Abstract: The invention relates to new compounds of formula (III): wherein R is a C1-C4 linear or branched alkyl group. The invention also relates to new compounds of formula (IV) wherein M is a metal. The invention also relates to methods of making compounds of formulas (III) and (IV) and to methods of making donepezil and pharmaceutically acceptable salts thereof, such as donepezil hydrochloride, using the compounds.

Abstract: The present invention provides novel crystalline forms of donepezil hydrochloride, processes for their preparation and pharmaceutical compositions containing them.

Abstract: 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine p-toluenesulfonate or a solvate thereof.

Abstract: This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-up-take inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.

Abstract: The present invention relates to 2,5-di-substituted-4-naphthyloxy-substituted-phenyl-amidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.

Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: The present invention relates to a new process for the preparation of intermediate compounds useful in the manufacture of donepezil, or a pharmaceutically-acceptable salt thereof, and also relates to processes for preparing donepezil and to the novel intermediates per se. In addition the invention relates to various hydrated forms of donepezil.

Abstract: Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

Abstract: The present invention provides a simple method of producing polymorphic crystal (III), which has high safety to environment and the bodies of operators; is gentle to environment; and can produce at low costs; and has a high refining effect. It is a method of producing polymorphic crystal (III) of donepezil hydrochloride (chemical name: 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine•monohydrochloride) represented by the following structural formula (formula (I)), which comprises dissolving donepezil (chemical name: 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine) in ethanol; and adding hydrochloric acid or hydrogen chloride thereto, followed by stirring.

Abstract: A pharmaceutical composition is provided according to the invention which is suited for the production of tablets by direct compression and which contains donepezil hydrochloride of polymorphic form I. The polymorphic form I of donepezil hydrochloride in the directly compressed tablet is also stable during long storage.

Abstract: The present invention provides a novel, industrially realizable and economically preferable process for production of highly pure 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride, i.e., donepezil hydrochloride shown in the following reaction scheme, in Polymorph (I) morphological crystal form. (I) In one of the key steps of the process, during the hydrogenation 5,6-dimethoxy 2-(pyridine-4-yhnethylene)indan-1-one hydrochloride is saturated using Pd carbon to get 4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl piperidine at more than 97% HPLC purity. In the crystallization step donepezil-hydrochloride is crystallized from an aqueous alcoholic solvent to get Polymorph (I) in at least 99.95% HPLC purity.

Abstract: The invention provides pyrrolidino-substituted 1,4-naphthoquinone derivatives that modulate the activity of protein kinases, and it relates to the use of the derivatives in pharmaceutical compositions for treating cardiovascular disorders and malignancies. The invention particularly provides medicaments for treating disorders associated with MAPKs signaling, ERKs signaling, p38 signaling, and JNKs signaling.

Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.

Abstract: The present invention relates to the oxalate salt of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methyl piperidine, commonly known as Donepezil, and its method of preparation.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.

Abstract: The present invention relates to the mesylate salt of 1-(4-(2-piperidinylethoxy)phenoxy)-2-(3-hydroxyphenyl)-6-hydroxynaphthalene.

Abstract: Novel crystalline forms of Donepezil base, processes for producing same, pharmaceutical compositions containing same and methods of treatment utilizing same are disclosed.

Abstract: The invention relates to donepezil salts formed with organic acids and a process for the preparation thereof. Said salts can be used for the preparation of pharmaceutical compositions. The invention also relates to a process for the preparation of said salts, pharmaceutical compositions containing them and the use of said compounds for the treatment of diseases.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.

Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrom, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.

Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation, and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

Abstract: A process for preparing crystalline form I of donepezil hydrochloride comprises: a) condensing 5,6-dimethoxy-2-piperidin-4-yl-methyl-indan-1-one with benzyl bromide and reacting a condensation product with hydrobromic acid to form donepezil hydrobromide; and b) hydrolyzing donepezil hydrobromide, followed by reacting with aqueous hydrochloric acid.

Abstract: New salts of donepezil, and new polymorphic forms of donepezil and its salts, and methods to prepare both the amorphous form and various polymorphic forms of donepezil or its salts.

Abstract: This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

Abstract: 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine or hydrochloride thereof, which is useful as a drug, can be produced in high purity by safer and easier operations suitable for industrial production by subjecting 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methyl-piperidine or a solvate thereof to catalytic hydrogenation in the presence of a palladium-alumina catalyst and if necessary, converting the thus obtained compound to its hydrochloride.

Abstract: Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives thereof, wherein: R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, arylC1-6alkoxy, heteroarylC1-6alkoxy, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, arylC1-6alkylamino, heteroarylC1-6alkyamino; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 and R4 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl,(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6 alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; and wherein any alkyl group or the alkyl moiety of any group cont

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: The present invention discloses a novel, stable polymorph of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine hydrochloride commonly known as Donepezil hydrochloride. Further the present invention discloses a process for producing Donepezil HCl amorphous and its polymorph Form (VI).

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.

Abstract: An efficient process for preparation of donepezil is provided. In one embodiment, the process for preparation of donepezil includes suspending a catalyst, which is palladium metal on carbon and the compound of the structure in an alcoholic solvent and hydrogenating the suspension at the hydrogen pressure of from about 1 to about 5 and a temperature of from about 40 to about 90° C. till the hydrogenation reaction is substantially complete to obtain a compound of the formula (VI): which then converted to donepezil. The processes of the invention are believed to be simple, eco-friendly, and commercially viable.

Abstract: Novel polycyclic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.

Abstract: Compounds of formula (I) or a derivative thereof, wherein; R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 is hydrogen or C1-6alkyl; R4 and R5 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; with the proviso that, when R3 is hydrogen, then R4 and R5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by

Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.

Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a compound represented by formula: (wherein R1 and R2 represent substituents), a pharmacologically acceptable salt thereof or hydrates thereof.

Abstract: This invention relates to novel {overscore (?)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.

Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula (IA), wherein R1, R2, R3 and R4 are as described in the specification.

Abstract: 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections

Abstract: Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl

Abstract: A process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine hydrochloride (Donepezil HCl) is disclosed. 5,6-Dimethoxy-2-(pyridin-4-yl) methylene inda-1-one is hydrogenated with a noble metal catalyst or a non-oxide derivative of a noble metal catalyst in a solvent at 20-100° C. and 10-90 psi gauge pressure. The resulting 4-[(5,6-dimethoxy-1-indanon)-2-yl] methyl piperidine is alkylated with an alkylating agent in an organic solvent at 20-80° C.

Abstract: The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action. It provides a compound represented by the formula: (In the formula, R1 represents a group represented by the formula: (wherein, R3, R4, R5 and R6 are the same as or different from each other and each represents a hydrogen atom, an optionally substituted C1-6 alkoxy group and the like; and m represents an integer from 0 to 6) and the like; and R2 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C2-6 alkenyl group or an optionally substituted C2-6 alkynyl group), a salt thereof or a hydrate of them.

Abstract: The invention provides a process for the preparation of a compound of the formula 6 comprising the hydrolysis and decarboxylation of a compound of the formula 5 according to the reaction: wherein R and R2 independently a C1-C4 alkyl group or an aralkyl group.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The invention relates to novel crystalline form VI of Donepezil hydrochloride and process for preparing the crystalline form VI, which is a simple, non-hazardous and commercially viable process.

Abstract: Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK3 receptor antagonists.

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.