Abstract: A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and uses of the compound, particularly in antisense therapy.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of the enzyme myeloperoxidase (MPO) is beneficial. Certain novel compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof are disclosed, together with processes for their preparation. The compounds of formulae (Ia) and (Ib) are MPO inhibitors and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: An anti-inflammation substrate for decreasing the proinflammation induced by the cytokines and inhibiting the lung function degeneration is provided. The anti-inflammation substrate includes one selected from the group consisting of a 7-[2-[4-(2-chlorobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine, a 7-[2-[4-(4-nitrobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine, a respective pharmaceutical acceptable salt thereof, and a combination thereof.

Abstract: A substance for enhancing an aortic smooth muscle relaxation is provided. The substance is one selected from the group consisting of a compound of formula (I), a pharmaceutical acceptable therefrom and a solvate therefrom, wherein either of R1 and R2 is one of a hydrogen and a nitro group.

Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, non-insulin dependent diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g.

Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

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: For example, a representative compound of the invention is:

Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.

Abstract: The present invention relates generally to compounds of the formula (I): wherein: X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the formula (3):

Abstract: Disclosed are methods for making novel A2B adenosine receptor antagonists having the structure of formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl.

Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

Abstract: Disclosed are novel A2B adenosine receptor antagonists compounds having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

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: 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 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: 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: 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 usefull 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. In one embodiment, the invention features a compound of formula I: wherein: R3 is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from:  and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.

Abstract: A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and rises of the compound, particularly in antisense therapy.

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: 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. In one embodiment, the invention features a compound of formula I: R3 is an optionally substituted group selected from: and wherein X1, X2, Z, R1, R2, and R6 are as described in the specification.

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 1-diphenylmethyl-pyrazole derivatives 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: 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 compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: wherein R1, R13, X, Y, Z, G and Q are as defined herein.

Abstract: Compounds of the formula R1 and R2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R3 is hydrogen, alkyl of 1 to 6 carbon atoms, or cycloalkyl of 3 to 10 carbon atoms; and R4 is phenyl or naphthyl substituted with alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or NR5R6; substituted or unsubstituted phenylalkyl wherein the alkyl group contains 1 to 6 carbon atoms; substituted or unsubstituted 5 to 10 membered heteroaryl having 1 to 3 heteroatoms selected from N, S and O; substituted or unsubstituted cycloalkyl of 3 to 10 carbon atoms; or substituted or unsubstituted cycloalkylalkyl of 4 to 10 carbon atoms; provided that phenyl or naphthyl is substituted with NR5R6 when R1 and R2 is alkyl, are useful in the treatment of various disorders associated bone loss by increased transcription and elevation of plasma calcitonin levels.

Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.

Abstract: The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##

Abstract: The subject invention concerns a compound of the formula (i): ##STR1## in which Q represents heteroaryl or heterocyclo optionally substituted with one or more substituents selected from the group consisting of C.sub.1-6 alkyl (optionally substituted with one or more halogens), C.sub.1-6 alkyl--S(O)n-- (where n is 0, 1 or 2), --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), halogen, C.sub.1-6 alkoxy, CN, NO.sub.2 and NR.sub.7 R.sub.8;R.sub.1 -R.sub.5, which may be the same or different, each represent C.sub.1-6 alkyl (optionally substituted with one or more halogens), C.sub.1-6 alkyl--S(O)n-- (where n is 0, 1 or 2), --CO.sub.2 H (or C.sub.1-16 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), halogen, C.sub.1-6 alkoxy, CN, NO.sub.2, NR.sub.7 R.sub.8 or H (provided R.sub.1 -R.sub.6 are not all H simultaneously);R.sub.6 represents H, C.sub.1-6 alkyl, --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), --CN, C.sub.

Abstract: Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula:CORE MOIETY--(R).sub.jIn these compounds, j is an integer from one to three; the core moiety is a cyclic core, the cyclic core being non-cyclic or at least one five- to seven-member non-heterocyclic ring or heterocycle; and R is selected from the group consisting of amine, hydrogen, halogen, hydroxyl, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group or formula I. At least one R having formula I: ##STR1## In formula I, n is an integer from four to twenty; and each R.sub.1 or R.sub.2 is independently hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or cyclic or heterocyclic group.

Abstract: Disclosed are compounds having the formulae: ##STR1## wherein: Q.sub.3,Q.sub.6a,Q.sub.6b and Q.sub.8 are independently a bond, C.sub.1-8 alkylene, C.sub.2-8 alkenylene and C.sub.2-6 alkynylene, andR.sub.3, R.sub.6a, R.sub.6b, and R.sub.8 are independently hydrogen, aryl or heteroaryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided that:Q.sub.3 R.sub.3 is not hydrogen or methyl in formulae (I) or (II); and at least one of R.sub.3 and R.sub.8 is aryl or heteroaryl in formula (I).The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition.

Abstract: A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These compounds generally are useful in affecting drug metabolism and, particularly, in extending the circulating half-life of compounds that are metabolized via P-450-mediated pathways.

Abstract: The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.

Abstract: O.sup.6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR',wherein X is O or S, R" and R"' are alkyl, or substituted derivatives thereof,R' is H, or alkyl or hydroxyalkylR is(i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocylic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hereto atom chosen from O, N, or S, or a substituted derivative thereof; or(ii) naphthyl or a substituted derivative thereofand pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.A process for preparation of the compounds is described. The compounds have utility in combination with alkylating agents in the chemotherapeutic treatment of tumour cells.

Abstract: The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrogen; C.sub.1-4 alkyl; amino; substituted or unsubstituted thiol; and halogen. Moreover, R.sub.4 of Formula I is represented by the formula R.sup.12 -X.sup.12 wherein R.sup.12 is a saturated or unsaturated linear hydrocarbon chain of 5-20 carbons optionally containing one or more interruptions within the chain by a heteroatom, and optionally substituted with one or more .dbd.O, or .dbd.S. Finally, X.sup.12 is selected from the group consisting of hydroxy, an aminoalkyl group, and a known amino acid bound by its .alpha.

Abstract: Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase.

Abstract: 1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition.

Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.

Abstract: The present invention relates to novel xanthine derivatives of the formula (I) which are selectively antagonistic to an adenosine A.sub.2 receptor, and pharmaceutically acceptable salts thereof. Formula (I): ##STR1## In the formula, R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom, a propyl group, a butyl group or an allyl group; R.sup.3 represents a hydrogen atom or a lower alkyl group; Y.sup.1 and Y.sup.2 are the same or different and each represents a hydrogen atom or a methyl group; and Z represents a substituted or unsubstituted phenyl group, a pyridyl group, an imidazolyl group, a furyl group or a thienyl group.

Abstract: This invention is directed to purine derivatives of the following formulae: ##STR1## wherein Z.sup.1 is --O--, --N(R.sup.10)-- or --CH.sub.2 O--;Z.sup.2 is --O--, --N(R.sup.10)-- or --OCH.sub.2 --;R.sup.1 and R.sup.4 are each independently hydrogen, halo, alkyl, --OR.sup.10, --C(O)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --N(R.sup.10)C(O)R.sup.10, or --N(H)S(O).sub.2 R.sup.13 ;R.sup.2 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(NH)N(H)C(O)OR.sup.13, --C(NH)N(H)C(O)R.sup.10, --C(NH)N(H)S(O).sub.2 R.sup.13, or --C(NH)N(H)C(O)N(H)R.sup.10 ;R.sup.3 is halo, alkyl, haloalkyl, haloalkoxy, ureido, cyano, guanidino, --OR.sup.10, --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --R.sup.12 --C(O)N(R.sup.10)R.sup.11, --CH(OH)C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --R.sup.12 --N(R.sup.10)R.sup.11, --C(O)OR.sup.10, --R.sup.12 --C(O)OR.sup.10, --N(R.sup.10)C(O)R.sup.