DK2624696T3 - Benzimidazolderivater som pi3-kinaseinhibitorer - Google Patents

Benzimidazolderivater som pi3-kinaseinhibitorer Download PDF

Info

Publication number
DK2624696T3
DK2624696T3 DK11831214.9T DK11831214T DK2624696T3 DK 2624696 T3 DK2624696 T3 DK 2624696T3 DK 11831214 T DK11831214 T DK 11831214T DK 2624696 T3 DK2624696 T3 DK 2624696T3
Authority
DK
Denmark
Prior art keywords
cancer
leukemia
compound
cell
formula
Prior art date
Application number
DK11831214.9T
Other languages
English (en)
Inventor
Junya Qu
Ralph Rivero
Robert Sanchez
Rosanna Tedesco
Original Assignee
Glaxosmithkline Llc Corp Service Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Llc Corp Service Company filed Critical Glaxosmithkline Llc Corp Service Company
Application granted granted Critical
Publication of DK2624696T3 publication Critical patent/DK2624696T3/da

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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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
    • 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
    • C07D401/10—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 carbon chain containing aromatic 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/10—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 carbon chain containing aromatic rings
    • 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
    • C07D409/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/10—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 carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (14)

1. Forbindelse med formel (la)
som er 2-methyl-1 -{[2-methyl-3-(trifluormethyl)phenyl]methyl}-6-(4- morpholinyl)-1 H-benzimidazol-4-carboxylsyre eller et farmaceutisk accepta-belt salt deraf.
2. Forbindelse ifølge krav 1 med formel (la) som er
2-methyl-1 -{[2-methyl-3-(trifluormethyl)phenyl]methyl}-6-(4- morpholinyl)-1 H-benzimidazol-4-carboxylsyre.
3. Farmaceutisk acceptabelt salt af forbindelsen med formel (la) ifølge krav 1.
4. Farmaceutisk acceptabelt salt af forbindelsen med formel (la) ifølge krav 3, hvor saltet er 1:1 Trissalt.
5. Farmaceutisk sammensætning, som omfatter en forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1 -4 og en farmaceutisk acceptabel bærer.
6. Farmaceutisk sammensætning ifølge krav 5 til anvendelse ved behandling af en modtagelig neoplasme hos et pattedyr med behov herfor.
7. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1-4 til anvendelse i terapi.
8. Kombination af (a) 2-methyl-1-{[2-methyl-3-(trifluormethyl)phenyl]methyl}-6-(4-morpholinyl)-1 H-benzimidazol-4-carboxylsyre eller et farmaceutisk acceptabelt salt deraf og (b) mindst et anti-neoplastisk middel; til anvendelse ved behandling af cancer.
9. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1-4, eller en farmaceutisk sammensæt-ning ifølge krav 5, eller en kombination ifølge krav 8, til anvendelse ved behandling af en PTEN-deficient følsom neoplasme udvalgt blandt hjerne (gli-omer), glioblastomer, leukæmier, Bannayan-Zonanas syndrom, Cowdens sygdom, Lhermitte-Duclos-sygdom, brystcancer, inflammatorisk brystcancer, kolorektal cancer, Wilms tumor, Ewings sarkom, rhabdomyosarkom, epen-dymom, medulloblastom, coloncancer, hoved- og halscancer, nyrecancer, lungecancer, levercancer, melanom, pladecellekarcinom, ovariecancer, pan-creascancer, prostatacancer, sarkom, cancer, osteosarkom, kæmpecelletu-mor i knogle, thyroideacancer, lymfatisk T-celle-leukæmi, kronisk myeloid leukæmi, kronisk lymfatisk leukæmi, hårcelleleukæmi, akut lymfatisk leukæ-mi, akut myeloid leukæmi, kronisk neutrofil leukæmi, akut lymfatisk T-celle-leukæmi, plasmacytom, immunoblastisk storcellet leukæmi, mantle celle-leukæmi, myelomatose, megakaryoblastleukæmi, akut megakaryocytleukæ-mi, promyelocytleukæmi, erythroleukæmi, malignt lymfom, Hodgkins lymfom, non-Hodgkins lymfom, lymfoblastært T-celle-lymfom, Burkitts lymfom, folliku-lært lymfom, neuroblastom, blærecancer, urotelial cancer, vulvacancer, cer-vixcancer, endometriecancer, renal cancer, mesotheliom, øsofaguscancer, spytkirtelcancer, hepatocellulær cancer, gastrisk cancer, nasopharynxcancer, kindcancer, mundcancer, GIST (gastrointestinal stromal tumor) og testikel-cancer.
10. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf til anvendelse, eller en farmaceutisk sammensætning til anvendelse, eller en kombination til anvendelse, ifølge krav 9, hvor den PTEN-deficiente neoplasme er udvalgt blandt prostatacancer, ikke-småcellet lungecancer, endometriecancer, gastrisk cancer, melanom, hoved- og halscancer, brystcancer, herunder triple-negativ brystkræft, og gliom.
11. Forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf til anvendelse, eller en farmaceutisk sammensætning til anvendelse, eller en kombination til anvendelse, ifølge krav 10, hvor prostatacanceren er hormon-refraktær prostatacancer.
12. Anvendelse af en forbindelse med formel (la) eller et farmaceutisk acceptabelt salt deraf, ifølge et hvilket som helst af kravene 1-4 til fremstilling af et lægemiddel til anvendelse ved behandling af en PTEN-deficient følsom neo-plasme, som er udvalgt blandt hjerne (gliomer), glioblastomer, leukæmier, Bannayan-Zonanas syndrom, Cowdens sygdom, Lhermitte-Duclos-sygdom, brystcancer, inflammatorisk brystcancer, kolorektal cancer, Wilms tumor, Ewings sarkom, rhabdomyosarkom, ependymom, medulloblastom, colon-cancer, hoved- og halscancer, nyrecancer, lungecancer, levercancer, mela-nom, pladecellekarcinom, ovariecancer, pancreascancer, prostatacancer, sarkom, cancer, osteosarkom, kæmpecelletumor i knogle, thyroideacancer, lymfatisk T-celle-leukæmi, kronisk myeloid leukæmi, kronisk lymfatisk leu-kæmi, hårcelleleukæmi, akut lymfatisk leukæmi, akut myeloid leukæmi, kronisk neutrofil leukæmi, akut lymfatisk T-celle-leukæmi, plasmacytom, im-munoblastisk storcellet leukæmi, mantle celle-leukæmi, myelomatose, mega-karyoblastleukæmi, akut megakaryocytleukæmi, promyelocytleukæmi, eryt-hroleukæmi, malignt lymfom, Hodgkins lymfom, non-Hodgkins lymfom, lym-foblastært T-celle-lymfom, Burkitts lymfom, follikulært lymfom, neuroblastom, blærecancer, urotelial cancer, vulvacancer, cervixcancer, endometriecancer, renal cancer, mesotheliom, øsofaguscancer, spytkirtelcancer, hepatocellulær cancer, gastrisk cancer, nasopharynxcancer, kindcancer, mundcancer, GIST (gastrointestinal stromal tumor) og testikelcancer.
13. Anvendelse ifølge krav 12, hvor den PTEN-deficiente følsomme neopla-sme er udvalgt blandt prostatacancer, ikke-småcellet lungecancer, endometriecancer, gastrisk cancer, melanom, hoved- og halscancer, brystcancer, herunder triple-negativ brystkræft, og gliom.
14. Anvendelse ifølge krav 13, hvor prostatacanceren er hormonrefraktær prostatacancer.
DK11831214.9T 2010-10-06 2011-09-23 Benzimidazolderivater som pi3-kinaseinhibitorer DK2624696T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US39031410P 2010-10-06 2010-10-06
US201161528397P 2011-08-29 2011-08-29
PCT/US2011/052857 WO2012047538A1 (en) 2010-10-06 2011-09-23 Benzimidazole derivatives as pi3 kinase inhibitors

Publications (1)

Publication Number Publication Date
DK2624696T3 true DK2624696T3 (da) 2017-03-13

Family

ID=45925614

Family Applications (1)

Application Number Title Priority Date Filing Date
DK11831214.9T DK2624696T3 (da) 2010-10-06 2011-09-23 Benzimidazolderivater som pi3-kinaseinhibitorer

Country Status (37)

Country Link
US (10) US20130196990A1 (da)
EP (2) EP3170813B1 (da)
JP (1) JP5719028B2 (da)
KR (1) KR101594002B1 (da)
CN (1) CN103124496B (da)
AR (1) AR083296A1 (da)
AU (1) AU2011312594B2 (da)
BR (1) BR112013008259A2 (da)
CA (1) CA2812608C (da)
CL (1) CL2013000935A1 (da)
CO (1) CO6700852A2 (da)
CR (1) CR20130192A (da)
CY (1) CY1118792T1 (da)
DK (1) DK2624696T3 (da)
DO (1) DOP2013000059A (da)
EA (1) EA022623B1 (da)
ES (2) ES2616238T3 (da)
HR (1) HRP20170279T1 (da)
HU (1) HUE033209T2 (da)
IL (1) IL225140A (da)
JO (1) JO3194B1 (da)
LT (1) LT2624696T (da)
MA (1) MA34591B1 (da)
ME (1) ME02663B (da)
MX (1) MX337662B (da)
MY (1) MY170236A (da)
NZ (1) NZ608069A (da)
PE (1) PE20140192A1 (da)
PL (1) PL2624696T3 (da)
PT (1) PT2624696T (da)
RS (1) RS55662B1 (da)
SG (1) SG188974A1 (da)
SI (1) SI2624696T1 (da)
TW (1) TWI513690B (da)
UY (1) UY33648A (da)
WO (1) WO2012047538A1 (da)
ZA (1) ZA201301951B (da)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ME02663B (me) * 2010-10-06 2017-06-20 Glaxosmithkline Llc Derivati benzimidazola kao inhibitori pi3 kinaze
US8778937B2 (en) * 2011-12-20 2014-07-15 Glaxosmithkline Llc Benzimidazole boronic acid derivatives as PI3 kinase inhibitors
RU2015132907A (ru) * 2013-01-09 2017-02-14 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Комбинация
WO2015042029A1 (en) * 2013-09-19 2015-03-26 Glaxosmithkline Llc Combination drug therapy
WO2015042027A1 (en) * 2013-09-19 2015-03-26 Glaxosmithkline Llc Combination drug therapy
RU2663999C2 (ru) * 2013-10-16 2018-08-14 Шанхай Инли Фармасьютикал Ко., Лтд Конденсированное гетероциклическое соединение, способ его получения, его фармацевтическая композиция и применения
CN103910682B (zh) * 2013-11-28 2016-03-02 大连理工大学 一种基于邻苯二胺环化的苯并咪唑类化合物制备方法
US20160310477A1 (en) * 2013-12-20 2016-10-27 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of mek type 1 and erk inhibitors
CN106573922A (zh) 2014-06-13 2017-04-19 吉利德科学公司 磷脂酰肌醇3‑激酶抑制剂
MX2016016530A (es) 2014-06-13 2017-03-27 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-quinasa.
WO2015191745A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
JP6383810B2 (ja) 2014-06-13 2018-08-29 ギリアード サイエンシーズ， インコーポレイテッド ホスファチジルイノシトール３−キナーゼ阻害剤としてのキナゾリノン誘導体
ES2833025T3 (es) 2014-06-13 2021-06-14 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-quinasa
DK3233862T3 (da) * 2014-12-19 2019-10-07 Janssen Pharmaceutica Nv Imidazopyridazinderivater som pi3k-beta-inhibitorer
ES2760507T3 (es) 2014-12-19 2020-05-14 Janssen Pharmaceutica Nv Derivados de imidazopiridazina enlazados a heterociclilo como inhibidores de PI3Kß
GB201504689D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
BR112018007068B1 (pt) 2015-10-09 2024-01-02 Janssen Pharmaceutica N.V. Derivados de quinoxalina e piridopirazina como inibidores de pi3kbeta, seu uso e composição farmacêutica que os compreende
WO2017121684A1 (en) * 2016-01-14 2017-07-20 Bayer Pharma Aktiengesellschaft 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridines
KR102472198B1 (ko) * 2016-06-16 2022-11-28 얀센 파마슈티카 엔.브이. Pi3k 베타 저해제로서의 아자벤즈이미다졸 유도체
CN109311875A (zh) 2016-06-16 2019-02-05 詹森药业有限公司 作为PI3Kβ抑制剂的二环吡啶、二环吡嗪、和二环嘧啶衍生物
US10960008B2 (en) * 2016-07-11 2021-03-30 Dana-Farber Cancer Institute, Inc. Methods for treating PTEN deficient epithelial cancers using a combination of anti-PI3KBETA and anti-immune checkpoint agents
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
WO2018057808A1 (en) 2016-09-23 2018-03-29 Gilead Sciences, Inc. Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
US11459308B2 (en) 2016-12-05 2022-10-04 Microbiotix, Inc. Broad spectrum inhibitors of filoviruses
KR20190133729A (ko) 2017-03-29 2019-12-03 얀센 파마슈티카 엔.브이. Pi3k-베타 억제제로서 퀴녹살린 및 피리도피라진 유도체
KR102688084B1 (ko) 2017-07-28 2024-07-24 주식회사유한양행 아미노피리미딘 유도체의 개선된 제조방법
WO2019106605A1 (en) 2017-12-01 2019-06-06 Board Of Regents, The University Of Texas System Combination treatment for cancer
US11253189B2 (en) 2018-01-24 2022-02-22 Medtronic Ardian Luxembourg S.A.R.L. Systems, devices, and methods for evaluating neuromodulation therapy via detection of magnetic fields
CN111000847B (zh) * 2020-01-02 2021-03-19 黑龙江中医药大学 一种治疗肺纤维化的药物制剂及其用途
CN111346095B (zh) * 2020-03-14 2021-06-08 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 用于治疗神经外科术后头痛的药物制剂

Family Cites Families (180)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0400835A1 (en) 1989-05-15 1990-12-05 Merck & Co. Inc. Substituted benzimidazoles as angiotensin II antagonists
IL95975A (en) 1989-10-24 1997-06-10 Takeda Chemical Industries Ltd N-benzyl- 2-alkylbenzimidazole derivatives, their production and pharmaceutical compositions containing them
US5559235A (en) 1991-10-29 1996-09-24 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
TW284688B (da) 1991-11-20 1996-09-01 Takeda Pharm Industry Co Ltd
PL175347B1 (pl) 1992-04-03 1998-12-31 Upjohn Co Trójpierścieniowe heterocykliczne aminy aktywne farmaceutycznie
US5502187A (en) 1992-04-03 1996-03-26 The Upjohn Company Pharmaceutically active bicyclic-heterocyclic amines
GB9210400D0 (en) 1992-05-15 1992-07-01 Merck Sharp & Dohme Therapeutic agents
US5342947A (en) 1992-10-09 1994-08-30 Glaxo Inc. Preparation of water soluble camptothecin derivatives
CZ154994A3 (en) 1993-07-02 1995-09-13 Senju Pharma Co Visual hypotensive agent
JPH0867674A (ja) 1993-07-02 1996-03-12 Senju Pharmaceut Co Ltd 眼圧降下剤
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
IL113472A0 (en) 1994-04-29 1995-07-31 Lilly Co Eli Non-peptidyl tachykinin receptor antogonists
US5491237A (en) 1994-05-03 1996-02-13 Glaxo Wellcome Inc. Intermediates in pharmaceutical camptothecin preparation
US5563143A (en) 1994-09-21 1996-10-08 Pfizer Inc. Catechol diether compounds as inhibitors of TNF release
DE19514579A1 (de) 1995-04-20 1996-10-24 Boehringer Ingelheim Kg Verwendung von alpha¶1¶¶L¶-Agonisten zur Behandlung der Harninkontinenz
WO1997025041A1 (en) 1996-01-09 1997-07-17 Eli Lilly And Company Benzimidzolyl neuropeptide y receptor antagonists
AU2139097A (en) 1996-03-01 1997-09-16 Eli Lilly And Company Methods of treating or preventing sleep apnea
CA2248013A1 (en) 1996-03-11 1997-09-18 Eli Lilly And Company Methods of treating or preventing interstitial cystitis
DE69819311T2 (de) 1997-03-07 2004-07-29 Metabasis Therapeutics Inc., San Diego Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
BR0009539A (pt) 1999-04-02 2006-06-06 Neurogen Corp composto, composição farmacêutica, método para tratamento ou prevenção de uma doença ou distúrbio associado com agonismo patogênico, agonismo inverso ou antagonismo do receptor gaba a, uso de um composto, método para localizar receptores gaba a em uma amostra de tecido, método para alterar a atividade transdutora de sinal de receptores gaba a, método para o tratamento ou prevenção de distúrbios psicológicos associados com modulação do complexo receptor gaba a, e, processo para a preparação de um composto
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
JP2000323278A (ja) 1999-05-14 2000-11-24 Toray Ind Inc 発光素子
CA2378047A1 (en) 1999-07-15 2001-01-25 Methvin Isaac Heterocyclic compounds for the treatment of migraine
US6534535B1 (en) 1999-08-12 2003-03-18 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
WO2001021634A1 (en) 1999-09-21 2001-03-29 Lion Bioscience Ag Benzimidazole derivatives and combinatorial libraries thereof
ATE283854T1 (de) 1999-12-03 2004-12-15 Ono Pharmaceutical Co Triazaspiro(5.5)undecan-derivate und drogen, die dasselbe als aktiven inhaltsstoff enthalten
EP1255750A1 (en) 2000-02-01 2002-11-13 Millenium Pharmaceuticals, Inc. INDOLE AND BENZIMIDAZOLE INHIBITORS OF FACTOR Xa
PA8535601A1 (es) 2000-12-21 2002-11-28 Pfizer Derivados benzimidazol y piridilimidazol como ligandos para gabaa
US6472095B2 (en) 2000-12-29 2002-10-29 Utc Fuel Cells, Llc Hybrid fuel cell reactant flow fields
TW593278B (en) 2001-01-23 2004-06-21 Wyeth Corp 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
WO2008108741A1 (en) 2007-03-07 2008-09-12 S*Bio Pte Ltd Combination of benzimidazole anti-cancer agent and a second anti-cancer agent
EP1377549A1 (en) 2001-03-12 2004-01-07 Millennium Pharmaceuticals, Inc. Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
CN1533390A (zh) 2001-03-19 2004-09-29 СҰҩƷ��ҵ��ʽ���� 包含三氮杂螺[5.5]十一烷衍生物作为活性成分的药物组合物
FR2822463B1 (fr) 2001-03-21 2004-07-30 Lipha Derives bicycliques de guanidines et leurs applications en therapeutique
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
PL373300A1 (en) * 2001-03-28 2005-08-22 Bristol-Myers Squibb Company Novel tyrosine kinase inhibitors
TWI236474B (en) 2001-04-03 2005-07-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
HUP0303801A2 (hu) 2001-04-20 2004-03-01 Wyeth Heterociklusos alkoxi-, alkil-tio- és alkil-amino-benzazol-származékok, mint 5-hidroxi-triptamin-6 ligandumok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
JP4323810B2 (ja) 2001-04-20 2009-09-02 ワイス ５−ヒドロキシトリプトアミン−６リガンドとしてのヘテロシクリルオキシ−、−チオキシ−および−アミノベンザゾール誘導体
US7030150B2 (en) 2001-05-11 2006-04-18 Trimeris, Inc. Benzimidazole compounds and antiviral uses thereof
WO2002102978A2 (en) 2001-06-15 2002-12-27 Genentech, Inc. Human growth hormone antagonists
US6841566B2 (en) 2001-07-20 2005-01-11 Boehringer Ingelheim, Ltd. Viral polymerase inhibitors
FR2827862A1 (fr) 2001-07-27 2003-01-31 Lipha Derives imidazolylalkylarylalcanoiques et leurs applications en therapeutique
DE10139416A1 (de) 2001-08-17 2003-03-06 Aventis Pharma Gmbh Aminoalkyl substituierte aromatische Bicyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
FR2829765A1 (fr) 2001-09-14 2003-03-21 Lipha Derives imidazolylalkoxylarylalcanoiques leurs applications en therapeutique
RU2288919C2 (ru) 2001-10-02 2006-12-10 Акадиа Фармасьютикалз, Инк. Производные бензимидазолидинона в качестве агентов мускариновых рецепторов
WO2004089942A2 (en) 2001-10-02 2004-10-21 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
JP4445262B2 (ja) 2001-10-09 2010-04-07 アムジェン インコーポレイテッド 抗炎症剤としてのイミダゾール誘導体
WO2003040114A1 (en) 2001-11-06 2003-05-15 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
EP1460067A4 (en) 2001-11-26 2005-12-07 Takeda Pharmaceutical BICYCLIC DERIVATIVE, PROCESS FOR PRODUCTION OF THE DERIVATIVE, AND USE THEREOF
WO2003062392A2 (en) 2002-01-18 2003-07-31 Ceretek Llc Methods of treating conditions associated with an edg receptor
DE60336633D1 (de) 2002-02-15 2011-05-19 Bridgestone Corp Kautschukzusammensetzung und daraus hergestellter pneumatischer reifen
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
PL401637A1 (pl) 2002-03-13 2013-05-27 Array Biopharma Inc. N3 alkilowane pochodne benzimidazolu jako inhibitory MEK
BR0306016A (pt) 2002-03-13 2005-01-04 Array Biopharma Inc Derivados de benzimidazol n3 alquilado como inibidores da mek
PA8569201A1 (es) 2002-03-13 2004-05-21 Array Biopharma Inc "derivados de bencimidazol n3 alquilado como inhibidores de mek" "n3 alkylated benzimimidazole derivatives as mek inhibitors"
SE0200843D0 (sv) 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
DE10228103A1 (de) 2002-06-24 2004-01-15 Bayer Cropscience Ag Fungizide Wirkstoffkombinationen
DE10229777A1 (de) 2002-07-03 2004-01-29 Bayer Ag Indolin-Phenylsulfonamid-Derivate
US7205412B2 (en) 2002-07-03 2007-04-17 Samsung Electronics Co., Ltd. Antibiotic additive and ink composition comprising the same
JP2005536533A (ja) 2002-08-08 2005-12-02 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 置換ベンゾイミダゾール化合物
US20040063938A1 (en) 2002-09-30 2004-04-01 Pfizer Inc Process for preparing haloalkyl pyrimidines
US20040166137A1 (en) 2002-11-08 2004-08-26 Lackey John William Hetero-substituted benzimidazole compounds and antiviral uses thereof
WO2004052862A1 (ja) 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
US7135493B2 (en) 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
WO2004082621A2 (en) 2003-03-15 2004-09-30 Bethesda Pharmaceuticals, Inc. Novel ppar agonists, pharmaceutical compositions and uses thereof
RU2005134659A (ru) * 2003-04-09 2007-05-27 Джапан Тобакко Инк. (Jp) Гетероароматическое пентациклическое соединение и его применение в медицине
JPWO2004093912A1 (ja) 2003-04-23 2006-07-13 協和醗酵工業株式会社 好中球性炎症疾患の予防および／または治療剤
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
SE0301699D0 (sv) * 2003-06-10 2003-06-10 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
US7563748B2 (en) 2003-06-23 2009-07-21 Cognis Ip Management Gmbh Alcohol alkoxylate carriers for pesticide active ingredients
BRPI0412003A (pt) 2003-07-02 2006-08-15 Sugen Inc arilmetil triazol e imidazopirazinas como inibidores de c-met
US7312215B2 (en) * 2003-07-29 2007-12-25 Bristol-Myers Squibb Company Benzimidazole C-2 heterocycles as kinase inhibitors
DE10342503A1 (de) * 2003-09-12 2005-04-14 Merck Patent Gmbh Benzyl-Benzimidazolylderivate
US7781595B2 (en) 2003-09-22 2010-08-24 S*Bio Pte Ltd. Benzimidazole derivatives: preparation and pharmaceutical applications
WO2005051928A1 (en) 2003-11-28 2005-06-09 Ranbaxy Laboratories Limited Process for production of tetrazolyl compounds
WO2005051929A1 (en) 2003-11-28 2005-06-09 Ranbaxy Laboratories Limited Conversion of aromatic nitriles into tetrazoles
US20050137234A1 (en) 2003-12-19 2005-06-23 Syrrx, Inc. Histone deacetylase inhibitors
WO2005079791A1 (en) 2004-02-12 2005-09-01 Boehringer Ingelheim Pharmaceuticals, Inc. Thiophene -2- carboxylic acid - (1h - benzimidazol - 2 yl) - amide derivatives and related compounds as inhibitors of the tec kinase itk (interleukin -2- inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders
JP4866723B2 (ja) 2004-02-26 2012-02-01 協和発酵キリン株式会社 好中球性炎症疾患の予防及び／または治療剤
ES2318472T3 (es) 2004-03-15 2009-05-01 Eli Lilly And Company Derivados de 5-(5-(aminoetil)-indol-1-ilmetil)-benzamida y compuestos relacionados como antagonistas del receptor opioide para el tratamiento de la obesidad.
RU2006136381A (ru) 2004-03-15 2008-04-27 Анормед, Инк. (Ca) Способ получения антагониста cxcr4
WO2005112932A2 (en) 2004-05-07 2005-12-01 Exelixis, Inc. Raf modulators and methods of use
WO2005118555A1 (en) 2004-06-04 2005-12-15 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2006000020A1 (en) 2004-06-29 2006-01-05 European Nickel Plc Improved leaching of base metals
EP1789045A2 (en) 2004-08-16 2007-05-30 Smithkline Beecham Corporation Chemical compounds
WO2006034003A2 (en) 2004-09-17 2006-03-30 Whitehead Institute For Biomedical Research Compounds, compositions and methods of inhibiting a-synuclein toxicity
US20090005344A1 (en) 2004-11-01 2009-01-01 Nkuada, Llc Compounds and Methods of Use Thereof
WO2007134169A2 (en) 2006-05-10 2007-11-22 Nuada, Llc Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
US20090264384A1 (en) 2004-11-01 2009-10-22 Nuada, Inc. Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof
US8003806B2 (en) 2004-11-12 2011-08-23 OSI Pharmaceuticals, LLC Integrin antagonists useful as anticancer agents
US20100093767A1 (en) 2004-12-03 2010-04-15 Takeda San Diego, Inc. Mitotic Kinase Inhibitors
DE602006016566D1 (de) 2005-01-10 2010-10-14 Bristol Myers Squibb Co Als antikoagulanzien verwendbare phenylglycinamid-derivate
WO2006078907A1 (en) 2005-01-20 2006-07-27 Amgen Inc. 2-substituted benzimidazole derivatives as vanilloid receptor ligands and their use in treatments
CN1834090B (zh) 2005-03-18 2011-06-29 中国科学院上海药物研究所 苯并咪唑类化合物、其制备方法以及用途
US7777040B2 (en) 2005-05-03 2010-08-17 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
WO2006132625A1 (en) 2005-06-03 2006-12-14 Ppg Industries Ohio, Inc. Composition for the vapor phase dehydrohalogenation of 1,1,2-trihaloethane to 1,1-dihaloethylene and methods for preparing and using such compositions
CN101227857B (zh) 2005-06-29 2011-10-19 电脑医师有限公司 具有导电桥的传感器组件
EP1904501A2 (en) 2005-07-11 2008-04-02 Smithkline Beecham Corporation Chemical compounds
JP2007063261A (ja) 2005-08-01 2007-03-15 Kyowa Hakko Kogyo Co Ltd Ｘ線照射による肺障害の予防及び／または治療剤
WO2007023880A1 (ja) 2005-08-24 2007-03-01 Kyowa Hakko Kogyo Co., Ltd. ケモカイン産生阻害剤
US7691885B2 (en) 2005-08-29 2010-04-06 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of kinases
TW200720261A (en) 2005-08-31 2007-06-01 Sankyo Co Phenylene derivatives
TWI393708B (zh) 2005-09-08 2013-04-21 Mei Pharma Inc 異羥肟酸脂化合物，其用途及其之合成方法
WO2007054965A2 (en) 2005-09-23 2007-05-18 Alembic Limited Process for preparation of tetrazoles from aromatic cyano derivatives
GB0520164D0 (en) 2005-10-04 2005-11-09 Novartis Ag Organic compounds
US7465795B2 (en) 2005-12-20 2008-12-16 Astrazeneca Ab Compounds and uses thereof
CA2634305A1 (en) 2005-12-20 2007-06-28 Marc Chapdelaine Substituted cinnoline derivatives as gabaa-receptor modulators and method for their synthesis
CN101389627A (zh) 2005-12-23 2009-03-18 阿斯利康(瑞典)有限公司 具有抗菌作用的吡咯并吡啶、吡咯并嘧啶和吡咯并氮杂
EP2016065B1 (en) 2005-12-28 2012-09-19 Vertex Pharmaceuticals Incorporated 1-(benzo[d][1,3]dioxol-5-yl)-n-(phenyl)cyclopropane-carboxamide derivatives and related compounds as modulators of atp-binding cassette transporters for the treatment of cystic fibrosis
WO2007084390A2 (en) 2006-01-13 2007-07-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP2009525966A (ja) 2006-01-26 2009-07-16 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド タンパク質輸送を調節するための化合物および方法
WO2007091950A1 (en) 2006-02-07 2007-08-16 Astrazeneca Ab Benzimidazoles and imidazopyridines useful in the treatment of diseases or disorders associated with cannabinoid receptor 2 (cb2) such as pain
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
US20090192169A1 (en) 2006-03-31 2009-07-30 Ian Egle Bicyclic Benzimidazole Compounds and Their Use as Metabotropic Glutamate Receptor Potentiators
DE102006025777A1 (de) 2006-05-31 2007-12-06 Merck Patent Gmbh Neue Materialien für organische Elektrolumineszenzvorrichtungen
EP1873157A1 (en) 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
TW200801513A (en) 2006-06-29 2008-01-01 Fermiscan Australia Pty Ltd Improved process
EP1878724A1 (en) 2006-07-15 2008-01-16 sanofi-aventis A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
WO2008012623A1 (en) 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2008019309A1 (en) 2006-08-04 2008-02-14 Metabasis Therapeutics, Inc. Novel inhibitors of fructose 1,6-bisphosphatase
US8236783B2 (en) 2006-08-15 2012-08-07 Duke University ROS-sensitive iron chelators and methods of using the same
WO2008032086A1 (en) * 2006-09-14 2008-03-20 Astrazeneca Ab 2-benzimidazolyl-6-morpholino-4-phenylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
JO3598B1 (ar) 2006-10-10 2020-07-05 Infinity Discovery Inc الاحماض والاسترات البورونية كمثبطات اميد هيدروليز الحامض الدهني
ES2383370T3 (es) 2006-10-19 2012-06-20 Signal Pharmaceuticals Llc Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa
US20080249081A1 (en) 2006-10-24 2008-10-09 Roger Olsson Compounds for the treatment of pain and screening methods therefor
PE20090054A1 (es) 2007-01-23 2009-01-26 Palau Pharma Sa Derivados de purina
WO2008096829A1 (ja) 2007-02-07 2008-08-14 Kyowa Hakko Kirin Co., Ltd. ３環系化合物
EP2134691B1 (en) 2007-03-08 2012-01-25 Janssen Pharmaceutica, N.V. Quinolinone derivatives as parp and tank inhibitors
EP2155719A1 (en) 2007-05-24 2010-02-24 Wyeth LLC Azacyclylbenzamide derivatives as histamine-3 antagonists
TW200906825A (en) 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
AU2008267444A1 (en) 2007-06-26 2008-12-31 Sanofi-Aventis A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
EP2014662A1 (de) 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft Indolylalkylthienopyrimidylamine als Modulatoren des EP2-Rezeptors
EP2014663A1 (de) 2007-07-12 2009-01-14 Bayer Schering Pharma AG Thienopyrimidylamine als Modulatoren des EP2-Rezeptors
CN101828111B (zh) 2007-08-21 2014-07-23 塞诺米克斯公司 人t2r苦味受体及其用途
WO2009027736A2 (en) 2007-08-27 2009-03-05 Astrazeneca Ab 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer
EP2217590A4 (en) 2007-09-17 2011-12-14 Glaxosmithkline Llc Pyridopyrimidine derivatives as PI3-kinase inhibitors
US20090118301A1 (en) 2007-11-02 2009-05-07 Arbor Vita Corporation Compositions and Methods for Treating Cancer
BRPI0819606A2 (pt) 2007-11-27 2017-05-09 Cellzome Ltd amino triazóis como inobidores de pi3k
EP2234487A4 (en) 2007-12-19 2011-09-07 Scripps Research Inst ANILIDES AND ANALOGUES AS INHIBITORS OF RHO KINASE
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
PL2231642T3 (pl) 2008-01-11 2014-04-30 Novartis Ag Pirymidyny jako inhibitory kinazy
CA2712267A1 (en) 2008-01-15 2009-07-23 Wyeth Llc 3h-[1,2,3]triazolo[4,5-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
TW200932218A (en) 2008-01-22 2009-08-01 Boehringer Ingelheim Int Substituted amino-benzimidazoles, medicaments comprising said compound, their use and their method of manufacture
FR2928924B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 6-heteroaryle-imidazo°1,2-a! pyridines, leur preparation et leur application en therapeutique
AU2009228945B2 (en) 2008-03-27 2013-05-02 Janssen Pharmaceutica Nv Quinazolinone derivatives as tubulin polymerization inhibitors
CN101981013B (zh) 2008-03-27 2013-05-29 詹森药业有限公司 作为parp和微管蛋白聚合抑制剂的四氢菲啶酮和四氢环戊二烯并喹啉酮
US20090253161A1 (en) 2008-04-03 2009-10-08 Duke University Fluorescent prochelators for cellular iron detection
JP5637982B2 (ja) 2008-04-09 2014-12-10 インフィニティー ファーマシューティカルズ， インコーポレイテッド 脂肪酸アミド加水分解酵素の阻害剤
AU2009254928A1 (en) 2008-06-04 2009-12-10 Astrazeneca Ab Thiazolo [5, 4-B] pyridine and oxazolo [5, 4-B] pyridine derivatives as antibacterial agents
JP2010031250A (ja) 2008-06-23 2010-02-12 Sumitomo Chemical Co Ltd 組成物及び該組成物を用いてなる発光素子
WO2010000020A1 (en) 2008-06-30 2010-01-07 Cathrx Ltd A catheter
US8846947B2 (en) 2008-07-03 2014-09-30 Glaxosmithkline Llc Benzimidazoles and related analogs as sirtuin modulators
AU2009269087A1 (en) * 2008-07-07 2010-01-14 Xcovery Holding Company Llc PI3K isoform selective inhibitors
WO2010006096A1 (en) 2008-07-11 2010-01-14 Smithkline Beecham Corporation Processes for the preparation of anti-viral compounds and compositions containing them
US8501957B2 (en) 2008-12-10 2013-08-06 China Medical University Benzimidazole compounds and their use as anticancer agents
SI2389372T1 (sl) 2009-01-23 2016-02-29 Rigel Pharmaceuticals, Inc. Sestavki in postopki za inhibicijo poti JAK
KR101411889B1 (ko) 2009-02-27 2014-06-27 이난타 파마슈티칼스, 인코포레이티드 Ｃ형 간염 바이러스 억제제
EP2419551A2 (de) 2009-03-18 2012-02-22 Basf Se Elektrolyt und oberflächenaktive additive für die galvanische abscheidung glatter, dichter aluminium-schichten aus ionischen flüssigkeiten
JP2012520884A (ja) 2009-03-18 2012-09-10 ザ ボード オブ トラスティーズ オブ ザ リランド スタンフォード ジュニア ユニバーシティー フラビウイルス科ウイルス感染症を治療する方法および組成物
US8969342B2 (en) 2009-03-20 2015-03-03 Brandeis University Compounds and methods for treating mammalian gastrointestinal microbial infections
WO2010114726A1 (en) 2009-03-31 2010-10-07 Merck Sharp & Dohme Corp. Aminobenzotriazole derivatives
JP5615902B2 (ja) 2009-04-02 2014-10-29 セントロ ナシオナル デ インベスティガシオネス オンコロヒカス（セエネイオ）Ｃｅｎｔｒｏ Ｎａｃｉｏｎａｌ Ｄｅ Ｉｎｖｅｓｔｉｇａｃｉｏｎｅｓ Ｏｎｃｏｌｏｇｉｃａｓ（Ｃｎｉｏ） イミダゾ［２，１−ｂ］［１，３，４］チアジアゾール誘導体
US20100305093A1 (en) 2009-04-09 2010-12-02 Exelixis, Inc. Inhibitors of mTOR and Methods of Making and Using
MX2011011396A (es) 2009-04-27 2012-01-30 High Point Pharmaceuticals Llc DERIVADOS DE IMIDAZO[1,2-A]PIRIDINA SUSTITUIDA, COMPOSICIONES FARMACEUTICAS Y METODOS DE USO COMO INHIBIDORES DE LA ß-SECRETASA.
WO2010126922A1 (en) 2009-04-30 2010-11-04 Glaxosmithkline Llc Benzimidazolecarboxamides as inhibitors of fak
CN102459249A (zh) 2009-05-22 2012-05-16 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧氮杂环庚三烯以及它们使用与制造方法
JP2012528165A (ja) 2009-05-26 2012-11-12 エクセリクシス， インク． ＰＩ３Ｋ／ｍＴＯＲの阻害剤としてのベンゾキサゼピンならびにそれらの使用および製造方法
WO2010141360A1 (en) 2009-06-05 2010-12-09 Merck Sharp & Dohme Corp. Biaryl benzotriazole derivatives
US9221765B2 (en) 2009-06-10 2015-12-29 North Carolina State University Inhibition and dispersion of bacterial biofilms with benzimidazole derivatives
WO2011000020A1 (en) 2009-06-12 2011-01-06 Sbc Research Pty Ltd Enhanced method of detection
JP2011003793A (ja) 2009-06-19 2011-01-06 Idemitsu Kosan Co Ltd 有機ｅｌ素子
WO2011009010A1 (en) 2009-07-15 2011-01-20 University Of Medicine And Dentistry Of New Jersey Novel compounds for inhibiting eef2 kinase activity
NZ600240A (en) 2009-10-29 2014-04-30 Bristol Myers Squibb Co Quinuclidine compounds as alpha-7 nicotinic acetylcholine receptor ligands
CN102753545A (zh) 2009-12-15 2012-10-24 盐野义制药株式会社 具有血管内皮脂酶抑制活性的噁二唑衍生物
ES2362337B1 (es) 2009-12-17 2012-05-16 Consejo Superior De Investigaciones Cient�?Ficas (Csic) Derivados de aminociclitoles, procedimiento de obtencion y usos.
ME02663B (me) * 2010-10-06 2017-06-20 Glaxosmithkline Llc Derivati benzimidazola kao inhibitori pi3 kinaze
CN105611843A (zh) 2013-10-11 2016-05-25 尤妮佳股份有限公司 宠物食品

Also Published As

Publication number Publication date
US20150246889A1 (en) 2015-09-03
PL2624696T3 (pl) 2017-07-31
AU2011312594B2 (en) 2014-10-02
CL2013000935A1 (es) 2013-07-05
US20140018534A1 (en) 2014-01-16
CN103124496B (zh) 2016-03-30
DOP2013000059A (es) 2013-05-31
US20130197221A1 (en) 2013-08-01
US20120088767A1 (en) 2012-04-12
UY33648A (es) 2012-04-30
KR101594002B1 (ko) 2016-02-15
EP2624696A4 (en) 2014-03-26
US9062003B2 (en) 2015-06-23
CN103124496A (zh) 2013-05-29
TW201307297A (zh) 2013-02-16
US20180263994A1 (en) 2018-09-20
US20130196990A1 (en) 2013-08-01
US8541411B2 (en) 2013-09-24
CY1118792T1 (el) 2017-07-12
BR112013008259A2 (pt) 2017-12-12
ES2714384T3 (es) 2019-05-28
US20140378456A1 (en) 2014-12-25
RS55662B1 (sr) 2017-06-30
CA2812608A1 (en) 2012-04-12
MX337662B (es) 2016-03-14
AR083296A1 (es) 2013-02-13
WO2012047538A1 (en) 2012-04-12
JP2013539753A (ja) 2013-10-28
LT2624696T (lt) 2017-03-10
MX2013003918A (es) 2013-06-05
NZ608069A (en) 2014-06-27
HRP20170279T1 (hr) 2017-04-07
JO3194B1 (ar) 2018-03-08
US9872860B2 (en) 2018-01-23
US20170112844A1 (en) 2017-04-27
US8674090B2 (en) 2014-03-18
MY170236A (en) 2019-07-11
TWI513690B (zh) 2015-12-21
AU2011312594A1 (en) 2013-04-11
HUE033209T2 (hu) 2017-11-28
ME02663B (me) 2017-06-20
PE20140192A1 (es) 2014-02-24
EA022623B1 (ru) 2016-02-29
CR20130192A (es) 2013-10-03
EP2624696B1 (en) 2016-12-21
SI2624696T1 (sl) 2017-04-26
MA34591B1 (fr) 2013-10-02
JP5719028B2 (ja) 2015-05-13
US10314845B2 (en) 2019-06-11
ZA201301951B (en) 2014-08-27
US20140142321A1 (en) 2014-05-22
US10660898B2 (en) 2020-05-26
US8435988B2 (en) 2013-05-07
CO6700852A2 (es) 2013-06-28
ES2616238T3 (es) 2017-06-12
EA201390302A1 (ru) 2013-09-30
EP2624696A1 (en) 2013-08-14
US8865912B2 (en) 2014-10-21
EP3170813A1 (en) 2017-05-24
US20190255064A1 (en) 2019-08-22
KR20130099142A (ko) 2013-09-05
US9156797B2 (en) 2015-10-13
PT2624696T (pt) 2017-03-21
SG188974A1 (en) 2013-06-28
EP3170813B1 (en) 2018-12-12
CA2812608C (en) 2020-07-14
IL225140A (en) 2016-09-29

Similar Documents

Publication Publication Date Title
DK2624696T3 (da) Benzimidazolderivater som pi3-kinaseinhibitorer
US8906910B2 (en) Imidazopyridine derivatives as PI3 kinase
US8778937B2 (en) Benzimidazole boronic acid derivatives as PI3 kinase inhibitors
WO2013028263A1 (en) Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
AU2014321456B2 (en) Combination drug therapy
EP2432321B1 (en) Thiazolopyrimidinone derivatives as pi3 kinase inhibitors