- NOVEL BENZIMIDAMIDES COMPOUNDS COMPRISING AN OXABORININ RING
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The invention relates to 4-(1-hydroxy-3,4-dihydro-1H-benzo[c][1,2]oxaborinin-3-yl)benzimidamide derivatives and their use in treating diseases and conditions of the skin (for example, Netherton syndrome, rosacea, atopic dermatitis, psoriasis and itch) cau
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- THIAZALOPYRROLIDINE INHIBITORS OF ROR-GAMMA
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Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
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- Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK)
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Thymidylate kinase (TMK) is an essential enzyme in bacterial DNA synthesis. The deoxythymidine monophosphate (dTMP) substrate binding pocket was targeted in a rational-design, structure-supported effort, yielding a unique series of antibacterial agents sh
- Martínez-Botella, Gabriel,Breen, John N.,Duffy, James E.S.,Dumas, Jacques,Geng, Bolin,Gowers, Ian K.,Green, Oluyinka M.,Guler, Satenig,Hentemann, Martin F.,Hernandez-Juan, Felix A.,Joseph-McCarthy, Diane,Kawatkar, Sameer,Larsen, Nicholas A.,Lazari, Ovadia,Loch, James T.,Macritchie, Jacqueline A.,McKenzie, Andrew R.,Newman, Joseph V.,Olivier, Nelson B.,Otterson, Linda G.,Owens, Andrew P.,Read, Jon,Sheppard, David W.,Keating, Thomas A.
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p. 10010 - 10021
(2013/01/16)
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- IMIDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
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The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
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Page/Page column 29
(2010/01/07)
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- Tricyclic oxazolidone derivatives useful as PR modulators
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Compounds of the following structure are described: wherein R1-R6, R16, m, V, W, X, Y, and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are use
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Page/Page column 17
(2008/06/13)
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- Oxazolidone derivatives as PR modulators
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Compounds of the following structure are described: wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
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Page/Page column 34
(2008/06/13)
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- Imidazolidin-2-one derivatives useful as PR modulators
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Compounds of the following structure are described: wherein R1-R6, R10, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful f
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Page/Page column 17
(2010/11/30)
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- Pyrrolidine and related derivatives useful as PR modulators
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Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compou
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Page/Page column 17
(2010/11/30)
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- Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of pde4 isozymes
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Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.0): 1 wherein R5 and R6 are
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- Pyrimidine carboxamides useful as inhibitors of pde4 isozymes
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Compounds of formula (1.0.0) are described, as well as the usefulness of a pharmaceutical composition for treating inflammatory, respiratory and allergic diseases and conditions, especially asthma; chronic obstructive pulmonary disease (COPD) including chronic bronchitis, emphysema, and bronchiectasis; chronic rhinitis; and chronic sinusitis.
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- INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
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The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this inv
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds
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- Inhibitors of prenyl-protein transferase
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The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
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