- INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
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Page/Page column 148; 149
(2021/01/29)
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- Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human
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The discovery and optimization of a novel series of GPR142 agonists are described. These led to the identification of compound 21 (LY3325656), which demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. Compound 21 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.
- Chen, Jiehao,Efanov, Alexander M.,Fang, Xiankang,Jiang, Yi,Jun Zhang, Xue,Li, Lei,Lin, Hua V.,Liu, Jia,Liu, Lian Zhu,Long Hu, Zhi,Ma, Tianwei,Thomas, Melissa K,Wang, Fan,Wang, Jingru,Xiao, Fei,Xu, Jianfeng,Zeng, Mi,Zhang, Lei,Zhen Zhang, Hai,Zhou, Jingye,Zou, Haixia,Zou, Zack
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supporting information
(2020/01/28)
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- Tetrahydropyranyl Benzamide Derivatives
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The present invention provides compounds of the Formula below wherein R, R1-R3 are as described herein; methods of treating patients for diabetes using the compounds, and processes for preparing the compounds
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Paragraph 0069-0070
(2018/07/31)
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
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Page/Page column 86
(2009/01/23)
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- ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA
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This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy.
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Page/Page column 56
(2008/06/13)
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- Novel farnesyl protein transferase inhibitors as antitumor agents
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Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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- Synthesis and structure-activity relationships of new (5R,8R,10R)-ergoline derivatives with antihypertensive or dopaminergic activity
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A series of new (5R,8R,10R)-ergoline derivatives was synthesized, and their antihypertensive and dopaminergic activities were tested in conscious spontaneously hypertensive rats and in rats with unilateral 6- hydroxydopamine-induced lesions of the substantia nigra. (5R,8R,10R)-6- Alkyl-8-ergolinemethanols, prepared from the corresponding ergolinecarboxylates, were converted to the tosylates, which were treated with various five-membered heterocycles containing nitrogen atoms to afford the new ergolines. (5R,8R,10R)-8-(1,2,4-Triazol-1-ylmethyl)-6-methylergoline (4s, maleate: BAM-1110) exhibited potent dopaminergic activity, about 18- fold greater than that of bromocriptine mesylate. (5R,8R,10R)-8-(1,2,4- Triazol-1-ylmethyl)-6-propylergoline (8b, fumarate: BAM-1602) showed extremely potent dopaminergic activity, being about 220 and 1.15 times more active than bromocriptine mesylate and pergolide mesylate, respectively. Several compounds exhibited potent antihypertensive activity. Structure- activity relationships for antihypertensive and dopaminergic activities are discussed.
- Ohno,Adachi,Koumori,Mizukoshi,Nagasaka,Ichihara,Kato -
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p. 1463 - 1473
(2007/10/02)
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