TWI691493B - 治療化合物及組成物 - Google Patents

治療化合物及組成物 Download PDF

Info

Publication number
TWI691493B
TWI691493B TW107138088A TW107138088A TWI691493B TW I691493 B TWI691493 B TW I691493B TW 107138088 A TW107138088 A TW 107138088A TW 107138088 A TW107138088 A TW 107138088A TW I691493 B TWI691493 B TW I691493B
Authority
TW
Taiwan
Prior art keywords
compound
nmr
specific examples
mhz
piper
Prior art date
Application number
TW107138088A
Other languages
English (en)
Chinese (zh)
Other versions
TW201930288A (zh
Inventor
G. 薩利圖羅法蘭西斯寇
O. 紹德斯傑佛瑞
顏順君
Original Assignee
美商阿吉歐斯製藥公司
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=TWI691493(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 美商阿吉歐斯製藥公司 filed Critical 美商阿吉歐斯製藥公司
Publication of TW201930288A publication Critical patent/TW201930288A/zh
Application granted granted Critical
Publication of TWI691493B publication Critical patent/TWI691493B/zh

Links

Images

Classifications

    • 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
    • A61K31/495—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
    • 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
    • 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
    • C07D215/38—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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (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)
TW107138088A 2009-06-29 2010-06-29 治療化合物及組成物 TWI691493B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW201930288A TW201930288A (zh) 2019-08-01
TWI691493B true TWI691493B (zh) 2020-04-21

Family

ID=43381412

Family Applications (4)

Application Number Title Priority Date Filing Date
TW107138088A TWI691493B (zh) 2009-06-29 2010-06-29 治療化合物及組成物
TW99121186A TWI472522B (zh) 2009-06-29 2010-06-29 治療化合物及組成物
TW106118093A TWI649313B (zh) 2009-06-29 2010-06-29 治療化合物及組成物
TW104100537A TWI598337B (zh) 2009-06-29 2010-06-29 治療化合物及組成物

Family Applications After (3)

Application Number Title Priority Date Filing Date
TW99121186A TWI472522B (zh) 2009-06-29 2010-06-29 治療化合物及組成物
TW106118093A TWI649313B (zh) 2009-06-29 2010-06-29 治療化合物及組成物
TW104100537A TWI598337B (zh) 2009-06-29 2010-06-29 治療化合物及組成物

Country Status (41)

Country Link
US (8) US8785450B2 (enExample)
EP (3) EP3241554B1 (enExample)
JP (2) JP5856052B2 (enExample)
KR (2) KR101850813B1 (enExample)
CN (2) CN104817498B (enExample)
AR (1) AR077292A1 (enExample)
AU (1) AU2010266386C1 (enExample)
BR (1) BRPI1011587B1 (enExample)
CA (2) CA2766882C (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 (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
JP5756457B2 (ja) 2009-04-06 2015-07-29 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 ピルビン酸キナーゼｍ２調節剤、治療組成物および関連する使用方法
CA2760929C (en) 2009-05-04 2018-01-02 Agios Pharmaceuticals, Inc. Pkm2 activators for use in the treatment of cancer
SG177384A1 (en) 2009-06-29 2012-02-28 Incyte Corp Pyrimidinones as pi3k inhibitors
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
PE20120693A1 (es) 2009-06-29 2012-07-04 Agios Pharmaceuticals Inc Compuestos heterociclos como moduladores de la piruvato cinasa m2 (pkm2)
EP3064595B1 (en) 2009-10-21 2019-02-27 Agios Pharmaceuticals, Inc. Methods for cell-proliferation-related disorders
CA2793836C (en) 2009-10-21 2020-03-24 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
WO2011072174A1 (en) * 2009-12-09 2011-06-16 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
US9193721B2 (en) 2010-04-14 2015-11-24 Incyte Holdings Corporation Fused derivatives as PI3Kδ inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
US8692001B2 (en) 2010-10-27 2014-04-08 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
JP5837091B2 (ja) 2010-12-17 2015-12-24 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 ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体
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
US9108984B2 (en) 2011-03-14 2015-08-18 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
US9388164B2 (en) 2011-05-03 2016-07-12 Agios Pharmaceuticals, Inc Methods of using pyruvate kinase activators
WO2012151452A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
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
CN103764147B (zh) * 2011-05-03 2018-05-22 安吉奥斯医药品有限公司 用于治疗的丙酮酸激酶活化剂
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
PL3196202T3 (pl) 2011-09-02 2019-09-30 Incyte Holdings Corporation Heterocykloaminy jako inhibitory pi3k
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
HK1213798A1 (zh) 2012-10-15 2016-07-15 安吉奥斯医药品有限公司 治療性化合物和組合物
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
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
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
WO2015003355A2 (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
WO2015003360A2 (en) 2013-07-11 2015-01-15 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
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
JP6564796B2 (ja) 2014-03-14 2019-08-21 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 治療活性化合物の医薬組成物
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
MD3831833T2 (ro) 2015-02-27 2023-04-30 Incyte Holdings Corp Procedee pentru prepararea unui inhibitor PI3K
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
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
AU2016276951B2 (en) 2015-06-11 2020-10-08 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
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
LT3362066T (lt) 2015-10-15 2022-02-10 Les Laboratoires Servier Sas Kombinuota terapija, skirta piktybinių susirgimų gydymui
MD3448859T2 (ro) 2017-03-20 2020-03-31 Forma Therapeutics Inc Compoziții de pirolopirol în calitate de activatori ai piruvatkinazei (PKR)
JP7301040B2 (ja) 2017-08-15 2023-06-30 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 ピルビン酸キナーゼ調節因子およびその使用
WO2019099651A1 (en) * 2017-11-16 2019-05-23 Agios Pharmaceuticals, Inc. Methods of using deuterated pyruvate kinase activators
TWI808108B (zh) * 2017-11-22 2023-07-11 美商阿吉歐斯製藥公司 N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型
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
IL279152B2 (en) 2018-06-05 2024-09-01 Crinetics Pharmaceuticals Inc Melanocortin subtype-2 receptor antagonists and uses thereof
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
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
EP3972957A1 (en) * 2019-05-22 2022-03-30 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
AU2020350763A1 (en) 2019-09-19 2022-04-07 Novo Nordisk Health Care Ag Pyruvate kinase R (PKR) activating compositions
EP4054583A4 (en) * 2019-11-07 2023-10-25 Crinetics Pharmaceuticals, Inc. MELANOCORTIN SUBTYPE 2 RECEPTOR (MC2R) ANTAGONISTS AND THEIR USES
ES3031394T3 (en) 2019-12-18 2025-07-08 Crinetics Pharmaceuticals Inc Gem-disubstituted piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
EP4081525B1 (en) 2019-12-23 2025-05-21 Crinetics Pharmaceuticals, Inc. Spirocyclic piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
US12286404B2 (en) 2020-01-28 2025-04-29 Teva Pharmaceuticals International Gmbh Solid state forms of Mitapivat and process for preparation thereof
CA3196829A1 (en) 2020-09-25 2022-03-31 Agios Pharmaceuticals, Inc. Pharmaceutical formulation
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
CA3211644A1 (en) 2021-03-19 2022-09-22 Christine FERRARA-COOK Melanocortin subtype-2 receptor (mc2r) antagonist for the treatment of disease
WO2022232460A1 (en) 2021-04-30 2022-11-03 Agios Pharmaceuticals, Inc. Methods for titrating mitapivat
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
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
CA3238252A1 (en) 2021-11-19 2023-05-25 Amit Choudhary Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof
KR20240124324A (ko) 2021-12-21 2024-08-16 시노허브 파마슈티컬 씨오., 엘티디 비스(아자니릴리덴)설포닐 구조를 함유하는 화합물 및 약제에서의 이의 용도
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
WO2024238709A2 (en) * 2023-05-18 2024-11-21 Concarlo Therapeutics, Inc. Small molecule inhibitors of p27
WO2024245143A1 (zh) 2023-05-26 2024-12-05 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5834485A (en) * 1996-05-20 1998-11-10 Chiroscience Limited Quinoline sulfonamides and their therapeutic use
US6313127B1 (en) * 1996-02-02 2001-11-06 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
TWI472522B (zh) * 2009-06-29 2015-02-11 Agios Pharmaceuticals Inc 治療化合物及組成物

Family Cites Families (263)

* 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
NL80628C (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
FI855180L (fi) 1985-01-18 1986-07-19 Nissan Chemical Ind Ltd Pyrazolsulfonamidderivat, foerfarande foer dess framstaellande och det innehaollande ograesgift.
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
DK0385237T3 (da) 1989-03-03 1994-07-25 Dainippon Pharmaceutical Co 2-(1-Piperazinyl)-4-phenylcycloalkanopyridinderivater, fremgangsmåde til fremstilling deraf og farmaceutisk præparat indeholdende dem
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
CA2096527A1 (en) 1990-12-31 1992-07-01 Brett H. Bussler Reducing 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
DE69322076D1 (de) 1992-02-28 1998-12-17 Zenyaku Kogyo Kk S-triazin-derivate und diese als aktiven wirkstoff enthaltende heilmittel gegen östrogen abhängige krankheiten
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
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
IL115420A0 (en) * 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
RU2126001C1 (ru) * 1995-01-10 1999-02-10 Самдзин Фармасьютикал Ко., Лтд Производные пиперазина и фармацевтическая композиция на их основе
ATE382041T1 (de) 1995-01-20 2008-01-15 Searle Llc Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
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
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
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
US5843485A (en) * 1996-06-28 1998-12-01 Incoe Corporation Valve-gate bushing for gas-assisted injection molding
WO1998002434A1 (en) 1996-07-13 1998-01-22 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
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
WO1998040379A1 (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
JP3887769B2 (ja) 1997-12-22 2007-02-28 バイエル コーポレイション 対称および非対称ジフェニル尿素を用いるｐ３８キナーゼの阻害
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
AU754204B2 (en) * 1998-09-01 2002-11-07 Bristol-Myers Squibb Company Potassium channel inhibitors and method
DE19841985A1 (de) 1998-09-03 2000-03-09 Schering Ag Dialkylsulfonsäure- und Dialkylcarbonsäure-Derivate
JP2002527359A (ja) 1998-09-18 2002-08-27 ビーエーエスエフ アクチェンゲゼルシャフト キナーゼインヒビターとしての４−アミノピロリピリミジン
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
AU5379900A (en) 1999-06-07 2000-12-28 Shire Biochem 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
US6596772B1 (en) 1999-08-27 2003-07-22 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
JP4744050B2 (ja) 1999-09-17 2011-08-10 ミレニアム・ファーマシューティカルズ・インコーポレイテッド ベンズアミドおよび関連するＸａ因子阻害剤
WO2001019798A2 (en) 1999-09-17 2001-03-22 Cor Therapeutics Inc. 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
US6723730B2 (en) 2000-07-20 2004-04-20 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
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
JP2004529164A (ja) * 2001-05-07 2004-09-24 スミスクライン・ビーチャム・コーポレイション スルホンアミド
WO2002095063A1 (en) 2001-05-23 2002-11-28 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. 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
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
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
DE60226875D1 (de) 2001-08-15 2008-07-10 Du Pont Orthosubstituierte arylamide zur bekämpfung von wirbellosen schädlingen
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
US7148236B2 (en) 2002-01-17 2006-12-12 Merck & Co., Inc. Modulators of acetylcholine receptors
CN100383124C (zh) * 2002-02-04 2008-04-23 霍夫曼-拉罗奇有限公司 作为npy拮抗剂的喹啉衍生物
US20040180889A1 (en) 2002-03-01 2004-09-16 Pintex Pharmaceuticals, Inc. Pin1-modulating compounds and methods of use thereof
ES2322950T3 (es) * 2002-03-13 2009-07-02 Janssen Pharmaceutica Nv Derivados de aminocarbonilo como nuevos inhibidores de histona-desacetilasa.
BR0307575A (pt) 2002-03-13 2004-12-21 Janssen Pharmaceutica Nv Derivados de sulfonila como inibidores de histona desacetilase
DK1497266T3 (da) * 2002-03-27 2008-10-06 Glaxo Group Ltd Quinolinderivater og deres anvendelse som 5HT6-ligander
WO2003093297A2 (en) 2002-05-03 2003-11-13 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
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
AU2003274373A1 (en) 2002-10-24 2004-05-13 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
US7361691B2 (en) 2002-12-02 2008-04-22 Arqule, Inc. Method of treating cancers using β-lapachone or analogs or derivatives thereof
EP1590364B1 (en) 2002-12-16 2011-10-05 Genmab A/S Human monoclonal antibodies against interleukin 8 (il-8)
EP1587519A4 (en) 2003-01-10 2006-05-31 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
DE602004011603T2 (de) * 2003-02-19 2009-01-29 F. Hoffmann-La Roche Ag Sulfonamidsubstituierte xanthinderivate zur verwendung als pepck-inhibitoren
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
WO2004086865A1 (en) * 2003-03-27 2004-10-14 Cytokinetics, Inc. Compounds, compositions and methods
CA2520546A1 (en) * 2003-03-28 2005-02-10 Janssen Pharmaceutica, N.V. Benzo[1,2,5]thiadiazole compounds
EP1618090A1 (en) 2003-04-11 2006-01-25 Novo Nordisk A/S 11ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS
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
WO2005035507A2 (en) 2003-10-10 2005-04-21 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
MXPA06008157A (es) 2003-12-24 2007-09-07 Johnson & Johnson Tratamiento de gliomas malignos con inhibidores de factor de crecimiento transformante-beta.
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
WO2005117591A2 (en) 2004-05-28 2005-12-15 Andrx Labs Llc Novel 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
AR051094A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
US7622486B2 (en) 2004-09-23 2009-11-24 Reddy Us Therapeutics, Inc. 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
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
WO2006063294A2 (en) * 2004-12-09 2006-06-15 Kalypsys, Inc. Novel inhibitors of histone deacetylase for the treatment of disease
WO2006070198A1 (en) 2004-12-30 2006-07-06 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
JPWO2006077821A1 (ja) 2005-01-19 2008-06-19 大日本住友製薬株式会社 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
CA2594708A1 (en) 2005-01-25 2006-08-03 Astrazeneca Ab Chemical compounds
EP1853586B1 (en) * 2005-02-18 2013-07-24 AstraZeneca AB Antibacterial piperidine derivatives
EP1879877B8 (en) 2005-05-03 2013-02-13 Ranbaxy Laboratories Limited Antimicrobial agents
JP2008540586A (ja) 2005-05-18 2008-11-20 フォルシュングスフェアブント ベルリン エー ファウ Ａｋａｐ−ｐｋａ相互作用の非ペプチド阻害剤
CA2611728A1 (en) 2005-06-08 2006-12-14 Millennium Pharmaceuticals, Inc. Methods for the identification, assessment, and treatment of patients with cancer therapy
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
EP1910321A4 (en) * 2005-07-05 2010-09-01 Astrazeneca Ab NEW COMPOUNDS, METHOD FOR THE PRODUCTION THEREOF, INTERMEDIATE PRODUCTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT OF 5-HT6-MEDIATED ILLNESSES SUCH AS ALZHEIMER'S DISEASE, COGNITIVE ILLUSTRATIONS, SCHOISOPHRENIC ASSOCIATED COGNITIVE DISORDERS, OBESITAS AND PARKINSON DISEASE
WO2007008143A1 (en) 2005-07-08 2007-01-18 Astrazeneca Ab Heterocyclic sulfonamide derivatives as inhibitors of factor xa
CA2618479C (en) * 2005-08-26 2014-12-30 Laboratoires Serono S.A. Pyrazine derivatives and use 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
US20090048227A1 (en) * 2005-12-22 2009-02-19 Chakravarty Pasun K Substituted-1-Phthalazinamines As Vr- 1 Antagonists
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
EP2004619A1 (en) * 2006-03-23 2008-12-24 Amgen Inc. 1-phenylsulfonyl-diaza heterocyclic amide compounds and their uses as modulators of hydroxsteroid dehydrogenases
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
WO2008019139A2 (en) 2006-08-04 2008-02-14 Beth Israel Deaconess Medical Center Inhibitors of pyruvate kinase and methods of treating disease
WO2008024284A2 (en) 2006-08-21 2008-02-28 Merck & Co., Inc. Sulfonylated piperazines as cannabinoid-1 receptor modulators
EP2059809B1 (en) 2006-08-30 2014-07-23 Metanomics GmbH Means and method for diagnosing hemolytic anemia
ES2382481T3 (es) 2006-09-01 2012-06-08 Otsuka Agritechno Co., Ltd Compuesto de N-piridilpiperidina, método para producir el mismo, y agente de control de plagas
EP2074345B1 (en) 2006-10-12 2011-01-05 Fluid Automation Systems S.A. Rocker valve mechanism and rocker valve
EP2527345B1 (en) 2006-10-16 2015-12-16 Thesan Pharmaceuticals, Inc. Therapeutic pyrazolyl thienopyridines
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
JP2010511727A (ja) 2006-12-04 2010-04-15 ニューロクライン バイオサイエンシーズ，インコーポレイテッド アデノシン受容体アンタゴニストとしての置換ピリミジン
SG10201504425SA (en) 2006-12-08 2015-07-30 Millennium Pharm Inc Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
ES2699585T3 (es) 2006-12-15 2019-02-11 Nantbio Inc Derivados de triazina y sus aplicaciones terapéuticas
US7897776B2 (en) * 2007-04-23 2011-03-01 Salutria Pharmaceuticals Llc 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
US20090029992A1 (en) 2007-06-11 2009-01-29 Agoston Gregory E Substituted pyrazole compounds
UA99624C2 (uk) 2007-07-18 2012-09-10 Янссен Фармацевтика Н.В. Сульфонаміди як trpm8-модулятори
JP5506674B2 (ja) 2007-07-20 2014-05-28 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な置換インダゾール誘導体
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
CA2702171A1 (en) 2007-10-10 2009-04-16 Takeda Pharmaceutical Company Limited Amide compound
AR069037A1 (es) * 2007-10-26 2009-12-23 Syngenta Participations Ag Derivados de piridin-imidazol y procedimientos para prepararlos
EP2053045A1 (en) 2007-10-26 2009-04-29 Syngenta Participations AG Novel imidazole derivatives
JP2011507910A (ja) 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
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
US20100144722A1 (en) 2008-09-03 2010-06-10 Dr. Reddy's Laboratories Ltd. Novel heterocyclic compounds as gata modulators
WO2010028099A1 (en) 2008-09-03 2010-03-11 The Johns Hopkins University Genetic alterations in 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
JP5632379B2 (ja) 2008-10-09 2014-11-26 アメリカ合衆国 ヒトピルビン酸キナーゼ活性化剤
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
RU2535217C2 (ru) 2009-02-06 2014-12-10 Ниппон Синяку Ко., Лтд. Производные аминопиразина и лекарственные средства
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
JP5756457B2 (ja) 2009-04-06 2015-07-29 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 ピルビン酸キナーゼｍ２調節剤、治療組成物および関連する使用方法
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
CN105175409A (zh) 2009-06-08 2015-12-23 南特生物科学公司 三嗪衍生物及其治疗应用
KR20120016676A (ko) 2009-06-09 2012-02-24 아브락시스 바이오사이언스, 엘엘씨 우레이도페닐치환 트리아진 유도체와 이들의 치료적 용도
CN102573487A (zh) 2009-06-09 2012-07-11 加利福尼亚资本权益有限责任公司 Hedgehog信号传导的吡啶基-三嗪抑制剂
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
US20120189670A1 (en) 2009-09-14 2012-07-26 Kirkpatrick D Lynn 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
EP3064595B1 (en) 2009-10-21 2019-02-27 Agios Pharmaceuticals, Inc. Methods for cell-proliferation-related disorders
CA2793836C (en) 2009-10-21 2020-03-24 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
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
WO2011072174A1 (en) 2009-12-09 2011-06-16 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
WO2011123618A1 (en) 2010-04-01 2011-10-06 Agios Pharmaceuticals, Inc. Methods of identifying a candidate compound
WO2011137089A1 (en) 2010-04-29 2011-11-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
US20130109643A1 (en) 2010-05-10 2013-05-02 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
US20130184222A1 (en) 2010-07-16 2013-07-18 Agios Pharmaceuticals, Inc Therapeutically active compositions and their methods of use
WO2012053941A2 (en) 2010-10-20 2012-04-26 Rawllin International Inc Mobile device with housing
PL2630146T3 (pl) 2010-10-21 2020-11-02 Medivation Technologies Llc Krystaliczna sól tosylanowa (8S,9R)-5-fluoro-8-(4-fluorofenylo)-9-(1-metylo-1H-1,2,4-triazol-5-ilo)-8,9-dihydro-2H-pirydo[4,3,2-de]ftalazyno-3(7H)-onu
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
JP5837091B2 (ja) 2010-12-17 2015-12-24 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 ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体
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
WO2012151452A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
CN103764147B (zh) 2011-05-03 2018-05-22 安吉奥斯医药品有限公司 用于治疗的丙酮酸激酶活化剂
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
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
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
HUE038403T2 (hu) 2012-01-06 2018-10-29 Agios Pharmaceuticals Inc Terápiásan alkalmazható vegyületek és alkalmazási módszereik
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
MX350432B (es) 2012-01-19 2017-09-06 Agios Pharmaceuticals Inc Compuestos terapeuticamente activos y sus metodos de empleo.
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
HK1213798A1 (zh) 2012-10-15 2016-07-15 安吉奥斯医药品有限公司 治療性化合物和組合物
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
AU2016276951B2 (en) 2015-06-11 2020-10-08 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
TWI808108B (zh) * 2017-11-22 2023-07-11 美商阿吉歐斯製藥公司 N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6313127B1 (en) * 1996-02-02 2001-11-06 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
US5834485A (en) * 1996-05-20 1998-11-10 Chiroscience Limited Quinoline sulfonamides and their therapeutic use
TWI472522B (zh) * 2009-06-29 2015-02-11 Agios Pharmaceuticals Inc 治療化合物及組成物
TWI598337B (zh) * 2009-06-29 2017-09-11 阿吉歐斯製藥公司 治療化合物及組成物

Also Published As

Publication number Publication date
SG177434A1 (en) 2012-02-28
CA2944788C (en) 2023-08-22
NZ622505A (en) 2015-12-24
ES2632954T3 (es) 2017-09-18
EP2448582A1 (en) 2012-05-09
CR20120001A (es) 2012-02-16
KR101712035B1 (ko) 2017-03-03
HRP20170955T1 (hr) 2017-11-17
US10029987B2 (en) 2018-07-24
EP3241554A1 (en) 2017-11-08
US20140323467A1 (en) 2014-10-30
AU2010266386A1 (en) 2012-02-02
CY1119443T1 (el) 2018-03-07
CY2023012I2 (el) 2023-11-15
JP5856052B2 (ja) 2016-02-09
FR23C1017I2 (fr) 2024-03-22
RU2561132C2 (ru) 2015-08-20
ECSP11011567A (es) 2012-02-29
SMT201700309T1 (it) 2017-07-18
DK2448582T3 (en) 2017-07-17
CA2766882A1 (en) 2011-01-06
BRPI1011587B1 (pt) 2020-03-24
BRPI1011587A2 (pt) 2016-03-22
NO2023017I1 (no) 2023-04-27
PE20120693A1 (es) 2012-07-04
KR20120107454A (ko) 2012-10-02
NI201200003A (es) 2012-11-12
KR101850813B1 (ko) 2018-04-20
US20240360083A1 (en) 2024-10-31
IL217277A0 (en) 2012-02-29
CN104817498B (zh) 2018-06-01
TW201103913A (en) 2011-02-01
AU2010266386C1 (en) 2017-03-09
EP2448582B1 (en) 2017-04-19
US20190241523A1 (en) 2019-08-08
CN104817498A (zh) 2015-08-05
MX2012000256A (es) 2012-04-19
US20170183311A1 (en) 2017-06-29
US8785450B2 (en) 2014-07-22
USRE49582E1 (en) 2023-07-18
RU2012102922A (ru) 2013-08-10
FR23C1017I1 (fr) 2023-06-23
NZ597379A (en) 2014-04-30
CY2023012I1 (el) 2023-11-15
HUE032969T2 (en) 2017-11-28
JP2015028083A (ja) 2015-02-12
US11866411B2 (en) 2024-01-09
CL2011003350A1 (es) 2012-06-08
EP3241554B1 (en) 2020-01-29
LTC2448582I2 (enExample) 2025-04-25
AU2010266386B2 (en) 2016-06-23
LTPA2023513I1 (enExample) 2023-05-25
JP2012532137A (ja) 2012-12-13
CA2944788A1 (en) 2011-01-06
TWI649313B (zh) 2019-02-01
US10988448B2 (en) 2021-04-27
TW201930288A (zh) 2019-08-01
TWI598337B (zh) 2017-09-11
LT2448582T (lt) 2017-07-10
TW201731828A (zh) 2017-09-16
UA107667C2 (uk) 2015-02-10
MY191825A (en) 2022-07-18
US20210198206A1 (en) 2021-07-01
CO6480955A2 (es) 2012-07-16
CN102481300B (zh) 2015-04-15
ZA201200054B (en) 2013-10-30
CR20170071A (es) 2017-03-28
WO2011002817A1 (en) 2011-01-06
NL301230I2 (nl) 2023-07-26
LUC00306I2 (enExample) 2025-09-22
EP2448582A4 (en) 2012-11-28
US20190345109A1 (en) 2019-11-14
TW201520197A (zh) 2015-06-01
KR20170012585A (ko) 2017-02-02
HUS2300018I1 (hu) 2023-05-28
SI2448582T1 (sl) 2017-09-29
IN2012DN00471A (enExample) 2015-06-05
CN102481300A (zh) 2012-05-30
US20100331307A1 (en) 2010-12-30
SG10201403696UA (en) 2014-10-30
US12428376B2 (en) 2025-09-30
PT2448582T (pt) 2017-07-10
CA2766882C (en) 2016-11-22
AR077292A1 (es) 2011-08-17
TWI472522B (zh) 2015-02-11
PL2448582T3 (pl) 2017-09-29
FIC20230017I1 (fi) 2023-05-02
IL217277A (en) 2016-06-30
SG10201811480WA (en) 2019-01-30
EP3708169A1 (en) 2020-09-16

Similar Documents

Publication Publication Date Title
TWI691493B (zh) 治療化合物及組成物
HK1246195A1 (en) Quinoline-8-sulfonamide derivatives having an anticancer activity
HK1170153B (en) Quinoline-8-sulfonamide derivatives having an anticancer activity
HK1170153A (en) Quinoline-8-sulfonamide derivatives having an anticancer activity