Abstract: In one aspect, the invention relates to binary compositions that disrupt ORco-mediated odorant sensing. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in organisms that express ORco receptors such as airborne insects, e.g., mosquitos, and ticks. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.

Abstract: A compound of the formula I where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as pesticidal agents.

Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: A compound of the formula I or where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as as pesticidal agents.

Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

Abstract: A compound of Formula (I) or Formula (II) where W is C—R3; X is C—R4; Y is C—R5; R1 and R6, independently of each other, is, for example, H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl or C1-C6-alkyl-C(?O); R2 is H; and R3, R4 and R5, independently of each other, are, for example, H, halogen, cyano, nitro, C1-C6-alkyl, or C1-C6-haloalkyl; provided that in formula II R1 is H and R6 is as defined above; and in formula I that (a) at least one of R1 and R3 to R6 is other than hydrogen, (b) R3 or R4 is other than C1 when in each instance the remaining five groups of R1 to R6 are hydrogen, and (c) (i) R3 is other than methyl, (ii) R4 is other than C1, (iii) R5 is other than C1 and (iv) R3 is not C1 when R5 is methoxy, when in each instance (i) to (iv) R1 is H, R6 is MeC(?O), and remaining groups of R2 to R5 are hydrogen; and/or salts thereof; and their use as as pesticidal agents.

Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.

Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.

Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.

Abstract: The invention provides 3-amino-1,2-benzisothiazole compounds of formula (I) wherein n, R1, R2, R3, R4 and A are defined as in the description.

Abstract: The present invention relates to 3-amino-1,2-benzisothiazole compounds of formula I wherein R1, R2, R3, R4, R5 and n are defined in the description. The present invention relates to insecticidal compounds of formula I and to their isomeric imino derivatives, as well as to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the 3-amino-1,2-benzisothiazole compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds.

Abstract: A compound of the formula I or where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as as pesticidal agents.

Abstract: A compound of Formula (I) or Formula (II) where W is C—R3; X is C—R4; Y is C—R5; R1 and R6, independently of each other, is, for example, H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl or C1-C6-alkyl-C(?O); R2 is H; and R3, R4 and R5, independently of each other, are, for example, H, halogen, cyano, nitro, C1-C6-alkyl, or C1-C6-haloalkyl; provided that in formula II R1 is H and R6 is as defined above; and in formula I that (a) at least one of R1 and R3 to R6 is other than hydrogen, (b) R3 or R4 is other than C1 when in each instance the remaining five groups of R1 to R6 are hydrogen, and (c) (i) R3 is other than methyl, (ii) R4 is other than C1, (iii) R5 is other than C1 and (iv) R3 is not C1 when R5 is methoxy, when in each instance (i) to (iv) R1 is H, R6 is MeC(?O), and remaining groups of R2 to R5 are hydrogen; and/or salts thereof; and their use as as pesticidal agents.

Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.

Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.

Abstract: The present invention relates to 3-amino-1,2-benzisothiazole compounds of formula I wherein R1, R2, R3, R4, R5 and n are defined in the description. The present invention relates to insecticidal compounds of formula I and to their isomeric imino derivatives, as well as to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the 3-amino-1,2-benzisothiazole compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds.

Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11beta-hydroxylase (CYP11B1), and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase and/or CYP11B1. Finally, the present invention also provides a pharmaceutical composition.

Abstract: The invention provides 3-amino-1,2-benzisothiazole compounds of formula (I) wherein n, R1, R2, R3, R4 and A are defined as in the description.

Abstract: Compounds having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein L, A, G, R1, R2 and R3 are as defined herein. These compounds are particularly useful in the treatment of pain, inflammatory hyperalgesia, and urinary dysfunctions, such as bladder overactivity and urinary incontinence.

Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.

Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.

Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

Abstract: The invention relates to new compounds, 3-phenylpropionic acid derivatives of formula (I) wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; X represents O, S, NH, N—C1–C10-alkyl, N-aryl, NSO2—C1–C10-alkyl, N—SO2-aryl, or N—SO2-heteroaryl; R1 to R8 each independently represents hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: The present invention relates to new and useful processes for the preparation of the anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride.

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: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.

Abstract: The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2 is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5.

Abstract: The invention relates to compounds of the formula 1 1

Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

Abstract: A compound of formula (I), where A is optionally substituted alkylene, alkenylene, alkynylene, cycloalkylene, alkylenoxy, oxy(C1-6)alkylene, alkylenthio, thio(C1-6)alkylene, C1-6alkylenamino, amino(C1-6)alkylene, [C1-6alkyleneoxy(C1-6)alkylene], [C1-6alkylenethio(C1-6)alkylene], [1-6alkylenesulfinyl(C1-6)alkylene], [C1-6alkylenesulfonyl(C1-6)alkylene] or [C1-6alkyleneamino(C1-6)alkylene]; provided that A is not CH2 or CH2O; B is N,N-oxide or CR8; Y is O, S or NR9; Z is O, S or NR10; and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 are specified radicals; compositions containing them; process for making them; and their use as insecticides or fungicides.

Abstract: The present application describes aryl sulfonyls of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa inhibitors.

Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) in which F1, F2, G, V, W, X, Y, Z and m are each as defined in the description, to processes for their preparation and to their use in agriculture, for example as crop protection agents (fungicides, herbicides and insecticides).

Abstract: A compound of formula (I), where A is optionally substituted alkylene, alkenylene, alkynylene, cycloalkylene, alkylenoxy, oxy(C1-6)alkylene, alkylenethio, thio(C1-6)alkylene, C1-6alkylenamino, amino(C1-6)alkylene, [C1-6alkyleneoxy(C1-6)alkylene], [C1-6alkylenethio(c1-6)alkylene], [1-6alkylenesulfinyl(c1-6)alkylene], [c1-6alkylenesulfonyl(C1-6)alkylenc] or [C1-6alkyleneamino(C1-6)alkylene]; provided that A is not CH2 or CH2O; B is N, N-oxide or CR8; Y is O, S or NR9; Z is O, S or NR10; and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 are specified radicals; compositions containing them; processes for making them; and their use as insecticides or fungicides.

Abstract: The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: 1

Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1

Abstract: The invention relates to hydrochloride, hydrobromide, hemi-citrate, acetate, p-tosylate, L-tartrate, hemi-succinate, and mesylate salt forms of 3-(4-bromo-2,6-difluoro-benzyloxy)-5-[3-(4-pyrrolidin-1-yl-butyl)-ureido]-isothiazole-4-carboxylic acid amide having the following formula: 1

Abstract: 1 A compund of formula (I) wherein X is O or S; n is 0 or 1; Y is O, S or NR7; R1 is hydrogen, halogen, C1-6 aklyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 haloalkylthio, C3-6 cycloalkyl, C1-6 alkoxy(C1-6)alkyl or SF5, R2 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylthio, C1-6 haloalkylthio, C1-6 alkylsulfinyl, C1-6 haloalkylsulfinyl, C1-6 alkylsulfonyl, C1-6 haloalkylsulfonyl, C1-6 haloalkyl, cyano, nitro, CHO, CH═NOR5, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl or SF5; or together R1 and R2 form a five or six membered saturated or unsturated carbocyclic ring, optionally substituted processes for preparing these compounds, compositions comprising them, methods of using them to combat fungal diseases and methods of using them to combat or control insect, acarine, mollusc and nematode pests.

Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.

Abstract: The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one, pharmaceutical compositions containing said ziprasidone mesylate dihydrates, and methods of adminsitering the ziprasidone mesylate dihydrates to treat psychotic diseases.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful or the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.