Abstract: Nipecotic acid-derived compounds of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.

Abstract: A process for preparing a compound of the formula (I) ##STR1## in which, R.sup.1 and R.sup.2 are the same or different and each is hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring which is unsubstituted or substituted and is a 5-membered or 6-membered N-heterocycle which optionally has a further heteroatom which is oxygen, nitrogen or sulfur; E is methylene; ring A is a unsubstituted or unsubstituted aryl ring, or a substituted or an unsubstituted heteroaryl ring; R.sup.3 is a C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen, or R.sup.3 and R.sup.4 together are a group of the formula --(CR.sup.a R.sup.b).sub.m --C(.dbd.Y)-- (IV), wherein each of R.sup.a and R.sup.b is hydrogen or C.sub.1 -C.sub.

Abstract: The following invention relates to compounds which are effective for inhbiting platelet aggregation, pharmaceutical compositions for effecting such activity and a method for inhibiting platelet aggregation.

Abstract: This invention is concerned with novel 1,3-dihydro-1-?1-(1-heteroarylpiperidin-4-yl)piperidin-4-yl!-2H-benzimidaz olones, derivatives thereof, their preparation, method of use and pharmaceutical compositions. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6 ', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.

Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, --A.dbd.B--C.dbd.D--, Ar and X have the meaning indicated in claim 1, and their salts show endothelin receptor-antagonistic properties.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein Z, X.sup.1, X.sup.2, x and R.sup.5 are as defined herein.

Abstract: The invention relates to compounds of the formula I ##STR1## in which n is a number in the range from 1 to 100; X is --R.sup.7 --, --CO--, --CO--CO--, --CO--R.sup.2 --CO--, --CO--NH--R.sup.5 --NH--CO--, --CO--O--R.sup.6 --O--CO-- or ##STR2## where p is a number in the range from 0 to 6, X' is O or a direct bond, E is C.sub.1 -C.sub.12 alkyl, phenyl, C.sub.7 -C.sub.12 phenylalkyl or C.sub.5 -C.sub.12 cycloalkyl, and E' is hydrogen or is as defined for E;Z, when X is R.sup.7, is O or NR.sup.1 ; Z, when X is ##STR3## is O; and Z, in all other cases, is O, NH or NR.sup.1 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.7 -C.sub.9 phenylalkyl, C.sub.5 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.8 alkanoyl, benzoyl or C.sub.1 -C.sub.4 alkyl-substituted benzoyl;R.sup.2 and R.sup.7 are C.sub.1 -C.sub.18 alkylene; C.sub.2 -C.sub.18 alkylene which is interrupted by O or S; phenylene; a mixed aromatic/aliphatic radical containing 7 to 12 carbon atoms; naphthylene; or an --R.sup.4 --D--R.sup.4 -- radical;R.sup.

Abstract: Substituted phthalimidocinnamic acid derivatives I ##STR1## wherein the variables are as defined in the description are useful as herbicides and for the desication and/or defoliation of plants.

Abstract: This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R, R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.

Abstract: Compounds, 1,3-dihydro-1-{1-?piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.

Abstract: Disclosed is a method for the inhibition of binding of a ligand to an RNA, the inhibition being mediated by a small organic molecule that binds to the RNA, thereby inhibiting ligand binding. A preferred class of small organic molecules are compounds exemplified by 2,5-Bis[3-(2-N,N-dimethylaminopropylamidino)phenyl]furan.

Abstract: This invention relates to substituted thiazole derivatives of the following general formula, the substituent groups of which are as defined in the specification herein: ##STR1## These compounds are useful as inhibitors of platelet aggregation and inhibitors of adhesion molecules and may be provided in pharmaceutical compositions and in methods of treating reperfusion thrombosis injury in patients. Also included are novel intermediates for preparing the compounds of the invention.

Abstract: Esters or phenol ethers of the formula I or II ##STR1## in which m and n are each an integer from the range from 1 to 6; A.sup.1 is an m-valent hydrocarbon radical having 1 to 30 carbon atoms; or an m-valent hydrocarbon radical having 2 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and the free valencies of which are located on carbon atoms and in which A.sup.1, in the case where m=2, additionally is a direct bond;A.sup.2 is an n-valent aromatic or araliphatic hydrocarbon radical having 6 to 30 carbon atoms; or an n-valent aromatic or araliphatic hydrocarbon radical having 5 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and n free valencies of which are located on those carbon atoms which are a constituent of aromatic rings;R.sup.1 is hydrogen; a hydrocarbon or hydrocarbonoxy radical having 1 to 36 carbon atoms, which is unsubstituted or substituted by --CO--N(R.sup.3).sub.2 or interrupted by --CO--N(R.sup.3)-- or --N(R.sup.

Abstract: The subject invention describes Novel dimer 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having the general Formula I: ##STR1## wherein n is 1-5;R.sup.1 to R.sup.4 are independently selected from hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulfonyl, C.sub.1-6 alkyl- or di-(C.sub.1-6 alkyl)amino, cyano, trifluoromethyl, nitro, trifluoromethylthio or trifluoromethylsulfonyloxy; R.sup.5 and R.sup.6 are independently hydrogen, or C.sub.1-6 alkyl;X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, or X is NR.sup.7, R.sup.7 being H, C.sub.1-6 alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are independently selected from the group consisting of hydroxy and the substituents defined under R.sup.7, any phenyl group being optionally substituted with one or more substituents selected from halogen, C.

Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.

Abstract: The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity.Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.

Abstract: The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl, phenyl, naphthyl, pyridyl or thienyl group, each phenyl, naphthyl, pyridyl or thienyl optionally being substituted,R.sub.2 represents a hydrogen atom or a substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, cycloalkyl, piperidino or substituted or unsubstituted amino group,X represents CO or SO.sub.2,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents alkyl, substituted or unsubstituted phenyl or trihalomethyl, or else R.sub.3 and R.sub.4 form, together with the carbon atoms which carry them, cyclo(C.sub.3 -C.sub.7)alkenyl,A represents phenyl, naphthyl or pyridyl ring, each phenyl, naphthyl or pyridyl ring optionally being substituted,their isomers, the corresponding quaternary ammonium salts of the piperidine and their addition salts with a pharmaceutically acceptable acid, an medicinal products containing the same are useful as antagonists of NK.sub.1 receptors.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: DC-89 derivatives represented by the formula ##STR1## wherein X represents CL or Br; R represents substituted or unsubstituted alkyl, substituted or unsubstituted aralkyl, COR.sup.1 or S.sub.2 OR.sup.7 ; and Y represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention exhibit excellent anti-tumor activity and are useful as anti-tumor agents.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Esters or phenol ethers of the formula I or II ##STR1## in which m and n are each an integer from the range from 1 to 6; A.sup.1 is an m-valent hydrocarbon radical having 1 to 30 carbon atoms; or an m-valent hydrocarbon radical having 2 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and the free valencies of which are located on carbon atoms; and in which A.sup.1, in the case where m=2, additionally is a direct bond;A.sup.2 is an n-valent aromatic or araliphatic hydrocarbon radical having 6 to 30 carbon atoms; or an n-valent aromatic or araliphatic hydrocarbon radical having 5 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and n free valencies of which are located on those carbon atoms which are a constituent of aromatic rings;R.sup.1 is hydrogen; a hydrocarbon or hydrocarbonoxy radical having 1 to 36 carbon atoms, which is unsubstituted or substituted by --CO--N(R.sup.3).sub.2 or interrupted by --CON(R.sup.3)-- or --N(R.sup.

Abstract: Trifluoromethylpyrroloindolecarboxylic acid ester derivatives, and optical isomers and pharmaceutically acceptable salts thereof are provided which are represented by the general formula (1): ##STR1## or the general formula (2): ##STR2## The compounds are antineoplastic agents which are selective to cancer cells, effective also to solid cancer, and less toxic.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Compounds of the formula I ##STR1## wherein R.sup.1 and Y have the meanings indicated herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, inflammations, arteriosclerosis and osteolytic disorders.

Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

Abstract: Substituted phenylcarbamates and ureas of formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom, or a C.sub.1-6 alkyl, C.sub.1-6 alkoxy or hydroxy group;R.sup.2 represents an oxadiazole or thiadiazole ring substituted by a group selected from C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --CH.sub.2 C.sub.2-5 alkenyl, --CH.sub.2 C.sub.2-5 alkynyl, phenyl or benzyl;X represents NH or an oxygen atom;m represents zero, 1 or 2;R.sup.3 represents C.sub.1-6 alkyl, benzyl, --(CH.sub.2).sub.n R.sup.4 or ##STR2## R.sup.4 represents a group selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, C(O)C.sub.6 H.sub.5, --CONR.sup.6 R.sup.7, --NR.sup.6 COR.sup.7, --SO.sub.2 NR.sup.6 R.sup.7 or --NR.sup.6 SO.sub.2 R.sup.7 (wherein each of R.sup.6 and R.sup.7 independently represent a hydrogen atom, a C.sub.1-6 alkyl or phenyl group);n represents 2 or 3;R.sup.5 represents COR.sup.8 or SO.sub.2 R.sup.8 (wherein R.sup.8 represents a hydrogen atom, a C.sub.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: Pyrrolo[3,4-c]pyrroles of formula ##STR1## wherein D and E are each independently of the other a group of formula ##STR2## The symbols Q, R.sub.8, R.sub.9, R.sub.10, R.sub.11, X, Y, Z, m and n are as defined in claim 1.These pyrrolo[3,4-c]pyrroles are distinguished by outstanding solid state fluorescence in the UV range as well as by the ease with which they can be converted to pyrrolopyrrole pigments even in the substrate in which they are incorporated.

Abstract: The present invention concerns .beta.,.beta.-dimethyl-4-piperidineethanamine compounds of the formula: ##STR1## (wherein groups R.sub.1 to R.sub.3 are defined as indicated in the description), and addition salts thereof.It also concerns a process for their preparation and their therapeutic use as inhibitors for the cholesterol biosynthesis, in particular as epoxysqualene cyclase inhibitors, for obtaining an as hypocholesterolemic, hypolipemic, antiatheromatic and/or antifungal drug.

Abstract: The present invention relates to an novel dipiperidine derivative represented by formula (1), or a pharmaceutically acceptable salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; Y represents a single bond or an oxygen atom; n represents 1, 2 or 3; W represents a methylene group or an oxygen atom; R.sup.2 represents a hydrogen atom or a carboxyl modifying group which can be eliminated in vivo; X.sup.1 and X.sup.3 are the same or different and each represents a hydrogen atom or a lower alkyl group.This compound is useful as platelet aggregation inhibitors, cancer metastasis inhibitors, wound remedies or bone resorption inhibitors.

Abstract: The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.

Abstract: This invention provides a novel series of substituted pyrrolidines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, m and M have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Abstract: Compounds, 1,3-dihydro-1-{1-[piperidin-4-yl]piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.

Abstract: This invention provides a series of novel substituted propanamides which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

Abstract: Pyrazole-glycolic acid amides of the following formula (1) (in which R.sup.1 to R.sup.5 each represent a hydrogen atom or a substituent having a broad definition), and herbicides containing them. The compounds have a high herbicidal effect against paddy weeds, especially Echinochloa crus-galli, while highly safe for paddy rice plants.

Abstract: This invention relates to novel imidazole and triazole substituted oxathiolane compounds and compositions containing said compounds having fungicidal and plant growth regulant activity and methods for preparing same.