Abstract: The invention provides a novel class of substituted isoindolinone derivatives. Pharmaceutical compositions, and methods of making and using the compounds, or pharmaceutically acceptable salts, hydrates, prodrugs, or mixtures thereof are also described.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: 1

Abstract: A novel calcium receptor active compound having the formula is provided:

Abstract: Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia.

Abstract: A compound of the formula (I) wherein X1 ? is bond or —O(CH2)m— (in which m is an integral number of 1, 2 or 3); X2 is bond, —(CH2)n—, etc. (in which n is an integral number of 1, 2 or 3); R1 is hydrogen or amino protective group; R2 is hydroxy(lower)alkyl or (lower)alkoxy(lower)alkyl; A is phenyl, pyridyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, etc.; and B is phenyl or pyridyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, nitro, etc.; and a pharmaceutically acceptable salt thereof which is useful as a medicament.

Abstract: The invention relates to substituted indole Mannich bases of formula (I), a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments, especially medicaments that are used to treat pain. In formula (I), R1,R2, R4-R7 have the meanings cited in claim 1, R3=formula (a) and R13=(substituted) phenyl.

Abstract: The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Compounds of formula (I): 1

Abstract: Compounds of the formula 1

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) 1

Abstract: The present invention relates to indole derivatives, dihydroindole derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: Compounds of the formula 1

Abstract: The present invention relates to novel compounds which are suitable as pharmaceuticals, to processes for their preparation and to their use as pharmaceuticals, in particular as antiviral agents.

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Abstract: The present invention provides methodology for carbon-nitrogen bond formation via vinyl or aryl amination. In the process of the invention, an sp2 hybridized radical is reacted with an azomethine moiety to form pyrrolidine and indole compounds. The methodology provides a facile process for the synthesis of compounds having the pyrrolidine or indole subunit and is especially advantageous for compounds having acid or base labile functional groups andor is comprised of chiral centers susceptible to acidbase epimerization.

Abstract: Tryptophan derivatives of formula (1) are described: 1

Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ar represents substituted or unsubstituted aryl, wherein the optional substituents are selected from alkyl, hydroxy or alkoxy or, if attached to adjacent carbon atoms any two substituents together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; A represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by 1 or 2 C1-6 alkyl groups; R1 represents hydrogen, alkyl, alkenyl or cycloalkyl; one or two of of the group of R2, R3 and R4 represents nitro the remaining members of the group of R2, R3 and R4 represent hydrogen; X represents a —CO—NH— moiety; and Z represents C2-4 n-alkylene group wherein each carbon is optionally substituted 1 or 2 C1-6 alkyl groups; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compo

Abstract: The present invention relates to indole derivatives, dihydroindole derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula wherein Z1 and Z2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole; A is selected from —C(X)-amine, —C(O)—SR3, —NH—C(X)R4, and —C(═NR3)—XR7; B is —Wm—Q(R2)3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R4; Q is C, Si, Ge, or Sn; W is —C(R3)pH(2−p)—; or when Q is C, W is selected from —C(R3)pH(2−p)—, —N(R3)mH(1−m)—, —S(O)p—, and —O—; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R is independently selected from a) halo, formyl, cyano, amino, nitro, thiocyanato, isothiocyanato, trimethylsilyl, and hydroxy; b) C1-C4 alkyl, alkenyl, alkynyl,

Abstract: Compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.

Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.

Abstract: Disclosed are compounds of the formula: 1

Abstract: The present invention is to provide a compound of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic heterocyclic ring, the ring B an optionally substituted 5- to 6-membered aromatic homocyclic ring or an optionally substituted 5- to 6-membered aromatic heterocyclic ring, R1 is a hydrogen atom, a hydroxy group or a lower alkyl group, and n is 0 or 1, or a salt thereof, which is effective for the prevention or treatment of ischemic cardiac disease, etc., and which is useful as an agent for preventing or treating ischemic cardiac disease, etc. such as myocardial infarction, arrhythmia, etc.

Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.

Abstract: Novel compounds having strong TXA2 receptor antagonist activities and PGI2 receptor agonist activities, which are effective for therapy and prevention of diseases related to TXA2, are disclosed. The compound of the present invention is represented by the following formula (I). (wherein the meanings of the symbols in the formula are as described in the specification).

Abstract: The present invention relates to indole derivatives represented by the general formula: (wherein R represents an ethyl group or a 2,2,2-trifluoroethyl group; Y represents a hydroxy group or a pivaloyloxy group; and the carbon atom marked with (R) represents a carbon atom in (R) configuration) and pharmaceutically acceptable salts thereof, which have potent and prolonged reducing effects on intraocular pressure and are useful as agents for lowering intraocular pressure.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: The invention provides a process for the production of a compound of formula I, which comprises reacting a compound of formula II with a compound of formula III, in the presence of a strong base and a palladium(0) catalyst, at an elevated temperature, in a solvent which does not adversely affect the reaction. Compounds of formula I may be further processed to compounds of formula V, which are useful in the treatment of inter alia migraine.

Abstract: Novel indoloylguanidine derivatives shown by formula (1), wherein R1 represents one or more, the same or different substituent(s) which is selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen atom, nitro group, an acyl group, carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group shown by formula: —OR3, —NR6R7, —SO2NR6R7 or —S(O)nR40; and R2 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, hydroxy group, an alkoxy group or a group shown by formula: —CH2R20; and which inhibit the Na+/H+ exchanger activity and are useful for the treatment and prevention of a disease caused by increased Na+/H+ exchanger activity, such as hypertension, arrhythmia, angina pectoris, cardiac hypertrophy, diabetes, disorders associated with ischemia or ischemic reperfusion, cerebro-ischemic disorders; or diseases caus

Abstract: The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one, pharmaceutical compositions containing said ziprasidone mesylate dihydrates, and methods of adminsitering the ziprasidone mesylate dihydrates to treat psychotic diseases.

Abstract: The indolyl-substituted phenylacetic acid derivatives are prepared by reacting the corresponding phenylacetic acids with the required amines. The indolyl-substituted phenylacetic acid derivatives are suitable as active compounds in medicaments, in particular in antiarteriosclerotic medicaments.

Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

Abstract: Ethylamine derivatives of the formula (I): (wherein R1 is hydrogen, hydroxyl, lower alkoxy or halogen; R2 is alkyl having 2 to 5 carbon atoms; R3 is hydrogen, alkyl having 2 to 5 carbon atoms, alkylcarbonyl having 2 to 5 carbon atoms, aryl having 6 to 10 carbon atoms or arylalkyl having 7 to 11 carbon atoms; the ring is a bicyclic compound which consists of at least one benzene ring and may comprise a saturated or unsaturated five- or six-membered ring which may or may not have heteroatoms, providing that when the ring is indole or 1,3-benzodioxole, R2 and R3 do not constitute, at the same time, two carbon atoms members, and when R3 is hydrogen, the ring is a bicyclic compound which is not indole, benzothiophene or benzodioxole and R2 is alkyl having 3 to 5 carbon atoms and pharmaceutically acceptable acid addition salts thereof. These compounds are promising as psychotropic drugs, antidepressants, drugs for Parkinson's disease and/or drugs for Alzeimer's disease.

Abstract: The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.

Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).

Abstract: Novel indoloylguanidine derivatives shown by formula (1), wherein R1 represents one or more, the same or different substituent(s) which is selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen atom, nitro group, an acyl group, carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group shown by formula: —OR3, —NR6R7, —SO2NR6R7 or —S(O)nR40; and R2 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, hydroxy group, an alkoxy group or a group shown by formula: —CH2R20; and which inhibit the Na+/H+ exchanger activity and are useful for the treatment and prevention of a disease caused by increased Na+/H+ exchanger activity, such as hypertension, arrhythmia, angina pectoris, cardiac hypertrophy, diabetes, disorders associated with ischemia or ischemic reperfusion, cerebro-ischemic disorders; or diseases caus

Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.

Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.

Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.

Abstract: Novel disubstituted bicyclic heterocycles, of which the following are exemplary:(a) 1-methyl-2-[(4-amidinophenyl)-oxymethyl]-5-[N-(hydroxycarbonylmethyl)-quin oline-8-sulphonylamino]-benzimidazole,(b) 1-methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(N-(hydroxycarbonylmethyl)-ami nocarbonylmethyl)-quinoline-8-sulphonylamino]-benzimidazole,(c) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-benzimidazole and(d) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-indole.These are useful for the treatment of thrombotic disease.

Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).

Abstract: This invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at positions C4 and C5, being optionally substituted on the N atom of the heterocyclic system, and where the unsaturated ring of the heterocyclic system is a 5,6, 7 or 8-membered ring. Also to the use of these compounds as anticonvulsants in certain medical conditions, and to processes for making them.

Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.

Abstract: A process for preparation of 3-amino-2-hydroxy-1-propyl ether of the formula ##STR1## wherein R.sup.1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic ring, R.sup.2 and R.sup.3 are the same or different hydrogen atom, a substituted or unsubstituted alkyl, or may form a ring together with an adjacent nitrogen atom, which ring may be interrupted with nitrogen atom, oxygen atom or sulfur atom,which is characterized in reacting an epoxy compound of the formula ##STR2## wherein X is halogen, in the presence of a fluoride salt, with an alcohol and then reacting an amine.According to the above method, an intermediates for synthesis of medicines is obtained in good yield and highly optical purity.

Abstract: The present invention relates to a family of cyanine dyes possessing lipophilic alkyl chains and either one or more reactive functional groups, bromo or chloro, or phenyl, sulfophenyl or polysulfophenyl substituents or combinations thereof. The dyes of the invention are useful for staining membranes in cells or isolated from cells, and are well-retained therein. Additionally, the reactive dyes of the invention are useful for preparing dye-conjugates, thereby conferring the membrane staining ability of the subject dye onto the resulting dye-conjugate.

Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R.sub.2 is a 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 4-hydroxyphenyl, 4-(arylalkyloxy)phenyl, 3,4-dihalophenyl, 4-hydroxy-3,5-dihalophenyl, 4-azidophenyl or 4-halophenyl group; wherein R.sub.3 is H, a linear or branched chain alkyl or alkenyl group, or a phenyl, 2-azidophenyl, 3-azidophenyl, 4-azidophenyl group, or an a alkenylacyl, 3-amino-3-butylpropyl, N-[N-(N-{4-azidobenzoyl}aminopropyl) aminopropyl], cis- or trans-cinnamyl, 2-amino-2-[(4'-azidophenyl)acetyl, (trifluoromethyl)aminoacetyl or D- or L-arginyl group bonded through the .alpha.-carbonyl moiety thereof; R.sub.4 is H, or a linear or branched chain alkyl group; wherein R.sub.5, R.sub.6 and R.sub.