Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure 1

Abstract: Compounds of formula (I) 1

Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.

Abstract: Compounds represented by structural formula I 1

Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.

Abstract: The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula I.

Abstract: Taxane derivatives having an alkyl substituted C13 side chain.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.

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: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.

Abstract: A nitrogen-containing heterocyclic compound represented by the following formula (I) or (II): wherein X1 and X2 are the same or different, each representing a hydrogen atom, an alkyl group, or an electron attractive group and at least one of which being an electron attractive group; R1 and R2 are the same or different, each representing a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an alkoxy group, and the ring Z represents a hydrocarbon ring which may have a substituent or a heterocycle which may have a substituent. The compound of the present invention is capable of emitting light or changing its color upon irradiation of light or under the action of an electric field.

Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.

Abstract: The instant invention provides compound of formula I wherein: R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—O(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—O(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl), —F, —Cl, or —Br; n is an integer from 5 to 8; R3 and R4 each are independently C1-C4 alkyl, or combine to form, with the nitrogen to which they are attached, piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, or hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof, intermediates, pharmaceutical formulations, processes, and methods of use.

Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are a-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: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.

Abstract: The present invention relates to a class of compounds represented by the Formula I 1

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: This invention provides novel benzothiophene compounds of formula I: which are useful for the inhibition of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further. relates to pharmaceutical formulations of compounds of formula I.

Abstract: Compounds of formula 1

Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, 2 and 3, to a plurality of processes for their preparation and to their use as pesticides.

Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.

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: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

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: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.

Abstract: The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloïds used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.

Abstract: A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atheroclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.

Abstract: Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2  (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.

Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.

Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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: The present invention relates to compounds of the formula

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.

Abstract: Compounds of formula I are useful antidepressant agents demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or indolyl.

Abstract: 1,2-Bis-adducts of stable hindered nitroxide compounds with substituted ethylenes are prepared by reacting two equivalents of nitroxyl compound with an ethylenically unsaturated compound such as styrene or an acrylate ester. These adducts are very effective inhibitors to prevent the premature polymerization of ethylenically unsaturated monomers when such monomers are distilled, processed or stored.

Abstract: The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

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: A compound of the formula: wherein R1 and R2 each represents hydrogen, lower alkyl which may be substituted or acyl; R3, R4 and R5 each represents lower alkyl which may be substituted or lower alkoxy which may be substituted or R4 and R5 taken together represent a 5- or 6-membered carbocyclic group; R6 represents lower alkyl; Ar represents an aromatic group which may be substituted; ring A represents a 5- to 8-membered nitrogen-containing heterocyclic ring which may be substituted; X represents lower alkylene which may be substituted; Y represents carbon or nitrogen; Za represents CH2, COCH2, OCH2, SCH2, NHCH2, etc.; Zb represents a bond or a divalent aliphatic hydrocarbon group which may be substituted and may contain O, N or S; and m represents an integer of 1 to 3, or a salt thereof is useful for a pharmaceutical composition for modulating sodium channel.

Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.

Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.

Abstract: The present invention relates to novel substituted phenols and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compositions containing the compounds are also includes.

Abstract: Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.