- TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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The present invention is directed to substituted indole compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, adisease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
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Page/Page column 51; 52
(2016/05/02)
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- PROCESS FOR THE PREPARATION OF ANDROGEN RECEPTOR ANTAGONISTS AND INTERMEDIATES THEREOF
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The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H- pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3- carboxamide (1A) and key intermediates thereof such as 2-chloro-4- (IH-pyrazol-3-yl)benzonitrile (V). AR antagonists are useful in the treatment of cancer, particularly prostate cancer and other diseases where AR antagonism is desired.
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Page/Page column 14
(2016/10/31)
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- PHENYLALANINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS
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Provided herein are compounds of formula I: wherein A, B, X, R1 , R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions
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Page/Page column 63
(2010/09/03)
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- 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS
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3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
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Page/Page column 147-148
(2010/04/03)
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- A simple, modular method for the synthesis of 3,4,5-trisubstituted pyrazoles
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(Chemical Equation Presented) A modular approach for the regiocontrolled preparation of pyrazoles bearing substituents on all three carbon atoms is described. Central to this method is the use of a switchable metal-directing group (MDG) to enable sequential direct lithiation of the 3- and 5-positions of the pyrazole ring. Pyrazole boronic esters obtained from these lithiated intermediates can undergo efficient Suzuki cross-coupling under the developed nonaqueous conditions, which minimize undesirable protolytic deboronation. Halogenation of the 4-position provides the means for substitution at the remaining carbon atom.
- McLaughlin, Mark,Marcantonio, Karen,Chen, G-Yi,Davies, Ian W.
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p. 4309 - 4312
(2008/09/21)
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- A facile synthetic route to new pyrazoloisoindolones
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A facile method for the synthesis of new pyrazoloisoindolones via a Suzuki cross-coupling reaction using a pyrazolylboronic ester is described.
- Gérard, Anne-Laure,Mahatsekake, Clément,Collot, Valérie,Rault, Sylvain
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p. 4123 - 4126
(2008/02/03)
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- Efficient and simple synthesis of 3-aryl-1H-pyrazoles
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Efficient preparation of 3-aryl-1H-pyrazoles by reaction of 1-protected-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoles with (het)aryl halides is described. The choice of THP protecting group is discussed.
- Gérard, Anne-Laure,Bouillon, Alexandre,Mahatsekake, Clément,Collot, Valérie,Rault, Sylvain
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p. 4665 - 4669
(2007/10/03)
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