- WNT PATHWAY INHIBITORS
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Wnt pathway inhibitors A class of compounds having general formula (I) has been identified. These compounds function as inhibitors of the Wnt pathway. Compounds of formula (I) are suitable for the treatment and/or prevention of any condition or disease in which it is desirable to inhibit signaling in the Wnt pathway, in particular inhibiting the proliferation of tumor cells, especially those associated with breast cancer, non-small cell lung cancer, pancreatic and colorectal cancers (e.g. colon carcinoma cells). The compounds also find use in methods of preventing metastasis and methods of promoting and/or directing cellular differentiation of progenitor cells.
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Page/Page column 43-44
(2013/07/05)
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- NOVEL TRPV3 MODULATORS
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Disclosed herein are modulators of TRPV3 of formula (I) wherein G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
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Paragraph 0443; 0458
(2013/06/27)
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- MST1 KINASE INHIBITORS AND METHODS OF THEIR USE
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Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.
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Page/Page column 17
(2012/09/11)
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- CYCLIC AMINOALKYLCARBOXAMIDE DERIVATIVE
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The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or -C(R6)(R7)-, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.
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Page/Page column 19
(2009/06/27)
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- SUBSTITUTED OXADIAZOLE ANALOGS AS CALCIUM CHANNEL ANTAGONISTS
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This invention relates to novel compounds of formula (I) (I) wherein R1, R2, R3, R4, R5, G1, G2, Y, n, and Ar1 are as defined in the specification, pharmaceutical compositions containing said compounds useful as calcium channel antagonists, and to methods
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Page/Page column 83
(2008/12/04)
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- NAPHTHALENONE COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS, AND USES THEREOF
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Compounds of Formula (I) and Formula (II) are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula(I) and Formula (II) have the following structures, where the definitions of the variables are provided herein.
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Page/Page column 61-62
(2008/12/06)
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- Method of treating addiction or dependence using a ligand for a monoamine receptor or transporter
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One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.
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- Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof
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One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, senile dementia, peptic ulcers, pulmonary obstruction disorders, and asthma.
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