- IAP ANTAGONISTS AND THEIR THERAPEUTIC APPLICATIONS
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The present invention relates to Formula I. compounds including their isomers, tautomeric forms and rotamers, salts together with their manufacturing process and their pharmacological use alone or in combination with other active ingredients for the treatment of cell and tissue malignances caused diseases, including uncontrolled cell or tissue growth, proliferation and cancer.
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Page/Page column 34-35
(2021/11/06)
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- CYCLIC AMINE DERIVATIVE AND MEDICAL USE THEREOF
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A cyclic amine derivative represented by general Formula (I): wherein R1 represents an alkyl group having 1 to 3 carbon atoms; A represents a group represented by general Formula (II-1), (II-2), or (II-3): R2 represents a hydrogen at
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Paragraph 0318-0321
(2020/12/25)
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- Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics
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The enormous prevalence of infections caused by parasitic nematodes worldwide, coupled to the rapid emergence of their resistance to commonly used anthelmintic drugs, presents an urgent need for the discovery of new drugs. Herein, we have identified several classes of small molecules with broad spectrum activity against these pathogens. Previously, we reported the identification of carnitine palmitoyltransferases (CPTs) as a representative class of enzymes as potential targets for metabolic chokepoint intervention that was elucidated from a combination of chemogenomic screening and experimental testing in nematodes. Expanding on these previous findings, we have discovered that several chemical classes of known small molecule inhibitors of mammalian CPTs have potent activity as anthelmintics. Cross-clade efficacy against a broad spectrum of adult parasitic nematodes was demonstrated for multiple compounds from different series. Several analogs of these initial hit compounds were designed and synthesized. The compounds we report represent a good starting point for further lead identification and optimization for development of new anthelmintic drugs with broad spectrum activity and a novel mechanism of action.
- Tyagi, Rahul,Maddirala, Amarendar Reddy,Elfawal, Mostafa,Fischer, Chelsea,Bulman, Christina A.,Rosa, Bruce A.,Gao, Xin,Chugani, Ryan,Zhou, Mingzhou,Helander, Jon,Brindley, Paul J.,Tseng, Chih-Chung,Greig, Iain R.,Sakanari, Judy,Wildman, Scott A.,Aroian, Raffi,Janetka, James W.,Mitreva, Makedonka
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p. 1130 - 1145
(2018/05/15)
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- PIPERIDINE-AMIDE DERIVATIVES
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The invention is concerned with novel piperidine-amide derivatives of formula (I) wherein R1, R2, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These comp
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Page/Page column 9
(2009/01/20)
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- POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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The present invention is to provide a novel compound (I), having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. Compound (I) wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
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Page/Page column 121; 151
(2010/11/24)
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- THERAPEUTIC COMPOUNDS: PYRIDINE AS SCAFFOLD
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Compounds of formulas I, IA, and IB or IC or pharmaceutically acceptable salts thereof: wherein A, A1, A2, A3, A4, R2, R3, R4 and n are as defined in the specifications well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 103
(2010/02/14)
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