- 5-SUBSTITUTED DIFLUOROPIPERIDINE COMPOUND CAPABLE OF PASSING THROUGH BLOOD-BRAIN BARRIER
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The present invention discloses 5-substituted difluoropiperidine compounds having a capacity to cross the blood-brain barrier; the compound has the structural formula represented by formula (I): The 5-substituted difluoropiperidine compounds, derivatives
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- SUBSTITUTED QUINAZOLINE COMPOUND HAVING BLOOD-BRAIN BARRIER PENETRATION CAPABILITY
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The present invention discloses substituted quinazoline compounds having a capacity to cross the blood-brain barrier; the compound has the structural formula represented by formula (I): The quinazoline compounds, derivatives and pharmaceutically acceptabl
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- Quinazoline derivative salt-type crystal forms and preparation method and application thereof
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The invention discloses quinazoline derivative salt-type crystal forms and a preparation method and application thereof. The quinazoline derivative salt-type crystal forms are specifically the hydrochloride crystal forms A, B, C, D, F, H, I, the sulphate
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- 3,3-DIFLUORO-PIPERIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS
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Disclosed are chemical entities of Formula (I): wherein X, Y, Z, R1, R3, R4 and R5 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
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- HETEROCYCLIC COMPOUND
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The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
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- PIPERIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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- FATTY ACID SYNTHASE INHIBITORS
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This invention relates to novel spirocyclic piperidines according to Formula (I) which are inhibitors of fatty acid synthase (FAS), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
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- Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists
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To generate novel human Orexin-2 Receptor (OX2R) antagonists, a spiropiperidine based scaffold was designed and a SAR study was carried out. Compound 4f possessed the highest OX2R antagonistic activity with an IC 50 value of 3 nM with 450-fold selectivity against Orexin-1 Receptor (OX1R).
- Fujimoto, Tatsuhiko,Tomata, Yoshihide,Kunitomo, Jun,Hirozane, Mariko,Marui, Shogo
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p. 6409 - 6413
(2011/11/29)
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