Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.

Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.

Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.

Abstract: This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain and respiratory conditions.

Abstract: This disclosure describes solid forms of the compound of Formula (I) and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain.

Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.

Abstract: Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures 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: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

Abstract: A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.

Abstract: A series of monoquarternary piperazium salts including a structure of a formula I or II are provided. In formula I or II, R1, Ra, and RX are as defined in the specification. The monoquarternary piperazium salt of KMUP or piperazine disclosed in the present invention is characterized by being presented in a pro-drug form and having various pharmaceutical functions.

Abstract: The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.

Abstract: The present invention provides solid state forms of Linagliptin, processes for preparing the solid state forms, and pharmaceutical compositions thereof.

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

Abstract: The synthesized piperazium salt of KMUPs disclosed in the present invention is characterized by presented pharmaceutics having functions to improve 5-HT function and eNOS expression of KMUPS in lung diseases, such as proliferation, obliteration, pulmonary artery hypertension. The pharmaceutical composition for inhibiting monocrotaline (MCT)-induced proliferation of pulmonary artery includes an effective amount of a complex salt of formula (I): wherein R2 and R4 are each selected independently from the group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group, and a halogen atom; RX contains a carboxylic group donated from one selected from a group consisting of a Statin, a Co-polymer, a poly-?-polyglutamic acid (?-PGA) derivative and sodium CMC; and ?RX substituent is an anion of the carboxylic group carrying a negative charge; and a pharmaceutically accepted carrier.

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.

Abstract: The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3—CH2—X-A-R1, and L2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.

Abstract: A pharmaceutical composition for improving a cardiac function is provided. The pharmaceutical composition comprises an effective amount of an active component being one of a KMUP-3 compound and a salt thereof.

Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected from the group consisting of oxazoyl, isoxazoyl, thiazolyl, and isothiazoyl; and Z1 is a 5-14 member substituted or unsubstituted heteroaryl ring; which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists of the formula: wherein R1 and R2 are independently lower alkyl; R4 is optionally substituted phenyl; X is hydrogen or methyl; and Y is —C(O)R, in which R is optionally substituted aryl or optionally substituted heteroaryl or a pharmaceutically acceptable salt thereof, and their use in treating mammals for various disease states.

Abstract: The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazol-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a pharmaceutically acceptable salt thereof, corresponding pharmaceutical formulations, combinations, preparation methods and methods or uses in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: This invention relates to a diagnostic probe comprising a compound of formula (I): such as 3-[2-[4-(5-aminopentyl-3-amidocarboxypropanoyl)]aminophenyl]ethyl]-8-benzyl-7-[2-ethyl(2-hydroxyethyl)amino]ethyl-1-propylxanthine, with one or more label moieties attached thereto. The compounds of the present invention are useful as diagnostic probes, including probes for diagnostic assays and imaging. Accordingly, the invention provides A1 adenosine receptor antagonist compounds with radioactive or non-radioactive labels suitable for executing such assays and imaging measurements. Labeled compounds are useful to obtain quantitative measurements of the A1 adenosine receptor antagonist compounds. They may be employed as an imaging agent in diagnostic procedures such as MRI and PET as well as cell or receptor based assays.

Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.

Abstract: There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.

Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, and their use in treating mammals for various disease states.

Abstract: A series of monoquarternary piperazium salts including a structure of a formula I or II are provided. In formula I or II, R1, Ra, and RX are as defined in the specification. The monoquarternary piperazium salt of KMUP or piperazine disclosed in the present invention is characterized by being presented in a pro-drug form and having various pharmaceutical functions.

Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof where X is a leaving group selected from halogens and sulphonic ester acid residues, and R1 to R3 are as defined herein, to obtain a compound of the formula (II) and deprotecting the obtained compound of the formula (II) to obtain the product xanthines.

Abstract: The invention relates to compounds of formula 1 wherein R1-R2 is a guanine derivative; X is oxygen or sulfur; R3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH2; R4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R4 to R1 forming a cyclic substrate, or a further group —R3—CH2—X—R1-R2. The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O6-alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.

Abstract: Provided herein are small molecule conjugates that are agonists or antagonists of one or more toll-like receptors.

Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.

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, 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: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial

Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial

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

Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures 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: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.

Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structure and their use in treating mammals for various disease states.

Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI. The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).

Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: A variety of N-substituted derivatives are based upon the base chemicals of that provide for the induction of cavernosal relaxation in animals. R2 is a derivative based on a hetroaromatic group, an aromatic group or a cyclohexane.

Abstract: The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures 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: The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the mixtures 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: The application relates to new substituted xanthines of general formula wherein R1 and R2 are defined as in claims 1 to 11, the tautomers, the enantiomers, the diastereomers, the mixtures 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: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R2 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation and calcitonin-induced osteoporosis using these compounds.