- ANTIDIABETIC BICYCLIC COMPOUNDS
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Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-co
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- SYK INHIBITORS
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The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease slates, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk. In certain embodiments, also disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, in combination with a vinca-alkaloid, or a pharmaceutically acceptable salt thereof.
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Paragraph 0279
(2016/02/26)
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- TREATMENT OF CHRONIC GRAFT VERSUS HOST DISEASE WITH SYK INHIBITORS
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The present disclosure provides methods of utilizing Syk inhibiting compounds in the treatment for graft versus host disease (GVHD) in a human, including acute graft versus host disease (aGVHD) and chronic graft versus host disease (cGVHD), including the use of compounds selected from the group consisting of the formulas below: (I) and (II).
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Page/Page column 32-33
(2016/11/17)
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- SYK INHIBITORS
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The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
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Paragraph 0242; 0243
(2015/07/02)
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- SYK INHIBITORS
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The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
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Page/Page column 99
(2015/07/15)
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- Novel Heterocyclic Compounds and Uses Thereof
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New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
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Paragraph 0390
(2013/08/28)
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- TRIAZOLE AMIDE DERIVATIVES FOR USE IN THERAPY
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The invention relates to triazole amide derivatives of formula (I) for use in therapy, in particular for treating diseases and conditions mediated by antagonism of the mGluR5 receptor, in particular substance related disorders. The invention also relates to certain novel derivatives. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
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Page/Page column 25-26
(2009/10/22)
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- NOVEL HETEROCYCLIC COMPOUNDS AND USES THEROF
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New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
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Page/Page column 117-118
(2009/10/22)
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- HETEROARYL COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
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Page/Page column 101
(2008/12/05)
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- CRF1 RECEPTOR LIGANDS COMPRISING FUSED BICYCLIC HETEROARYL MOIETIES
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Substituted heteroaryl fused pyridine, pyrazine, and related heterobicyclic compounds that act as selective modulators of CRF1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, gastrointestinal disorders, and eating disorders. Methods of treatment of such disorders as well as packaged pharmaceutical compositions are also provided. Compounds provided herein are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
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Page/Page column 85
(2008/12/07)
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- A general and efficient route to 6-methyl-pyrazin-2-yl-amines: Alkylation of 2,6-dichloropyrazine via malonate derivatives
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(Chemical Equation Presented) We have developed a convenient two-stage process for the synthesis of 6-methylpyrazine-2-yl-amines from commercially available materials. The procedure involves the synthesis of (6-chloro-pyrazin-2-yl)-acetic acid via arylati
- Colbon, Paul J. J.,Foster, Alison C.,Giles, Melvyn E.,Patel, Zakariya,Singleton, John T.
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experimental part
p. 1451 - 1456
(2009/04/07)
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- NOVEL PROCESS FOR THE PREPARATION OF 6-METHYL-PYRAZIN-2-YLAMINE
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A new process for the preparation of 6-methyl-pyrazin-2- ylamine is described. The process involves reacting 2,6- dichloropyrazine with a dialkylmalonate followed by subsequent decarboxylation rendering a new compound, 6-chloro-pyrazin-2- yl -'acetic acid. Further decarboxylation and amination renders the desired product.
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Page/Page column 2; 4-5
(2008/06/13)
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- NOVEL N-PYRAZINIL-PHENYLSULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS FOR USE IN THE TREATMENT OF ASTHMA
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The invention provides a compound of formula (I), wherein R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
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Page/Page column 28-29
(2010/11/26)
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- A convenient one-pot Negishi coupling of amino-heteroaryl chlorides and alkyl bromides
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A simple Ni-catalysed cross-coupling protocol for amino-heteroaryl chlorides with alkylzinc reagents has been developed. The alkylzinc reagents can be commercially available dialkylzincs or alkylzinc halides, or can be conveniently generated in situ from diethylzinc and primary alkyl bromides in the presence of the same inexpensive Ni catalyst used to effect the subsequent coupling reaction.
- Walters, Iain A.S.
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p. 341 - 344
(2007/10/03)
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- SULPHONAMIDE COMPOUNDS THAT MODULATE CHEMOKINE RECEPTOR ACTIVITY (CCR4)
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The invention relates to sulphonamide compounds, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
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- Research on heterocyclic compounds. XXXVII. Synthesis and antiinflammatory activity of methyl-substituted imidazo[1,2-a]pyrazine derivatives
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A series of methyl-substituted imidazo[1,2-a]pyrazines 8 bearing a carboxylic acid group on the imidazole ring were synthesized. The structures of new compounds were confirmed by 1H- and 13C-NMR spectral data; the correct assignment of carbon resonances was made by means of HETCOR and COLOC experiments. Antiinflammatory, analgesic and ulcerogenic activities in vivo were evaluated and compared with those of antiinflammatory imidazopyrazines (2 and 3) and indomethacin. The inhibitory action on cyclooxygenase activity was evaluated in vitro. Compounds 8 were found to be less potent than indomethacin in these assays. SARs are discussed.
- Rimoli,Avallone,De Caprariis,Luraschi,Abignente,Filippelli,Berrino,Rossi
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p. 195 - 203
(2007/10/03)
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- Studies on Pyrazines. 6. A Facile Separation Method for a Mixture of the Isomeric 2-Amino-3,5, and 6-methylpyrazines
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This paper describes a facile separation method for a mixture of the isomeric aminomethylpyrazines by two-stage processes.Thus the mixture of aminomethylpyrazines was converted into that of the aminobromomethylpyrazines, which could be separated by chromatography on silica gel.Each of the bromopyrazines was hydrogenated to regenerate the original aminopyrazine as a pure form.
- Sato, Nobuhiro
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p. 143 - 147
(2007/10/02)
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