Abstract: Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract: The present invention relates to a novel solvate of ivabradine hydrochloride, a process of its preparation and its use for the preparation of specific polymorphic forms of ivabradine hydrochloride.

Abstract: Process for the enzymatic synthesis of the compound of formula (I), (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)N-methyl methanamine: and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.

Abstract: The invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.

Abstract: Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.

Abstract: The present invention is directed to a method of enhancing visual function in a subject, comprising administering to the subject in need of such enhancement, a therapeutically effective amount of an inhibitor of a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the HCN channel inhibitor.

Abstract: Process for the synthesis of the compound of formula (I): wherein R represents a para-methoxybenzyl (PMB) group or the following group: Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: The present invention relates to pharmaceutical compositions with delayed release which contain ivabradine adipate as active substance. The present invention furthermore relates to processes for the preparation of this composition and certain salts of ivabradine.

Abstract: The invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.

Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.

Abstract: The present invention relates to a novel solvate of ivabradine hydrochloride, a process of its preparation and its use for the preparation of specific polymorphic forms of ivabradine hydrochloride.

Abstract: Stable crystalline Form II and stable crystalline Form III of ivabradine hydrochloride and processes for their preparation are disclosed.

Abstract: Ivabradine hydrochloride Form IV, its pharmaceutical composition, process for its preparation, and its use as therapeutically active ingredient.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: Process for the synthesis of the compound of formula (I): wherein R represents a para-methoxybenzyl (PMB) group or the following group: Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: The present invention relates to an If blocker or a pharmaceutically acceptable salt thereof for the treatment and/or prevention of a canine patient suffering from heart diseases, preferably heart diseases such as dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia. Each of these diseases may or may not result in heart failure (HF) in canine patients. The invention also relates to improving the quality of life, improving the general health condition as well as a prolonging the life expectancy in canine patients suffering from heart diseases and/or heart failure due to one or more of the following etiologies dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: The present invention provides a compound comprising a general formula 1: In general formula 1, X is at least one of O and S. A is a ring bridge. Y1 is at least one of H, alkyl, fluoroalkyl, aryl and heteroaryl. Z1, Z2, Z3 are, individually or alternatively, at least one of H, carbonyl, OH, O-alkyl, O-acyl, N—R1R2 (where R1 or R2 are, individually or alternatively, at least one of H, alkyl, acyl, and sulfonyl), alkyl, acyl, fluoroalkyl, aryl, and heteroaryl. R1 is at least one of alkyl, acyl, alkoxycarbonyl, aryloxycarbonyl, and aminocarbonyl. R2 is at least one of H, alkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aminocarbonyl, aryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminoacyl and peptidyl. The present invention furthermore relates to the use of the compound as a pharmaceutical active compound, and to the use of the pharmaceutical active compound to treat bacterial diseases, neurodegenerative diseases and tumors.

Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).

Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.

Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

Abstract: According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A?42 and hence are useful in treatment of Alzheimer's disease and related conditions.

Abstract: The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease.

Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.

Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).

Abstract: Methods for the preparation of Ivabradine sulfate and form I crystal thereof. In particular, the Ivabradine sulfate and the preparation methods thereof, and the stable form I crystal of Ivabradine sulfate and the preparation methods thereof.

Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.

Abstract: Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.

Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.

Abstract: Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.

Abstract: Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.

Abstract: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.

Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.