Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.

Abstract: This invention relates to the discovery of prodrugs of 3- or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.

Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.

Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly hyperproliferative diseases such as cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly hyperproliferative diseases such as cancer.

Abstract: The invention concerns compounds of general formula (I): Wherein n, X, Y, R1 and R2 are as defined herein. The invention also concerns a method for preparing the compounds and their therapeutic use.

Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc.

Abstract: A compound of formula: wherein X is a C2-10 spacer, and R is a substituted or unsubstituted C6-30 aryl, a substituted or unsubstituted C5-30 heteroaryl, or Where R? and R? are independently a substituted or unsubstituted aryl or a substituted or unsubstituted alkyl, wherein said compound is a vitamin D receptor (VDR) antagonist, a compound comprising same, and a method of treating a patient for a disease that can be treated prophylactically or therapeutically by administration of a VDR antagonist, which method comprises administering an effective amount of aforementioned compound or composition, whereupon the patient is treated prophylactically or therapeutically for the disease.

Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: The invention provides antitumour compounds of formula (I), wherein R1 is an aromatic substituent; R2 is hydrogen or a substituent when the dotted line is absent, or R2 is absent when the dotted line represents a bond to give a double bond between the nitrogen which bears R2 and the carbon which bears R3; R3 is an oxo group ?O when the dotted line is absent or is a substituent when the dotted line represents a bond to give a double bond between the nitrogen bearing R2 and the carbon bearing R3; R4 is hydrogen or a substituent; and pharmaceutically acceptable salts thereof.

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: The present invention provides: an organic EL element exhibiting high luminance, a high external quantum efficiency and a long high temperature driving life at 50° C.; an illuminator and a display device employing the organic EL element; and a material preferably used for the organic EL element.

Abstract: The invention provides variolin derivatives of formula (I), wherein: R1 and R2 are each independently selected from the group consisting of H, OH, OR, SH, SR, SOR, SO2R, NO2, NH2, NHR, N(R)2, NHCOR, N(COR)2, NHSO2R, CN, halogen, C(?O)H, C(?O)R, CO2H, CO2R, C1-C12 alkyl, C1-C12 haloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; and R3 is selected from the group consisting of H, OH and OMe; wherein the or each group R is independently selected from the group consisting of OH, C1-C12 alkyl, C1-C12 haloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted unsubstituted aralkyl, substituted or unsubstituted arylalkenyl and substituted or unsubstituted heteroaromatic, and wherein the group R1, R2 or R3 is a group of formula N(R)2 or N(COR)2, each of the R groups may be the same or different, or the two R groups, together with the nitrogen atom to which they are attached, m

Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain non-imidazole tertiary amine derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: Pyrimidine derivatives of the formula (I) and physiologically acceptable salts thereof, in which R1, R2, R3, R4, W, X, Y and Z are as defined in claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of diseases of the cardiovascular system and for the treatment and/or therapy of potency disorders

Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed

Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diamine compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B, and are useful for lowering blood glucose concentrations in mammals.

Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.

Abstract: The present invention relates to modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating obesity using such compounds and compositions.

Abstract: The present invention relates to a compound of Formula (I) and its use in treating lung and breast cancer.

Abstract: This invention relates to diaminopyrroloquinazoline compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B, and are useful for lowering blood glucose concentrations in mammals.

Abstract: Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor (“EGFR”) tyrosine kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also relates to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.

Abstract: The present invention relates to tricyclic 2-pyrimidone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: Substituted pyrazolopyrimidines and thiazolopyrimidines, specifically, compounds corresponding to the structure (I A), (I B) or (II) processes for their preparation, substance libraries containing them, pharmaceutical formulations containing these compounds, the use of these compounds for the production of medicaments for the treatment and/or prophylaxis of pain and related treatment methods are provided.

Abstract: The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I, wherein A, B and R1 to R5 are as defined herein. The compounds of formula I are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The invention relates to an organic electroluminescent device which contains 2,5-diaminoterephthalic acid derivatives of formula 1a as emitter substances in one or several emitter layers in a pure or doped manner. The ring A is a triple unsaturated benzene ring wherein R4? and R8? are zero or ring A is a double unsaturated ring respectively provided with a double bond in the 1,2 position and 4,5 position, and wherein R10 is a nitrile radical —CN or a radical C(?X1)—X2R1, R11 is a nitrile radical —CN or a radical —C(?X3)—X4R5, X1 and X3 are oxygen, sulfur or imino, X2 and X4 are oxygen, sulfur or optionally substituted amino, R1–R8, R4? and R8? are H, C1–20-alkyl, aryl, heteroaryl, R4 and R8 can be halogen, nitro, cyanogen or amino, R2–R4, R6–R8, R4? and R8? can be trifluoromethyl or pentafluorophenyl, and wherein certain radicals can form a saturated or unsaturated ring.

Abstract: This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, A1CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula —Alk—O—CO—Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic

Abstract: The present invention provides a process of a compound of the formula (I): wherein R is heteroaryl or the like, ring A is a heteroalicyclic group or the like comprising reacting a compound of the formula (II): wherein Hal is halogen and the other symbols are the same as the above, in the presence of a sulfinic acid salt and further in the presence of an acid or a salt with an organic base, and a novel crystal form of 2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine phosphate monohydrate.

Abstract: The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno[2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as anxiety, depression, schizophrenia, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

Abstract: The invention relates to compounds of the formula (I) in which R1, E2 and X are as defined above.

Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S.

Abstract: The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A, B and D are the same as or different from each other and each represents a group represented by the formula —(CR1R2)m— (wherein R1 and R2 are the same as or different from each other and each represents a C1-6 alkyl group etc.), —NR3— (wherein R3 represetns hydrogen etc.) etc.; E and G are the same as or different from each other and each represents a group represented by the formula —(CR6R7)p— (wherein R6and R7 are the same as or different from each other and each represents hydrogen etc.; and p represents an integer of 0, 1 or 2); J represents a carbon atom or nitrogen atom, each substituted with C1-6 alkyl group optionally substituted with a halogen atom, etc.

Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, wherein A is selected from NCN, NCONH2, and NOR9. The present invention relates to compounds which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.

Abstract: Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.

Abstract: Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ?O and ?S; W is —C(?O)—, —S(?O)—, or —S(O)2—; or W may be —CH2— if X is —C(?O)—; X is selected from —CH2—, —N(R4)—, and —O—, except that when W is —CH2—, X is —C(?O)—; Y is a bond or —C(R40)(R45)—; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and X1, X2, X3, X4, X5, X6, X7, X8, X9, X10 and X11 are selected such a tricyclic heteroaryl ring system is formed as further defined in the specification.

Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.

Abstract: Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.

Abstract: The invention relates to 4-amino-5,6-substituted thiopheno [2,3-d] pyrimidines, pharmaceutical compositions containing the same and their use to treat or prevent diseases and conditions mediated by the phosphodiesterase enzyme 7B (PDE7B). Diseases and conditions mediated by PDE7B include osteoporosis, osteopenia and asthma.

Abstract: A compound selected from those of formula (I): in which: W represents N or C—R1; in which R1 is as defined in the description, X represents N or C—R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, —NH, and —Nalkyl, Z represents a group selected from oxygen, sulphur, —NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group —CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula: in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof

Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.

Abstract: The invention relates to an electroluminescent device, in which the luminescent layer contains a luminescent compound and a compound of the general formula I as doping agent, wherein B is an unsaturated carbocyclic or heterocyclic 4-8-link ring, which can also contain an alicyclic bridge, the rings D and E are five- or six-link rings, which each can contain one more hetero-atom N, O and S, the radicals R are one or more substituents H or straight-chain or branched C1-C6-alkyl, X and Y are carbon or nitrogen, R1; R2 and R9 are H or straight-chain or branched C1-C6-alkyl, R3 and R9 are hydrogen, straight-chain or branched C1-C6-alkyl, hydroxy, —OR16, —COOR16, N,N-dialkylamino, acetylamino or halogen, wherein R16 is hydrogen, or straight-chain or branched C1-C6-alkyl, R1 and R2 or R2 and R3 and/or R9 and R9 together can form an alicyclic, heterocyclic or aromatic ring, and A1 and A2, which can be the same or different, are cyan, nitro or —COOR16. The compounds I are partly new.

Abstract: The present invention relates to tricyclic 2-pyrimidone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.