Abstract: The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract: The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.

Abstract: The invention relates to compounds of formula wherein hetaryl I, hetaryl II, and R1 are as described herein. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease.

Abstract: A process for preparing a thiazole compound of formula (3): wherein X1 represents a hydrogen atom or a halogen atom comprising reacting a compound of formula (1): wherein X1 is as defined above, and X2 represents a halogen atom, with ammonia and formaldehyde to obtain a hexahydrotriazine compound of formula (2): wherein X1 is as defined above, and hydrolyzing the compound of formula (2).

Abstract: The invention provides 5-substituted thiazol-2-yl amino compounds of Formula (I): pharmaceutical compositions comprising such compounds and the use of such compounds for the treatment or prevention of diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Ab 1, Aurora-A, Ber-Ab1, Bmx, CDKI/cyclinB, CHK2, Fes, FGFR3, Flt3, GSK3?, JNK1?1, Lck, MKK4 and TrkB kinases.

Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

Abstract: Compounds of the following structure are described: wherein R1-R6, R10, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

Abstract: The object of the present invention is a ready-to-use agent for coloring keratin fibers containing (i) at least one heterocyclic hydrazone derivative of formula (I), (ii) at least one aromatic enamine of formula (IIa) or an acid addition compound thereof (IIb) and (iii) at least one oxidant, a multicomponent kit and a method for coloring keratin fibers by use of said agent

Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.

Abstract: The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recit

Abstract: A method of obtaining a high purity 2-cyanoimino-1,3-thiazolidine, at a high yield, by cyclization reaction of dimethyl N-cyanoiminodithiocarbonate ester with 2-aminoethane thiol or the salt thereof in the presence of an alkali metal hydroxide is disclosed.

Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus.

Abstract: A method for producing high purity 2-cyanoimino-1,3-thiazolidine comprising the steps of: reacting an alkali metal cyanide compound, an alkali metal hydroxide, a lower alcohol and chlorine in an aqueous solution to form an carboimidic acid ester solution, then adding an organic solvent thereto, followed by adding a cyanamide solution to form an N-cyanocarbonimidic acid ester, and further extracting the resultant ester with an organic solvent extracting solution, followed by washing with an aqueous solution of a reducing agent solution to obtain a high purity, stable N-cyanocarbonimidic acid ester as a first step; and reacting the N-cyanocarbonimidic acid ester obtained in the first step with 2-aminoethanethiol to be cyclicized as a second step to thereby obtain a 2-cyanoimino-1,3-thiazolidine.

Abstract: Insecticidal aminothiazole derivatives and the use as an insecticide and acaricide of the compounds of formula (1): wherein R1 is cyano or fluoroalkyl, R2 is halogen, SCN or aryl, R3 is H, C1-C6 alkyl, SO2R5 or C(O)R6, R4 and R6 are, independently, aryl, phenylalkyl, alkyl, cycloalkyl groups, being optionally substituted by one or more of halogen, cyano, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, nitro, alkoxycarbonyl, alkylcarbonyloxy, alkylenedioxy, alkylcarbonyl, amino, alkylamino, haloalkoxy, alkylthio, alkylsulfonyl, haloalkenyl, alkoxycarbonylalkyl or alkoxycarbonylalkoxy; said aryl, phenylalkyl groups may additionally be fused to a cycloalkyl ring, R5 is C1-C6 alkyl, haloalkyl, X is O, S, NR7, R7 is alkyl, cycloalkyl, alkoxy, alkenylalkyloxy, alkynylalkyloxy, alkoxycarbonylalkyloxy.

Abstract: Compounds of formula (I), particularly a compound of formula (Ia), are non-peptide TPO mimetics, useful in the treatment of thrombocytopenia.

Abstract: The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.

Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.

Abstract: The invention relates to novel aryl and heteroaryl sulfonates of formula (Ia) and to methods for producing them and to novel aryl and heteroaryl sulfonates of formula (I) for treating and/or preventing diseases, especially for treating pain and neurodegenerative diseases, A representing (C6-C10)-aryl or 5-10-membered heteroaryl, D representing (C6-C10)-arylene or 5-10-membered heteroarylene, R1 representing (C4-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—, —SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl, in formula (Ia); and R1 representing (C3-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—,—SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl.

Abstract: The invention relates to a write-once optical data carrier in which organic and/or inorganic light-absorbing compounds are used as the information layer, especially for high-density optical data carriers which function with a blue laser in the wavelength range of 360-460 nm. The invention also relates to the application of the above-mentioned light-absorbing compound to a suitable substrate (especially polycarbonate), e.g. by spin coating.

Abstract: A method for producing high purity 2-cyanoimino-1,3-thiazolidine comprising the steps of:

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.

Abstract: Compounds are provided which have the structure 1

Abstract: The present invention relates to novel triazolo-pyridines of the formula I 1

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.

Abstract: The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor (“CRF receptor”) and useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.

Abstract: Compounds of the formula 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: A compound according to Formula (I), hereinbelow: wherein A—B represents a covalent bond or an optionally substituted 1,3 or 1,4 aryl ring selected from the group consisting of: X is independently selected from the group consisting of H, Br, CH3, CN, and NR1R2, wherein R1 and R2 represent hydrogen or C1-4 alkyl; branched or cyclic, optionally containing O or N; and Ar represents optionally substituted phenyl or an optionally substituted 5 or 6 membered heterocylic ring containing one or more heteroatoms selected from N, O and S; provided that when Y is hydrogen, at least one Ar contains a heteroatom selected from N, S and O.

Abstract: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.

Abstract: This invention provides compounds having the structure: 1

Abstract: A compound according to Formula (I), hereinbelow: wherein A represents a covalent bond, or a 1,2, 1,3 or 1,4-disubstituted aryl amine ring selected from the group consisting of:  wherein R is independently selected from the group consisting of H, OMe, Cl, Br, F, NO2, and CN; n is an integer from 1 to 4; each X is independently selected from the group consisting of H, Br, CH3, NO2, CN, and NR1R2; each Ar is independently optionally substituted phenyl or an optionally substituted 5 or 6 membered heterocyclic ring comprising one or more heteroatoms selected from N, O and S; and R1 and R2 are, independently, hydrogen or C1-4 alkyl, branched or cyclic, optionally containing O or N.

Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) (wherein R1, R2 and R3 are each H, C3-C6 cycloalkyl group, group of the formula —A1—Ql or the like; X may be the same or different and are each halogen atom, nitro group, phenyl group, group of the formula —A2—R7 or the like; n is 1 to 4; Y may be same or different and are each halogen atom, cyano group, phenyl group, group of the formula —A2—R7 or the like; m is 1 to 5; Z1 and Z2 are each 0 or S), fluorine-containing aniline compound represented by the general formula (ST-I) as starting material for said phthalic acid diamide derivative (wherein Ra is halogen atom, C1-C6 alkyl group or the like and Rb, Rc and Rd is H or C2-C6 perfluoroalkyl group), and an agricultural and horticultural insecticide containing said phthaldiamide derivative, as well as to provide a method for use of said insecticide.

Abstract: The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.

Abstract: The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: Phenylalkylcarboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 represents an alkyl group and the like, R.sup.2 represents an alkylene group, R.sup.3 represents a hydrogen atom and the like, X represents a substituted or unsubstituted aryl group and the like, Y represents an oxygen atom and the like, Z represents an alkylene group and the like, and W represents an alkyl group and the like),the pharmacologically acceptable salts thereof or the pharmacologically acceptable esters thereof are useful as therapeutic or preventive agents for hyperglycemia and the like.

Abstract: Selected amino acid hydroxyethylamino 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: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.

Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.

Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: Naphthalene derivatives of the formula ##STR1## where the rings A and B may be benzofused,X is nitrogen or a radical of the formula CH or CH.dbd.CH--CH,Z is a heterocyclic radical or additionally, when x is CH.dbd.CH--CH, a 5- or 6-membered aromatic carbocyclic radical, andR.sup.1, R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl, are useful in nonlinear optics.

Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1alkyl, alkoxy, alkylaminoR.sup.2alkyl;Aa direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofBhydrogen, halogen,alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylUCH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;Xhydrogen, cyano, nitro, halogen,alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof,amino which may bear one or two of the abovementioned groups;m1 or 2,Yoxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.

Abstract: A process for the production of 2-cyanoiminothiazolidine by reaction of 2-aminoethanethiol (cysteamine) with a dialkyl-N-cyanoimidocarbonate.

Abstract: X is an acid radical, andA is a metal ion or an equivalent ammonium ion.