- PROSTAGLANDIN E2 (PGE2) EP4 RECEPTOR ANTAGONISTS
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The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.
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Page/Page column 78; 82; 159; 163
(2021/04/10)
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- CYCLIC COMPOUNDS AND METHODS OF USING SAME
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The present application relates to compounds of Formula (I), as defined herein, and pharmaceutically acceptable salts thereof which are MALT1 inhibitors. The present application also describes pharmaceutical composition comprising a compound of Formula (I), and pharmaceutically acceptable salts thereof, and methods of using the compounds and compositions for treating diseases, such as cancer, autoimmune disorders, and inflammatory disorders.
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Page/Page column 192-193
(2021/07/02)
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- Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)
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The discovery of potent, peptide site directed, tyrosine kinase inhibitors has remained an elusive goal. Herein we describe the discovery of two such clinical candidates that inhibit the tyrosine kinase Src. Compound 1 is a phase 3 clinical trial candidat
- Smolinski, Michael P.,Bu, Yahao,Clements, James,Gelman, Irwin H.,Hegab, Taher,Cutler, David L.,Fang, Jane W. S.,Fetterly, Gerald,Kwan, Rudolf,Barnett, Allen,Lau, Johnson Y. N.,Hangauer, David G.
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supporting information
p. 4704 - 4719
(2018/06/20)
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- BIARYL COMPOSITIONS AND METHODS FOR MODULATING A KINASE CASCADE
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The application relates to biaryl compounds, pharmaceutical compositions comprising the compounds, and methods of use the compounds for treating cell proliferation disorders.
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Page/Page column 92-93
(2018/03/06)
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- 3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00602; 00605; 00606
(2017/10/06)
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- 8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER
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Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.
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- IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
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The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
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Page/Page column 87
(2011/05/11)
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- IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
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The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
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Page/Page column 38
(2011/11/12)
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- Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials
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Novel antibacterial biaryl oxazolidinones bearing an aza-, an oxa-, or a thiabicyclo[3.1.0]hex-6-yl ring system were synthesized, and their in vitro antibacterial activity and structure-activity relationships (SAR) were evaluated. Most of the synthesized
- Komine, Takashi,Kojima, Akihiko,Asahina, Yoshikazu,Saito, Tatsuhiro,Takano, Hisashi,Shibue, Taku,Fukuda, Yasumichi
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supporting information; experimental part
p. 6558 - 6562
(2009/10/23)
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- Facile cyanomethylation of bromopyridines by nucleophilic substitution with lithioacetonitrile
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Substituted bromopyridines undergo facile nucleophilic substitution with lithioacetonitrile under mild conditions to afford the corresponding cyanomethylated products.
- Skerlj,Bogucki,Bridger
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p. 1488 - 1490
(2007/10/03)
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