Abstract: The present invention relates to urethanes derived from azacycloalkanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y, E and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

Abstract: The present invention relates to azacycloalkylalkanoyl peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease, and disseminated intravascular coagulation, to methods for the prevention or treatment of thrombosis in a mammal in need of such therapy comprising the administration of a therapeutically effective amount of such compounds, and to pharmaceutical compositions comprising such compounds.

Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.

Abstract: Novel compounds are provided having the structural formula R[—N(NO2)—L—R1]n wherein R, L, R1 and n are defined herein. The compounds are useful in a variety of contexts, but are primarily to be used as high energy oxidizing agents in explosive compositions, propellant formulations, gas-generating compositions and the like. The compounds are also useful as pharmaceutical agents. Compositions containing the compounds are also provided, including energetic compositions, as are methods for using the novel compounds and compositions.

Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.

Abstract: This invention relates to muscarinic receptor antagonist compounds selected from the group of compounds represented by Formula I: wherein the substituents are as defined in the specification; and their pharmaceutically acceptable salts, individual isomers or a racemic or non-racemic mixture; pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.

Abstract: Squaric acid derivatives of formula (1) are described: 1

Abstract: Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof 1

Abstract: Novel compounds of the formula 1

Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Abstract: The invention relates to new compounds of general formula and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

Abstract: Compounds having Formula I ##STR1## are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: A durability enhancing agent comprising the reaction product of an acrylic oligomer or acrylic polymer and an ultraviolet light absorbing compound, a hindered amine light stabilizer or mixture thereof, said durability enhancing agent further comprising more than one carbamate functional group, or group convertible to a carbamate group, and optionally, including other reactive functionality capable of undergoing a crosslinking reaction. Also included is a curable coating composition comprising the durability enhancing agent, a method for obtaining a coated substrate and the coated article obtained thereby.

Abstract: Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartatc (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, amioglycoside antibiotics-induced hearing loss, migraine headaches, chronic pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

Abstract: Disclosed are hydroxamic and carboxylic acid derivatives which are useful inhibitors of matrix metalloproteinase and/or TNF.alpha.-mediated diseases, including degenerative diseases and certain cancers.

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 Substance P and NKA, 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 provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.

Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

Abstract: The present invention provides a silacyclopentadiene derivative represented by the following Formula (1): ##STR1## wherein X.sub.1 and Y.sub.1 represent independently a halogen atom, an amino group, a hydroxyl group, or an amino group or a hydroxyl group each having a substituent; R.sub.1 to R.sub.4 represent independently a hydrogen atom, a halogen atom, an alkyl group, an amino group, a silyl group, an aryl group, a cyano group, or the respective groups describe above each having a substituent; out of the groups represented by R.sub.1 to R.sub.4, those adjacent may be combined with each other to form rings; when R.sub.1 and R.sub.4 are phenyl groups or when combined are R.sub.1 with R.sub.2 and R.sub.3 with R.sub.4 respectively to form benzene rings, X.sub.1 and Y.sub.1 are not a chlorine atom or a hydroxyl group; and when R.sub.1 and R.sub.4 are methyl groups, X.sub.1 and Y.sub.1 are not bromine atoms.

Abstract: Pharmacologically active novel esters and amides of di-substituted 1,4 piperidine as 5-HT.sub.4 antagonists of formula (I) ##STR1## wherein A, X, Y and R have the meanings specified in the description, and a process for their preparation, are disclosed.

Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.

Abstract: It has now been found that certain novel oximino and hydrazono derivatives of N-benzyl-4-benzhydryl- and 4-benhydrolpiperidines, and their corresponding N-oxides and agriculturally acceptable salts are useful as insecticides. These compounds are represented by Formula I: where R is hydrogen, halogen, alkyl, alkoxy, dialkylamino; R.sup.1 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkylcarbonyl and alkylaminocarbonyl; X is oxygen, or NR.sup.2, Q is fluoro and hydroxy; Z is halogen, haloalkyl, haloalkoxy, pentahalothio, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, and --OCF.sub.2 O-- attached to two adjacent carbon atoms of the phenyl ring; n is 0 or 1; and, when X is NR.sup.2, R.sup.2 is hydrogen, alkyl, alkylcarbonyl, alkoxycarbonyl, or R.sup.1 and R.sup.2 taken together may be --C.sub.m H.sub.2.spsb.m, or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --, where m is 3-9. Preferred compounds include those where R is hydrogen; R.sup.

Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.

Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.

Abstract: A compound of formula XXII ##STR1## wherein Ar', Q' and Q" are as defined in the specification are useful intermediates for making neurokinin receptor active compounds.

Abstract: Benzoic acid compounds of the formula ##STR1## wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.

Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.

Abstract: Substituted N-phenyl- and N-heteroarylalkylcarbamates of formula (I), in which Q is a group (1), (2) or (3); R is halogen, trifluoromethyl, cyano, nitro or C.sub.1 -C.sub.3 haloalkoxy; Z is hydrogen or halogen; or Z and R together in the 2- and 3-position of the phenyl ring form a group --OCF.sub.2 O--; R.sub.1 is C.sub.1 -C.sub.5 alkyl; R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, methyl or ethyl; X is oxygen, sulfur, --SO-- or --SO.sub.2 --, Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or cyano; n is 0, 1 or 2; n.sub.1 is 0 or 1; and m is 0 or 1, with the proviso that m is 1 if Q is group (1) or (2); and the diastereomers and enantiomers thereof, exhibit pre- and post-emergence herbicidal properties. The preparation of these compounds and their use as herbicidally active ingredients are described.

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.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 --R.sup.4, R.sup.7 --R.sup.8, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: Compounds represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, wherein: A.sup.1 is --CH.sub.2 R.sup.6, --OR.sup.6, --N(R.sup.6)(R.sup.7), --S(O).sub.e R.sup.13, --(C(R.sup.6)(R.sup.7)).sub.1-6 --OR.sup.6, --(C(R.sup.6)(R.sup.7).sub.1-6 --N(R.sup.6)(R.sup.7) or --(C(R.sup.6) (R.sup.7)).sub.1-6 --S(O).sub.e R.sup.13 and A.sup.2 is H, or A.sup.1 and A.sup.2 together are .dbd.O, .dbd.C(R.sup.6)(R.sup.7), .dbd.NOR.sup.6 or .dbd.S;Q is phenyl, naphthyl, --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6 or heteroaryl;T is H, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl;b is 0, 1 or 2;b.sub.1 is 1 or 2;X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O).sub.e --, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)--, --OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.6)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --, --N(R.sup.6)C(O)O-- or --OC(O)--;R.sup.6, R.sup.7, R.sup.8a, and R.sup.

Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which R.sub.1, R.sub.2 and R.sub.3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy;ALK.sup.1 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups;Y represents a piperidine ring which is attached through nitrogen to ALK.sup.1 ;R.sub.4 represents hydrogen or a C.sub.1-4 alkyl group; the broken line in --- represents a bond, or is absent and the free valency on Y is taken up by hydrogen and the free valency on CR.sub.4 is taken up by hydrogen or a C.sub.1-4 alkyl group;ALK.sup.2 is absent or represents a C.sub.1-4 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups; andR.sub.5 and R.sub.6 independently represent hydrogen, alkyl, phenyl, alkyl (optionally substituted) or R.sub.5 and R.sub.

Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.