- 5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b
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A series of 5-N,N-disubstituted-5-aminopyrazole-3-carboxylic acids were prepared and found to act as highly potent and selective agonists of the G-Protein Coupled Receptor (GPCR) GPR109b, a low affinity receptor for niacin and some aromatic d-amino acids. Little activity was observed at the highly homologous higher affinity niacin receptor, GPR109a.
- Skinner, Philip J.,Webb, Peter J.,Sage, Carleton R,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Tamura, Susan Y.,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
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- POLYCYCLIC AMIDES AS UBE2K MODULATORS FOR TREATING CANCER
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Provided are compounds of Formula (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating conditions associated with modulation of UBE2K.
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Paragraph 0061; 0063-0064
(2021/07/10)
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- PYRAZOLO[1,5-D][1,2,4]TRIAZINE-5(4H)-ACETAMIDES AS INHIBITORS OF THE NLRP3 INFLAMMASOME PATHWAY
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The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasone production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R1, R2 and R3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.
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Page/Page column 57-58
(2021/10/22)
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- Nitrogen-containing ring derivative inhibitor as well as preparation method and application thereof
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The invention relates to a nitrogen-containing ring derivative inhibitor as well as a preparation method and an application thereof. In particular, the present invention relates to a compound represented by general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound, and uses of the compound as a P2X3 inhibitor in treatment of P2X3 receptor dysfunction diseases, especially in treatment of neurogenic diseases.
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Paragraph 0759-0761; 0766-0769; 0853-0855; 0860-0863
(2021/05/12)
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- PYRAZOLOPYRIMIDINE AS MALT-1 INHIBITORS
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The invention provides a compound of formula (I): herein R1, R2 and R3 of series (x), (y) and (z) are as defined in the specification which are potent inhibitors of the enzyme MALT1 and are useful in an immunooncology approach to the treatment of cancer, especially bladder cancer, colon cancer, hepatocellular cancer or small cell or non-small cell lung cancer.
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Page/Page column 78-79
(2019/01/06)
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- PYRAZOLO-PYRIMIDINE COMPOUNDS
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The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.
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Page/Page column 44
(2011/12/13)
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- PYRAZOLE COMPOUNDS AND USE THEREOF
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The pyrazole compound of the present invention is represented by the following general formula (I). The pyrazole compound of the present invention or a salt thereof or a solvate thereof potently inhibits liver glycogen phosphorylase, and, therefore, is useful as a therapeutic or prophylactic agent for diabetes. wherein each symbol denotes as described in the specifications.
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Page/Page column 21
(2009/05/29)
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- PYRAZOLOPYRIMIDINES, A PROCESS FOR THEIR PREPARATION AND THEIR USE OF MEDICINE
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Substituted pyrazolopyrimidine derivatives of formula (I) wherein R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 independently represent e.g. hydrogen or C1-6-alkyl; R8 represents a radical R9 or a radical R10, whereby one of the two radicals R8 represents R9 and the other radical R8 represents Ret; R9 represents e.g. a phenyl or thiophene group, and R10 represents e.g. hydrogen or methyl; are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
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Page/Page column 20
(2008/06/13)
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- Pyrazole compounds and their use as antidiabetes agents
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The present invention provides a pyrazole compound that has liver glycogen phosphorylase inhibitory activity and is useful as a therapeutic or prophylactic agent for diabetes, the pyrazole compound represented by the following general formula (I): wherein Ring Q represents an aryl or heteroaromatic group, R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azido group, R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group, an azido group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group, R4 and R5 are identical with or different from each other and represent a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, a C3-8 cycloalkyl group, a substituted or unsubstituted saturated heterocyclic group, a substituted or unsubstituted aryl group, a C7-14 aralkyl group, a heteroaromatic group, or the like, or a pharmacologically acceptable salt thereof.
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- 5-AMINOPYRAZOLE CARBOXYLIC ACID DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF
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The present invention relates to certain pyrazole carboxylic acid or ester derivatives of Formula (I) and pharmaceutically acceptable salts thereof which exhibit useful pharmacological properties, for example, as agonists for the GPCR referred to herein as RUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, such as, dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
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Page/Page column 62
(2008/06/13)
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- PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME
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A pyrazole compound represented by the general formula (I) or a salt thereof which has a hepatic glycogen phosphorylase inhibitory activity and therefore is useful as a therapeutic or prophylactic agent for diabetes or a pharmacologically salt thereof : wherein the ring Q represents an aryl group or an aromatic heterocyclic group; R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or an azide group; R3 represents a halogen atom, a hydroxyl group, a C1-6 alkyl group, a halo-C1-6 alkyl group, a C1-6 alkoxy group, an azide group, an amino group, an acylamino group or a C1-6 alkylsulfonylamino group; R4 and R5 independently represent a hydrogen atom, a C1-6 alkyl group which may be substituted, a a C3-8 cycloalkyl group, a saturated heterocyclic group which may be substituted, an aryl group which may be substituted, a C7-14 aralkyl group, an aromatic heterocyclic group or the like.
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Page/Page column 246-247
(2008/06/13)
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- NOVEL THIAZOLOPYRAZOLES AND METHODS OF THEIR USE
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This invention concerns novel thiazolopyrazole compounds of formula (I) and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention.
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Page/Page column 55
(2008/06/13)
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