- NOVEL IN-VIVO PROBE FOR REAL TIME LONGITUDINAL MONITORING OF INDUCIBLE NITRIC-OXIDE SYNTHASE IN LIVING CELLS AND ANIMALS
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The present disclosure relates to an in vivo fluorescent or radioactive probe represented by a compound of formula I which is capable of longitudinal imaging of inducible nitric oxide synthase (iNOS) expression in living cells and living animals on a real time basis. The probe of the present disclosure can exhibit specific and high affinity binding to the iNOS enzyme with reduced enzyme inhibitory property and also enables longitudinal monitoring of iNOS expression along with its activity or NO production in a same experimental subject throughout the progression of a physiological or disease process without employing separate subjects as controls and experimental. The present disclosure further provides a rapid and inexpensive real time method for visualizing iNOS expression and its activity in living cells and living animals precisely, conveniently and reversibly along with simultaneous in vivo imaging of its catalytic product, nitric oxide (NO) in live physiological settings.
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Paragraph 0077
(2018/06/06)
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- Benzodiazepine and Pyridodiazepine Derivatives
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The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
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Page/Page column 39-40
(2011/12/12)
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- DIBENZO[B,F][1,4]OXAZAPINE COMPOUNDS
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The present invention relates to 11-(piperazin-l-yl)dibenzo[b,f][l,4]oxazapine compounds of the formula I (I) where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.
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- ENANTIOPURE HETEROCYCLIC COMPOUND USEFUL FOR THE PREPARATION OF PEPTIDES WHICH CAN BE POTENTIALLY USED AS MEDICAMENTS
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Enantiopure heterocyclic compound Enantiopure heterocyclic compound of formula (I) in which J is chosen from C, N, O and S; Z is H or a group for protecting the amino functional group, R3 denotes H or an organic residue, m is 0, 1 or 2 and n is 0, 1 or 2, and in which the heterocycle is preferably substituted with at least one substituent other than CH2-COOR3.
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Page/Page column 16-17
(2008/06/13)
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- Sulfonyl derivatives
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Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1is hydrogen, hydroxyl, nitro or the like; R2and R3are each independently hydrogen, halogeno or the like; R4and R5are each dependently hydrogen, halogeno or the like; Q1is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2is a single bond, oxygen or the like; Q3is, e.g., a group represented by formula (a): T1is carbonyl or the like; and X1and X2are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.
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- NOVEL SULFONYL DERIVATIVES
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Sulfonyl derivatives represented by the following general formula (I): Q1-Q2-T1-Q3-SO2-QA and drugs containing the same (wherein Q1 is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q2 is a single band, oxygen, sulfur, C1-C6 alkylene or the like; QA is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T1 is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
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