Abstract: Substituted benzo[d]isoxazol-3-yl amine compounds corresponding to formula I which exhibit an strong affinity to the KCNQ2/3 K+ channel, and which are suitable for treating or inhibiting pain and/or disorders or disease states that are at least partly mediated by the KCNQ2/3 K+ channel.

Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

Abstract: The present invention provides compositions and methods for preventing inflammation and retinal edema resulting from an ocular surgical procedure by administering to a patient undergoing surgery a therapeutically effective amount of a composition comprising an active agent selected from the group consisting of RTK inhibitors and anti-VEGF compounds, and a pharmaceutically acceptable carrier, wherein the RTK inhibitor blocks tyrosine autophosphorylation of VEGFR-1, VEGFR-2, VEGFR-3, Tie-2, PDGFR, c-KIT, Flt-3, and CSF-1R.

Abstract: The present invention provides methods for inhibiting increased vascular permeability and/or pathologic ocular angiogenesis and providing neuroprotection of the affected retina via administration of a combination of one or more molecules that potently inhibit select receptor tyrosine kinases (RTKs) or vascular endothelial growth factor (VEGF) and one or more neuroprotectants.

Abstract: The present invention features a novel therapy for treating diabetes, hypertension, migraine, epilepsy, sleep apnea, depression, impulse control disorders or alcohol addiction which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) in combination with an anticonvulsant sulfamate compound (e.g., topiramate) or an anticonvulsive sulfonylurea compound (e.g. zonisamide).

Abstract: The present invention provides isoxazole derivatives represented by the following formula (I): (wherein R1 represents a hydrogen atom, C1-C20 hydrocarbon group or —C(?O)OR1a (wherein R1a represents a C1-C10 alkyl group, etc.); R2 and R3 represent a hydrogen atom, halogen atom, hydroxy group, C1-C20 alkyl group or C6-C20 aryl group, etc.; R4 represents a hydrogen atom, halogen atom, hydroxy group, cyano group, nitro group, amino group, C1-C20 hydrocarbon group, C1-C10 alkoxy group, C1-C10 acyl group, 5- to 7-membered heterocyclic group, etc.; R5 represents a hydrogen atom, halogen atom, hydroxy group, optionally substituted C1-C20 hydrocarbon group, C1-C20 alkoxy group, 5- to 7-membered heterocyclic group, etc.; and, n represents 0, 1, 2, 3 or 4), and a process of producing the same. The compounds are useful as intermediates for synthesis of pharmaceutical compounds, agricultural chemicals, dye compounds, etc. having the isoxazole skeleton.

Abstract: The present invention relates to 3-amido-1,2-benzoisoxazole derivatives and their salts represented by formula 1, processes for preparation and usees thereof. More particularly, it relates to a method for improving its bioavailability introducing amino acid residue to the amine group of a 3-amido-1,2-benzoisoxazole. The compounds according to the present invention are used as an antagonist against Leukotriene-B-4 receptor, an inhibitor or therapeutics of osteoroposis, thus inhibiting osteolysis and stimulating osteogensis.

Abstract: The present invention is directed to a method of treating action tremor or severe essential tremor. Action tremor includes essential tremor, postural tremor, drug-induced or toxic tremor, primary orthostatic tremor, dystonic tremor, neuropathic tremor, and cerebellar tremor. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of zonisamide, or a pharmaceutically acceptable salt thereof. The methods of the present invention are useful in reducing symptoms of tremor. The compounds of the present method can also be used in conjunction with other therapeutic agents commonly used to treat tremor thus enhancing the therapeutic effect of treating tremor.

Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.

Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.

Abstract: A novel class of 3-oxo-3H-benzo[d]isoxazole carboxamide compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases.

Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutic amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein Z1 is N or CR3; Z2 is N or CR4; Z3is O or S; A is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc or a mixture thereof; R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, hydroxy alkoxy, aryl, acyl, halo, cyano, haloalkyl, NHCOOR5 and SO2NH2; R5 is aryl, arylalkyl, heteroaryl or heteroarylalkyl; at least one of R1, R2, R3 and R4 is other than hydrogen; and at least one of Z1 and Z2 is other than N.

Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.

Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

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: Tricyclic benzoylpyrazole derivatives of the formula I wherein X, Y, R1, R2, R6, R7, R3, R4, R5, l, R8 and R9 are as defined in the disclosure and their agriculturally useful salts; processes and intermediates for preparing the tricyclic benzoylpyrazole derivatives; compositions comprising them and the use of these derivatives or of the compositions comprising them for controlling undesirable plants are described.

Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.

Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.

Abstract: The present application describes methods of using a combination of 1-(3?-aminobenzisoxazol-5?-yl)-3-trifluoromethyl-5-[[4-[(2?-dimethylaminomethyl)imidazol-1?-yl]-2-fluorophenyl]aminocarbonyl]pyrazole-hydrochloric acid salt, a factor Xa inhibitor, and Clopidogrel as anticoagulant agents for treatment of thromboembolic disorders and pharmaceutical compositions containing the same.

Abstract: Selective androgen receptor modulators (SARMs) having antagonist activity in hormone-dependent tumors while exhibiting no activity or agonist activity against other nontumor tissues containing the androgen receptor as well as methods for identifying, designing and using SARMs are provided.

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.

Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

Abstract: The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group optionally substituted by the substituents listed in the specification.

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, and R3 are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to group A streptogramin derivatives of general formula (I) and processes for preparing the same: which has particularly advantageous antibacterial activity.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.

Abstract: The present invention relates to novel LXR ligands of Formula (I) and the pharmaceutically acceptable salts and esters thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.

Abstract: Compounds having the formula 1

Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability.

Abstract: The present application describes modulators of CCR3 of formula (I):

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: 1

Abstract: Compounds of the formula: useful for treatment of disorders such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.

Abstract: This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38.

Abstract: The present invention is directed to a method of treating action tremor or severe essential tremor. Action tremor includes essential tremor, postural tremor, drug-induced or toxic tremor, primary orthostatic tremor, dystonic tremor, neuropathic tremor, and cerebellar tremor. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of zonisamide, or a pharmaceutically acceptable salt thereof. The methods of the present invention are useful in reducing symptoms of tremor. The compounds of the present method can also be used in conjunction with other therapeutic agents commonly used to treat tremor thus enhancing the therapeutic effect of treating tremor.

Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S ; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salt

Abstract: This invention is generally directed to methods for treating or preventing a disease or disorder comprising administering to a patient in need thereof an effective amount of a Jun N-terminal kinase (JNK) inhibitor, such as an isothiazoloanthrone, isoxazoloanthrone, isoindolanthrone, or derivative thereof having the general formula: 1

Abstract: The present application describes N-[4-(1H-imidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides and derivatives thereof of, which are useful as inhibitors of factor Xa.

Abstract: The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.

Abstract: The present application describes methods of using a combination of 1-(3′-aminobenzisoxazol-5′-yl)-3-trifluoromethyl-5-[[4-[(2′-dimethylaminomethyl)imidazol-1′-yl]-2-fluorophenyl]aminocarbonyl]pyrazole-hydrochloric acid salt, a factor Xa inhibitor, and Clopidogrel as anticoagulant agents for treatment of thromboembolic disorders and pharmaceutical compositions containing the same.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.