Abstract: Disclosed herein are a process for producing mixed crystals of disodium 5′-guanylate and disodium 5′-inosinate which comprises precipitating mixed crystals of disodium 5′-guanylate and disodium 5′-inosinate (I+G mixed crystals) by adding an aqueous mixed solution of disodium 5′-guanylate and disodium 5′-inosinate and a hydrophilic organic solvent at the same time into a crystallization vessel in such manner that the ratio of the hydrophilic organic solvent to the liquid phase in the crystallization vessel is maintained in a range of 30 to 70 vol %, as well as such process for producing I+G mixed crystals wherein said producing of I+G mixed crystals is carried out by seeding crystallization wherein crystals of 5′-IMP2Na or/and I+G mixed crystals are used as seed crystals.

Abstract: The present invention provides compounds of formula I 1

Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract: The present invention is directed to a compound represented by the following formula (1) and to a process for producing a compound (5) from the compound (1).

Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.

Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.

Abstract: The present invention relates to substituted xanthines of general formula 1

Abstract: The invention relates to new purine derivatives of general formula 1

Abstract: The present invention relates to substituted xanthines of general formula 1

Abstract: Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.

Abstract: The present invention relates to substituted xanthines of general formula 1

Abstract: The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect.

Abstract: The present invention relates to substituted xanthines of general formula 1

Abstract: The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): 1

Abstract: Chiral peptide nucleic acids are provided which hybridise strongly with complementary nucleic acids and have potential as antigene and antisense agents and as tools in molecular biology. The compounds have the formulae. where n is 1 to 200, B is a protected or unprotected base, X may be OH, Y may be H, and R′ and R″, which are the same or different, are H, C1-C6 alkyl, aryl or aralkyl or R′ or R″, together the carbon atoms to which they are attached, form a cycloalkyl ring and protected derivatives thereof.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Methods of and compositions for pulmonary delivery of therapeutic agents which are capable of forming covalent bonds with a site of interest or which have formed a covalent bond with a pulmonary solution protein are disclosed. Therapeutic agents useful in the invention include wound healing agents, antibiotics, anti-inflammatories, anti-oxidants, anti-proliferatives, immunosupressants, anti-infective and anti-cancer agents.

Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) 1

Abstract: A compound of formula (I) 1

Abstract: The present invention relates to methods of treating periodontal disease.

Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I 1

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.

Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.

Abstract: The present invention relates generally to compounds of formula (IA): (IA) 1

Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

Abstract: Compounds of the theophylline and 3-isobutyl-1-methylxanthine (IBMX) based on N-7 substituted derivatives, X being florine, chlorine, bromine or iodine, are provided. These compounds possess pharmacologically inhibitory activities on PDE-5 Phosphodiesterase, relaxation of corpus carvernosal smooth muscle and increase of intracarvernosal pressure (&Dgr;ICP). A process is also provided for the synthesis of some novel theophyline derivatives.

Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. The present inhibitors are novel purine derivatives, attached at position 8 of the purine skeleton to a diamine.

Abstract: Various substituted nitrogen heterocyclic derivatives and their pharmaceutically acceptable salt derivatives are provided for use as medicaments, and particularly, as antimitotic, anti-viral, anti-cancer, anti-degenerative, immunosuppressive, and anti-microbial drugs or, vaccines. These heterocyclic derivatives can be used as an active agent in a pharmaceutical, as well as a diagnostic utility. To this end, several families of heterocyclic derivatives are provided including pyrrolopyrimidines, pyrazolopyrimidines, purines, and imidazopyridines. In particular, certain tri-substituted and tetra-substituted purines and pyrazolopyrimidines and their deaza analogues are provided for inhibiting cyclin-dependent kinase (“cdk”) proteins, viruses, and immunostimulation.

Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.

Abstract: Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided.

Abstract: The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally containing one or more heteroatoms selected from 0, N or S; k represents 0 or 1; n represents an integer of 1 to 50; X represents —O—, —N(H)—, —N(C1-6alkyl)-, —N(C3-8cycloalkyl)-, —N(C1-8alkyl)(C3-8 cycloalkyl), —N[(CH2CH2O)m(C1-12 alkyl, aryl, or aralkyl)]-, —CH2O—, —CH2NH—, —CH2N(C1-6alkyl)-, —CH2N(C3-8cycloalkyl)-, or —C1-12alkyl-; Q represents (—CH2)p, (—CH═CH—)p, (—C≡C—)p, (—(O)p1CH2—)p or (—CH2(O)p1)p R6 and R7 independently represent O or S; and all other variables are as defined herein; processes for their preparation, pharmaceutical formulations containing them, and their use in me

Abstract: Compounds represented by the formula 1: 1

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Disclosed are compounds of the formula

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: 1

Abstract: The present invention provides compounds having the formula I: X is (C1-C8)alkylene, (C2-C8)alkenylene, (C2-C8)alkynylene, wherein one of the carbon atoms in the alkylene, alkenylene or alkynylene groups is optionally replaced with a group having the formula —O—, —N(R4)C(O)—, —OC(O—, S—, —S(O)—or —SO2—, or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising compounds having the formula I. The compounds of the invention are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents for treatment of diseases that are mediated by A2B adenosine receptors.

Abstract: The present invention relates to novel compounds of formula (I): processes for their preparation, pharmaceutical formulations containing them, and their use in medicine, particularly in the prophylaxis and treatment of inflammatory conditions, immune disorders, septic shock circulatory disorders, and gastrointestinal inflammation and disorders.

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Abstract: Novel piperidinyl compounds substituted in the 1- and 4-positions are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: Therapeutic oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. Replacement of phosphorodiester inter-sugar linkages found in wild type oligomers with four atom linking groups forms unique di- and poly-nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.

Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: 1

Abstract: Disclosed are compositions inducing cleavage of an RNA substrate, as well as their use for inducing cleavage of RNA substrates in vitro and in vivo. The compositions contain part of an active center, with the other part of the active center provided by the RNA substrate. The subunits of the active center region of the compositions are nucleotides and/or nucleotide analogues. The disclosed compositions also have flanking regions contributing to the formation of a specific hybridization with an RNA substrate. Preferred compositions form, in combination with an RNA substrate, a structure resembling a hammerhead structure. The active center of the disclosed compositions is characterized by the presence of I15.1 which allows cleavage of RNA substrates having C16.1.

Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity, as well as methods for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity

Abstract: A purine derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y1)—D, where Y1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring and has two nitrogen atoms in the six-membered ring. The moiety A can be a purine moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.

Abstract: The invention provides methods for solution-phase synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.