Abstract: The present invention relates to a semi-hydrochloride of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid, to processes for its preparation and to antibacterial compositions comprising it. The semihydrochloride of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.

Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2–C6 alkyl, and R5 and R6 are each independently H or C1–C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.

Abstract: The present invention relates to a new process for preparing beta-ketoester compound of the following formula (1), which is a useful intermediate for the synthesis of such quinoline antibiotics as Ciprofloxacin, Levofloxacin, Gemifloxacin, Trovafloxacin, etc. The quinoline antibiotics obtained from the above compound of formula (1) show potent antibacterial activity, and so are advantageously used as a therapeutic agent for bacterial infections of humans or animals.

Abstract: The present application describes novel cyclic ?-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease and/or as TNF-? inhibitors.

Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.

Abstract: A process for preparing 4-haloalkylnicotinic esters of the formula (I), where RF is (C1-C4)-haloalkyl and R is (C1-C6)-alkyl; which comprises a) reacting an aminoketone of the formula (II), RF—C(O)—CH?CH—NH2 ??(II) ?in a condensation reaction under reduced pressure with a compound of the formulae (III) to (V), (R1Z)CH?CH—COOR??(III), (R1Z)2CH—CH2—COOR??(IV), HC?C—COOR??(V), where R1 is (C1-C6)-alkyl and Z is O, S, NR1 or C(O)O, ?to give a compound of the formulae (VI) and/or (VII), RF—C(O)—CH?CH—NH—CH?CH—COOR??(VI) RF—C(O)—CH?CH—NH—CH(ZR1)—CH2—COOR??(VII) b) and subjecting the reaction product to a ring closure reaction.

Abstract: The present invention relates to an excellent remedial agent for chronic rheumatoid arthritis, comprising an aminostilbazole derivative represented by the following formula [1] or a salt thereof as an active ingredient: A-B-D-E??[1] Wherein A represents heteroaryl or an oxide thereof, B represents ethenylene, D represents phenylene, E represents the formula: —N(R)SO2—G [wherein G represents phenyl, R represents hydrogen, alkyl, or —COR0 (R0 represents alkyl, alkoxy, aryloxy, 5- to 6-membered heteroaryl, heteroarylmethyl, aminoalkylene or cyclicaminoalkylene) or the like].

Abstract: The invention provides processes for preparing N-protected ?-amino aldehyde compounds which are useful as synthetic intermediates for preparing glycopeptide antibiotic derivatives. The processes include cleaving a carbon-carbon double bond to form the N-protected ?-amino aldehyde compound.

Abstract: A process for the preparation of methyl 2-(3-chloropropoxy)-indole-3-carboxylate, which comprises reacting a 3-chloro-3-carboxylate indole compound with 3-chloropropanol in the presence of an acid having a pKa of from 0 to 2.

Abstract: There is provided a process for the preparation of 3-cyano-6-alkoxy-7-nitro-4-quinolone intermediates useful for the preparation of protein tyrosine kinase (PTK) inhibitors which are useful in the treatment of cancer of the formula: wherein R is alkyl(C1-C3) prepared by reacting a substituted anthranilate with N,N-dimethylformamide dimethyacetal to obtain a N,N-dimethylamidine which is condensed with t-butylcyanoacetate to obtain a N-(2-cyano-2-t-butoxycarbonylvinyl)anthranilate, which is hydrolyzed to yield a N-(2-cyano-2-carboxyvinyl)anthranilate followed by decarboxylating to obtain a N-(2-cyano-2-carboxyvinyl)anthranilate followed by cyclizing to obtain a 3-cyano-6-alkoxy-7-nitro-4-quinolone.

Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Abstract: A process comprising reacting compound GF-I with a reducing agent to form compound GF-II wherein Y is selected from the group consisting of H, benzyl, substituted benzyl, CH2OC1-8 alkyl, CH2OC3-8 cycloalkyl, allyl, tetrahydropyranyl, tetra-hydrofuranyl, substituted tetrahydropyranyl, substituted tetra-hydrofuranyl, Si(C1-4 alkyl)3, and Si(Ph)x(C1-4 alkyl)3-x where x is equal to 1, 2 or 3; and wherein said process is conducted: (a) in the presence of a reducing agent; (b) in the presence of an aprotic solvent; and (c) under reaction conditions; is provided.

Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: Novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.

Abstract: Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO2—, —N(R3)C(O)O— or —N(R3)CON(R3a)—; and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of a 4 integrins to their ligands and are of use in the prophylaxis and treatment of diseases or disorders involving inflammation.

Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, Z and R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2??I in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; ?where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from 1 to 5 halogen atoms and/or

Abstract: A new method is described here for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide comprising the following steps: a) (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with formic acid to give the compound of formula: b) the compound thus obtained is reacted with tert-butylamine to give the compound of formula: c) the compound thus obtained is then treated with acids to give the desired compound. The method in question makes it possible to obtain (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide with high yields and purity without using toxic and hazardous reagents.

Abstract: The present invention relates to compounds of the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X and Y are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.