Abstract: Novel cycloalkane carboxamide derivatives having an action that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkane carboxamide derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein R1 and R2 represent (substituted) alkyl groups, (substituted) alkenyl groups, (substituted) alkynyl groups, (substituted) aromatic hydrocarbon groups or (substituted) heterocyclic groups, ring A represents an alkylidene group having 5 to 7 carbon atoms, and ring B represents a formyl group or a hydroxymethyl group).

Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions: (I)

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

Abstract: The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted.

Abstract: The present invention relates to heteroaroyl-substituted alanines of the formula I in which the variables A and R1 to R7 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.

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, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract: The present invention relates to novel, non-secosteroidal, phenyl-furan compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii) an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: Difunctional aromatic diamines (e.g. Ethacure® 100 and 300) are derivatized with furan-2,5-dicarboxylic acid (FDCA) to form FDCA-derived bisamides; the derivatives have enhanced curative properties when used as curatives for polyureas, hybrid epoxy-urethanes, hybrid urea-urethanes, chain extenders for polyurethane and polyurea elastomers, and also for reaction injection molding (RIM) products.

Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii)an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.

Abstract: Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.

Abstract: New polyols; oligomers, and polymers made from the polyols; and binders made from the new polyols, oligomers, or polymers that can be used in binders, where the binders typically include one or more polyols, and a polyfunctional acid or a polyfunctional nitrile.

Abstract: The present invention relates to the use of compounds of the general Formula (1): wherein in Formula (1), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.

Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.

Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.

Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN? is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and the other of RP3

Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.

Abstract: The present invention relates to furancarbonylguanidine derivatives, a preparation method thereof and a pharmaceutical composition comprising the same. Furancarbonylguanidine derivatives of the present invention inhibit NHE-1 (sodium-hydrogen exchanger isoform 1), which helps recovery of heart function damaged from ischemia/reperfusion and decreases myocardial infarction rate, indicating that they have protective effect on myocardial cells. Thus, furancarbonylguanidine derivatives of the present invention can be effectively used for the prevention and the treatment of ischemic heart diseases such as myocardial infarction, arrhythmia, angina pectoris, etc, and also a promising candidate for a heart protecting agent applied to reperfusion therapy including thrombolytics or cardiac surgery including coronary artery bypass graft, percutaneous transluminal coronary angioplasty, etc.

Abstract: The invention relates to novel carboxamides of formula (I), in which M represents a phenyl ring, pyridine ring or pyrimidine, pyridazine or pyrazine ring, respectively monosubstituted by R8, or represents a thiazole ring substituted by R8-A; R8 represents hydrogen, fluorine, chlorine, methyl, isopropyl, methylthio or trifluoromethyl; R8 can also represent methoxy; R8-A represents hydrogen, methyl, methylthio or trifluoromethyl; L1 represents C1-C10 alkene (alkanediyl); Q represents O, S, SO, SO2 or NR9; L2 represents a direct bond, SiR10R11 or CO; R represents hydrogen, C1-C8 alkyl, C1-C8 alkoxy, C1-C4 alkoxy-C1-C4-alkyl, C1-C4 alkylthio-C1-C4-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 haloalkyl, C2-C6-haloalkenyl, C2-C6 haloalkynyl or C3-C6 cycloalkyl; A represents the group of formula (AI); the remaining substituents are defined in claim 1.

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, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

Abstract: This invention relates to novel furancarboxamides of the formula (I) in which R, R1 and m are as defined in the disclosure, to a plurality of processes for preparing these substances and to their use for controlling unwanted micro-organisms.

Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: Compounds of the formulae IA and Ib. in which X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel antiarrhythmic active compounds, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.

Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.

Abstract: A novel compound which inhibits certain integrins, particularly ?v integrins. Additionally, the novel compound may be used in a method of treating tumors or cancer which comprises administering a pharmaceutically effective amount of the compound to a patient. Additionally, the novel compound may be used in a method of inhibiting angiogensis. Finally, a method of producing the novel compound is disclosed.

Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: The method for producing N-alkoxy-N-alkylamides of general formula (I): wherein R1 represents C1-10-alkyl, cyclo-C5-7-alkyl, cyclo-C5-7-alkenyl, C2-10-alkenyl, aryl, aryl-C1-3-alkyl, heteroaryl, heteroaryl-C1-3-alkyl or heterocyclyl; and R2 represents C1-6 alkyl. In the process, an ester of general formula (II): R1COOR3, wherein R1 has the above-mentioned meaning, and R3 represents C1-6-alkyl, 4-nitrophenyl, 2,4-dinitrophenyl, succinimido or benzotriazole-1-yl, is reacted with hydroxylamine, a hydroxylamine derivative or with a hydroxylammonium salt, and the reaction product is alkylated in the presence of a phase transfer catalyst.

Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.

Abstract: Disclosed is a method of preparing an optically pure (R)- or (S)-tetrahydrofuranyl ketone. By such a method, (R)- or (S)-2-tetrahydrofuran amide is converted to (R)- or (S)-2-tetrahydrofuran nitrile through dehydration in the presence of a dehydrating agent and an amine base. Then, thus prepared (R)- or (S)-2-tetrahydrofuran nitrile is nucelophilic addition-reacted with a nucleophile, followed by hydrolyzing, thereby produce (R)- or (S)-tetrahydrofuranyl ketone having high optical purity, while minimizing production of other by-products.

Abstract: A compound of formula Id and pharmaceutically acceptable salts and esters thereof, wherein the substituent designations are as provided in the specification. Compounds of the invention are useful for treating reperfusion injury.

Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.

Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.

Abstract: Crystalline particles of escitalopram oxalate with a particle size of at least 40 &mgr;m is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.

Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.