- INDANYLAMINOPYRIDYLCYCLOPROPANECARBOXYLIC ACIDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are as defined herein, which compounds have valuable pharmacological properties, in particular their ability to bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular type 2 diabetes. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
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Paragraph 0303; 0304
(2018/06/09)
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- BENZYLOXYPYRIDYLCYCLOPROPANECARBOXYLIC ACIDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The present invention relates to compounds of general formula (I), wherein the groups R, R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 42
(2018/08/20)
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- BENZYLAMINOPYRIDYLCYCLOPROPANECARBOXYLIC ACIDS, PHARMACEUTICALCOMPOSITIONS AND USES THEREOF
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The present invention relates to compounds of general formula (I), wherein the groups R, R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 45
(2018/08/20)
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- IMIDAZOPYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER
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A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.
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Paragraph 00240
(2018/04/12)
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- ARYLOXYMETHYL CYCLOPROPANE DERIVATIVES AS PDE10 INHIBITORS
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The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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Paragraph 0125; 0128
(2016/10/31)
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- TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF
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A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.
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Paragraph 0459; 0460
(2016/07/27)
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- PYRIMIDINE PDE10 INHIBITORS
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The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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Page/Page column 41
(2013/03/26)
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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 89
(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 39
(2011/11/12)
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- LINCOMYCIN DERIVATIVES AND ANTIBACTERIAL AGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 represents N-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
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Page/Page column 43-44
(2010/03/02)
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- Ring-closing metathesis reactions on azinium salts: Straightforward access to quinolizinium cations and their dihydro derivatives
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(Chemical Equation Presented) The ring-closing metathesis reaction of 1-butenyl-2-vinylpyridinium salts and 2-butenyl-1-vinylpyridinium salts using Grubbs second generation and Hoveyda-Grubbs catalysts proved to be an efficient approach to 3,4-dihydro- and 1,2-dihydroquinolizinium salts and the corresponding quinolizinium derivatives by an improved thermal oxidation in the presence of Pd/C without solvent. A comparative study showed that the quinolizinium system was obtained in better yields through the 3,4-dihydroquinolizinium route, thus allowing the synthesis of quinolizinium derivatives or improvements in the yields of some examples reported previously.
- Nunez, Ana,Abarca, Beatriz,Cuadro, Ana M.,Alvarez-Builla, Julio,Vaquero, Juan J.
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scheme or table
p. 4166 - 4176
(2009/09/08)
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- Synthesis of Substituted 1,4-Divinylbenzenes by Heck Reactions with Compressed Ethene
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Substituted 1,4-divinylbenzenes 3a-i were synthesized by twofold Heck coupling from the corresponding 1,4-dibromo- (electron withdrawing substituents) or 1,4-diiododialkoxybenzenes 1a-i and ethene. Oligomerizations could be suppressed by increasing the pressure of ethene to 30 bar, simultaneously improving the yields of the title compounds.
- Detert, Heiner,Sugiono, Erli
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p. 358 - 362
(2007/10/03)
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- Alternating poly(pyridyl vinylene phenylene vinylene)s: Synthesis and solid state organizations
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Poly(pyridyl vinylene phenylene vinylenes) were synthesized by Heck coupling procedures. These materials display large red shifts in their optical absorption which upon protonation or alkylation of the pyridyl nitrogen. Some of the polymers were found to be liquid crystalline. The protonated or alkylated versions exhibit highly organized structures due to charge-transfer interactions between polymer chains.
- Fu, Dian-Kui,Xu, Bing,Swager, Timothy M.
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p. 15487 - 15494
(2007/10/03)
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