- NOVEL COMPOUNDS
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This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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Paragraph 0265; 0266
(2013/06/27)
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- 1,2,4 -TRIAZOLES AS ALLOSTERIC MODULATORS OF MGLU5 RECEPTOR ACTIVITY FOR THE TREATMENT OF SCHIZOPHRENIA OF DEMENTIA
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This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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Page/Page column 74
(2013/06/27)
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- NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF
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The invention relates to compounds of general formula (I) wherein R1,R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in
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Page/Page column 59
(2012/02/01)
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- An efficient catalytic method for the Beckmann rearrangement of ketoximes to amides and aldoximes to nitriles mediated by propylphosphonic anhydride (T3P)
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An efficient method for the Beckmann rearrangement of ketoximes to amides mediated by a catalytic amount (15 mol %) of propylphosphonic anhydride (T3P) is described. Aldoximes underwent second order Beckmann rearrangement to provide the corresponding nitriles in excellent yields on reacting with T3P (15 mol %) at room temperature. The main advantages of this environmentally friendly protocol include procedural simplicity, and particularly ease of isolation of the products.
- Augustine, John Kallikat,Kumar, Rajesha,Bombrun, Agnes,Mandal, Ashis Baran
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p. 1074 - 1077
(2011/03/22)
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- HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
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Page/Page column 108
(2010/08/18)
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- Routes to HIV-integrase inhibitors: efficient synthesis of bicyclic pyrimidones by ring expansion or amination at a benzylic position
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Ring expansion of [6,6] bicyclic pyrimidones led, through an aziridinium intermediate, to potent HIV-integrase inhibitors with a [7,6] core. A more flexible and diversity-oriented synthesis of functionalized pyrimidohexahydrodiazepines was then developed;
- Ferreira, Maria del Rosario Rico,Cecere, Giuseppe,Pace, Paola,Summa, Vincenzo
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scheme or table
p. 148 - 151
(2009/04/14)
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- DIAZEPINE OXAZOLIDINONES AS ANTIBACTERIAL AGENTS
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The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation.
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Page/Page column 24
(2008/06/13)
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- Aminobenzoxazoles as therapeutic agents
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A compound of Formula (I), wherein the substituents are as defined herein, which are useful as kinase inhibitors.
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Page/Page column 71-72
(2010/02/15)
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- PYRROLOPYRIMIDINE DERIVATIVE
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A pyrrolo[3,2-d]pyrimidine derivative represented by the formula (I) or a pharamaceutically acceptable salt of the derivative. The derivative or salt is useful as a GSK-3 inhibitor.
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- Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases
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The preparation and SAR of a series of iNOS inhibitors leading to the most potent compound, incorporating a (1,4)-5-imino thiazepane (R = n-Pr) is disclosed. A series of 3- and 5-imino analogs from oxazepane, thiazepane, and diazepane was prepared and eva
- Shankaran,Donnelly, Karla L.,Shah, Shrenik K.,Caldwell, Charles G.,Chen, Ping,Hagmann, William K.,MacCoss, Malcolm,Humes, John L.,Pacholok, Stephen G.,Kelly, Theresa M.,Grant, Stephan K.,Wong, Kenny K.
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p. 5907 - 5911
(2007/10/03)
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- Hexahydro-5-imino-1,4-1,4-thiazepine derivatives as inhibitors of nitric oxide synthases
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Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn, eczema or psoriasis and respiratory conditions such as bronchitis, asthma, oxidant-induced lung injury and acute respiratory distress (ARDS), glomerulonephritis, restenosis, inflammatory sequelae of viral infections, myocarditis, heart failure, atherosclerosis, osteoarthritis, rheumatoid arthritis, septic arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension, retinitis and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.
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- Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
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Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastroint
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