Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

Abstract: Substituted 3,4-dihydro-pyrimido[1,2a]pyrimidines and 3,4-dihydro-pyrazino[1,2a]pyrimidines of general formula I, the invention also relates to a method for the production thereof, substance libraries containing these compounds, medicaments which contain these compounds in the production of medicaments for treating pain, urinary incontinence, itching, tinnitus aurium and/or diarrhea and to pharmaceutical compositions containing these compounds.

Abstract: Compounds of the formula are neuropeptide Y antagonists and are effective in treating feeding disorders, cardiovascular diseases and other physiological disorders related to an excess of neuropeptide Y.

Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia,  or represents a chain of formula Ib,  and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.

Abstract: Disclosed herein are compounds having the structural formula A 1

Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.

Abstract: Novel pyrrolo[2,3-d]pyrimidine compounds useful as inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 as well as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases are described.

Abstract: The invention provides pharmaceutically useful thieno[2,3-d]pyrimidinediones, processes for their production, pharmaceutical compositions containing them and methods of treatment involving their use.

Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases: 1

Abstract: The present invention is concerned with compounds of formula 1

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides substituted piperidines, and compositions containing these compounds. Also provided are methods using the compounds of the invention for the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.

Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.

Abstract: Compounds of the formula (I) wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, hererocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except hydrogen may be optionally substituted; R2 and R3 independently represent hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heteroaryl, heteroarylC1-6alkyl, heterocyclyl, or heterocyclylC1-6alkyl any one of which except hydrogen may be optionally substituted, or R2 and R3 together with the nitrogen atom to which they are attached form a 4- to 10-membered optionally substituted monocyclic or bicyclic ring; Ar is an aryl or heteroaryl ring either of which may be optionally substituted; one of X1 and X2 is N and the other is NR4, wherein R4 is hydrogen, C1-6alkyl, or arylC1-6alkyl; or pharmaceutically acceptable salts thereof; their use as inhibitors of Raf kinases and pharmaceutical compositions containing them.

Abstract: This invention concerns compounds of formula 1

Abstract: This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvent thereof, which is an inhibitor of cysteine proteases, particularly cathespin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor

Abstract: The present invention provides compounds of formula (I): 1

Abstract: The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): 1

Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.

Abstract: The invention provides a process for the production of a compound of formula (A), or a pharmaceutically acceptable salt or solvate thereof, 1

Abstract: The invention provides a process for the production of a compound of formula (A) or a pharmaceutically acceptable salt or solvate thereof: 1

Abstract: A process for preparing 4,6-diaminopyrimido[5,4-d]pyrimidines of formula I, 1

Abstract: Compounds of the formula 1

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, R2, R3, W, X, Y, and Z are substituents as defined herein, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: Disclosed are compounds of formula wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: The present invention provides compounds, compositions and methods for the inhibition or treatment of conditions or disorders modulated by the STAT transcription factors, particularly STAT4 and STAT6. Additionally, the compounds are useful for the diagnosis of conditions dependent on STAT signaling.

Abstract: Pyrimidone compounds of formula (I): 1

Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

Abstract: This invention concerns compounds of formula 1

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.

Abstract: This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I): 1

Abstract: Triazolo[4,5-d]pyrimidine compounds are provided of the formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. Compositions containing the compounds are also provided, together with processes for their preparation and methods of use in the treatment of diseases, including myocardial infarction and unstable angina.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

Abstract: A pyrimidine nucleus-containing compound represented by the formula (I): wherein ring A represents the ring of the formula (a): in which R1 is a nitro group, an amino group, a substituted amino group or a halogen atom, or the ring of the formula (b): in which R1′ is the group such as an alkyl group or an alkenyl group; R2 to R5 independently represent the group such as an alkyl group or an alkenyl group; with the proviso that at least one of R2 to R5 is an alkenyl group, or acid addition salts 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 novel compounds of formula I: (R1, R2, R3, L1, L2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.

Abstract: 3-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl group, an acetyl group, a phenylalkyl C.sub.1 -C.sub.4 radical, the aromatic system being unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen,R.sup.2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, hydroxyl, trifluoromethyl, C.sub.1 -C.sub.

Abstract: 3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which may be unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, hydroxyl, trifluoromethyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups, and may contain 1 nitrogen atom, or to a 5- or 6-membered ring, which may contain 1-2 oxygen atoms,A is NH or an oxygen atom,Y is CH.sub.2, CH.sub.2 --CH.sub.2, CH.sub.2 --CH.sub.2 --CH.sub.2 or CH.sub.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to form fungicidal compositions.

Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity, in particular against rice blast disease. The new compounds are processed with carriers, and optionally an adjuvant, to make fungicidal compositions.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2, R.sup.3, L.sup.1, L.sup.2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.

Abstract: A quinazolinone derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 ; wherein R.sup.1 represents a hydrocarbon group of C.sub.10-30 ; wherein R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group, or a benzyl group, or together represent a heterocyclic ring having 3-7 members; and n represents an integer of 1-5; wherein when A is R.sup.1, B is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 and when A is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3, B is R.sup.1 ; and wherein R.sup.4 is selected from the group consisting of a hydrogen atom, a halogen atom, a lower alkyl group, a lower acyl group, a nitro group, a cyano group, an amino group, a lower alkoxycarbonyl group, a lower alkylamino group, a lower alkoxy group, a lower acyloxy group, a carbamoyl group, a lower alkylcarbamoyl group, and a lower acylamino group.

Abstract: 6-Aryl pyrazolo?3,4-d!pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.

Abstract: This invention relates to 2- or 3-(substituted aminoalkoxyphenyl)quinazolin-4-ones which are partial estrogen agonists and are useful in treating osteoporosis, prostatic hypertrophy, breast cancer and endometrial cancer.

Abstract: Disclosed are quinazoline derivatives represented by formula (I): wherein R.sup.1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R.sup.10 represents hydrogen, lower alkyl, or the like; R.sup.11 and R.sup.12 represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R.sup.11 and R.sup.12 are combined together with N to form a heterocyclic group; and n represents 0, 1 or 2, and pharmaceutically acceptable salts thereof. These compounds have adenosine uptake inhibitory activity and are useful for the protection of myocardium and for the prevention or treatment of renal diseases such as nephritis and diabetic nephropathy.

Abstract: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.

Abstract: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3) alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which are taken together to form a 4- to 7- membered ring;(C) R.sub.3 is selected from the group consisting of H, --CH.sub.3, --CH.sub.2 CH.sub.3, and --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3- position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri- substituted with --OR.sub.4, --NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, or phenyl;R.sub.4 is H or (C.sub.1 -C.sub. 4) straight-chain alkyl;R.sub.5 and R.sub.

Abstract: Pyrimido?5,4-d!pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are:4-?(3-Chloro-4-fluorophenyl)amino!-6-?1-methyl-4-piperidinylamino!pyrimido? 5,4-d!pyrimidine, and4-?(3-Chloro-4-fluorophenyl)amino!-6-?trans-4-dimethyl-aminocycohexylamino! pyrimido?5,4-d!pyrimidine.