Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.

Abstract: Methods for the manufacture of Mycophenolate are disclosed. Mycophenblate mofetil is biochemically synthesized using Mycophenolic Acid and 2-morpholino ethanol with the help of an enzyme. Mycophenolate mofetil is also chemically synthesized non-catalytically by refluxing mycophenolic acid with 2-morpholino ethanol in the absence of a third solvent or a catalyst.

Abstract: The present invention provides novel, reduced benzothiophenes of formula I wherein R is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl) chloro or bromo; n is 2 or 3; and R2 and R3 each are independently C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidino, dimethyl-1-pyrrolidino, 4-morpholino or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Further provided are methods for alleviating the symptoms of post-menopausal syndrome, and inhibiting endometriosis, uterine fibrosis, and aortal smooth muscle cell proliferation.

Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are &agr;-substituted with ether, thioether amino, 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: Compounds of the formula 1

Abstract: A compound of general formula (I) and physiologically acceptable salts wherein R represents phthalidyl, (2-oxo-5-methyl-1,3-diox-olen-4-yl)methyl or the group CHR4 OCO(O)pR5 wherein R4 is hydrogen or C1-4 alcyl, p is zero or I, R5 is C1-6 alkly, C5-8 cycloalyl (optionally substituted by C1-3 alkyl or carboxyl), C1-4 alkyl substituted by C1-3 alkoxy or carboxy), C1-4 alkyl substituted by one or more groups selected from amino, (C1-4 alkylamino di(C1-4 alkyl)amino or carboxyl, phenyl (optionally substituted by carboxyl or aminoalkyl, C1-4 alkylaminoalkyl or di(C1-4 alkyl)aminoalcyl, or R5 is a 5-8 membered heterocyclic group containing 1 or 2 heteroatoms selected from oxygen or nitrogen, processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.

Abstract: The invention relates to benzofuranylsulfonates of the general formula (I), their preparation and their use for the treatment of inflammation.

Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.

Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.

Abstract: This invention concerns compounds of formula 1

Abstract: N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.

Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1

Abstract: A method for treating diseases in which tryptase inhibitors may be of thereapeutic value, which comprises the administration of a thereapeutic amount of a compound of the formula   The invention also comprises novel compounds of the formula (I). Exemplary is 2-[2-(4-amidinophenyl)ethyl]-1-methyl-benzimidazol-5-yl-carboxylic acid-N-(pyridin-3-yl-methyl)-N-methyl-amide-hydrochloride.

Abstract: Disclosed are compounds of the formula 1

Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-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: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.

Abstract: The present invention provides novel compound of the formula: wherein Ra is —OH or —O—(C1-C4 alkyl); R1a is —OH or —O—(C1-C4 alkyl); n is 2 or 3; R2 and R3 are each independently: —C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidinyl, 1-pyrrolidinyl substituted with one or two methyl groups, 4-morpholino or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides method of treating endometriosis using novel benzothiophene compounds of formula I wherein R is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R1 is —H, —OH, —O(C1-C4 alkyl),, —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl) chloro or bromo; R2 is —H or —OH; n is 2 or 3; and R3 and R4 each are independently C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)3, CO(CH2)4, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; R6 is and pharmaceutically acceptable salts thereof; useful in treating estrogen deficient pathology.

Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether amino, 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 application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Abstract: Compounds of the formula (I) in which A represents N or a cyanomethylene radical, B represents S, O or NH and R1, R2, R3 and x have the meaning given in the description, are highly suitable for dyeing and printing high-molecular-weight materials, in particular automotive cover fabrics.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

Abstract: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O--or --S--;or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of estrogen.

Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I whereinR.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of progestin.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 AND R.sup.2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic dermatitis, shock, and other inflammatory diseases and for blocking the leucotriene D4 receptor, pharmaceutical compositions containing such compounds and methods of blocking leucotriene D4 receptors using such compositions.

Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.

Abstract: The present invention provides intermediate compounds and processes for the preparation of compounds of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides novel 5-HT.sub.1F agonists of formula ##STR1## where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.

Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.

Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.

Abstract: Derivatives of 2,3-dihydro-5-benzofuranol, intermediates thereof, and processes useful for their preparation. These compounds are free radical scavengers and are useful in the treatment of conditions capable of being treated by free radical scavengers, such as stroke, nervous system trauma and reperfusion damage.

Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compounds of Formula I wherein Q, Z, R.sup.2 are as defined within.

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 relates to a novel process for preparing 2,3-dihydro-benzofuranol derivatives and to the novel intermediates produced thereby.

Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.

Abstract: A compound having the structure: ##STR1## wherein (a) W is --C(X')--NRR' or --NR--C(X')R';(b) X and X' are independently O or S;(c) each Y is independently hydrogen or straight, branched or cyclic alkanyl having from 1 to about 3 carbon atoms, or the two Y's are bonded to form an alkanyl ring having from 3 to about 7 carbon atoms;(d) Z is unsubstituted branched or cyclic alkyl, or unsubstituted or alkanyl-substituted phenyl or benzyl, Z having from 3 to about 10 atoms other than hydrogen;(e) R and R' are each independently selected from hydrogen, hydroxy straight, branched or substituted alkyl having from 1 to about 6 carbon atoms, and cyclic alkyl having from 3 to about 7 carbon atoms; unsubstituted or substituted aryl, heteroaryl or heterocyclic groups; or R and R' are bonded together to form a ring having from from 3 to about 8 atoms wherein about 1 to about 4 atoms may be heteroatoms;pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

Abstract: Compounds and methods for use in immunosuppressive and anti-inflammatory treatment are described. The compounds are triptolide analogs with improved water solubility and low toxicity.

Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: The middle value selection circuit includes three high value selection circuits and one low value selection circuit. Each high value selection circuit consists of a pair of first NPN transistors and a first constant current circuit. The emitter of each first NPN transistor of the high value selection circuit is connected to the first constant current circuit and the base of the second NPN transistor of the low value selection circuit. The base of this second NPN transistor is connected to the second constant current circuit and to an output terminal. The collector of the second NPN transistor is connected to its base. The first constant current circuit produces a current whichis twice the output current of the second constant current circuit. Two analog signals having mutually different combination among three input analog signals are applied to the NPN transistors of one high value selection circuit.