WO2003059884A1 - Modulators of lxr - Google Patents
Modulators of lxr Download PDFInfo
- Publication number
- WO2003059884A1 WO2003059884A1 PCT/US2002/041306 US0241306W WO03059884A1 WO 2003059884 A1 WO2003059884 A1 WO 2003059884A1 US 0241306 W US0241306 W US 0241306W WO 03059884 A1 WO03059884 A1 WO 03059884A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- aryl
- phenyl
- Prior art date
Links
- 0 CC1(*)C=CC(C(N(C[Al])C2=O)=C(*)C(C(F)(F)F)=C2C#N)=CC=C1 Chemical compound CC1(*)C=CC(C(N(C[Al])C2=O)=C(*)C(C(F)(F)F)=C2C#N)=CC=C1 0.000 description 19
- CFQXJPQXCBNNGN-UHFFFAOYSA-N CC(C=C(c(cc1)ccc1Cl)N(C1=O)N=C2CCCCC2)=C1C#N Chemical compound CC(C=C(c(cc1)ccc1Cl)N(C1=O)N=C2CCCCC2)=C1C#N CFQXJPQXCBNNGN-UHFFFAOYSA-N 0.000 description 1
- QTMKNCZDUKCLAQ-UHFFFAOYSA-O CC(CC(c1ccccc1)=C1C#N)(c2ccccc2)[NH2+]C1=O Chemical compound CC(CC(c1ccccc1)=C1C#N)(c2ccccc2)[NH2+]C1=O QTMKNCZDUKCLAQ-UHFFFAOYSA-O 0.000 description 1
- JCBAVTRNIZTODS-UHFFFAOYSA-N CC(CC1)CCC1=NN(C(c1ccccc1)=CC(C(F)(F)F)=C1C#N)C1=O Chemical compound CC(CC1)CCC1=NN(C(c1ccccc1)=CC(C(F)(F)F)=C1C#N)C1=O JCBAVTRNIZTODS-UHFFFAOYSA-N 0.000 description 1
- SXCDFHMRBSIALG-UHFFFAOYSA-O CC(CCC1)CC1=N[NH+](C(c1ccccc1)=CC(C(F)(F)F)=C1C#N)C1=O Chemical compound CC(CCC1)CC1=N[NH+](C(c1ccccc1)=CC(C(F)(F)F)=C1C#N)C1=O SXCDFHMRBSIALG-UHFFFAOYSA-O 0.000 description 1
- OGQMCYLHGWWGDQ-UHFFFAOYSA-N CC(c1ccc(CN(C(c2ccccc2)=CC(C(F)(F)F)=C2C#N)C2=O)cc1)=O Chemical compound CC(c1ccc(CN(C(c2ccccc2)=CC(C(F)(F)F)=C2C#N)C2=O)cc1)=O OGQMCYLHGWWGDQ-UHFFFAOYSA-N 0.000 description 1
- VQRLELPDQDHRRW-UHFFFAOYSA-N CC1(C)OC(CN(C(c2ccccc2)=CC(C(F)(F)F)=C2C#N)C2=O)CO1 Chemical compound CC1(C)OC(CN(C(c2ccccc2)=CC(C(F)(F)F)=C2C#N)C2=O)CO1 VQRLELPDQDHRRW-UHFFFAOYSA-N 0.000 description 1
- JYSDPCJCMLAIEC-UHFFFAOYSA-N CCC(CC1)CCC1=NN(C(c1ccc[s]1)=CC(C(F)(F)F)=C1C#N)C1=O Chemical compound CCC(CC1)CCC1=NN(C(c1ccc[s]1)=CC(C(F)(F)F)=C1C#N)C1=O JYSDPCJCMLAIEC-UHFFFAOYSA-N 0.000 description 1
- QFLIIQVXDWNISE-UHFFFAOYSA-N CCCCCCCCOCc1ccc(CN(C(c2cc(C)ccc2)=CC(C(F)(F)F)=C2C#N)C2=O)cc1 Chemical compound CCCCCCCCOCc1ccc(CN(C(c2cc(C)ccc2)=CC(C(F)(F)F)=C2C#N)C2=O)cc1 QFLIIQVXDWNISE-UHFFFAOYSA-N 0.000 description 1
- FQYYWARVBWGGQF-UHFFFAOYSA-N CCN(CC)C(c1cccc(C(N(Cc2ccccc2)C2=O)=CC(C(F)(F)F)=C2C#N)c1)=O Chemical compound CCN(CC)C(c1cccc(C(N(Cc2ccccc2)C2=O)=CC(C(F)(F)F)=C2C#N)c1)=O FQYYWARVBWGGQF-UHFFFAOYSA-N 0.000 description 1
- PSUPUEVNANRBIR-UHFFFAOYSA-N CCOC(c1cc(Oc(cc2)ccc2C(N(Cc2ccc(C)cc2C)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1)=O Chemical compound CCOC(c1cc(Oc(cc2)ccc2C(N(Cc2ccc(C)cc2C)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1)=O PSUPUEVNANRBIR-UHFFFAOYSA-N 0.000 description 1
- XTJJFXUGNHLSAU-UHFFFAOYSA-N CCc1cc(C(N(Cc2ccc(C)c(C)c2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 Chemical compound CCc1cc(C(N(Cc2ccc(C)c(C)c2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 XTJJFXUGNHLSAU-UHFFFAOYSA-N 0.000 description 1
- XULCZPJTEFIMLV-UHFFFAOYSA-N CCc1ccc(CN(C(c2cccc(C)c2)=CC(C(F)(F)F)=C2C#N)C2=O)cc1 Chemical compound CCc1ccc(CN(C(c2cccc(C)c2)=CC(C(F)(F)F)=C2C#N)C2=O)cc1 XULCZPJTEFIMLV-UHFFFAOYSA-N 0.000 description 1
- WEVHKXLJRAWCMU-UHFFFAOYSA-N COC(c1ccc(COc2cc(C(N(Cc3ccccc3)C3=O)=CC(C(F)(F)F)=C3C#N)ccc2)cc1)=O Chemical compound COC(c1ccc(COc2cc(C(N(Cc3ccccc3)C3=O)=CC(C(F)(F)F)=C3C#N)ccc2)cc1)=O WEVHKXLJRAWCMU-UHFFFAOYSA-N 0.000 description 1
- KVKFQVOBWASLDZ-UHFFFAOYSA-O COc(cc1)ccc1C([NH2+]C1=[O]C(CCCC2)C2=N)=CC(C(F)(F)F)=C1C#N Chemical compound COc(cc1)ccc1C([NH2+]C1=[O]C(CCCC2)C2=N)=CC(C(F)(F)F)=C1C#N KVKFQVOBWASLDZ-UHFFFAOYSA-O 0.000 description 1
- GUFWHQBUCBMLFM-UHFFFAOYSA-N Cc1cc(C(N(CC(C2C=CC=C3)C23Cl)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 Chemical compound Cc1cc(C(N(CC(C2C=CC=C3)C23Cl)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 GUFWHQBUCBMLFM-UHFFFAOYSA-N 0.000 description 1
- HTHAKHSOOWRNTH-UHFFFAOYSA-N Cc1cc(C(N(Cc2c[s]c(-c3ccccc3)n2)C2=O)=CC(C(F)(F)F)=C2C#N)cc(C)c1 Chemical compound Cc1cc(C(N(Cc2c[s]c(-c3ccccc3)n2)C2=O)=CC(C(F)(F)F)=C2C#N)cc(C)c1 HTHAKHSOOWRNTH-UHFFFAOYSA-N 0.000 description 1
- DIRKRRGXUQFGLX-UHFFFAOYSA-N Cc1cc(C(N(Cc2ccc(C(F)(F)F)cc2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 Chemical compound Cc1cc(C(N(Cc2ccc(C(F)(F)F)cc2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 DIRKRRGXUQFGLX-UHFFFAOYSA-N 0.000 description 1
- IZASSLPJAYHNNA-UHFFFAOYSA-N Cc1cc(C(N(Cc2ccc(COC)cc2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 Chemical compound Cc1cc(C(N(Cc2ccc(COC)cc2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 IZASSLPJAYHNNA-UHFFFAOYSA-N 0.000 description 1
- SXXIGBAVPSDTTG-UHFFFAOYSA-N Cc1cc(C(N(Cc2ccccc2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 Chemical compound Cc1cc(C(N(Cc2ccccc2)C2=O)=CC(C(F)(F)F)=C2C#N)ccc1 SXXIGBAVPSDTTG-UHFFFAOYSA-N 0.000 description 1
- FOTDLWCKHWLEBR-UHFFFAOYSA-N Cc1cc(CN(C(c(cc2)ccc2Oc2ccccc2)=CC(C(C(F)(F)F)(F)F)=C2C#N)C2=O)ccc1 Chemical compound Cc1cc(CN(C(c(cc2)ccc2Oc2ccccc2)=CC(C(C(F)(F)F)(F)F)=C2C#N)C2=O)ccc1 FOTDLWCKHWLEBR-UHFFFAOYSA-N 0.000 description 1
- NOOVSAFOSUSHCK-UHFFFAOYSA-N Cc1ccc(C)c(CN(C(c2ccccc2)=CC(C(F)(F)F)=C2C#N)C2=O)c1 Chemical compound Cc1ccc(C)c(CN(C(c2ccccc2)=CC(C(F)(F)F)=C2C#N)C2=O)c1 NOOVSAFOSUSHCK-UHFFFAOYSA-N 0.000 description 1
- SDVRDDUILYXROT-UHFFFAOYSA-N Cc1ccc(CN(C(c(cc2)ccc2OC2OCCCC2)=CC(C(F)(F)F)=C2C#N)C2=O)c(C)c1 Chemical compound Cc1ccc(CN(C(c(cc2)ccc2OC2OCCCC2)=CC(C(F)(F)F)=C2C#N)C2=O)c(C)c1 SDVRDDUILYXROT-UHFFFAOYSA-N 0.000 description 1
- MHLPCRFKFJSFDZ-UHFFFAOYSA-N Cc1ccc(CN(C(c(cc2)ccc2Oc(cc2)ccc2Br)=CC(C(F)(F)F)=C2C#N)C2=O)c(C)c1 Chemical compound Cc1ccc(CN(C(c(cc2)ccc2Oc(cc2)ccc2Br)=CC(C(F)(F)F)=C2C#N)C2=O)c(C)c1 MHLPCRFKFJSFDZ-UHFFFAOYSA-N 0.000 description 1
- ARNKWYXFZXTVOG-UHFFFAOYSA-N Cc1ccc(CN(C(c(cc2)ccc2Oc2cc(C)cc(C)c2)=CC(C(F)(F)F)=C2C#N)C2=O)c(C)c1 Chemical compound Cc1ccc(CN(C(c(cc2)ccc2Oc2cc(C)cc(C)c2)=CC(C(F)(F)F)=C2C#N)C2=O)c(C)c1 ARNKWYXFZXTVOG-UHFFFAOYSA-N 0.000 description 1
- QUGOVALGZHZZHQ-UHFFFAOYSA-N Cc1ccc(CN(C(c(cc2)ccc2Oc2cccc(C(O)=O)c2)=CC(C(F)(F)F)=C2C#N)C2=O)c(C=[IH])c1 Chemical compound Cc1ccc(CN(C(c(cc2)ccc2Oc2cccc(C(O)=O)c2)=CC(C(F)(F)F)=C2C#N)C2=O)c(C=[IH])c1 QUGOVALGZHZZHQ-UHFFFAOYSA-N 0.000 description 1
- VLPDWGCFLQALLA-UHFFFAOYSA-N Cc1ccc(CN(C(c2ncc[s]2)=CC(C(C(F)(F)F)(F)F)=C2C#N)C2=O)c(C)c1 Chemical compound Cc1ccc(CN(C(c2ncc[s]2)=CC(C(C(F)(F)F)(F)F)=C2C#N)C2=O)c(C)c1 VLPDWGCFLQALLA-UHFFFAOYSA-N 0.000 description 1
- TVOMCJNVEIKQIP-UHFFFAOYSA-N Cc1ccc(CNC(CC#N)=O)c(C)c1 Chemical compound Cc1ccc(CNC(CC#N)=O)c(C)c1 TVOMCJNVEIKQIP-UHFFFAOYSA-N 0.000 description 1
- BNXPCVGBSLTWQU-UHFFFAOYSA-N Cc1cccc(C(N(Cc2cccc(C(F)(F)F)c2)C2=O)=CC(C(F)(F)F)=C2C#N)c1 Chemical compound Cc1cccc(C(N(Cc2cccc(C(F)(F)F)c2)C2=O)=CC(C(F)(F)F)=C2C#N)c1 BNXPCVGBSLTWQU-UHFFFAOYSA-N 0.000 description 1
- GCVZBEDFQNFAPW-UHFFFAOYSA-O N#CC(C1=O)=C(C(F)(F)F)C=C(c2ccccc2)[NH+]1N=C(CCCC1)C1c1ccccc1 Chemical compound N#CC(C1=O)=C(C(F)(F)F)C=C(c2ccccc2)[NH+]1N=C(CCCC1)C1c1ccccc1 GCVZBEDFQNFAPW-UHFFFAOYSA-O 0.000 description 1
- NYXQKHZBWWEXAY-UHFFFAOYSA-N N#CC1=C(C(F)(F)F)C=C(c2ccccc2)N(Cc2ccc(C(F)(F)F)cc2)C1=O Chemical compound N#CC1=C(C(F)(F)F)C=C(c2ccccc2)N(Cc2ccc(C(F)(F)F)cc2)C1=O NYXQKHZBWWEXAY-UHFFFAOYSA-N 0.000 description 1
- UZJNCSFBCFBIEX-UHFFFAOYSA-N N#CC1=C(C(F)(F)F)C=C(c2ccccc2)N(Cc2ccccc2)C1=S Chemical compound N#CC1=C(C(F)(F)F)C=C(c2ccccc2)N(Cc2ccccc2)C1=S UZJNCSFBCFBIEX-UHFFFAOYSA-N 0.000 description 1
- WKWBOZPKWLHXMR-UHFFFAOYSA-N N#CCC(NCCCc1ccccc1)=O Chemical compound N#CCC(NCCCc1ccccc1)=O WKWBOZPKWLHXMR-UHFFFAOYSA-N 0.000 description 1
- XBYXVCRXCIJINE-UHFFFAOYSA-N N#CCC(NCc(c(C=[IH])c1)ccc1Cl)=O Chemical compound N#CCC(NCc(c(C=[IH])c1)ccc1Cl)=O XBYXVCRXCIJINE-UHFFFAOYSA-N 0.000 description 1
- UKKHUKFEKBKULS-UHFFFAOYSA-N N#CCC(NCc(cc1)ccc1Cl)=O Chemical compound N#CCC(NCc(cc1)ccc1Cl)=O UKKHUKFEKBKULS-UHFFFAOYSA-N 0.000 description 1
- OBRPXZYTBBNYPA-UHFFFAOYSA-N N#CCC(NCc1ccccc1Cl)=O Chemical compound N#CCC(NCc1ccccc1Cl)=O OBRPXZYTBBNYPA-UHFFFAOYSA-N 0.000 description 1
- XCTQPMCULSZKLT-UHFFFAOYSA-N N#CCC(Nc1ccccc1)=O Chemical compound N#CCC(Nc1ccccc1)=O XCTQPMCULSZKLT-UHFFFAOYSA-N 0.000 description 1
- NALMTAGQHWNRBI-UHFFFAOYSA-O Nc(cccc1)c1[O]=C(CC#N)[NH3+] Chemical compound Nc(cccc1)c1[O]=C(CC#N)[NH3+] NALMTAGQHWNRBI-UHFFFAOYSA-O 0.000 description 1
- KZOWVHBIEBBVQS-UHFFFAOYSA-N O=C(Cc1ccccc1)NCC1=C(C(F)(F)F)C=C(c2ccccc2)N(Cc2ccccc2)C1=O Chemical compound O=C(Cc1ccccc1)NCC1=C(C(F)(F)F)C=C(c2ccccc2)N(Cc2ccccc2)C1=O KZOWVHBIEBBVQS-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/84—Nitriles
- C07D213/85—Nitriles in position 3
-
- 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
- C07D401/06—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 only aliphatic carbon atoms
-
- 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
- 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
- C07D405/06—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 only aliphatic carbon atoms
-
- 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
- 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
- C07D409/04—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 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
- C07D413/06—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 only aliphatic carbon atoms
-
- 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
- C07D417/06—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 only aliphatic carbon atoms
-
- 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
Definitions
- LXRs liver X receptors
- pyridone derivatives are provided for modulating the activity of LXRs.
- plication of diabetes includes, but is not limited to, microvascular complications and macrovascular complications.
- R 6 and R 7 together form substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, or -(CH 2 ) x X(CH 2 ) y - where x and y are each 2, and X is O or NR 8 , where the substituents are selected from one or more Q 1 .
- R 6 and R 7 together form substituted or unsubstituted butylene, substituted or unsubstituted pentylene, substituted or unsubstituted hexylene, or substituted or unsubstituted pentenylene, where the substituents are selected from one or more Q 1 .
- the compounds for use in the compositions and methods provided herein have formula XV11 ;
- the active ingredient may be administered at once, or may be divided into a number of smaller doses to be administered at intervals of time. It is understood that the precise dosage and duration of treatment is a function of the disease being treated and may be determined empirically using known testing protocols or by extrapolation from in vivo or in vitro test data. It is to be noted that concentrations and dosage values may also vary with the severity of the condition to be alleviated. It is to be further understood that for any particular subject, specific dosage regimens should be adjusted over time according to the individual need and the professional judgment of the person administering or supervising the administration of the compositions, and that the concentration ranges set forth herein are exemplary only and are not intended to limit the scope or practice of the claimed compositions.
- Solutions or suspensions used for parenteral, intradermal, subcutaneous, or topical application can include any of the following components: a sterile diluent, such as water for injection, saline solution, fixed oil, polyethylene glycol, glycerine, propylene glycol or other synthetic solvent; antimicrobial agents, such as benzyl alcohol and methyl parabens; antioxidants, such as ascorbic acid and sodium bisulfite; chelating agents, such as ethylenediaminetetraacetic acid (EDTA); buffers, such as acetates, citrates and phosphates; and agents for the adjustment of tonicity such as sodium chloride or dextrose.
- a sterile diluent such as water for injection, saline solution, fixed oil, polyethylene glycol, glycerine, propylene glycol or other synthetic solvent
- antimicrobial agents such as benzyl alcohol and methyl parabens
- antioxidants such as ascorbic acid and sodium bisul
- the composition can contain along with the active ingredient: a diluent such as lactose, sucrose, dicalcium phosphate, or carboxymethyl- cellulose; a lubricant, such as magnesium stearate, calcium stearate and talc; and a binder such as starch, natural gums, such as gum acacia- gelatin, glucose, molasses, polvinylpyrrolidine, celluloses and derivatives thereof, povidone, crospovidones and other such binders known to those of skill in the art.
- a diluent such as lactose, sucrose, dicalcium phosphate, or carboxymethyl- cellulose
- a lubricant such as magnesium stearate, calcium stearate and talc
- a binder such as starch, natural gums, such as gum acacia- gelatin, glucose, molasses, polvinylpyrrolidine, celluloses and derivatives thereof, povidone,
- compositions containing active ingredient in the range of 0.005% to 100% with the balance made up from non-toxic carrier may be prepared.
- a pharmaceutically acceptable non-toxic composition is formed by the incorporation of any of the normally employed excipients, such as, for example pharmaceutical grades of mannitol, lactose, starch, magnesium stearate, talcum, cellulose derivatives, sodium crosscarmellose, glucose, sucrose, magnesium carbonate or sodium saccharin.
- the solid dosage forms are tablets, capsules, granules, and bulk powders.
- Types of oral tablets include compressed, chewable lozenges and tablets which may be enteric-coated, sugar-coated or film-coated.
- Capsules may be hard or soft gelatin capsules, while granules and t powders may be provided in non-effervescent or effervescent form with the combination of other ingredients known to those skilled in the art.
- Emetic-coatings include fatty acids, fats, waxes, shellac, ammoniated shellac and cellulose acetate phthalates.
- Film coatings include hydroxyethylcellulose, sodium carboxymethylcellulose, polyethylene glycol 4000 and cellulose acetate phthalate.
- the concentration of the pharmaceutically active compound is adjusted so that an injection provides an effective amount to produce the desired pharmacological effect.
- the exact dose depends on the age, weight and condition of the patient or animal as is known in the art.
- the unit-dose parenteral preparations are packaged in an ampoule, a vial or a syringe with a needle. All preparations for parenteral administration must be sterile, as is known and practiced in the art.
- intravenous or intraarterial infusion of a sterile aqueous solution containing an active compound is an effective mode of administration.
- Another embodiment is a sterile aqueous or oily solution or suspension containing an active material injected as necessary to produce the desired pharmacological effect.
- compositions for other routes of administration include topical application, transdermal patches, and rectal administration.
- rectal suppositories are used herein mean solid bodies for insertion into the rectum which melt or soften at body temperature releasing one or more pharmacologically or therapeutically active ingredients.
- Pharmaceutically acceptable substances utilized in rectal suppositories are bases or vehicles and agents to raise the melting point. Examples of bases include cocoa butter (theobroma oil), glycerin-gelatin, carbowax
- reporter gene systems include, for example, alkaline phosphatase Berger, J., et al. ( 1 988) Gene 66 1 -1 0; Kain, S.R. (1 997) Methods. Mol. Biol. 63 49-60), ⁇ -galactosidase (See, U.S. Patent No. 5,070,01 2, issued Dec, 3, 1 991 to Nolan et al., and Bronstein, I ., et al., (1 989) J. Chemilum. Biolum. 4 99-1 1 1 ), chlora phenicol acetyltransferase (See Gorman et al., Mol Cell Biol.
- WO 01 /82917 dyslipidemia, obesity, atherosclerosis, lipid disorders, cardiovascular disorders, or gallstone disease (see, e.g., International Patent Applciation Publication No. WO 00/37077); acne vulgaris or acneiform skin conditions (see, e.g. , International Patent Application Publication No. WO 00/49992); atherosclerosis, diabetes, Parkinson's disease, inflammation, immunological disorders, obesity, cancer or Alzheimer's disease (see, e.g. , International Patent Application Publication No. WO 00/1 7334); conditions characterized by a perturbed epidermal barrier function or conditions of disturbed differentiation or excess proliferation of the epidermis or mucous membrane (see, e.g. , U.S. Patent Nos. 6, 1 84,21 5 and 6, 1 87,814, and International Patent Application Publication No. Wo 98/32444) are provided.
- the compound is, in one embodiment, administered with a cholesterol biosynthesis inhibitor, particularly an HMG-CoA reductase inhibitor.
- HMG-CoA reductase inhibitor is intended to include all pharmaceutically acceptable salts, esters, free acids and lactone forms of compounds which have HMG-CoA reductase inhibitory activity and, therefore, the use of such salts, esters, free acids and lactone forms is included within the scope the compounds claimed herein.
- Compounds which have inhibitory activity for HMG-CoA reductase can be readily identified using assays well-known in the art. For instance, suitable assays are described or disclosed in U.S. Patent No. 4,231 ,938 and WO 84/021 31 .
- dehydroepiandrosterone also referred to as DHEA or its conjugated sulphate ester, DHEA-SO 4
- antiglucocorticoids also referred to as DHEA or its conjugated sulphate ester, DHEA-SO 4
- antiglucocorticoids also referred to as DHEA or its conjugated sulphate ester, DHEA-SO 4
- TNF ⁇ inhibitors such as acarbose, miglitol, and voglibose
- pramlintide a synthetic analog of the human hormone amylin
- other insulin secretagogues such as repaglinide, gliquidone, and nateglinide
- insulin as well as the active agents discussed above for treating atherosclerosis.
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02787071.6A EP1465869B1 (en) | 2001-12-21 | 2002-12-20 | Modulators of lxr |
ES02787071T ES2421511T3 (es) | 2001-12-21 | 2002-12-20 | Moduladores de LXR |
JP2003559988A JP5082033B2 (ja) | 2001-12-21 | 2002-12-20 | Lxrのモジュレーター |
CA002469435A CA2469435A1 (en) | 2001-12-21 | 2002-12-20 | Modulators of lxr |
AU2002351412A AU2002351412B2 (en) | 2001-12-21 | 2002-12-20 | Modulators of LXR |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US34270701P | 2001-12-21 | 2001-12-21 | |
US60/342,707 | 2001-12-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2003059884A1 true WO2003059884A1 (en) | 2003-07-24 |
Family
ID=23342938
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2002/041306 WO2003059884A1 (en) | 2001-12-21 | 2002-12-20 | Modulators of lxr |
Country Status (7)
Cited By (82)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004111014A1 (en) * | 2003-06-06 | 2004-12-23 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives as modulators of atp-binding cassette transporters |
WO2005019264A2 (en) * | 2003-08-18 | 2005-03-03 | Wyeth | Human lxr alpha variants |
EP1511483A2 (en) * | 2002-03-27 | 2005-03-09 | Smithkline Beecham Corporation | Methods of treatment with lxr modulators |
WO2005100396A1 (en) * | 2004-04-16 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with retinoid x receptor alpha (rxra) |
WO2006030032A1 (en) * | 2004-09-17 | 2006-03-23 | Janssen Pharmaceutica N.V. | Novel pyridinone derivatives and their use as positive allosteric modulators of mglur2-receptors |
WO2006059778A1 (ja) * | 2004-12-01 | 2006-06-08 | Banyu Pharmaceutical Co., Ltd. | 置換ピリドン誘導体 |
WO2006077012A2 (en) * | 2005-01-18 | 2006-07-27 | Genfit S.A. | USE OF LXR LIGANDS FOR THE MODULATION OF DENDRITIC CELLS (DCs) |
EP1773337A2 (en) * | 2004-07-24 | 2007-04-18 | Exelixis, Inc. | Modulators of nuclear receptors |
FR2903105A1 (fr) * | 2006-07-03 | 2008-01-04 | Sanofi Aventis Sa | Derives de 2-benzoyl-imidazopyridines, leur preparation et leur application en therapeutique |
WO2008149965A1 (ja) | 2007-06-07 | 2008-12-11 | Astellas Pharma Inc. | ピリドン化合物 |
WO2009154190A1 (ja) | 2008-06-17 | 2009-12-23 | アステラス製薬株式会社 | ピリドン化合物 |
US7704989B2 (en) | 2006-07-03 | 2010-04-27 | Sanofi-Aventis | Derivatives of imidazo[1,2-a]pyridine-2-carboxamides, preparation method thereof and use of same in therapeutics |
WO2010042925A3 (en) * | 2008-10-10 | 2010-07-29 | Vm Discovery Inc. | Compositions and methods for treating alcohol use disorders, pain and other diseases |
EP2228369A1 (en) | 2003-12-23 | 2010-09-15 | Astex Therapeutics Ltd. | Pyrazole derivatives as protein kinase modulators |
WO2011024872A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
WO2011024873A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
WO2011024869A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
WO2011024871A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
US7923573B2 (en) | 2004-10-27 | 2011-04-12 | Daiichi Sankyo Company, Limited | Benzene compound having 2 or more substituents |
WO2012033353A2 (ko) | 2010-09-07 | 2012-03-15 | 서울대학교 산학협력단 | 세스터터핀 화합물 및 이들 물질의 용도 |
US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
US8217176B2 (en) | 2008-02-26 | 2012-07-10 | Takeda Pharmaceutical Company Limited | Fused heterocyclic derivative and use thereof |
US8252937B2 (en) | 2007-09-14 | 2012-08-28 | Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones |
US8299101B2 (en) | 2007-03-07 | 2012-10-30 | Janssen Pharmaceuticals, Inc. | 1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive mGluR2-receptor modulators |
US8343953B2 (en) | 2005-06-22 | 2013-01-01 | Astex Therapeutics Limited | Pharmaceutical compounds |
US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
US8497294B2 (en) | 2007-03-14 | 2013-07-30 | Astex Therapeutics Limited | Compositions comprising (S)-2-amino-1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol as modulator of protein kinases |
US8541461B2 (en) | 2005-06-23 | 2013-09-24 | Astex Therapeutics Limited | Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators |
US8604032B2 (en) | 2010-05-21 | 2013-12-10 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
US8637542B2 (en) | 2008-03-14 | 2014-01-28 | Intellikine, Inc. | Kinase inhibitors and methods of use |
US8642604B2 (en) | 2006-04-04 | 2014-02-04 | The Regents Of The University Of California | Substituted pyrazolo[3,2-d]pyrimidines as anti-cancer agents |
US8691849B2 (en) | 2008-09-02 | 2014-04-08 | Janssen Pharmaceuticals, Inc. | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
US8691813B2 (en) | 2008-11-28 | 2014-04-08 | Janssen Pharmaceuticals, Inc. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
US8697709B2 (en) | 2008-10-16 | 2014-04-15 | The Regents Of The University Of California | Fused ring heteroaryl kinase inhibitors |
US8703777B2 (en) | 2008-01-04 | 2014-04-22 | Intellikine Llc | Certain chemical entities, compositions and methods |
US8703778B2 (en) | 2008-09-26 | 2014-04-22 | Intellikine Llc | Heterocyclic kinase inhibitors |
US8785454B2 (en) | 2009-05-07 | 2014-07-22 | Intellikine Llc | Heterocyclic compounds and uses thereof |
US8785470B2 (en) | 2011-08-29 | 2014-07-22 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8809349B2 (en) | 2011-01-10 | 2014-08-19 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
US8841323B2 (en) | 2006-03-15 | 2014-09-23 | Janssen Pharmaceuticals, Inc. | 1, 4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of MGLUR2-receptors |
US8901133B2 (en) | 2010-11-10 | 2014-12-02 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8906939B2 (en) | 2007-03-07 | 2014-12-09 | Janssen Pharmaceuticals, Inc. | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
US8937060B2 (en) | 2009-05-12 | 2015-01-20 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders |
US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8946205B2 (en) | 2009-05-12 | 2015-02-03 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
US8969363B2 (en) | 2011-07-19 | 2015-03-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8980899B2 (en) | 2009-10-16 | 2015-03-17 | The Regents Of The University Of California | Methods of inhibiting Ire1 |
US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
US8993591B2 (en) | 2010-11-08 | 2015-03-31 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a] pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors |
US9012448B2 (en) | 2010-11-08 | 2015-04-21 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors |
US9056877B2 (en) | 2011-07-19 | 2015-06-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9085577B2 (en) | 2009-05-12 | 2015-07-21 | Janssen Pharmaceuticals, Inc. | 7-aryl-1,2,4-triazolo[4,3-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
US9096611B2 (en) | 2008-07-08 | 2015-08-04 | Intellikine Llc | Kinase inhibitors and methods of use |
US9114138B2 (en) | 2007-09-14 | 2015-08-25 | Janssen Pharmaceuticals, Inc. | 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones |
US9271967B2 (en) | 2010-11-08 | 2016-03-01 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
US9321772B2 (en) | 2011-09-02 | 2016-04-26 | The Regents Of The University Of California | Substituted pyrazolo[3,4-D]pyrimidines and uses thereof |
US9359365B2 (en) | 2013-10-04 | 2016-06-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9359349B2 (en) | 2007-10-04 | 2016-06-07 | Intellikine Llc | Substituted quinazolines as kinase inhibitors |
US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
US9512125B2 (en) | 2004-11-19 | 2016-12-06 | The Regents Of The University Of California | Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents |
US9629843B2 (en) | 2008-07-08 | 2017-04-25 | The Regents Of The University Of California | MTOR modulators and uses thereof |
US9708315B2 (en) | 2013-09-06 | 2017-07-18 | Janssen Pharmaceutica Nv | 1,2,4-triazolo[4,3-a]pyridine compounds and their use as positive allosteric modulators of MGLUR2 receptors |
US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
WO2017123568A2 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9775844B2 (en) | 2014-03-19 | 2017-10-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US10106542B2 (en) | 2013-06-04 | 2018-10-23 | Janssen Pharmaceutica Nv | Substituted 6,7-dihydropyrazolo[1,5-a]pyrazines as negative allosteric modulators of mGluR2 receptors |
US10131668B2 (en) | 2012-09-26 | 2018-11-20 | The Regents Of The University Of California | Substituted imidazo[1,5-a]pYRAZINES for modulation of IRE1 |
US10155002B2 (en) | 2011-04-13 | 2018-12-18 | Epizyme, Inc. | Aryl- or heteroaryl-substituted benzene compounds |
US10160761B2 (en) | 2015-09-14 | 2018-12-25 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
US10537573B2 (en) | 2014-01-21 | 2020-01-21 | Janssen Pharmaceutica Nv | Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use |
US10669296B2 (en) | 2014-01-10 | 2020-06-02 | Rgenix, Inc. | LXR agonists and uses thereof |
US10759806B2 (en) | 2016-03-17 | 2020-09-01 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors |
US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US11110096B2 (en) | 2014-04-16 | 2021-09-07 | Infinity Pharmaceuticals, Inc. | Combination therapies |
US11147818B2 (en) | 2016-06-24 | 2021-10-19 | Infinity Pharmaceuticals, Inc. | Combination therapies |
US11174220B2 (en) | 2019-12-13 | 2021-11-16 | Inspirna, Inc. | Metal salts and uses thereof |
US11214536B2 (en) | 2017-11-21 | 2022-01-04 | Inspirna, Inc. | Polymorphs and uses thereof |
US11369606B2 (en) | 2014-01-21 | 2022-06-28 | Janssen Pharmaceutica Nv | Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use |
US11642348B2 (en) | 2012-10-15 | 2023-05-09 | Epizyme, Inc. | Substituted benzene compounds |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1465869B1 (en) * | 2001-12-21 | 2013-05-15 | Exelixis Patent Company LLC | Modulators of lxr |
ES2367539T3 (es) | 2001-12-21 | 2011-11-04 | X-Ceptor Therapeutics, Inc. | Moduladores heterocíclicos de receptores nucleares. |
US7790745B2 (en) * | 2005-10-21 | 2010-09-07 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline LXR Modulators |
US7741317B2 (en) * | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
CN101547688A (zh) * | 2006-09-19 | 2009-09-30 | 惠氏公司 | Lxr激动剂用于治疗骨关节炎的用途 |
WO2008036238A2 (en) * | 2006-09-19 | 2008-03-27 | Wyeth | Use of lxr modulators for the prevention and treatment of skin aging |
CN101668759A (zh) | 2007-05-04 | 2010-03-10 | 百时美施贵宝公司 | [6,5]-双环gpr119g蛋白-偶合受体激动剂 |
CN101668756A (zh) | 2007-05-04 | 2010-03-10 | 百时美施贵宝公司 | [6,6]和[6,7]-双环gpr119 g蛋白偶合受体激动剂 |
US7928230B2 (en) * | 2007-07-17 | 2011-04-19 | Bristol-Myers Squibb Company | Method for modulating GPR119 G protein-coupled receptor and selected compounds |
AR068813A1 (es) * | 2007-08-30 | 2009-12-09 | Takeda Pharmaceutical | Derivados de pirazol sustituidos como antagonistas del receptor de androgenos (ar), un agente farmaceutico que los comprende y su uso en el tratamiento del cancer de prostata |
US20090209601A1 (en) * | 2008-02-15 | 2009-08-20 | Wyeth | Use of rxr agonists for the treatment of osteoarthritis |
TW201006821A (en) | 2008-07-16 | 2010-02-16 | Bristol Myers Squibb Co | Pyridone and pyridazone analogues as GPR119 modulators |
EP2556069B1 (en) | 2010-04-08 | 2015-04-01 | Bristol-Myers Squibb Company | 4-(1-(pyrimidin-2-yl)piperidin-4-yloxy)pyridin-2-one compounds as gpr119 modulators |
US8729084B2 (en) | 2010-05-06 | 2014-05-20 | Bristol-Myers Squibb Company | Benzofuranyl analogues as GPR119 modulators |
WO2012158784A2 (en) * | 2011-05-16 | 2012-11-22 | Theodore Mark Kamenecka | Modulators of the nuclear hormone receptor ror |
EP2967073B9 (en) | 2013-03-15 | 2019-04-10 | Bristol-Myers Squibb Company | Lxr modulators |
US9834542B2 (en) | 2013-03-15 | 2017-12-05 | Bristo-Myers Squibb Company | LXR modulators |
WO2014207601A1 (en) | 2013-06-27 | 2014-12-31 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
US10583102B2 (en) | 2014-10-06 | 2020-03-10 | The Johns Hopkins University | Targeting liver nuclear receptors as a treatment for wilson disease |
CN109715637B (zh) | 2016-07-22 | 2022-04-05 | 百时美施贵宝公司 | 葡萄糖激酶激活剂及其使用方法 |
WO2020112889A2 (en) | 2018-11-26 | 2020-06-04 | Denali Therapeutics Inc. | Methods for treating dysregulated lipid metabolism |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5571696A (en) | 1991-09-17 | 1996-11-05 | The Salk Institute For Biological Studies | Receptors |
Family Cites Families (242)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US51813A (en) * | 1866-01-02 | Improvement in the manufacture of paper-pulp | ||
US147493A (en) * | 1874-02-17 | Improvement in curtain-cord holders | ||
US73277A (en) * | 1868-01-14 | Improvement in gates | ||
US624583A (en) * | 1899-05-09 | Paper box | ||
US176064A (en) * | 1876-04-11 | Improvement in screw-cutting machines | ||
US339105A (en) * | 1886-03-30 | John l | ||
US72073A (en) | 1867-12-10 | Improved boot and shoe-heels | ||
US17334A (en) * | 1857-05-19 | Machinery for dressing sewing-thread | ||
US236581A (en) * | 1881-01-11 | haworth | ||
US54759A (en) * | 1866-05-15 | Improvement in pantographic machines | ||
US103705A (en) * | 1870-05-31 | Improvement in scissors-sharpener | ||
US294995A (en) * | 1884-03-11 | Ments | ||
US226727A (en) * | 1880-04-20 | Car-coupling | ||
US160818A (en) * | 1875-03-16 | Improvement in bucket-ears | ||
US2556A (en) * | 1842-04-16 | Stove | ||
US557843A (en) * | 1896-04-07 | Octave-coupler for organs | ||
US137805A (en) * | 1873-04-15 | Improvement in broom-corn dusters | ||
US122964A (en) * | 1872-01-23 | 1872-01-23 | Improvement in watches | |
US755934A (en) * | 1904-02-17 | 1904-03-29 | George M Potter | Detonator. |
US1226832A (en) * | 1916-08-09 | 1917-05-22 | Fred M Webber | Pneumatic pitman-balance for swing-jaw rock and ore crushers. |
US1261371A (en) * | 1917-05-02 | 1918-04-02 | John Ellingsen | Window construction. |
US5625041A (en) * | 1990-09-12 | 1997-04-29 | Delta Biotechnology Limited | Purification of proteins |
US2077412A (en) * | 1930-06-04 | 1937-04-20 | Eugene J Lorand | Process for the preparation of a molded cellulose foam from viscose and product thereof |
US2345058A (en) * | 1939-11-25 | 1944-03-28 | Aetna Standard Eng Co | Method of galvanizing |
US2824341A (en) * | 1953-11-25 | 1958-02-25 | Harold B Neal | Awning |
DE1189994B (de) * | 1957-11-20 | 1965-04-01 | Hoechst Ag | Verfahren zur Herstellung von 1-Aminopyridon-(6)-derivaten |
CH477475A (de) * | 1966-07-25 | 1969-08-31 | Geigy Ag J R | Verfahren zur Herstellung von neuen Derivaten der 6-Amino-penicillansäure |
US3576814A (en) * | 1970-01-30 | 1971-04-27 | Rohm & Haas | N-aryl pyrid-2-ones |
US3710795A (en) * | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
GB1429184A (en) | 1972-04-20 | 1976-03-24 | Allen & Hanburys Ltd | Physically anti-inflammatory steroids for use in aerosols |
US4044126A (en) | 1972-04-20 | 1977-08-23 | Allen & Hanburys Limited | Steroidal aerosol compositions and process for the preparation thereof |
USRE28819E (en) | 1972-12-08 | 1976-05-18 | Syntex (U.S.A.) Inc. | Dialkylated glycol compositions and medicament preparations containing same |
US4159202A (en) | 1973-12-20 | 1979-06-26 | Hoechst Aktiengesellschaft | Photopolymer having 2-pyridone side group |
US3954734A (en) | 1974-01-21 | 1976-05-04 | Parke, Davis & Company | Novel antibacterial amide compounds and process means for producing the same |
US4038065A (en) | 1974-10-11 | 1977-07-26 | Rohm And Haas Company | 1-alkylpyrid-2-one |
US4028084A (en) * | 1974-10-11 | 1977-06-07 | Rohm And Haas Company | Derivatives of 3-carboxy pyrid-2-ones |
US3951982A (en) * | 1974-11-21 | 1976-04-20 | Parke, Davis & Company | Trialkylsilyl esters of 6(substituted amino)phenyl-1,-dihydro-2-oxonicotinic acid, methods for their production and conversion to the corresponding acid chlorides |
US4053470A (en) | 1974-12-23 | 1977-10-11 | Parke, Davis & Company | Substituted-1,2-dihydro-2-oxonicotinyl-cephalosporins |
IT1039699B (it) | 1975-07-03 | 1979-12-10 | Prephar | Composizione spermicida a base di derivati benzisotiazolici |
DE2637477A1 (de) * | 1976-08-20 | 1978-02-23 | Hoechst Ag | Dihydro-oxo-nicotinsaeuren und verfahren zu ihrer herstellung |
JPS5350179A (en) * | 1976-10-15 | 1978-05-08 | Rikagaku Kenkyusho | Novel 2-pyridone compounds and their preparation |
US4101661A (en) | 1977-06-03 | 1978-07-18 | Warner-Lambert | Novel antibacterial amide compounds and process means for producing the same |
CA1115278A (en) | 1979-01-10 | 1981-12-29 | Benjamin J. Pierce | Anti-inflammatory 4-pyridones and their preparation |
GB2045236A (en) | 1979-03-26 | 1980-10-29 | Hoechst Uk Ltd | Oxapenem derivatives |
FR2456713A1 (fr) * | 1979-05-17 | 1980-12-12 | Emballage Ste Gle Pour | Melanges vitrifiables |
US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
US4444784A (en) * | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
JPS5726653A (en) | 1980-05-09 | 1982-02-12 | Ciba Geigy Ag | Substituted phenyl ether |
MX7065E (es) | 1980-06-06 | 1987-04-10 | Sankyo Co | Un procedimiento microbiologico para preparar derivados de ml-236b |
US4309552A (en) * | 1980-08-07 | 1982-01-05 | A. H. Robins Company, Inc. | Synthesis of 4-nitro-1,2-hydrocarbyl pyrazolidines and process for preparation thereof |
ATE21105T1 (de) | 1980-11-06 | 1986-08-15 | Hoechst Uk Ltd | 7-oxo-4-thia-1-aza(3.2.0)heptan- und 7-oxo-4-thia-1-aza-(3.2.0)hept-2-en-derivate. |
US4328245A (en) | 1981-02-13 | 1982-05-04 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4410545A (en) | 1981-02-13 | 1983-10-18 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4358603A (en) | 1981-04-16 | 1982-11-09 | Syntex (U.S.A.) Inc. | Acetal stabilized prostaglandin compositions |
US4409239A (en) | 1982-01-21 | 1983-10-11 | Syntex (U.S.A.) Inc. | Propylene glycol diester solutions of PGE-type compounds |
US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
US4585894A (en) * | 1983-10-19 | 1986-04-29 | Eli Lilly And Company | Process for producing 9-carbamoyl fluorene derivatives |
IL73261A (en) | 1983-10-19 | 1988-03-31 | Lilly Co Eli | Process for producing 9-carbamoyl-9-aminoalkyl fluorene derivatives,and certain intermediates thereof |
US5583024A (en) | 1985-12-02 | 1996-12-10 | The Regents Of The University Of California | Recombinant expression of Coleoptera luciferase |
DD244341A1 (de) | 1985-12-18 | 1987-04-01 | Akad Wissenschaften Ddr | Verfahren zur herstellung neuer 1h-pyrid-2-one |
US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
US5221623A (en) | 1986-07-22 | 1993-06-22 | Boyce Thompson Institute For Plant Research, Inc. | Use of bacterial luciferase structural genes for cloning and monitoring gene expression in microorganisms and for tagging and identification of genetically engineered organisms |
US5071773A (en) * | 1986-10-24 | 1991-12-10 | The Salk Institute For Biological Studies | Hormone receptor-related bioassays |
JPS63112566A (ja) | 1986-10-28 | 1988-05-17 | Nissan Chem Ind Ltd | ピリミジノン誘導体、その製法および殺虫・殺ダニ・殺菌剤 |
US4968707A (en) | 1987-06-10 | 1990-11-06 | Pfizer Inc. | Oxazolidin-2-one derivatives as hypoglycemic agents |
US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
US5070012A (en) | 1988-03-30 | 1991-12-03 | The Board Of Trustees Of The Leland Stanford Junior University | Monitoring of cells and trans-activating transcription elements |
DE3823991A1 (de) | 1988-07-15 | 1990-02-15 | Basf Ag | Heterocyclisch substituierte (alpha)-aryl-acrylsaeureester und fungizide, die diese verbindungen enthalten |
US5194438A (en) * | 1988-07-15 | 1993-03-16 | Basf Aktiengesellschaft | α-arylacrylates substituted by a trifluoromethylpyrimidinyloxy radical, fungicidal compositions and methods |
DE3922392A1 (de) | 1989-07-07 | 1991-01-17 | Merck Patent Gmbh | Chromanderivate |
FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
US5683888A (en) | 1989-07-22 | 1997-11-04 | University Of Wales College Of Medicine | Modified bioluminescent proteins and their use |
DE3934176A1 (de) * | 1989-10-13 | 1991-04-18 | Basf Ag | Cyclische amide |
US5283173A (en) | 1990-01-24 | 1994-02-01 | The Research Foundation Of State University Of New York | System to detect protein-protein interactions |
EP0487745A4 (en) | 1990-06-19 | 1993-01-20 | Meiji Seika Kabushiki Kaisha | Pyridine derivative with angiotensin ii antagonism |
US5380721A (en) * | 1990-09-10 | 1995-01-10 | Sterling Winthrop Inc. | Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents |
US5283179A (en) | 1990-09-10 | 1994-02-01 | Promega Corporation | Luciferase assay method |
US5883255A (en) * | 1990-10-31 | 1999-03-16 | Smithkline Beecham Corporation | Substituted indolizino 1,2-b!quinolinones |
WO1993020818A1 (en) | 1990-10-31 | 1993-10-28 | Smithkline Beecham Corporation | SUBSTITUTED INDOLIZINO[1,2-b]QUINOLINONES |
IE913790A1 (en) | 1990-10-31 | 1992-05-22 | Smithkline Beecham Corp | SUBSTITUTED INDOLIZINO [1,2-b]QUINOLINONES |
US5177080A (en) * | 1990-12-14 | 1993-01-05 | Bayer Aktiengesellschaft | Substituted pyridyl-dihydroxy-heptenoic acid and its salts |
IL100917A0 (en) * | 1991-02-16 | 1992-11-15 | Fisons Plc | Pyridinone and pyrimidinone derivatives,their preparation and pharmaceutical compositions containing them |
US5332750A (en) | 1991-09-04 | 1994-07-26 | Merck Patent Gesellschaft Mit Beschrankter Haftung | 1,2-dihydro-2-oxopyridines |
DE4129340A1 (de) | 1991-09-04 | 1993-03-11 | Merck Patent Gmbh | 1,2-dihydro-2-oxopyridine |
DE4221583A1 (de) * | 1991-11-12 | 1993-05-13 | Bayer Ag | Substituierte biphenylpyridone |
US5278289A (en) | 1991-11-12 | 1994-01-11 | Johnson Alan J | Antihemophilic factor stabilization |
US5504070A (en) | 1991-12-05 | 1996-04-02 | Berlex Laboratories, Inc. | Inhibitors of the conversion of big endothelin to endothelin |
DE69228047T2 (de) | 1991-12-10 | 1999-05-27 | Bristol Myers Squibb Co | Führer für Schienbeinosteotomie |
DE4141187A1 (de) | 1991-12-13 | 1993-06-17 | Bayer Ag | Verfahren zur herstellung von substituierten pyrazolinen |
AU668694B2 (en) | 1991-12-19 | 1996-05-16 | Sanofi-Synthelabo | Saccharin derivative proteolytic enzyme inhibitors |
US5378720A (en) | 1991-12-19 | 1995-01-03 | Sterling Winthrop Inc. | Saccharin derivative proteolytic enzyme inhibitors |
ES2113399T3 (es) | 1991-12-26 | 1998-05-01 | Mitsubishi Chem Corp | Derivados de beta-oxo-beta-bencenopropano-tio-amida. |
WO1993016698A1 (en) | 1992-02-21 | 1993-09-02 | Smithkline Beecham Corporation | SUBSTITUTED FURO[3',4':6,7]INDOLIZINO[1,2-b]QUINOLINONES |
DE4206045A1 (de) | 1992-02-27 | 1993-09-02 | Bayer Ag | Sulfonylbenzyl substituierte pyridone |
ATE198601T1 (de) | 1992-05-20 | 2001-01-15 | Merck & Co Inc | Ester derivate von 4-aza-steroiden |
US5536727A (en) | 1992-05-20 | 1996-07-16 | Merck & Co., Inc. | 17-Ethers and thioethers of 4-aza-steroids |
US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
GB9213694D0 (en) | 1992-06-27 | 1992-08-12 | Keynes Roger J | Improvements in or relating to neuroregeneration |
US5728553A (en) * | 1992-09-23 | 1998-03-17 | Delta Biotechnology Limited | High purity albumin and method of producing |
GB9221329D0 (en) | 1992-10-10 | 1992-11-25 | Delta Biotechnology Ltd | Preparation of further diagnostic agents |
DE4319041A1 (de) * | 1992-10-23 | 1994-04-28 | Bayer Ag | Trisubstituierte Biphenyle |
DE4319040A1 (de) | 1992-10-23 | 1994-04-28 | Bayer Ag | Alkoxymethylsubstituierte Pyridonbiphenyle |
DE4309552A1 (de) | 1993-03-24 | 1994-09-29 | Bayer Ag | Substituierte Stickstoff-Heterocyclen |
US5814645A (en) | 1993-03-24 | 1998-09-29 | Bayer Aktiengesellschaft | Arylor hetaryl substituted nitrogen heterocycles and their use as pesticides |
DE4313747A1 (de) | 1993-04-27 | 1994-11-03 | Bayer Ag | Verfahren zur Herstellung von substituierten Biphenyltetrazolen |
DE4316077A1 (de) | 1993-05-13 | 1994-11-17 | Bayer Ag | Substituierte Mono- und Bihydridylmethylpyridone |
AP9400651A0 (en) | 1993-07-15 | 1995-12-30 | Pfizer | Azacyclic-heterocyclic compounds as angiotensin II receptor antagonists. |
WO1995003803A1 (en) | 1993-08-03 | 1995-02-09 | Smithkline Beecham Corporation | SUBSTITUTED FURO[3',4':6,7]INDOLIZINO[1,2-b]QUINOLINONES |
US5514716A (en) | 1994-02-25 | 1996-05-07 | Sterling Winthrop, Inc. | Hydroxamic acid and carboxylic acid derivatives, process for their preparation and use thereof |
DE4407488A1 (de) * | 1994-03-07 | 1995-09-14 | Bayer Ag | Verwendung von Biphenyl- und Pyridylmethylpyridonen |
KR100327273B1 (ko) | 1994-04-08 | 2002-05-10 | 고사이 아끼오 | 에테르화합물,그의용도및그의제조에유용한중간체 |
US5466233A (en) | 1994-04-25 | 1995-11-14 | Escalon Ophthalmics, Inc. | Tack for intraocular drug delivery and method for inserting and removing same |
DE4414648A1 (de) | 1994-04-27 | 1995-11-02 | Merck Patent Gmbh | Verfahren zur Umsetzung von substituierten Pyrid-2-onen mit Arylalkylhalogeniden |
US5598269A (en) * | 1994-05-12 | 1997-01-28 | Children's Hospital Medical Center | Laser guided alignment apparatus for medical procedures |
WO1996003378A1 (fr) | 1994-07-26 | 1996-02-08 | Sankyo Company, Limited | Derives d'amide n-phenyle et d'uree |
JP3466765B2 (ja) | 1994-07-27 | 2003-11-17 | キッコーマン株式会社 | ビオチン化ホタルルシフェラーゼ、ビオチン化ホタルルシフェラーゼ遺伝子、新規な組み換え体dna、ビオチン化ホタルルシフェラーゼの製造法及び生物発光分析法 |
US5698571A (en) | 1994-10-05 | 1997-12-16 | Eli Lilly And Company | 5-HT1F mediated inhibition of neurogenic meningeal extravasation: a method for the treatment of migraine |
US5744482A (en) | 1994-10-05 | 1998-04-28 | Eli Lilly And Company | Serotonin agonist in combination with a tachykinin receptor antagonist in the treatment or prevention of migraine |
WO1996012181A1 (en) | 1994-10-12 | 1996-04-25 | Research & Diagnostics Systems, Inc. | Reticulocyte assay control |
US5659042A (en) | 1994-10-25 | 1997-08-19 | Allergan | Method for preparing esters of halonicotinic acids |
US5607967A (en) * | 1994-10-27 | 1997-03-04 | Merck & Co., Inc. | Treatment of alzheimer's disease with 5-(tetradecyloxy)-2-furan carboxylic acid |
US5955108A (en) | 1994-12-16 | 1999-09-21 | Quadrant Healthcare (Uk) Limited | Cross-linked microparticles and their use as therapeutic vehicles |
US5618943A (en) * | 1994-12-29 | 1997-04-08 | Allergan | Acetylenes disubstituted with a 5 OXO substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity |
EP0800517A1 (en) | 1994-12-29 | 1997-10-15 | Allergan | Acetylenes disubstituted with a 5 or 8 substituted tetrahydronaphthyl or dihydronaphthyl group and with an aryl or heteroaryl groups having retinoid-like biological activity |
US5514825A (en) | 1994-12-29 | 1996-05-07 | Allergan, Inc. | Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity |
US5599967A (en) | 1994-12-29 | 1997-02-04 | Allergan | Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl of heteroaryl group having retinoid-like biological activity |
US5618931A (en) * | 1994-12-29 | 1997-04-08 | Allergan | Acetylenes disubstituted with a 5 substituted dihydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity |
US5648514A (en) * | 1994-12-29 | 1997-07-15 | Allergan | Substituted acetylenes having retinoid-like biological activity |
US5543534A (en) * | 1994-12-29 | 1996-08-06 | Allergan | Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl groups having retinoid-like biological activity |
US6005086A (en) | 1995-01-13 | 1999-12-21 | The Salk Institute For Biological Studies | Farnesoid activated receptor polypeptides, and nucleic acid encoding the same |
US5789426A (en) | 1995-01-20 | 1998-08-04 | Cornell Research Foundation, Inc. | Method for the treatment of fibroproliferative disorders by application of inhibitors of protein hydroxylation |
US5869428A (en) | 1995-03-13 | 1999-02-09 | Ishihara Sangyo Kaisha Ltd. | Pyridonesulfonylurea compounds, process for their production and herbicides containing them |
US5741657A (en) * | 1995-03-20 | 1998-04-21 | The Regents Of The University Of California | Fluorogenic substrates for β-lactamase and methods of use |
DE19518739A1 (de) | 1995-05-22 | 1996-11-28 | Basf Ag | N-Aminopyridonderivate |
JPH08325248A (ja) | 1995-05-26 | 1996-12-10 | Chugoku Kayaku Kk | テトラゾール類の新規な合成試薬及びそれを用いたテトラゾール類の製造方法 |
US5612363A (en) * | 1995-06-02 | 1997-03-18 | Berlex Laboratories, Inc. | N,N-di(aryl) cyclic urea derivatives as anti-coagulants |
DE69620756T2 (de) | 1995-06-07 | 2002-11-14 | Searle & Co | Kombinationstherapie zur behandlung des kongestiven herzversagens mit spironolacton und angiotensin ii-antagonist |
NZ310730A (en) | 1995-06-07 | 2001-01-26 | G | Epoxy-steroidal aldosterone antagonist and angiotensin II antagonist combination therapy for treatment of congestive heart failure |
WO1996040256A1 (en) | 1995-06-07 | 1996-12-19 | G.D. Searle & Co. | Method to treat cardiofibrosis with a combination of an angiotensin ii antagonist and spironolactone |
WO1996041633A1 (en) | 1995-06-08 | 1996-12-27 | Eli Lilly And Company | Methods of treating cold and allergic rhinitis |
AU5966096A (en) | 1995-06-09 | 1997-01-09 | Eli Lilly And Company | Methods of treating cold and allergic rhinitis |
US5849587A (en) | 1995-06-09 | 1998-12-15 | Cornell Research Foundation, Inc. | Method of inhibiting viral replication in eukaryotic cells and of inducing apoptosis of virally-infected cells |
DE19527568A1 (de) | 1995-07-28 | 1997-01-30 | Merck Patent Gmbh | Endothelin-Rezeptor-Antagonisten |
US6008204A (en) | 1995-09-01 | 1999-12-28 | Allergan Sales, Inc. | Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities |
US5776699A (en) | 1995-09-01 | 1998-07-07 | Allergan, Inc. | Method of identifying negative hormone and/or antagonist activities |
US5958954A (en) | 1995-09-01 | 1999-09-28 | Allergan Sales, Inc. | Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities |
US5952345A (en) | 1995-09-01 | 1999-09-14 | Allergan Sales, Inc. | Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities |
CA2230479A1 (en) * | 1995-09-21 | 1997-03-27 | Andaris Limited | Transcytosis vehicles and enhancers for drug delivery |
US5888830A (en) | 1995-09-22 | 1999-03-30 | Berlex Laboratories, Inc. | Apparatus and process for multiple chemical reactions |
EP0859661B1 (en) | 1995-09-22 | 2001-05-16 | Berlex Laboratories, Inc. | Apparatus and process for multiple chemical reactions |
JP2002500618A (ja) * | 1995-10-31 | 2002-01-08 | イーライ・リリー・アンド・カンパニー | 抗血栓性ジアミン |
US5994375A (en) | 1996-02-12 | 1999-11-30 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants |
AU4837996A (en) | 1996-02-29 | 1997-09-16 | Delta Biotechnology Limited | High purity albumin production process |
US5877207A (en) * | 1996-03-11 | 1999-03-02 | Allergan Sales, Inc. | Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities |
WO1997035480A1 (en) | 1996-03-15 | 1997-10-02 | Eli Lilly And Company | Method of treating common cold or allergic rhinitis |
US5869497A (en) * | 1996-03-15 | 1999-02-09 | Eli Lilly And Company | Method of treating or ameliorating the symptoms of common cold or allergic rhinitis |
DE19619950A1 (de) | 1996-04-17 | 1997-10-23 | Bayer Ag | Heterocyclisch-substituierte Phenylglycinolamide |
EP0802192A1 (de) | 1996-04-17 | 1997-10-22 | Bayer Ag | Heterocyclisch-substituierte Phenylglycinolamide mit antiatherosklerotischer Wirkung und Verfahren zu ihrer Herstellung |
US5747542A (en) | 1996-06-21 | 1998-05-05 | Allergan | Oxo-substituted tetrahydronaphthalene derivatives having retinold and/or retinoid antagonist-like biological activity |
US5723666A (en) * | 1996-06-21 | 1998-03-03 | Allergan | Oxime substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity |
US5773594A (en) | 1996-06-21 | 1998-06-30 | Allergan | Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity |
US5763635A (en) | 1996-06-21 | 1998-06-09 | Allergan | Tetrahydronaphthalene derivatives substituted in the 8 position with alkyhidene groups having retinoid and/or retinoid antagonist-like biological activity |
AU724541B2 (en) | 1996-06-21 | 2000-09-21 | Allergan, Inc. | Substituted tetrahydronaphthalene and dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity |
US5741896A (en) * | 1996-06-21 | 1998-04-21 | Allergan | O- or S- substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity |
US6555690B2 (en) * | 1996-06-21 | 2003-04-29 | Allergan, Inc. | Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity |
US5808124A (en) | 1996-06-21 | 1998-09-15 | Allergan | O- or S-substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity |
US5618503A (en) * | 1996-06-28 | 1997-04-08 | Chemical Research & Licensing Company | Antimony pentafluoride |
DE19627421A1 (de) | 1996-07-08 | 1998-01-15 | Bayer Ag | Verwendung von substituierten Biphenylen |
US5753635A (en) | 1996-08-16 | 1998-05-19 | Berlex Laboratories, Inc. | Purine derivatives and their use as anti-coagulants |
US5962473A (en) | 1996-08-16 | 1999-10-05 | Eli Lilly And Company | Methods of treating or ameliorating the symptoms of common cold or allergic rhinitis with serotonin 5-HT1F |
US5693641A (en) | 1996-08-16 | 1997-12-02 | Berlex Laboratories Inc. | Bicyclic pyrimidine derivatives and their use as anti-coagulants |
AU4074897A (en) | 1996-09-18 | 1998-04-14 | Eli Lilly And Company | A method for the prevention of migraine |
US5955604A (en) | 1996-10-15 | 1999-09-21 | The Regents Of The University Of California | Substrates for β-lactamase and uses thereof |
JP2001502343A (ja) * | 1996-10-17 | 2001-02-20 | ビーエーエスエフ アクチェンゲゼルシャフト | 栽培植物の有害菌類の防除方法 |
ZA979961B (en) | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
EP1082958A3 (en) | 1996-11-15 | 2002-12-11 | Eli Lilly And Company | 5-HT1F agonists in chronic pain |
US5728846A (en) * | 1996-12-12 | 1998-03-17 | Allergan | Benzo 1,2-g!-chrom-3-ene and benzo 1,2-g!-thiochrom-3-ene derivatives |
CN1248916A (zh) * | 1997-01-24 | 2000-03-29 | 加利福尼亚大学董事会 | FXR、PPARα和LXRα激活剂恢复屏障功能、促进表皮分化和抑制增生的用途 |
US5855654A (en) | 1997-01-30 | 1999-01-05 | Rohm And Haas Company | Pyridazinones as marine antifouling agents |
US5760276A (en) | 1997-03-06 | 1998-06-02 | Allergan | Aryl-and heteroarylcyclohexenyl substituted alkenes having retinoid agonist, antagonist or inverse agonist type biological activity |
JP2002501503A (ja) | 1997-04-30 | 2002-01-15 | イーライ・リリー・アンド・カンパニー | 抗血栓症剤 |
EP0980367A4 (en) * | 1997-04-30 | 2003-03-19 | Lilly Co Eli | ANTITHROMBOTIC AGENTS |
JP3771672B2 (ja) | 1997-05-27 | 2006-04-26 | 曙ブレーキ工業株式会社 | ブレーキペダル操作検出装置 |
DE19729061A1 (de) | 1997-07-08 | 1999-01-14 | Agfa Gevaert Ag | Farbfotografisches Aufzeichnungsmaterial |
US6380201B1 (en) * | 1997-08-05 | 2002-04-30 | Eli Lilly And Company | Methods of treating or ameliorating the symptoms of common cold or allergic rhinitis with serotonin 5-HT1F agonists |
GB9718913D0 (en) | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
GB9723078D0 (en) | 1997-10-31 | 1998-01-07 | Cerebrus Ltd | Chemical compounds |
US6156784A (en) | 1997-12-18 | 2000-12-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compounds useful as phosphotyrosine mimics |
EP1045836B1 (en) | 1997-12-18 | 2008-03-05 | Boehringer Ingelheim Pharmaceuticals Inc. | Pyridones as src family sh2 domain inhibitors |
WO1999040062A1 (en) | 1998-02-05 | 1999-08-12 | Novo Nordisk A/S | Hydrazone derivatives |
EP1076655A1 (en) | 1998-04-08 | 2001-02-21 | Novartis AG | N-pyridonyl herbicides |
TR200003113T2 (tr) | 1998-04-27 | 2001-05-21 | Centre National De La Recherche Scientifique | 3-(amino- veya aminoalkil) piridinon türevleri ve bunların HIV bağımlı hastalıkların tedavisinde kullanılması. |
DE19826671A1 (de) | 1998-06-16 | 1999-12-23 | Hoechst Schering Agrevo Gmbh | 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel |
WO2000017334A2 (en) | 1998-09-23 | 2000-03-30 | Ludmila Solomin | Analysis of ligand activated nuclear receptors i(in vivo) |
WO2000025134A1 (en) | 1998-10-23 | 2000-05-04 | Glaxo Group Limited | Assays for ligands for nuclear receptors |
EP1006108A1 (en) | 1998-12-01 | 2000-06-07 | Cerebrus Pharmaceuticals Limited | 3-Hydroxy-2(1H)-pyridinone or 3-hydroxy-4(1H)-pyridinone derivatives useful as reactive oxygen species (ROS) scavengers |
EP1006112A1 (en) | 1998-12-01 | 2000-06-07 | Cerebrus Pharmaceuticals Limited | 3-Hydroxy-2(1H)-pyridinone or 3-hydroxy-4(1H)-pyridinone derivatives useful as reactive oxygen species (ROS) scavengers |
GB2345058A (en) | 1998-12-01 | 2000-06-28 | Cerebrus Pharm Ltd | Hydroxypyridone compounds useful in the treatment of oxidative damage to the central nervous system |
US6294503B1 (en) | 1998-12-03 | 2001-09-25 | Ishihara Sangyo Kaisha, Ltd. | Fused heterocycle compounds, process for their preparation, and herbicidal compositions containing them |
DE69940958D1 (de) | 1998-12-23 | 2009-07-16 | Glaxo Group Ltd | Bestimmungsmethode fur liganden der nuklearen rezeptoren |
US6465258B1 (en) | 1999-01-07 | 2002-10-15 | Tularik, Inc. | FXR receptor-mediated modulation cholesterol metabolism |
US6071955A (en) | 1999-02-25 | 2000-06-06 | The Regents Of The University Of California | FXR, PPARA and LXRA activators to treat acne/acneiform conditions |
US6316503B1 (en) * | 1999-03-15 | 2001-11-13 | Tularik Inc. | LXR modulators |
DE60013417T2 (de) | 1999-03-26 | 2005-09-15 | City Of Hope, Duarte | Verfahren zum screenen von fxr-rezeptormodulatoren |
AU4641400A (en) | 1999-06-02 | 2000-12-18 | Ishihara Sangyo Kaisha Ltd. | Fused tricyclic compounds, process for their preparation, and herbicidal compositions containing them |
BR0011696A (pt) | 1999-06-18 | 2002-04-30 | Cv Therapeutics Inc | Composições e métodos para aumento do efluxo de colesterol e elevação de hdl usando proteìna abc1 transportadora de cassete de ligação de atp |
JP2004500332A (ja) | 1999-07-08 | 2004-01-08 | テュラリク インコーポレイテッド | Hdlコレステロール値を上昇させる組成物および方法 |
CA2382562A1 (en) | 1999-09-01 | 2001-03-08 | University Of British Columbia | Compositions and methods for modulating hdl cholesterol and triglyceride levels |
AU7026800A (en) | 1999-09-11 | 2001-04-17 | Glaxo Group Limited | Pharmaceutical formulation of fluticasone propionate |
WO2001022964A1 (en) | 1999-09-27 | 2001-04-05 | Georgetown University | Dopamine transporter inhibitors and their use |
US6444471B1 (en) | 1999-10-18 | 2002-09-03 | Research & Diagnostic Systems, Inc. | Reticulocyte containing complete blood control |
EP1523976A3 (en) | 1999-11-23 | 2005-06-22 | Glaxo Group Limited | Pharmaceutical formulations of salmeterol |
HUP0203735A3 (en) | 1999-12-06 | 2005-03-29 | Hoffmann La Roche | 4-pyridinyl-n-acyl-l-phenylalanines, pharmaceutical compositions containing them and their use |
US20020160067A1 (en) | 2001-04-25 | 2002-10-31 | Oncology Science Corporation | Therapeutic preparation and method for producing a therapeutic preparation using coffee beans as a substrate |
WO2001047493A1 (en) | 1999-12-24 | 2001-07-05 | Glaxo Group Limited | Pharmaceutical aerosol formulation of salmeterol and fluticasone propionate |
AU2000235960A1 (en) | 2000-02-14 | 2001-08-27 | Tularik, Inc. | Lxr modulators |
US6378919B1 (en) | 2000-04-04 | 2002-04-30 | International Truck Intellectual Property Company, L.L.C. | Cylindrical lock with slam latch and auxiliary cable release |
JP2001302637A (ja) | 2000-04-20 | 2001-10-31 | Nippon Kayaku Co Ltd | 感熱転写記録用色素及び感熱転写シート |
US20020048572A1 (en) | 2000-05-03 | 2002-04-25 | Bei Shan | Treatment of hypertriglyceridemia and other conditions using LXR modulators |
NZ522773A (en) | 2000-06-12 | 2005-06-24 | Eisai Co Ltd | 1,2-dihydropyridine compounds, manufacturing method thereof and use thereof |
US6387951B1 (en) | 2000-08-29 | 2002-05-14 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
US6313107B1 (en) | 2000-08-29 | 2001-11-06 | Allergan Sales, Inc. | Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI |
DE60116642T2 (de) | 2000-08-29 | 2006-11-09 | Allergan, Inc., Irvine | Verbindungen mit cytochrom p450ra1 hemmenden aktivität |
US6291677B1 (en) | 2000-08-29 | 2001-09-18 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
US6369225B1 (en) * | 2000-08-29 | 2002-04-09 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
US6369261B1 (en) * | 2000-08-29 | 2002-04-09 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
US6380256B1 (en) * | 2000-08-29 | 2002-04-30 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
US6252090B1 (en) * | 2000-08-29 | 2001-06-26 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
US6303785B1 (en) | 2000-08-29 | 2001-10-16 | Allergan Sales, Inc. | Compounds having activity as inhibitors of cytochrome P450RAI |
UY27003A1 (es) | 2000-11-06 | 2002-07-31 | Schering Ag | Productos radiofarmacéuticos para el diagnóstico de la enfermedad de alzheimer |
HUP0500880A2 (en) | 2000-12-11 | 2006-05-29 | Tularik Inc | Cxcr3 antagonists and pharmaceutical compositions thereof |
US8176425B2 (en) | 2001-02-02 | 2012-05-08 | Ensequence, Inc. | Animated screen object for annotation and selection of video sequences |
ES2299567T3 (es) | 2001-05-05 | 2008-06-01 | Smithkline Beecham Plc | N-aroilaminas ciclicas. |
EP1435955A2 (en) | 2001-05-05 | 2004-07-14 | SmithKline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
US6861424B2 (en) | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
GB0115862D0 (en) | 2001-06-28 | 2001-08-22 | Smithkline Beecham Plc | Compounds |
EP1399441B1 (en) | 2001-06-28 | 2006-07-05 | Smithkline Beecham Plc | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
EP1465869B1 (en) * | 2001-12-21 | 2013-05-15 | Exelixis Patent Company LLC | Modulators of lxr |
WO2004103974A1 (ja) | 2003-05-23 | 2004-12-02 | Japan Tobacco Inc. | 置換2-オキソキノリン化合物およびその医薬用途 |
CN1289803C (zh) | 2004-05-16 | 2006-12-13 | 王永钦 | 汽车冷却风扇驱动机构总成 |
-
2002
- 2002-12-20 EP EP02787071.6A patent/EP1465869B1/en not_active Expired - Lifetime
- 2002-12-20 WO PCT/US2002/041306 patent/WO2003059884A1/en active Application Filing
- 2002-12-20 JP JP2003559988A patent/JP5082033B2/ja not_active Expired - Lifetime
- 2002-12-20 AU AU2002351412A patent/AU2002351412B2/en not_active Ceased
- 2002-12-20 US US10/327,813 patent/US7998986B2/en active Active
- 2002-12-20 ES ES02787071T patent/ES2421511T3/es not_active Expired - Lifetime
- 2002-12-20 CA CA002469435A patent/CA2469435A1/en not_active Abandoned
-
2010
- 2010-09-22 JP JP2010212875A patent/JP2010280732A/ja not_active Withdrawn
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5571696A (en) | 1991-09-17 | 1996-11-05 | The Salk Institute For Biological Studies | Receptors |
US5696233A (en) | 1991-09-17 | 1997-12-09 | The Salk Institute For Biological Studies | Orphan steroid hormone receptors |
US5710004A (en) | 1991-09-17 | 1998-01-20 | The Salk Institute For Biological Studies | Methods of using novel steroid hormone orphan receptors |
Non-Patent Citations (8)
Title |
---|
DATABASE CAPLUS [online] GUTCAIT A. ET AL.: "Synthesis, structure and properties of 1-amino-6-phenyl-4-trifluoromethyl-3-cyano-2-pyridone", XP002968162, accession no. ACS Database accession no. 1987:458776 * |
DATABASE CAPLUS [online] JURE M. ET AL.: "1-Methyl-6-phenyl-4-trifluoromethyl-3-cyano-2-pyridone and its properties", XP002968163, accession no. ACS Database accession no. 1988:167259 * |
GLICKMAN ET AL., J. BIOMOLECULAR SCREENING, vol. 7, no. 1, 2002, pages 3 - 10 |
LATVIJAS PSR ZINATNU AKADEMIJAS VESTIS, KIMIJAS SERIJA, vol. 5, 1986, pages 607 - 612 * |
LATVIJAS PSR ZINATNU AKADEMIJAS VESTIS, KIMIJAS SERIJA, vol. 5, 1987, pages 627 - 631 * |
LEHMANN. ET AL., J. BIOL CHEM., vol. 272, no. 6, 1997, pages 3137 - 3140 |
OWICKI, J., BIOMOL SCREEN, vol. 5, no. 5, October 2000 (2000-10-01), pages 297 |
See also references of EP1465869A4 * |
Cited By (161)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1511483A2 (en) * | 2002-03-27 | 2005-03-09 | Smithkline Beecham Corporation | Methods of treatment with lxr modulators |
EP1511483A4 (en) * | 2002-03-27 | 2009-03-18 | Smithkline Beecham Corp | PROCESSING METHODS USING LXR MODULATORS |
WO2004111014A1 (en) * | 2003-06-06 | 2004-12-23 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives as modulators of atp-binding cassette transporters |
US8642609B2 (en) | 2003-06-06 | 2014-02-04 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
WO2005019264A3 (en) * | 2003-08-18 | 2007-08-02 | Wyeth Corp | Human lxr alpha variants |
WO2005019264A2 (en) * | 2003-08-18 | 2005-03-03 | Wyeth | Human lxr alpha variants |
US7341850B2 (en) | 2003-08-18 | 2008-03-11 | Wyeth | Human LXRα variants |
JP2007531502A (ja) * | 2003-08-18 | 2007-11-08 | ワイス | 新規ヒトLXRαバリアント |
US8691806B2 (en) | 2003-12-23 | 2014-04-08 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
US8247576B2 (en) | 2003-12-23 | 2012-08-21 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
EP2228369A1 (en) | 2003-12-23 | 2010-09-15 | Astex Therapeutics Ltd. | Pyrazole derivatives as protein kinase modulators |
US9283226B2 (en) | 2003-12-23 | 2016-03-15 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
WO2005100396A1 (en) * | 2004-04-16 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with retinoid x receptor alpha (rxra) |
JP2008507564A (ja) * | 2004-07-24 | 2008-03-13 | エグゼリクシス, インコーポレイテッド | 核レセプターのモジュレーター |
EP1773337A2 (en) * | 2004-07-24 | 2007-04-18 | Exelixis, Inc. | Modulators of nuclear receptors |
EP1773337A4 (en) * | 2004-07-24 | 2009-11-11 | Exelixis Inc | MODULATORS OF NUCLEAR RECEPTORS |
WO2006030032A1 (en) * | 2004-09-17 | 2006-03-23 | Janssen Pharmaceutica N.V. | Novel pyridinone derivatives and their use as positive allosteric modulators of mglur2-receptors |
JP2008513414A (ja) * | 2004-09-17 | 2008-05-01 | ジャンセン ファーマシュウティカル エヌ ヴィ | 新規ピリジノン誘導体およびmGluR2ポジティブアロステリックモジュレーターとしてのその使用 |
US8399493B2 (en) | 2004-09-17 | 2013-03-19 | Janssen Pharmaceuticals, Inc. | Pyridinone derivatives and their use as positive allosteric modulators of mGluR2-receptors |
EA013740B1 (ru) * | 2004-09-17 | 2010-06-30 | Орто-Макнейл-Янссен Фармасьютикалз, Инк. | Новые пиридиноновые производные и их применение в качестве позитивных аллостерических модуляторов mglur2-рецепторов |
US7923573B2 (en) | 2004-10-27 | 2011-04-12 | Daiichi Sankyo Company, Limited | Benzene compound having 2 or more substituents |
US9512125B2 (en) | 2004-11-19 | 2016-12-06 | The Regents Of The University Of California | Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents |
AU2005310467B2 (en) * | 2004-12-01 | 2011-06-23 | Msd K.K. | Substituted pyridone derivative |
WO2006059778A1 (ja) * | 2004-12-01 | 2006-06-08 | Banyu Pharmaceutical Co., Ltd. | 置換ピリドン誘導体 |
WO2006077012A3 (en) * | 2005-01-18 | 2006-11-02 | Genfit S A | USE OF LXR LIGANDS FOR THE MODULATION OF DENDRITIC CELLS (DCs) |
WO2006077012A2 (en) * | 2005-01-18 | 2006-07-27 | Genfit S.A. | USE OF LXR LIGANDS FOR THE MODULATION OF DENDRITIC CELLS (DCs) |
US8343953B2 (en) | 2005-06-22 | 2013-01-01 | Astex Therapeutics Limited | Pharmaceutical compounds |
US8541461B2 (en) | 2005-06-23 | 2013-09-24 | Astex Therapeutics Limited | Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators |
US8841323B2 (en) | 2006-03-15 | 2014-09-23 | Janssen Pharmaceuticals, Inc. | 1, 4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of MGLUR2-receptors |
US9266834B2 (en) | 2006-03-15 | 2016-02-23 | Janssen Pharmaceuticals, Inc. | 1, 4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of MGLUR2-receptors |
US9493467B2 (en) | 2006-04-04 | 2016-11-15 | The Regents Of The University Of California | PI3 kinase antagonists |
US8642604B2 (en) | 2006-04-04 | 2014-02-04 | The Regents Of The University Of California | Substituted pyrazolo[3,2-d]pyrimidines as anti-cancer agents |
WO2008003854A3 (fr) * | 2006-07-03 | 2008-03-06 | Sanofi Aventis | Derives de 2-benzoyl-imidazopyridines, leur preparation et leur application en therapeutique |
US7902219B2 (en) | 2006-07-03 | 2011-03-08 | Sanofi-Aventis | 2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof |
US7704989B2 (en) | 2006-07-03 | 2010-04-27 | Sanofi-Aventis | Derivatives of imidazo[1,2-a]pyridine-2-carboxamides, preparation method thereof and use of same in therapeutics |
FR2903105A1 (fr) * | 2006-07-03 | 2008-01-04 | Sanofi Aventis Sa | Derives de 2-benzoyl-imidazopyridines, leur preparation et leur application en therapeutique |
WO2008003854A2 (fr) * | 2006-07-03 | 2008-01-10 | Sanofi-Aventis | Derives de 2-benzoyl-imidazopyridines, leur preparation et leur application en therapeutique |
US8404848B2 (en) | 2006-07-03 | 2013-03-26 | Sanofi | Derivatives of imidazo[1,2-a]pyridine-2-carboxamides, preparation method thereof and use of same in therapeutics |
US9067891B2 (en) | 2007-03-07 | 2015-06-30 | Janssen Pharmaceuticals, Inc. | 1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mGluR2-receptors |
US8906939B2 (en) | 2007-03-07 | 2014-12-09 | Janssen Pharmaceuticals, Inc. | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
US8299101B2 (en) | 2007-03-07 | 2012-10-30 | Janssen Pharmaceuticals, Inc. | 1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive mGluR2-receptor modulators |
US8497294B2 (en) | 2007-03-14 | 2013-07-30 | Astex Therapeutics Limited | Compositions comprising (S)-2-amino-1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol as modulator of protein kinases |
WO2008149965A1 (ja) | 2007-06-07 | 2008-12-11 | Astellas Pharma Inc. | ピリドン化合物 |
US9132122B2 (en) | 2007-09-14 | 2015-09-15 | Janssen Pharmaceuticals, Inc. | 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′]bipyridinyl-2′-ones |
US11071729B2 (en) | 2007-09-14 | 2021-07-27 | Addex Pharmaceuticals S.A. | 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′]bipyridinyl-2′-ones |
US8252937B2 (en) | 2007-09-14 | 2012-08-28 | Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones |
US9114138B2 (en) | 2007-09-14 | 2015-08-25 | Janssen Pharmaceuticals, Inc. | 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones |
US9359349B2 (en) | 2007-10-04 | 2016-06-07 | Intellikine Llc | Substituted quinazolines as kinase inhibitors |
US11433065B2 (en) | 2008-01-04 | 2022-09-06 | Intellikine Llc | Certain chemical entities, compositions and methods |
US9216982B2 (en) | 2008-01-04 | 2015-12-22 | Intellikine Llc | Certain chemical entities, compositions and methods |
US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
US8785456B2 (en) | 2008-01-04 | 2014-07-22 | Intellikine Llc | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
US9655892B2 (en) | 2008-01-04 | 2017-05-23 | Intellikine Llc | Certain chemical entities, compositions and methods |
US8703777B2 (en) | 2008-01-04 | 2014-04-22 | Intellikine Llc | Certain chemical entities, compositions and methods |
US9822131B2 (en) | 2008-01-04 | 2017-11-21 | Intellikine Llc | Certain chemical entities, compositions and methods |
US8217176B2 (en) | 2008-02-26 | 2012-07-10 | Takeda Pharmaceutical Company Limited | Fused heterocyclic derivative and use thereof |
US8399449B2 (en) | 2008-02-26 | 2013-03-19 | Takeda Pharmaceutical Company Limited | Fused heterocyclic derivative and use thereof |
US8637542B2 (en) | 2008-03-14 | 2014-01-28 | Intellikine, Inc. | Kinase inhibitors and methods of use |
US9637492B2 (en) | 2008-03-14 | 2017-05-02 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
WO2009154190A1 (ja) | 2008-06-17 | 2009-12-23 | アステラス製薬株式会社 | ピリドン化合物 |
US9096611B2 (en) | 2008-07-08 | 2015-08-04 | Intellikine Llc | Kinase inhibitors and methods of use |
US9629843B2 (en) | 2008-07-08 | 2017-04-25 | The Regents Of The University Of California | MTOR modulators and uses thereof |
US9828378B2 (en) | 2008-07-08 | 2017-11-28 | Intellikine Llc | Kinase inhibitors and methods of use |
US8691849B2 (en) | 2008-09-02 | 2014-04-08 | Janssen Pharmaceuticals, Inc. | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
US9790228B2 (en) | 2008-09-26 | 2017-10-17 | Intellikine Llc | Heterocyclic kinase inhibitors |
US8703778B2 (en) | 2008-09-26 | 2014-04-22 | Intellikine Llc | Heterocyclic kinase inhibitors |
US9296742B2 (en) | 2008-09-26 | 2016-03-29 | Intellikine Llc | Heterocyclic kinase inhibitors |
US8729081B2 (en) | 2008-10-10 | 2014-05-20 | Vm Discovery Inc. | Compositions and methods for treating alcohol use disorders, pain and other diseases |
WO2010042925A3 (en) * | 2008-10-10 | 2010-07-29 | Vm Discovery Inc. | Compositions and methods for treating alcohol use disorders, pain and other diseases |
US8697709B2 (en) | 2008-10-16 | 2014-04-15 | The Regents Of The University Of California | Fused ring heteroaryl kinase inhibitors |
US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
US8476431B2 (en) | 2008-11-03 | 2013-07-02 | Itellikine LLC | Benzoxazole kinase inhibitors and methods of use |
US8691813B2 (en) | 2008-11-28 | 2014-04-08 | Janssen Pharmaceuticals, Inc. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
US8785454B2 (en) | 2009-05-07 | 2014-07-22 | Intellikine Llc | Heterocyclic compounds and uses thereof |
US9315505B2 (en) | 2009-05-07 | 2016-04-19 | Intellikine Llc | Heterocyclic compounds and uses thereof |
US8946205B2 (en) | 2009-05-12 | 2015-02-03 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
US9737533B2 (en) | 2009-05-12 | 2017-08-22 | Janssen Pharmaceuticals. Inc. | 1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders |
US9226930B2 (en) | 2009-05-12 | 2016-01-05 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders |
US8937060B2 (en) | 2009-05-12 | 2015-01-20 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders |
US9085577B2 (en) | 2009-05-12 | 2015-07-21 | Janssen Pharmaceuticals, Inc. | 7-aryl-1,2,4-triazolo[4,3-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
US10071095B2 (en) | 2009-05-12 | 2018-09-11 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of neurological and psychiatric disorders |
US9206182B2 (en) | 2009-07-15 | 2015-12-08 | Intellikine Llc | Substituted isoquinolin-1(2H)-one compounds, compositions, and methods thereof |
US9522146B2 (en) | 2009-07-15 | 2016-12-20 | Intellikine Llc | Substituted Isoquinolin-1(2H)-one compounds, compositions, and methods thereof |
US8569323B2 (en) | 2009-07-15 | 2013-10-29 | Intellikine, Llc | Substituted isoquinolin-1(2H)-one compounds, compositions, and methods thereof |
WO2011024871A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
US8614208B2 (en) | 2009-08-26 | 2013-12-24 | Takeda Pharmaceutical Company Limited | Fused heterocyclic ring derivative and use thereof |
WO2011024869A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
WO2011024873A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
US8927718B2 (en) | 2009-08-26 | 2015-01-06 | Takeda Pharmaceutical Company Limited | Fused heterocyclic ring derivative and use thereof |
US8907089B2 (en) | 2009-08-26 | 2014-12-09 | Takeda Pharmaceutical Company Limited | Fused heterocyclic ring derivative and use thereof |
US8486965B2 (en) | 2009-08-26 | 2013-07-16 | Takeda Pharmaceutical Company Limited | Pyrrolo[2,3-b]pyridine derivative and use thereof for treatment of cancer |
WO2011024872A1 (ja) | 2009-08-26 | 2011-03-03 | 武田薬品工業株式会社 | 縮合複素環誘導体およびその用途 |
US8980899B2 (en) | 2009-10-16 | 2015-03-17 | The Regents Of The University Of California | Methods of inhibiting Ire1 |
US9181221B2 (en) | 2010-05-21 | 2015-11-10 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
US9738644B2 (en) | 2010-05-21 | 2017-08-22 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
US8604032B2 (en) | 2010-05-21 | 2013-12-10 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
WO2012033353A2 (ko) | 2010-09-07 | 2012-03-15 | 서울대학교 산학협력단 | 세스터터핀 화합물 및 이들 물질의 용도 |
US8993591B2 (en) | 2010-11-08 | 2015-03-31 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a] pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors |
US9012448B2 (en) | 2010-11-08 | 2015-04-21 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors |
US9271967B2 (en) | 2010-11-08 | 2016-03-01 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors |
US8901133B2 (en) | 2010-11-10 | 2014-12-02 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9388183B2 (en) | 2010-11-10 | 2016-07-12 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8809349B2 (en) | 2011-01-10 | 2014-08-19 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
USRE46621E1 (en) | 2011-01-10 | 2017-12-05 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
US11312718B2 (en) | 2011-01-10 | 2022-04-26 | Infinity Pharmaceuticals, Inc. | Formulations of (S)-3-(1-(9H-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one |
US9840505B2 (en) | 2011-01-10 | 2017-12-12 | Infinity Pharmaceuticals, Inc. | Solid forms of (S)-3-(1-(9H-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1 (2H)-one and methods of use thereof |
US10550122B2 (en) | 2011-01-10 | 2020-02-04 | Infinity Pharmaceuticals, Inc. | Solid forms of (S)-3-(1-(9H-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one and methods of use thereof |
US9290497B2 (en) | 2011-01-10 | 2016-03-22 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
US10155002B2 (en) | 2011-04-13 | 2018-12-18 | Epizyme, Inc. | Aryl- or heteroaryl-substituted benzene compounds |
US11052093B2 (en) | 2011-04-13 | 2021-07-06 | Epizyme, Inc. | Aryl-or heteroaryl-substituted benzene compounds |
US10420775B2 (en) | 2011-04-13 | 2019-09-24 | Epizyme, Inc. | Aryl-or heteroaryl-substituted benzene compounds |
US9056877B2 (en) | 2011-07-19 | 2015-06-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9605003B2 (en) | 2011-07-19 | 2017-03-28 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9718815B2 (en) | 2011-07-19 | 2017-08-01 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8969363B2 (en) | 2011-07-19 | 2015-03-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9115141B2 (en) | 2011-08-29 | 2015-08-25 | Infinity Pharmaceuticals, Inc. | Substituted isoquinolinones and methods of treatment thereof |
US8785470B2 (en) | 2011-08-29 | 2014-07-22 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9546180B2 (en) | 2011-08-29 | 2017-01-17 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9321772B2 (en) | 2011-09-02 | 2016-04-26 | The Regents Of The University Of California | Substituted pyrazolo[3,4-D]pyrimidines and uses thereof |
US9895373B2 (en) | 2011-09-02 | 2018-02-20 | The Regents Of The University Of California | Substituted pyrazolo[3,4-D]pyrimidines and uses thereof |
US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9255108B2 (en) | 2012-04-10 | 2016-02-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
US9527847B2 (en) | 2012-06-25 | 2016-12-27 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
US10131668B2 (en) | 2012-09-26 | 2018-11-20 | The Regents Of The University Of California | Substituted imidazo[1,5-a]pYRAZINES for modulation of IRE1 |
US10822340B2 (en) | 2012-09-26 | 2020-11-03 | The Regents Of The University Of California | Substituted imidazolopyrazine compounds and methods of using same |
US11613544B2 (en) | 2012-09-26 | 2023-03-28 | The Regents Of The University Of California | Substituted imidazo[1,5-a]pyrazines for modulation of IRE1 |
US11642348B2 (en) | 2012-10-15 | 2023-05-09 | Epizyme, Inc. | Substituted benzene compounds |
US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
US10106542B2 (en) | 2013-06-04 | 2018-10-23 | Janssen Pharmaceutica Nv | Substituted 6,7-dihydropyrazolo[1,5-a]pyrazines as negative allosteric modulators of mGluR2 receptors |
US10584129B2 (en) | 2013-06-04 | 2020-03-10 | Janssen Pharmaceuticals Nv | Substituted 6,7-dihydropyrazolo[1,5-a]pyrazines as negative allosteric modulators of mGluR2 receptors |
US9708315B2 (en) | 2013-09-06 | 2017-07-18 | Janssen Pharmaceutica Nv | 1,2,4-triazolo[4,3-a]pyridine compounds and their use as positive allosteric modulators of MGLUR2 receptors |
US9828377B2 (en) | 2013-10-04 | 2017-11-28 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US10329299B2 (en) | 2013-10-04 | 2019-06-25 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9359365B2 (en) | 2013-10-04 | 2016-06-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US10669296B2 (en) | 2014-01-10 | 2020-06-02 | Rgenix, Inc. | LXR agonists and uses thereof |
US10537573B2 (en) | 2014-01-21 | 2020-01-21 | Janssen Pharmaceutica Nv | Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use |
US11369606B2 (en) | 2014-01-21 | 2022-06-28 | Janssen Pharmaceutica Nv | Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use |
US11103506B2 (en) | 2014-01-21 | 2021-08-31 | Janssen Pharmaceutica Nv | Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use |
US11541059B2 (en) | 2014-03-19 | 2023-01-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US10675286B2 (en) | 2014-03-19 | 2020-06-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US9775844B2 (en) | 2014-03-19 | 2017-10-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US11944631B2 (en) | 2014-04-16 | 2024-04-02 | Infinity Pharmaceuticals, Inc. | Combination therapies |
US11110096B2 (en) | 2014-04-16 | 2021-09-07 | Infinity Pharmaceuticals, Inc. | Combination therapies |
US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
US10941162B2 (en) | 2014-10-03 | 2021-03-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US10253047B2 (en) | 2014-10-03 | 2019-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US10160761B2 (en) | 2015-09-14 | 2018-12-25 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
US11247995B2 (en) | 2015-09-14 | 2022-02-15 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
US11939333B2 (en) | 2015-09-14 | 2024-03-26 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
WO2017123568A2 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
US10759806B2 (en) | 2016-03-17 | 2020-09-01 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors |
US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
US11147818B2 (en) | 2016-06-24 | 2021-10-19 | Infinity Pharmaceuticals, Inc. | Combination therapies |
US11214536B2 (en) | 2017-11-21 | 2022-01-04 | Inspirna, Inc. | Polymorphs and uses thereof |
US11459292B2 (en) | 2019-12-13 | 2022-10-04 | Inspirna, Inc. | Metal salts and uses thereof |
US11878956B2 (en) | 2019-12-13 | 2024-01-23 | Inspirna, Inc. | Metal salts and uses thereof |
US11174220B2 (en) | 2019-12-13 | 2021-11-16 | Inspirna, Inc. | Metal salts and uses thereof |
Also Published As
Publication number | Publication date |
---|---|
AU2002351412A1 (en) | 2003-07-30 |
US20030181420A1 (en) | 2003-09-25 |
JP2005536450A (ja) | 2005-12-02 |
AU2002351412B2 (en) | 2010-05-20 |
JP2010280732A (ja) | 2010-12-16 |
EP1465869B1 (en) | 2013-05-15 |
ES2421511T3 (es) | 2013-09-03 |
US7998986B2 (en) | 2011-08-16 |
EP1465869A1 (en) | 2004-10-13 |
CA2469435A1 (en) | 2003-07-24 |
EP1465869A4 (en) | 2005-12-28 |
JP5082033B2 (ja) | 2012-11-28 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EP1465869B1 (en) | Modulators of lxr | |
JP5237799B2 (ja) | ピラゾールベースのlxrモジュレーター | |
JP5017607B2 (ja) | 核レセプターのモジュレーター | |
EP0733033B1 (en) | Pharmaceutically active substituted aromatic compounds | |
JP5225980B2 (ja) | 11−β−ヒドロキシステロイドデヒドロゲナーゼ1の阻害剤としてのピエリジニル置換ピロリジノン | |
JP5236628B2 (ja) | 11−β−ヒドロキシステロイドデヒドロゲナーゼ1阻害剤としての、シクロヘキシルイミダゾールラクタム誘導体 | |
US20050272036A1 (en) | Ketones | |
US6005109A (en) | Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity | |
CN101248048B (zh) | 吡唑基lxr调节剂 | |
KR910003586B1 (ko) | 피리딘 화합물 및 그의 약제학적 용도 | |
AU2008239179A1 (en) | Fused bicyclic heteroaryl derivatives | |
CN101679392B (zh) | 喹诺酮化合物和药物组合物 | |
US20120309786A1 (en) | 3-amino-pyridine derivatives for the treatment of metabolic disorders | |
EP1539158A1 (en) | Aryl piperidine derivatives as inducers of ldl-receptor expression for the treatment of hypercholesterolemia | |
US6103900A (en) | Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
AK | Designated states |
Kind code of ref document: A1 Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW |
|
AL | Designated countries for regional patents |
Kind code of ref document: A1 Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LU MC NL PT SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG |
|
DFPE | Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101) | ||
121 | Ep: the epo has been informed by wipo that ep was designated in this application | ||
WWE | Wipo information: entry into national phase |
Ref document number: 2469435 Country of ref document: CA |
|
WWE | Wipo information: entry into national phase |
Ref document number: 2003559988 Country of ref document: JP |
|
WWE | Wipo information: entry into national phase |
Ref document number: 2002787071 Country of ref document: EP |
|
WWP | Wipo information: published in national office |
Ref document number: 2002787071 Country of ref document: EP |