Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.

Abstract: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.

Abstract: Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an active ingredient, and processes for the preparation thereof.

Abstract: The invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the spiro-piperidine head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, methods for preparing the compounds and pharmaceutical compositions, and their use in the treatment of dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders.

Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.

Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.

Abstract: The invention provides a compound of formula (I), wherein: T is C(O) or S(O)2; W is C(O) or S(O)2; X is CH2, O or NH; Y is CR5 or N; R1 is optionally substituted aryl or optionally substituted heterocyclyl; R2 is hydrogen or C1-6alkyl; R3 is hydrogen or optionally substituted C1-6alkyl; and R4 is alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds comprising saturated heterocycles coupled to a fused ring system.

Abstract: Substituted phenylalkynes of formula (I) compositions containing them and their methods of use to treat histamine related disorders are described, wherein R1, R2, R3, R4, R5 and n are as defined.

Abstract: Disclosed are novel 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: Compounds of formula (I) in which R1, R2 and X4 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.

Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.

Abstract: The invention provides a compound of formula (I): T is C(O) or S(O)2; W is CH2, (CH2)2, CH(CH3), CH(CH3)O or cyclopropyl; X is O, CH2, C(O), S, S(O), S(O)2 or NR3; m is 0 or 1; R1 is optionally substituted aryl or optionally substituted heterocyclyl; R2 is alkyl (optionally substituted by OH), cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.

Abstract: Novel diaminothiazoles of formula (I): are discussed. These compounds selectively inhibit the activity of Cdk4 and are thus useful in the treatment or control of cancer, in particular, the treatment or control of solid tumors. This invention also provides pharmaceutical compositions containing such compounds and methods of treating or controlling cancer, most particularly, the treatment or control of breast, lung, colon, and prostate tumors.

Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, cycloalkyl(C1–C6 alkyl)- or aryl(C1–C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.

Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:

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

Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds 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, diabetes, and myocardial infarction.

Abstract: The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2–10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel, thereby modulating the biological activities thereof.

Abstract: Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.

Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as

Abstract: The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q?, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C?O, NHC(?), and C(?O)NH, and Q? is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.

Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?

Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.

Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C1–C8-alkyl optionally substituted by cyano or halogen, Ar2 is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy or C1–C8-alkoxycarbonyl, R1 is C1–C8-alkyl substituted by hydroxy, C1–C8-alkoxy, acyloxy, —N(R2)R3, halogen, carboxy, C1–C8-alkoxycarbonyl, phenyl-C1–C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R?3 are each independently hydrogen or C1–C8-alkyl, or R2 is hydrogen and R3 is acyl or SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen, C1–C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1–C8-alkyl, halogen, cyano or C1–C8-alkoxy, or R4 and R5 toge

Abstract: The invention relates to sulfonyl amine derivatives of formula IA wherein R5A, X1, X2, R9 and R10 are as defined herein, which derivatives are useful as bradykinin B1 receptor antagonists.

Abstract: The invention concerns amide derivatives of Formula (I), wherein R3 is (1-6C)alkyl or halogeno; m is 1-3 and R1 is selected from substituents such as: (A) hydroxy, halogeno, (1-6C)alkyl, (1-6C)alkoxy, aryl, heteroaryl and heterocyclyl; and (B) di-[(1-6C)alkyl]amino-(1-6C)alkyl, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, aryloxy, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 is aryl or cycloalkyl which bears 1-3 substituents such as: (C) hydrogen, hydroxy, halogeno and heterocyclyl; and (D) heteroaryl-(1-6C)alkoxy and heterocyclyl-(1-6C)alkoxy, provided that a substituent on R4 is selected from paragraph (C) only if at least one R1 group is selected from paragraph (B); processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

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: The present invention relates to bicyclic heterocyclic groups of general formula wherein Ra, Rb, Rc, Rd and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostate hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.

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

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: This invention relates to the (R)-isomers of compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: wherein p, R1, R2, R3 and A are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.

Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1

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

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell poliferation.

Abstract: The present invention relates to substituted indole derivatives of formula I wherein R1 is hydrogen or optionally substituted C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl or C3-8-cycloalkyl-C1-6-alkyl, or R1 is optionally substituted aryl, aryl-C1-6-alkyl, heteroaryl, heteroaryl-C1-6-alkyl or R1 is —NR′R″ wherein R′ and R″ are independently selected from hydrogen and optionally substituted C1-6-alkyl, aryl, aryl-C1-6-alkyl, heteroaryl and heteroaryl-C1-6-alkyl, or R1 is a saturated or partially saturated 5- to 6-membered ring containing one, two or three hetero atoms selected from O or S, and a group N—R9 wherein R9 is hydrogen or optionally substituted C1-6-alkyl; R2 is C1-6-alkyl W, n, X, R3-R8 are as defined in the description. The compounds of the invention are potent dopamine D4 ligands.

Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.

Abstract: The present invention relates to a phenoxypropylamine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof or a pharmaceutically acceptable salt thereof and hydrates thereof, which simultaneously show selective affinity for and antagonistic activity against 5-HT1A receptor, as well as 5-HT reuptake inhibitory activity, and can be used as antidepressants quick in expressing an anti-depressive effect.

Abstract: A chromene compound which develops yellow to red color, a high color density and a little initial color and which, when used in combination with an existing photochromic compound that exhibits blue color so as to develop a neutral tint, maintains uniformity in the color tone at the time of developing color or fading color, or exhibits a very large color fading rate.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1

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.