- NOVEL APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS
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The present invention relates to inhibitors of apoptosis signal-regulating kinase 1 ("ASK1"), a process for synthesis of the compounds of the present invention, composition comprising the compounds and use of the compounds for inhibition of ASK1.
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- Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors
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Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]pyridin
- Fidanze, Steven D.,Liu, Dachun,Mantei, Robert A.,Hasvold, Lisa A.,Pratt, John K.,Sheppard, George S.,Wang, Le,Holms, James H.,Dai, Yujia,Aguirre, Ana,Bogdan, Andrew,Dietrich, Justin D.,Marjanovic, Jasmina,Park, Chang H.,Hutchins, Charles W.,Lin, Xiaoyu,Bui, Mai H.,Huang, Xiaoli,Wilcox, Denise,Li, Leiming,Wang, Rongqi,Kovar, Peter,Magoc, Terrance J.,Rajaraman, Ganesh,Albert, Daniel H.,Shen, Yu,Kati, Warren M.,McDaniel, Keith F.
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supporting information
p. 1804 - 1810
(2018/04/23)
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- CATHEPSIN K INHIBITOR AND APPLICATION THEREOF
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The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.
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Paragraph 0390
(2018/07/29)
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- BROMODOMAIN INHIBITORS
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The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specificati
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Paragraph 0784
(2014/09/29)
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- DIHYDRO-PYRROLOPYRIDINONE INHIBITORS
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The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
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Paragraph 1266
(2014/09/29)
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- TETRACYCLIC BROMODOMAIN INHIBITORS
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The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Υ2, Υ3, A1, A2, A3 and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
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Page/Page column 106
(2014/09/29)
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- 4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES
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The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.
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Page/Page column 19
(2010/08/08)
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- SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.
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Page/Page column 319-320
(2008/12/05)
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- SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened orhedgehog activity.
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Page/Page column 319-320
(2008/12/05)
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- ACYL BIPIPERIDINYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
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Page/Page column 31
(2008/12/06)
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- BIPIPERIDINYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
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Page/Page column 30; 117
(2008/12/07)
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- PROCESSES FOR THE PREPARATION OF COMPOUNDS
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The present invention provides improved synthetic methods for the preparation of compounds that modulate proliferation or differentiation in a cell or tissue.
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Page/Page column 230
(2010/11/28)
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- BIOTRANSFORMATION OF ORGANIC SULFIDES. PART 6. FORMATION OF CHIRAL para-SUBSTITUTED BENZYL METHYL SULFOXIDES BY HELMINTHOSPORIUM SPECIES NRRL 4671
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The fungus Helminthosporium species NRRL 4671 has been used for the biotransformation of a series of para-substituted benzyl sulfides with substituent groups consisting of trifluoromethyl, halo, hydroxy, methoxy, acetoxy, nitro, cyano, amino, acetamido, acyl and carboxylic acid units.In all cases, sulfoxide formation occurred in good yoeld and with predominant (S) chirality at the sulfur position.A minor amount of sulfone product was also obtained from the halo- and methoxy-substituted substrates.
- Holland, Herbert L.,Brown, Frances M.,Larsen, Brett G.
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p. 1561 - 1568
(2007/10/02)
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