Abstract: The invention describes compositions and kits comprising at least one organic nitric oxide enhancing salt of an angiotensin ? antagonist, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: The present invention relates to a process for producing an alkoxy-(tetrazol-1-yl)benzaldehyde compound represented by Formula (2): wherein A1 is an alkoxy group, and A2 is a hydrogen atom, alkyl group or fluorine-substituted alkyl group, the process comprising reacting a 1-(alkoxyphenyl)-1H-tetrazole compound represented by Formula (1): wherein A1 and A2 are as defined above, with hexamethylenetetramine in a sulfonic acid solvent, followed by hydrolysis. According to the present invention, an alkoxy-(tetrazol-1-yl)benzaldehyde compound can be safely and efficiently produced by formylating a 1-(alkoxyphenyl)-1H-tetrazole compound.

Abstract: New form of irbesartan having favourable chargeability is prepared from the alcoholic/etheric or ketonic solution of irbesartan after slow cooling with sporadic or light agitation and alternatively new crystalline form of an acid addition salt of irbesartan is prepared from the aqueous solution of a sodium salt of irbesartan after strongly acidifying aforesaid solution and subsequently adjusting pH with an alkali. Those are used in manufacturing a pharmaceutical composition.

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof, and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.

Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention provides the preparation of olmesartan medoxomil containing less than about 0.1% of one or more of the impurities OLM-Me, OLM-Cl, and OLM-eliminate.

Abstract: The invention relates to a new process for the preparation of sartans 2-butyl-3-[[2?-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1?-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one is disclosed, which proceeds via novel intermediate, 4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]phenylboronic acid (Formula (II)) or its analogs. Compound (II) reacts with 5-(2-bromophenyl)-1-(triphenylmethyl)-1H-tetrazole (III) in the presence of catalyst, using conditions of Suzuki reaction, to give trityl irbesartan (I), whereas analogs to compound (II) may give candesartan, valsartan, telmisartan, losartan and olmesartan.

Abstract: Methods, composition, and intermediates are disclosed that are useful for making 4-Tetrazolyl-4-phenylpiperidine Compounds according to Formula I, where Ar1 is —C3-C8 cycloalkyl, phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Ar2 is phenyl, naphthyl, anthryl, phenanthryl or -(5-7-membered) heteroaryl, each being unsubstituted or substituted with one or more R2 groups; Z1 and Z2 are each independently a —(C1-C4 alkyl) group; R1 is —(CH2)nC(O)N(R3)(R4) where R3 and R4 are each independently H or —(C1-C4 alkyl); R2 is halogen, —C1-C3 alkyl, —O—(C1-C3 alkyl), —NH(C1-C3 alkyl) or —N(C1-C3 alkyl)2; n is an integer ranging from 1 to 4; m is an integer ranging from 0 to 4; and, in certain embodiments, the phenyl moiety attached to the 4-position of the piperidine ring of a compound according to Formula I can be optionally substituted with one or more R2 groups.

Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R? group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R? is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.

Abstract: The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2?-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I).

Abstract: It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).

Abstract: A process for making energetic cast cured binders by making di-tetrazoles to produce di-functional tetrazole diols for producing tetrazole base polymers. Embodiments of the present invention relates generally to a process for preparation of a monomer including reacting an effective amount of nitrile(s) with inorganic azide and a divalent zinc salt in a first solvent, cooling to room temperature producing a di-tetrazole, purifying the di-tetrazole by recrystallization in a second solvent; and reacting an effective amount of the purified di-tetrazole with a third solvent, a soluble reversible or non-reversible base, and 2-chloro-ethanol, cooling to room temperature producing a di-functional tetrazole diol.

Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,

Abstract: This invention provides a method for treating cancer in mammals through cellular-organelle-crystallization-induced-death (herein defined as “Cocid”), a method for treating cancer using cellular organelle and/or cytoskeleton crystallizing agents (e.g. tetrazolium salts and their derivatives), pharmaceutical compositions containing a therapeutically effective amount of organelle and/or cytoskeleton crystallizing agents, and compositions containing organelle and/or cytoskeleton crystallizing agents in combination with a pharmaceutically acceptable carrier, diluent or excipient. The crystallizing agents with or without a pharmaceutically acceptable carrier, diluent or excipient, are used in combination with surgery and/or non-surgical anti-tumor treatments.

Abstract: The use of novel new heterocyclic borane and carborane salt ingredients for use as energetic, high density propellant fuels and fuel additives, or for gas generator and hydrogen storage applications. These subject and unique heterocyclic borane and carborane salts are comprised of both aromatic and non-aromatic heterocyclic cations with the necessary borane and/or carborane anions. Such salts with partially fluorinated borane or carborane anions would be candidate ingredients for metallized (e.g. boron, aluminum) propellant formulations. The high density provided by these unique heterocyclic borane and carborane compounds will be attractive for volume-limited propulsion systems.

Abstract: A cross-linked polyisocyanate polymer and a process for preparation of a polymer having the general structure (I) including reacting an effective amount of tetrazole polyol with isocyanate resin, combining at a temperature in the range of about 50° C. to about 100° C. for a time period in the range of about 1 to about 24 hours and cooling to room temperature producing a cross-linked polyisocyanate polymer.

Abstract: The present invention is a light-emitting device material characterized by containing a pyrene compound represented by the following general formula (1): wherein R1 to R10 are specific functional groups, provided that at least one of the R1 to R10 is a substituent represented by the following general formula (2): wherein R11 to R14 are specific functional groups, provided that any one of the R11 to R14 is used for a single bond with a pyrene skeleton; X1 is a group represented by the following general formula (3): wherein R15 is a specific functional group; and Y1 to Y4 is selected from among a nitrogen atom and a carbon atom, provided that at least one of the Y1 to Y4 is a nitrogen atom and at least one thereof is a carbon atom, and no substituents exist on the nitrogen atom in the case of the nitrogen atom. This material provides a light-emitting device having high luminous efficiency and excellent durability.

Abstract: An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II) wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Abstract: The present invention provides a compound of the formula (Cat)+z[M++(5-nitro-1H-tetrazolato-N2)?x(H2O)y] where x is 3 or 4, y is 2 or 3, x+y is 6, z is 1 or 2, and M++ is selected from the group consisting of iron, cobalt, nickel, copper, zinc, chromium, and manganese, and (Cat)+ is selected from the group consisting of ammonium, sodium, potassium, rubidium and cesium. A method of preparing the compound of that formula is also disclosed.

Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.

Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.

Abstract: The compounds of the formula (I) in which R1 represents cycloalkyl, and its stereoisomers and any mixtures thereof are highly suitable as microbicides for protecting plants and materials.

Abstract: The compounds of the formula (I) in which R1 represents hydrogen or in each case optionally substituted alkyl, alkenyl, alkynyl or phenyl are highly suitable as microbicides for protecting plants and materials.

Abstract: To supply the reagent, medium, and method for detection of Alicyclobacilus acidoterrestris, with which acidoterrestris can be rapidly detected and easily distinguished from acidocaldarius. After a sample including fruit juice is added to the medium for detection of Alicyclobacilus acidoterrestris containing chlor-2,3,5-triphenyl-2H-tetrazolium, acidoterrestris bacteria are detected based upon color change to red of the colony on the medium, which is kept at the temperature of 40 to 50° C.

Abstract: A compound having a structure is disclosed herein. Compositions, medicaments, and therapeutic methods related thereto are also disclosed.

Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.

Abstract: A process for preparation of polymers including reacting an effective amount of tetrazole diols or tetrazole polyols with isocyanate resins to produce tetrazole based linear isocyanate polymers.

Abstract: An ionic liquid is disclosed A precursor composition that comprises at least one ionic liquid and at least one energetic material is also disclosed, as is a method of synthesizing an ionic liquid and a method of desensitizing an explosive composition.

Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.

Abstract: The invention relates to a method or process for the manufacture of blood pressure lowering agents, such as valsartan, novel intermediates as well as process steps in said synthesis. The method or process leads via the novel intermediate salts of the formula IA, or a tautomer thereof, wherein [Kat]n+ is a cation and n is 1, 2, 3, 4, 5 or 6.

Abstract: Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances.

Abstract: A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.

Abstract: The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula wherein R1, R2 and R3, independently of one another, represent hydrogen, halogen or an organic radical, in racemic form or as an enantiomer, a tautomer, an analog thereof or a salt thereof.

Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, , alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, pertluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

Abstract: A process for making energetic urethane cured binders by making poly-tetrazoles to produce multi-functional tetrazole polyols for producing tetrazole base polymers. Embodiments of the present invention relate generally to a process for preparation of a monomer including reacting an effective amount of nitrile(s) with inorganic azide and a divalent zinc salt in a first solvent, cooling to room temperature producing poly tetrazole purifying the poly tetrazole by recrystallization or precipitation in a second solvent, and reacting an effective amount of the purified poly-tetrazole with a third solvent, a soluble reversible or non-reversible base, and 2-chloro-ethanol, cooling to room temperature producing tetrazole polyol. Embodiments of the present invention further include the monomers produced by the processes described herein.

Abstract: A process for making energetic cured binders by making poly-tetrazoles to produce multi-functional tetrazole polyols for producing tetrazole base polymers. Embodiments of the present invention relate generally to a process for preparation of a monomer including reacting an effective amount of nitrile(s) with inorganic azide and a divalent zinc salt in a first solvent, cooling to room temperature producing poly tetrazole, purifying the poly tetrazole by precipitation in a second solvent, and reacting an effective amount of the purified poly tetrazole with a third solvent, a soluble reversible or non-reversible base, and 2-chloro-ethanol, cooling to room temperature producing tetrazole polyol.

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof, and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.

Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.

Abstract: A process for the preparation of phenyltetrazole derivatives of formula (II) wherein R and Y are as defined in the disclosure, by direct ortho-metallation of (tetrazol-5-?l)benzene. The compounds of formula (II) are useful intermediates for the preparation of angiotensin II antagonists.

Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.

Abstract: A poly(tetrazole) is formed by a water-based method. A gas generating composition 12 containing the poly(tetrazole) is contained within an exemplary gas generator 10. A gas generating system 200 incorporates the poly(tetrazole) therein. A vehicle occupant protection system 180 incorporates the gas generating system 200.

Abstract: Valsartan of formula (I) is prepared by hydrolysis of valsartan benzyl ester with an alkali metal hydroxide, washing with an organic solvent, acidifying with hydrochloric acid and isolating valsartan from the reaction mixture

Abstract: There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C?O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

Abstract: An additive for copper plating comprising, as an effective ingredient, a nitrogen-containing biphenyl derivative represented by the following formula (I): [wherein X represents a group selected from the following groups (II)-(VII): and Y represents a lower alkyl group, lower alkoxy group, nitro group, amino group, sulfonyl group, cyano group, carbonyl group, 1-pyridyl group, or the formula (VIII): (wherein R? represents a lower alkyl group)], a copper plating solution formed by adding the additive for copper plating to a copper plating solution containing a copper ion ingredient and an anion ingredient, and a method of manufacturing on an electronic circuit substrate having a fine copper wiring circuit, which comprises electroplating in the copper plating solution using as the cathode an electronic circuit substrate in which fine microholes or microgrooves in the shape of an electronic circuit are formed on the surface.

Abstract: Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules.