Sulfonamide compounds and uses as tnap inhibitors
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
JP6385352B2 (ja) 2012-10-15 2018-09-05 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 治療化合物および組成物
WO2014071512A1 (en) * 2012-11-06 2014-05-15 Universite Laval Combination therapy and methods for the treatment of respiratory diseases
CN104822672B (zh) * 2012-11-08 2018-08-28 安吉奥斯医药品有限公司 治疗性化合物和组合物以及其作为pkm2调节剂的用途
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
WO2014139144A1 (en) * 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
AU2014287121B2 (en) 2013-07-11 2018-11-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
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
CA2942072C (en) 2014-03-14 2022-07-26 Agios Pharmaceuticals, Inc. Pharmaceutical compositions and use of (s)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-( 4-cyanopyridin-2-yl)-n-( 5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
WO2015191677A1 (en) 2014-06-11 2015-12-17 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
PH12017501538B1 (en) 2015-02-27 2024-02-14 Incyte Holdings Corp Salts of p13k inhibitor and processes for their preparation
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
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
PL3307271T3 (pl) 2015-06-11 2024-02-05 Agios Pharmaceuticals, Inc. Sposoby stosowania aktywatorów kinazy pirogronianowej
IL258684B2 (en) 2015-10-15 2023-04-01 Agios Pharmaceuticals Inc Combination therapy including an isocitrate dehydrogenase (1idh) inhibitor for use in the treatment of acute myelogenous leukemia (aml) characterized by the presence of a mutant allele of 1idh
RS62829B1 (sr) 2015-10-15 2022-02-28 Servier Lab Kombinovana terapija za lečenje maligniteta
KR102007135B1 (ko) 2017-03-20 2019-08-02 포르마 세라퓨틱스 인크. 피루베이트 키나제 (pkr) 활성화제로서의 피롤로피롤 조성물
SG11202001353PA (en) 2017-08-15 2020-03-30 Agios Pharmaceuticals Inc Pyruvate kinase modulators and use thereof
WO2019099651A1 (en) * 2017-11-16 2019-05-23 Agios Pharmaceuticals, Inc. Methods of using deuterated pyruvate kinase activators
SG11202004587XA (en) * 2017-11-22 2020-06-29 Agios Pharmaceuticals Inc Crystalline forms of n-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
CN108440505A (zh) * 2018-03-30 2018-08-24 中南大学 依他匹隆的全合成方法
CN112469418A (zh) 2018-06-01 2021-03-09 因赛特公司 治疗pi3k相关病症的给药方案
SG11202012071TA (en) 2018-06-05 2021-01-28 Crinetics Pharmaceuticals Inc Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
WO2020132459A1 (en) * 2018-12-20 2020-06-25 The Regents Of The University Of Michigan Quinolinyl-pyrazine-carboxamide compounds and uses thereof
KR20210128435A (ko) 2019-02-13 2021-10-26 아지오스 파마슈티컬스 아이엔씨. 티에노[3,2-b] 피롤[3,2-d]피리다지논 유도체, 및 암, 비만증, 및 당뇨병 관련 장애의 치료를 위한 pkm2 유도체로서 이의 용도
MX2021014228A (es) * 2019-05-22 2022-02-21 Agios Pharmaceuticals Inc Formas cristalinas de sal de n-(4-(4 (ciclopropilmetil)piperazin 1- carbonil)fenil)quinolin-8-sulfonamida.
US11878049B1 (en) * 2019-06-14 2024-01-23 Agios Pharmaceuticals, Inc. Mitapivat therapy and modulators of cytochrome P450
US20220378756A1 (en) 2019-09-19 2022-12-01 Forma Therapeutics, Inc. Activating pyruvate kinase r
EP4054583A4 (en) * 2019-11-07 2023-10-25 Crinetics Pharmaceuticals, Inc. MELANOCORTIN SUBTYPE 2 RECEPTOR (MC2R) ANTAGONISTS AND THEIR USES
EP4603142A3 (en) 2019-12-23 2025-08-27 Crinetics Pharmaceuticals, Inc. Spirocyclic piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
EP4097085A1 (en) 2020-01-28 2022-12-07 Teva Pharmaceuticals International GmbH Solid state forms of mitapivat and process for preparation thereof
JP2023542701A (ja) 2020-09-25 2023-10-11 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 薬学的製剤
JP2024510260A (ja) 2021-03-19 2024-03-06 クリネティックス ファーマシューティカルズ，インク． 疾患の治療のためのメラノコルチンサブタイプ－２受容体（ｍｃ２ｒ）アンタゴニスト
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
MX2023012823A (es) 2021-04-30 2023-12-07 Agios Pharmaceuticals Inc Métodos para ajustar la dosis de mitapivat.
WO2022231627A1 (en) 2021-04-30 2022-11-03 Agios Pharmaceuticals, Inc. Methods for titrating mitapivat for use in treating thalassemia
TW202329935A (zh) 2021-11-16 2023-08-01 美商阿吉歐斯製藥公司 用於治療ｍｄｓ相關聯之貧血及其他病況之化合物
WO2023092094A2 (en) 2021-11-19 2023-05-25 The Broad Institute, Inc. Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof
CN118510768A (zh) 2021-12-21 2024-08-16 赛诺哈勃药业（成都）有限公司 含二氮杂亚基磺酰结构的化合物及其在医药上的用途
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
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
NL80569C (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
DK0565593T3 (da) 1990-12-31 1999-09-27 Monsanto Co Reducering af pesticidinteraktion i afgrøder
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
AU665238B2 (en) 1992-02-28 1995-12-21 Zenyaku Kogyo Kabushiki Kaisha S-triazine derivative and remedy for estrogen-dependent diseases containing the same as active ingredient
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
WO1996022287A1 (en) 1995-01-20 1996-07-25 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
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
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
JP2000504336A (ja) * 1996-02-02 2000-04-11 ゼネカ・リミテッド 薬学製剤として有用なヘテロ環式化合物
GB9602166D0 (en) 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
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
JP2000510866A (ja) * 1996-05-20 2000-08-22 ダーウィン・ディスカバリー・リミテッド Ｔｎｆとｐｄｅ―ｉｖのインヒビターとしてのキノリンスルホンアミド
US5843485A (en) 1996-06-28 1998-12-01 Incoe Corporation Valve-gate bushing for gas-assisted injection molding
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
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
CA2271744A1 (en) 1996-11-14 1998-05-22 Isao Hashiba Cyanoethylmelamine derivatives and process for producing the same
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
US6359134B1 (en) * 1997-05-30 2002-03-19 Takeda Chemical Industries, Ltd. 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
EP1042305B1 (en) 1997-12-22 2005-06-08 Bayer Pharmaceuticals Corp. INHIBITION OF p38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS
US7517880B2 (en) 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
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
WO2000012077A1 (en) 1998-09-01 2000-03-09 Bristol-Myers Squibb Company Potassium channel inhibitors and method
DE19841985A1 (de) 1998-09-03 2000-03-09 Schering Ag Dialkylsulfonsäure- und Dialkylcarbonsäure-Derivate
CN1326457A (zh) 1998-09-18 2001-12-12 巴斯福股份公司 作为激酶抑制剂的4－氨基吡咯并嘧啶
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
AU775625B2 (en) 1999-08-27 2004-08-05 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
JP2003509412A (ja) 1999-09-17 2003-03-11 シーオーアール セラピューティクス インコーポレイテッド Ｘａ因子阻害剤
EP1216228B1 (en) 1999-09-17 2008-10-29 Millennium Pharmaceuticals, Inc. BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa
AU2001245353A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of 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
KR20030024799A (ko) 2000-07-20 2003-03-26 뉴로젠 코포레이션 캡사이신 수용체 리간드
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
EP1389194A2 (en) * 2001-04-27 2004-02-18 Vertex Pharmaceuticals Incorporated Inhibitors of bace
WO2002089793A1 (en) 2001-05-07 2002-11-14 Smithkline Beecham Corporation Sulfonamides
US20040152648A1 (en) 2001-05-23 2004-08-05 Axel Ullrich Pyruvate-kinase as a novel target molecule
US6967212B2 (en) 2001-05-30 2005-11-22 Bristol-Myers Squibb Company Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
US7144883B2 (en) 2001-06-11 2006-12-05 Biovitrum Ab Bicyclic sulfonamide compounds
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
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
RU2283839C2 (ru) 2001-08-15 2006-09-20 Е.И.Дюпон Де Немур Энд Компани Ортозамещенные ариламиды, способ борьбы с насекомыми, композиция для борьбы с насекомыми, промежуточное соединение
US7038046B2 (en) 2001-08-17 2006-05-02 Ciba Specialty Chemicals Corporation 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
US7169788B2 (en) 2001-10-30 2007-01-30 Merck & 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
ES2304498T3 (es) * 2002-02-04 2008-10-16 F. Hoffmann-La Roche Ag Derivados de quinolina como antagonistas de npy.
WO2003073999A2 (en) 2002-03-01 2003-09-12 Pintex Pharmaceuticals, Inc. Pini-modulating compounds and methods of use thereof
KR20040090978A (ko) 2002-03-13 2004-10-27 얀센 파마슈티카 엔.브이. 히스톤 디아세틸라제의 신규한 저해제로서의 설포닐-유도체
WO2003076400A1 (en) 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. New inhibitors of histone deacetylase
MXPA04009318A (es) * 2002-03-27 2005-01-25 Glaxo Group Ltd Derivados de quinolina y su uso como ligados 5-ht6.
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
EP1546121B1 (en) 2002-07-18 2012-08-29 Janssen Pharmaceutica NV Substituted triazine kinase inhibitors
CA2494962C (en) 2002-08-09 2011-06-14 Merck & Co., Inc. Tyrosine kinase inhibitors
JP2004107220A (ja) 2002-09-13 2004-04-08 Mitsubishi Pharma Corp ＴＮＦ−α産生抑制剤
CA2501228A1 (en) 2002-10-24 2004-05-06 Sterix Limited Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 and type 2
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
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)
CA2513399A1 (en) 2003-01-10 2004-07-29 Threshold Pharmaceuticals, Inc. Treatment of cancer with 2-deoxyglucose
US7358262B2 (en) 2003-01-29 2008-04-15 Whitehead Institute For Biomedical Research Identification of genotype-selective anti-tumor agents
WO2004073619A2 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
WO2004074438A2 (en) * 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
EP1599477B1 (en) * 2003-02-19 2008-01-30 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
ATE524452T1 (de) * 2003-03-27 2011-09-15 Cytokinetics Inc Sulfonamide zur behandlung von kongestivem herzversagen, deren zusammensetzungen und verwendungen.
WO2005012275A2 (en) * 2003-03-28 2005-02-10 Janssen Pharmaceutica, N.V. Benzo [1, 2, 5] thiadiazole compounds as cck2 modulators
JP4629657B2 (ja) 2003-04-11 2011-02-09 ハイ・ポイント・ファーマスーティカルズ、エルエルシー １１β−ヒドロキシステロイドデヒドロゲナーゼ１型化活性化合物
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
CA2542031A1 (en) 2003-10-10 2005-04-21 Bayer Pharmaceuticals Corporation Pyrimidine 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
KR20070007055A (ko) 2003-12-24 2007-01-12 사이오스 인코퍼레이티드 Ｔｇｆ-베타 억제제를 이용한 악성 신경교종의 치료법
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
CA2556589A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
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
CA2577309C (en) 2004-06-24 2013-10-22 Temple University - Of The Commonwealth System Of Higher Education Alpha, beta-unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides and therapeutic uses thereof
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
EP2316458A1 (en) 2004-09-20 2011-05-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
CA2581454A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine 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
US20070249625A1 (en) 2004-10-20 2007-10-25 Jakob Busch-Petersen 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
JP2008526723A (ja) 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Ｃｄｋ、ｇｓｋ及びオーロラキナーゼの活性を調節するピラゾール誘導体
US20100160304A1 (en) 2005-01-19 2010-06-24 Dainippon Sumitomo Pharma Co., Ltd Aromatic sulfone compound as aldosterone receptor modulator
AU2006208834A1 (en) 2005-01-25 2006-08-03 Astrazeneca Ab Chemical compounds
WO2006087543A1 (en) 2005-02-18 2006-08-24 Astrazeneca Ab Antibacterial piperidine derivatives
SI1879877T1 (sl) 2005-05-03 2013-02-28 Ranbaxy Laboratories Limited Protimikrobna sredstva
DE112006002052A5 (de) 2005-05-18 2008-05-08 Forschungsverbund Berlin E.V. Nicht-Peptidische Inhibitoren der AKAP-PKA-Wechselwirkung
AU2006254834B2 (en) 2005-06-08 2012-09-20 Millennium Pharmaceuticals, Inc. Treatment of patients with cancer therapy
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
JP2009501705A (ja) 2005-07-05 2009-01-22 アストラゼネカ・アクチエボラーグ 新規化合物、その製造方法、中間体、医薬組成物、並びにアルツハイマー病、認知障害、統合失調症に伴う認識機能障害、肥満及びパーキンソン病のような５−ｈｔ６介在疾患の治療におけるそれらの使用
US20080214495A1 (en) 2005-07-08 2008-09-04 Astrazeneca Ab Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa
EA015937B1 (ru) 2005-08-26 2011-12-30 Мерк Сероно С.А. Производные пиразина и их применение в качестве ингибиторов pi3k
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
JP2009521444A (ja) 2005-12-22 2009-06-04 メルク エンド カムパニー インコーポレーテッド カルシウムチャンネルブロッカーとなる置換ピペリジン
BRPI0706654A2 (pt) 2006-01-20 2011-04-05 Smithkline Beecham Corp composição farmacêutica, método para tratar condições ou distìrbios em um mamìfero, uso de um composto, e, composto
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
US20090054453A1 (en) 2006-03-17 2009-02-26 Lilian Alcaraz Novel Tetralins as 5-HT6 Modulators
MX2008012064A (es) 2006-03-23 2008-12-17 Amgen Inc Compuestos de amida 1-fenilsulfonil-diaza-heterociclica y sus usos como moduladores de hidroxiesteroide deshidrogenadas.
US8008481B2 (en) 2006-03-31 2011-08-30 Ericsson Anna M Indazole compounds
TW200815426A (en) 2006-06-28 2008-04-01 Astrazeneca Ab New pyridine analogues II 333
US8877791B2 (en) 2006-08-04 2014-11-04 Beth Israel Deaconess Medical Center, Inc. Inhibitors of pyruvate kinase and methods of treating disease
US20090247499A1 (en) 2006-08-21 2009-10-01 Fletcher Joan M Sulfonylated piperazines as cannabinoid-1 receptor modulators
EP2059809B1 (en) 2006-08-30 2014-07-23 Metanomics GmbH Means and method for diagnosing hemolytic anemia
WO2008026658A1 (ja) 2006-09-01 2008-03-06 Otsuka Chemical Co., Ltd. Ｎ－ピリジルピペリジン化合物、その製造方法及び有害生物防除剤
CN101548123B (zh) 2006-10-12 2011-06-08 弗路德自动控制系统有限公司 摇杆阀机构和摇杆阀
ES2435430T3 (es) 2006-10-16 2013-12-19 Thesan Pharmaceuticals, Inc. Pirazolil tienopiridinas terapéuticas
EP2086329B1 (en) 2006-10-26 2014-07-23 The 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
US20100234341A1 (en) 2006-12-04 2010-09-16 Marion Lanier Substituted pyrimidines as adenosine receptor antagonists
CA2913963A1 (en) 2006-12-08 2008-06-19 Millenium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
WO2008076883A2 (en) 2006-12-15 2008-06-26 Abraxis Bioscience, Inc. Triazine derivatives and their therapeutical applications
US7897776B2 (en) 2007-04-23 2011-03-01 Salutria Pharmaceuticals Llc Sulfonamide containing compounds for treatment of inflammatory disorders
WO2008131547A1 (en) 2007-04-30 2008-11-06 Prometic Biosciences Inc. 'triazine derivatives, compositions containing such derivatives, and methods of treatment of cancer and autoimmune diseases using such derivatives'
AU2008262291A1 (en) 2007-06-11 2008-12-18 Miikana Therapeutics, Inc. Substituted pyrazole compounds
MX2010000690A (es) 2007-07-18 2010-06-25 Janssen Pharmaceutica Nv Sulfonamidas como moduladores de trpm8.
SG183049A1 (en) 2007-07-20 2012-08-30 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
TW200906818A (en) 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
US8552050B2 (en) 2007-08-16 2013-10-08 Beth Israel Deaconess Medical Center Activators of pyruvate kinase M2 and methods of treating disease
BRPI0818366A2 (pt) 2007-10-10 2015-04-07 Takeda Pharmaceutical Composto, pró-droga, medicamento, método inibidor de faah, métodos de profilaxia ou tratamento para ansiedade, ou depressão, ou de alívio da dor, e de profilaxia ou tratamento para dor inflamatória ou dor neuropática, e, uso do composto.
KR20100101580A (ko) 2007-10-26 2010-09-17 신젠타 파티서페이션즈 아게 신규한 이미다졸 유도체
EP2053045A1 (en) 2007-10-26 2009-04-29 Syngenta Participations AG Novel imidazole derivatives
AU2008345225A1 (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.
WO2010007756A1 (ja) 2008-07-14 2010-01-21 塩野義製薬株式会社 Ｔｔｋ阻害作用を有するピリジン誘導体
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
DK2326735T3 (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
ES2620634T3 (es) 2008-10-09 2017-06-29 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Activadores de piruvato quinasa humana
US20100273808A1 (en) 2008-11-21 2010-10-28 Millennium Pharmaceticals, 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
KR101677778B1 (ko) 2009-02-06 2016-11-18 니뽄 신야쿠 가부시키가이샤 아미노피라진 유도체 및 의약
JP6067226B2 (ja) 2009-03-13 2017-01-25 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 細胞増殖関連疾患のための方法および組成物
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
EP2427441B1 (en) 2009-05-04 2016-12-14 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
WO2010144338A1 (en) 2009-06-08 2010-12-16 Abraxis Bioscience, Llc Triazine derivatives and their therapeutical applications
BRPI1011527A2 (pt) 2009-06-09 2016-07-26 California Capital Equity Llc derivados de triazina substituídos com ureidofenil e suas aplicações terapêuticas.
AU2010258974A1 (en) 2009-06-09 2012-01-12 California Capital Equity, Llc Pyridil-triazine inhibitors of hedgehog signaling
AR077292A1 (es) 2009-06-29 2011-08-17 Agios Pharmaceuticals Inc Derivados de piperazin - quinolin sulfonamidas y composiciones farmaceuticas
CA2766873C (en) 2009-06-29 2018-08-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
EP2477625A4 (en) 2009-09-14 2012-10-24 Phusis Therapeutics Inc PHARMACEUTICAL COMPOSITIONS AND FORMULATIONS COMPRISING PLECKSTRINE HOMOLOGY DOMAIN INHIBITORS AND METHODS OF USE
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
WO2011050211A2 (en) 2009-10-21 2011-04-28 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
JP5967827B2 (ja) 2009-12-09 2016-08-10 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 Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物
WO2011109441A1 (en) 2010-03-01 2011-09-09 Myrexis, Inc. Compounds and therapeutic uses thereof
EP2543660A4 (en) * 2010-03-04 2014-04-30 Ajinomoto Kk PROPHYLACTIC OR THERAPEUTIC ACTIVE AGAINST DIABETES OR ADIPOSITAS
US20130197106A1 (en) 2010-04-01 2013-08-01 Agios Pharmaceuticals, Inc Methods of identifying a candidate compound
JP2013525438A (ja) 2010-04-29 2013-06-20 アメリカ合衆国 ヒトピルビン酸キナーゼ活性剤
WO2011143160A2 (en) 2010-05-10 2011-11-17 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
CA2801074A1 (en) 2010-06-04 2011-12-08 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
BR112013001122B1 (pt) 2010-07-16 2021-06-08 Agios Pharmaceuticals, Inc composto de fórmula ii, uso do composto e composição farmacêutica compreendendo dito composto
WO2012053939A2 (en) 2010-10-20 2012-04-26 Rawllin International Inc Mobile device
AR083502A1 (es) 2010-10-21 2013-02-27 Biomarin Pharm Inc Sal tosilada de (8s,9r)-5-fluoro-8-(4-fluorofenil)-9-(1-metil-1h-1,2,4-triazol-5-il)-8,9-dihidro-2h-pirido[4,3,2-de]ftalazin-3(7h)-ona cristalina
FR2967674B1 (fr) 2010-11-23 2012-12-14 Pf Medicament Derives d'heteroarylsulfonamides, leur preparation et leur application en therapeutique humaine
JP5907986B2 (ja) 2010-11-29 2016-04-26 ガリオン ファーマシューティカルズ インコーポレイテッド 呼吸制御障害または呼吸制御疾患の処置用の呼吸刺激薬としての化合物
EP2651898B1 (en) 2010-12-17 2015-12-09 Agios Pharmaceuticals, Inc. Novel n-(4-(azetidine-1-carbonyl)phenyl)-(hetero-)arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
US9328077B2 (en) 2010-12-21 2016-05-03 Agios Pharmaceuticals, Inc Bicyclic PKM2 activators
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
HUE065700T2 (hu) 2011-05-03 2024-06-28 Agios Pharmaceuticals Inc Piruvát-kináz aktivátorok terápiában történõ alkalmazásra
CN103608016A (zh) 2011-05-03 2014-02-26 安吉奥斯医药品有限公司 丙酮酸激酶激活剂在治疗中的用途
TW201636330A (zh) 2011-05-24 2016-10-16 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
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
WO2013056153A1 (en) 2011-10-13 2013-04-18 Kung Charles 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
CA2860623A1 (en) 2012-01-06 2013-07-11 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
WO2013107405A1 (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)
EP2824099A4 (en) 2012-03-09 2015-11-11 Carna Biosciences Inc NOVEL TRIAZINE DERIVATIVE
WO2014015422A1 (en) 2012-07-27 2014-01-30 Ontario Institute For Cancer Research Cellulose-based nanoparticles for drug delivery
JP6385352B2 (ja) 2012-10-15 2018-09-05 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 治療化合物および組成物
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
PL3307271T3 (pl) 2015-06-11 2024-02-05 Agios Pharmaceuticals, Inc. Sposoby stosowania aktywatorów kinazy pirogronianowej
SG11202004587XA (en) * 2017-11-22 2020-06-29 Agios Pharmaceuticals Inc Crystalline forms of n-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

Also Published As

Publication number Publication date
RU2561132C2 (ru) 2015-08-20
SG10201403696UA (en) 2014-10-30
CY1119443T1 (el) 2018-03-07
IN2012DN00471A (enExample) 2015-06-05
FIC20230017I1 (fi) 2023-05-02
SMT201700309T1 (it) 2017-07-18
US10988448B2 (en) 2021-04-27
JP2015028083A (ja) 2015-02-12
SG177434A1 (en) 2012-02-28
US20170183311A1 (en) 2017-06-29
AU2010266386C1 (en) 2017-03-09
TW201731828A (zh) 2017-09-16
EP3241554A1 (en) 2017-11-08
TW201520197A (zh) 2015-06-01
CN104817498B (zh) 2018-06-01
LT2448582T (lt) 2017-07-10
TWI691493B (zh) 2020-04-21
RU2012102922A (ru) 2013-08-10
NZ622505A (en) 2015-12-24
TW201930288A (zh) 2019-08-01
LUC00306I2 (enExample) 2025-09-22
PT2448582T (pt) 2017-07-10
US20190241523A1 (en) 2019-08-08
US8785450B2 (en) 2014-07-22
DK2448582T3 (en) 2017-07-17
US20190345109A1 (en) 2019-11-14
JP2012532137A (ja) 2012-12-13
CL2011003350A1 (es) 2012-06-08
IL217277A (en) 2016-06-30
CO6480955A2 (es) 2012-07-16
HUS2300018I1 (hu) 2023-05-28
US11866411B2 (en) 2024-01-09
NZ597379A (en) 2014-04-30
KR20120107454A (ko) 2012-10-02
JP5856052B2 (ja) 2016-02-09
US10029987B2 (en) 2018-07-24
US20140323467A1 (en) 2014-10-30
ZA201200054B (en) 2013-10-30
HRP20170955T1 (hr) 2017-11-17
USRE49582E1 (en) 2023-07-18
UA107667C2 (uk) 2015-02-10
EP3708169A1 (en) 2020-09-16
US20210198206A1 (en) 2021-07-01
HUE032969T2 (en) 2017-11-28
TWI649313B (zh) 2019-02-01
TWI598337B (zh) 2017-09-11
NI201200003A (es) 2012-11-12
CA2766882C (en) 2016-11-22
NO2023017I1 (no) 2023-04-27
MX2012000256A (es) 2012-04-19
AU2010266386A1 (en) 2012-02-02
SI2448582T1 (sl) 2017-09-29
CA2944788A1 (en) 2011-01-06
CN104817498A (zh) 2015-08-05
US20100331307A1 (en) 2010-12-30
BRPI1011587B1 (pt) 2020-03-24
IL217277A0 (en) 2012-02-29
US12428376B2 (en) 2025-09-30
EP2448582A1 (en) 2012-05-09
KR20170012585A (ko) 2017-02-02
NL301230I2 (nl) 2023-07-26
KR101850813B1 (ko) 2018-04-20
SG10201811480WA (en) 2019-01-30
CY2023012I2 (el) 2023-11-15
CR20120001A (es) 2012-02-16
TW201103913A (en) 2011-02-01
ECSP11011567A (es) 2012-02-29
EP3241554B1 (en) 2020-01-29
KR101712035B1 (ko) 2017-03-03
PE20120693A1 (es) 2012-07-04
EP2448582B1 (en) 2017-04-19
US20240360083A1 (en) 2024-10-31
CN102481300B (zh) 2015-04-15
CA2944788C (en) 2023-08-22
LTPA2023513I1 (enExample) 2023-05-25
CN102481300A (zh) 2012-05-30
FR23C1017I1 (fr) 2023-06-23
AR077292A1 (es) 2011-08-17
WO2011002817A1 (en) 2011-01-06
MY191825A (en) 2022-07-18
CR20170071A (es) 2017-03-28
CA2766882A1 (en) 2011-01-06
BRPI1011587A2 (pt) 2016-03-22
PL2448582T3 (pl) 2017-09-29
AU2010266386B2 (en) 2016-06-23
LTC2448582I2 (enExample) 2025-04-25
CY2023012I1 (el) 2023-11-15
EP2448582A4 (en) 2012-11-28
TWI472522B (zh) 2015-02-11
FR23C1017I2 (fr) 2024-03-22

Similar Documents

Publication Publication Date Title
ES2632954T3 (es) Derivados de quinolina-8-sulfonamida que tienen una actividad anticancerosa
ES2569712T3 (es) Activadores de PKM2 bicíclicos
HK1246195A1 (en) Quinoline-8-sulfonamide derivatives having an anticancer activity
HK1170153A (en) Quinoline-8-sulfonamide derivatives having an anticancer activity
HK1170153B (en) Quinoline-8-sulfonamide derivatives having an anticancer activity