Abstract: New pyridazin-3(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4.

Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.

Abstract: The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatilis, psoriasis or irritable bowel disease.

Abstract: There is provided a combination product comprising; (A) melagatran or a pharmaceutically acceptable derivative thereof; and (B) dexamethasone or a pharmaceutically acceptable derivative there of, wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, as well as the use of such a combination product in the treatment of conditions including disseminated intravascular coagulation.

Abstract: New pyridazin-3(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4.

Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: The present invention provides compounds of formula (I) possessing inhibitory activity against ? adrenergic receptors and phosphodiesterase (PDE), including type 3 phosphodiesterase (PDE-3). The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated and for treating cardiovascular disease, stroke, epilepsy, an ophthalmic disorder or migraine.

Abstract: The present invention relates to novel compounds of formula (I), processes for their preparation, compositions comprising them and their use in the treatment or prevention of diseases capable of being modulated by the inhibition of cell adhesion.

Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract: A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: Method for preparing compounds of the formula (III) by reacting compounds of the formula (II) with a) an alcoholate or b) an alcohol R1-OH and a base in the presence of a Cu-containing catalyst and of a ligand, where X1-5 are independently of one another either carbon or nitrogen, or in each case two adjacent X1R1, with i=1?6, linked by a formal double bond together O, S, NRH or Nrl. The ligands preferably employed are acyclic and/or cyclic oligo- and polyglycols, oligo- and polyamides or oligo- and polyamine glycols of the general formula (IV) k is an integer >0 and n is an integer >1; X and Y are independently of one another O, NH or NR1.

Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: Substituted nitrogen-containing heterocycles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration,

Abstract: The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4alkyl and (4?) a C1-4alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4alkoxy-C1-4alkyl, (3?) a mono-C1-4alkyl-carbamoyl-C1-4alkyl, (4?) a C1-4alkoxy and (5?) a mono-C1-4alkylcarbamoyl-C1-4alkoxy, or the like; R3 is a C1-4alkyl; R4 is a C1-4alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: The present invention provides a process for the preparation of phenylacetic acid compounds 2 where R2 is an optionally substituted aryl, R6 is NO2, NH2, alkyl, halogen, or a function group readily derived there from and R4a is hydrogen C1-6 alkyl, tert-butyl or benzyl The compounds of formula 2a are useful intermediates for the preparation of HIV reverse transcriptase inhibitors

Abstract: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein

Abstract: The present invention provides a novel epoxy compound, which can be converted into a cured epoxy resin product having liquid crystal properties by curing with a curing agent. Since the cured epoxy resin product of the present invention exhibits good heat conductivity, it is also useful as an insulating material requiring high heat releasability such as a printed circuit substrate and the like.

Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.

Abstract: A phenylpyridazine derivative represented by the formula (1): Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. The present invention provides water-soluble phenylpyridazine derivatives and medicines containing them, which have excellent inhibitory activity against interleukin-? production, high water solubility and high oral absorbability.

Abstract: This invention relates to novel pyridazinone derivatives of formula I wherein R1–R4, R7, R8 and X1 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.

Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d

Abstract: The present invention relates to salts of 2-(6-{2-[(2R)-2-methyl-1-pyrrolidin-1-yl]-ethyl}-2-naphthalen-2-yl)-2H-pyridazin-3-one, processes for their preparation, pharmaceutical compositions comprising such compounds, method of using them, and a process for preparing the active agent.

Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.

Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2), COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently markered non-steroidal anti-inflammatory drugs (NSAIDs).

Abstract: The present invention relates to substituted cyclopentene compounds of the general formula I, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use thereof for the production of pharmaceutical preparations.

Abstract: Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1? production, high water solubility and good oral absorbability.

Abstract: Methods of and systems for remediating hydrazine spills, solutions and hydrazine-contaminated objects including areas thereof. Initially, an aqueous solution comprising a dicarbonyl-compound can be prepared. The aqueous solution can then be provided for application to an object contaminated with a hydrazine group compound. The hydrazine group compounds are converted to a stable organic compound as a result of a reaction of the dicarbonyl-compound and hydrazine group compound. Conversion assists in the remediation of the hydrazine group compound from the object. The stable organic compound produced as a result of the reaction between the dicarbonyl-compound and hydrazine group compound can then be treated with a metal catalyst and hydrogen to produce glutamine or a derivative thereof. Both the stable organic compound and glutamine can undergo microbiological degradation without further remedial intervention.

Abstract: A color photographic material is described containing a compound of formula (I) wherein, if n=1, R1 is, inter alia, a radical of formula (II), and, if n=2, R1 is unsubstituted or C1–C4alkyl- or hydroxy-substituted phenylene or naphthylene; or —R12—X—R13—, and other residues are as defined in claim 1. The compound of formula (I) is effective as scavenger of the oxidized form of the developer (Dox scavenger), especially when contained in an interlayer between light sensitive layers. Selected compounds of this class can also be used as additives, for example as dye stabilizer, in color photographic materials, or as an antioxidant for organic materials.

Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.

Abstract: The invention relates to novel phenylpyridazinones of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and processes for preparing them.

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(?O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(?O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1? protease activity in a mammal utilizing the compounds and compositions.

Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.

Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.

Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors

Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.

Abstract: The compounds of formula I in which Ar1, A, R6, R7, R8 and Ar2 have the meanings as given in the description are novel effective bronchial therapeutics

Abstract: The invention relates to novel substituted benzoylcyclohexanediones of the general formula (I), in which m, n, A, R1, R2, R3, R4 and Z are each as defined in the description, and also to processes for their preparation and to their use as herbicides.

Abstract: aP2 inhibiting compounds are provided having the formula wherein A, X, R and Z are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitors alone or in combination with other therapeutic agents, including other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

Abstract: The use of mitochondrial KATP channel openers, particularly compounds of general formula (I), for the treatment or prevention of inflammation by inducing apoptosis of inflammatory cells.

Abstract: Disclosed are compounds of formula (I): wherein R1, R2, W and X of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

Abstract: Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1? production, high water solubility and good oral absorbability.