- PLASMA KALLIKREIN INHIBITORS
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The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
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- INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL
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The present invention relates to pharmaceutical compounds of the Formula (I), or a pharmaceutically acceptable salt or composition thereof, and methods of their use for the treatment of pain, respiratory conditions, as well as inhibiting the Transient Receptor Potential Al ion channel (TRPA1).
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- HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
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Provided are certain histone deacetylase (HDAC) inhibitors of Formula (I), compositions thereof, and methods of their use.
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Paragraph 0200
(2016/11/21)
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- INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL
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The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential Al ion channel (TRPA1).
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- IMIDAZOPYRIDAZINE COMPOUNDS
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The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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- IMIDAZOPYRIDAZINE COMPOUNDS
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The present invention relates to the use of novel compounds of formula (I): wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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- CYCLOPROPYL-FUSED PYRROLIDINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE IV INHIBITORS
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The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.
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Page/Page column 28; 29; 30
(2008/06/13)
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- NOVEL AMINOALCOHOL-SUBSTITUTED ARYLDIHYDROISOQUINOLINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
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The invention relates to aminoalcohol-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one aminoalcohol-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the aminoalcohol- substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.
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Page/Page column 111
(2008/06/13)
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- Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
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The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with β-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold.
- Simpkins, Ligaya M.,Bolton, Scott,Pi, Zulan,Sutton, James C.,Kwon, Chet,Zhao, Guohua,Magnin, David R.,Augeri, David J.,Gungor, Timur,Rotella, David P.,Sun, Zhong,Liu, Yajun,Slusarchyk, William S.,Marcinkeviciene, Jovita,Robertson, James G.,Wang, Aiying,Robl, Jeffrey A.,Atwal, Karnail S.,Zahler, Robert L.,Parker, Rex A.,Kirby, Mark S.,Hamann, Lawrence G.
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p. 6476 - 6480
(2008/09/16)
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- Design, synthesis and activity of novel derivatives of Oxybutynin and Tolterodine
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Novel derivatives of Tolterodine (1) and Oxybutynin (2) have been designed using conformationally restricted azabicyclics as replacement for open-chain amines. The synthesis and structure-activity relationships are presented.
- Kaur, Kirandeep,Aeron, Shelly,Bruhaspathy, Miriyala,Shetty, Shankar J.,Gupta, Suman,Hegde, Laxminarayan H.,Silamkoti, Arun D. V.,Mehta, Anita,Chugh, Anita,Gupta, Jang B.,Sarma,Kumar, Naresh
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p. 2093 - 2096
(2007/10/03)
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