Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.

Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A ?or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: Compositions of flupirtine for management of neuropathic or inflammatory pain optionally including one or more other analgesics including opiates, NSAIDS and other active agents in immediate and controlled release forms. Methods and systems for administration of these compositions.

Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.

Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases.

Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.

Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they

Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.

Abstract: The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (? receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.

Abstract: The present invention relates to compositions for electroporation which are useful in elevating a percutaneous absorbability of drugs, etc. By adding polyhydric alcohols to compositions for electroporation, the percutaneous absorbability of drugs is elevated.

Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.

Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: The present invention relates to a 5-phenylbenzylamine compound represented by the formula [1]: wherein Ring A represents a phenyl group having a substituent(s), Ra, Rb1 and Rb2 each represent hydrogen atom, a halogen atom, a lower alkyl group, a halogeno-lower alkyl group or a lower alkoxy group, Rc1 represents hydrogen atom, a lower alkyl group optionally substituted by a heterocyclic group, or an acyl group, Rc2 and Re each represent hydrogen atom or a lower alkyl group, Rd represents hydrogen atom, a lower alkyl group or an acyl group, and Rf represents a lower alkyl group or a cyclic lower alkyl group, or a pharmaceutically acceptable salt thereof, a process for preparing the same and synthetic intermediate thereof.

Abstract: Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH?CH?, CH?2, ? or Cy, X is trivalent straight-chain alkylene (3–10C) or trivalent straight-chain 1-alkenylene (3–10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is ?2CH; and is otherwise trivalent straight-chain alkylene (5–10C) or trivalent straight-chain 1-alkenylene (5–10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1–6C); and n is 0–5; wherein each ? and Cy independently may optionally be substituted by alkyl (1–6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1–4C), or two substituents may form a 5–7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.

Abstract: A method for modifying at least one non-ester-containing parent compound, and the compounds produced using such method, which compounds are deployed to temporarily incapacitate at least one subject are disclosed. The modified compounds are rapidly metabolized to inactive and non-toxic metabolites when exposure to the modified compounds is halted.

Abstract: Epothilone derivatives are co-administered with an antidiarrheal agent, e.g., a DPP-IV inhibitor, in the treatment of a proliferative disease.

Abstract: (R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparation and pharmaceutical preparations thereof are also described. The quaternary salts of the invention are useful in the inhibition of chemotaxis of neutrophils and monocytes induced by the fraction C5a of the complement and are used in the treatment of psoriasis, pemphigus and pemphigoid, rheumatoid arthritis, intestinal chronic inflammatory pathologies including ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, cystic fibrosis, chronic obstructive pulmonary disease and glomerulonephritis. The compounds of the invention are advantageously used in the prevention and the treatment of injury caused by ischemia and reperfusion.

Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.

Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.

Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administerable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.

Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity)

Abstract: Spontaneously dispersible pharmaceutical compositions comprising a piperidine, e.g. 1-acylpiperidine Substance P Antagonist and its use in the treatment of CNS disorders, e.g. depression and social phobia, and respiratory diseases, e.g. asthma and chronic bronchitis.

Abstract: Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating disorders.

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF? and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF? and/or one or more other involved cytokines, alone or in combination with other agents.

Abstract: Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.

Abstract: The invention provides compounds of general formula (I) wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.

Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obsructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

Abstract: A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independently C1-3alkyl optionally substituted by fluoro or chloro; or R1 and R2 together with the carbon atom to which they are attached, form a C3-5cycloalkyl ring optionally substituted by fluoro; R3 is defined within; and n is 0-5; wherein the values of R3 may be the same or different; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Abstract: The present application is directed to compounds having the structure of Formula I: where R1 is phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl or trazolyl, each optionally substituted by a straight or branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, or iodo; where Ra and Rb are independently selected from hydrogen, a straight or branched C1-C6 alkyl, NO2, C1-C6 alkoxy, chloro, fluoro, bromo, or iodo; and where X is O or CH3. The compounds may be incorporated into pharmaceutical compositions and administered to patients as a treatment for pain, gastrointestinal disorders, spinal injury, or disorders of the sympathetic nervous system.

Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.

Abstract: The invention relates to compounds of formula (I) where R1 represents a hydrogen or halogen atom or an —S(O)z—(C1-C4)alkyl, —S(O)z—(C1-C4)R3, —SO2—NH—(C1-C4)alkyl, —NHCO(C1-C4) alkyl, —CO(C1-C4)alkyl or —NHSO2—(C1-C4)alkyl group; m and n independently represent 0, 1 or 2; A represents a group of formula (a) or (b): where X is N or CH; R2 represents an —SO2—R3, —CO—R3 or —CO—(C1-C4)—alkyl group; R3 represents a phenyl group, optionally substituted by a (C1-C4)alkyl or (C1-C4)alkoxy group, one or two halogen atoms or a heterocycle; R4 represents a hydrogen or halogen atom or a (C1-C6)alkyl, (C1-C4)alkoxy, —COOH, —COO(C1-C4)alkyl, —CN, —CONR5R6, —NO2, —NHSO2(C1-C4)alkyl or —SO2NR5R6 group; z is 1 or 2; R5 and R6 independently represent a hydrogen atom or a (C1-C4)alkyl, phenyl or phenyl (C1-C4)alkyl group; and their salts or solvates, to a process for their preparation, to synthetic intermediates and to the pharmaceutical compositions comprising them.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: The invention concerns phenoxypropanolamines of formula (I) in which R1 represents a hydrogen, a group —S(O)z—(C1-C4)alk-R?, (R? being H, phenyl or (C1-C4)alkoxy), —NHSO2—(C1-C4)alk or NHCO(C1-C4)alk; m and n are each independently 0, 1 or 2; R2 and R3 independently represent a hydrogen, a (C5-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy, hydrogen(C1-C4)alkoxy-(C1-C4)alkyl, mono- or di(C1-C4)alkamino(C1-C4)alkyl, pyrrolidino(C1-C4)alkyl, phenylamino or (C2-C4)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R4, an aralkyl or heteroaralkyl group optionally substituted with a group R4, R2 and R3 can also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C1-C4)alkyl, amino (C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, or a group —CO(C1-C4)alk or a group —NHSO2—(C1-C4)alk; a group (C1-C4)alk, a group (C1-C4)alkoxy, a halogen, —COOH, —COO(C1-C4)alk, —CN, —CONR3R4, —NO2, —SO2NH2 or —NHSO2(C1-C4)alk;

Abstract: This invention provides compounds of Formula I having the structure wherein: A, X, Y, Z, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

Abstract: The invention relates to novel compounds which are substituted amino-aza-cycloalkane derivatives of the general formula I. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of the plasmodium falciparum protease plasmepsin II or related aspartic proteases.