Abstract: Compounds characterized by thiolactone or thiomorpholino cores display useful antibiotic and radioprotective properties. The latter properties are believed to arise from an ability of the compounds to inhibit proteins involved in apoptosis.

Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: There is provided compounds of formula (I), wherein X1, X2, X3, Y4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.

Abstract: The invention generally relates to compositions and methods for treatment of disease caused by Yersinia spp. infection. More specifically, the invention relates to protein tyrosine phosphatase inhibitors and derivatives and analogs thereof, pharmaceutical compositions containing the protein tyrosine phosphatase inhibitors and analogs, methods of making the protein tyrosine phosphatase inhibitors and analogs and methods of use thereof.

Abstract: The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Abstract: Indoles of Formula I having —X-aryl-(CH2)x-oxazolidinedione and —X-heteroaryl-(CH2)x-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and —X— is a bond or —CH2—, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

Abstract: A one-pot process for making energetic cast cured binders making di-tetrazoles to produce di-functional di-tetrazole diols for making tetrazole base polymers. Embodiments of the present invention relate generally to a process for preparation of a di-functional 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 said di-tetrazole by recrystallization in a second solvent, and reacting an effective amount of said 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-tetrazole diol and is prepared in a one-pot process. Embodiments of the present invention further include the monomers produced by the one-pot process described herein.

Abstract: The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).

Abstract: The present invention provides a method of determining the susceptibility of a subject to treatment with a leukotriene modifier by determining the subject's cysteinyl leukotriene (CysLT) level and the subject's level of eosinophilic airway inflammation and identifying a subject with a high ratio of CysLT levels to eosinophilic airway inflammation as susceptible to treatment with the leukotriene modifier. Also discussed is a method of treatment of subjects who are susceptible to treatment that includes administering a leukotriene modifier to such a subject.

Abstract: A drug effective for prevention and therapy of endometriosis is disclosed. The drug for prevention and/or therapy of endometriosis according to the present invention comprises an antiallergic agent as an effective ingredient.

Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.

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: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.

Abstract: Disclosed herein are substituted indole cysteinyl leukotriene receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

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: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.

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: A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed herein. Details are provided herein. Compositions, methods, and medicaments related thereto are also disclosed.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

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 invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.

Abstract: A method for treating a bone metabolic disease by administering to a human a pharmacologically effective amount of an angiotensin II receptor antagonist which is a compound of the following formula (I), a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof: wherein R1 represents a C1-C4 alkyl; R2 and R3 are the same or different and each represent hydrogen or a C1-C4 alkyl; R4 represents hydrogen or a C1-C4 alkyl; R5 represents hydrogen, a C1-C4 alkyl, a C2-C5 alkanoyloxymethyl, 1-(C2-C5 alkanoyloxy)ethyl, a C1-C4 alkoxycarbonyloxymethyl, 1-(C1-C4 alkoxycarbonyloxy)ethyl, a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl, a (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl or a phthalidyl; and R6 represents a carboxy or a tetrazole-5-yl.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.

Abstract: The present application describes deuterium-enriched olmesartan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Compounds of formula (I), useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.

Abstract: An object of the present invention is to research a therapeutic agent for a keratoconjunctival disorder. A compound represented by the following general formula (1) or a salt thereof exhibits an excellent improving effect on corneal disorder models, and therefore is useful as a therapeutic agent for a keratoconjunctival disorder such as dry eyes, corneal ulcer, keratitis or conjunctivitis. In the formula, the ring Y represents a substituted or unsubstituted nitrogen-containing heterocyclic ring; R1 represents a carboxy group or a substituted or unsubstituted nitrogen-containing 5-membered heterocyclic ring; and R2 and R3 may be the same or different and represent a hydrogen atom, a substituted or unsubstituted alkyl group or a substituted or unsubstituted alkylcarbonyl group.

Abstract: The present invention relates to compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts, esters, or prodrugs 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 a compound of the present invention.

Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.

Abstract: A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, in particular inflammatory or obstructive airway diseases.

Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.

Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating autoimmune diseases. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.

Abstract: A leukotriene C4 and D4 antagonist is used to inhibit tumor metastasis by acting to inhibit tumor cell adhesion to endothelial cells, thereby preventing tumor cell extravasation.

Abstract: The present invention provides a method of treating hypertension, liver failure, loss of patency of ductus arteriosus, glaucoma or ocular hypertension in a patient, comprising administering to the patient a therapeutically effective amount of a selective EP4 receptor agonist of Formula I or a prodrug thereof, a pharmaceutically acceptable salt of the selective EP4 receptor agonist or prodrug or a stereoisomer or diastereomeric mixture of the EP4 receptor agonist, prodrug or salt, wherein the variables X, Z, Q, , and R2 are as defined in the specification.

Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.

Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.

Abstract: The invention is concerned with novel heteroarylacetamides of formula (I) Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb)??(I) wherein Ra to Re are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for making the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: The present invention encompasses compounds or Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: A pharmaceutical composition for the prophylaxis or treatment of glaucoma which comprises an angiotensin II antagonist and at least one compound selected from an adrenaline receptor blocker, a prostaglandin and a carbonic anhydrase inhibitor; and a method for the prophylaxis or treatment of glaucoma by administering the composition to a patient.

Abstract: A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides methods of inhibiting plasminogen activator inhibitor-1 (PAI-1) in a mammal, utilizing compounds of the formula: wherein: A is C or N; B is O, S, N, or CH?CH; X is CO, CH(OH), CH2, or —CH—S-2-benzothiazole; Y is H, alkyl, or halo; Z is O, S, or N; R is H, nitro, alkyl, alkoxy, halo, or CF3; R1 is alkyl, aryl, aralkyl, halo, Het-alkyl, or optionally substituted aryl; Het is G is O, S, or N; R2 is H, halo, alkyl, or —OR5; R3 and R4 are H, halo, alkyl, aryl, nitro, amino, alkylsulfoamide, arylsulfoamide, cycloalkyl, heterocycle, or optionally substituted aryl; R5 is H, alkyl, —CH(R7)R8, —C(CH2)nCO2R9, —C(CH3)2CO2R9, CH(R7)(CH2)nCO2R9, or —CH(R7)C6H4CO2R9; R6 is alkylene; R7 is H, alkyl, aryl, aralkyl, cycloalkyl, phthalic acid, or Q-alkyl; Q is R8 is —CO2R11, —CONHR11, tetrazole, or —PO3R11; R9 is H, alkyl, aryl, or aralkyl; W is O, N, or S; R11 is H, alkyl, aryl, or aralkyl; n=1-6; or a pharmaceutically acceptable salt or ester form thereof.

Abstract: The present invention relates to compositions and methods for promoting tissue regeneration, preferably neural tissue regeneration. Compositions of the invention include (i) certain diphenyl sulfides, diphenyl sulfoxides, diphenyl sulfones, and sulfide, sulfoxide and sulfones of dibenzothiophene and thioxanthene, as well as various analogues and derivatives of these compounds; (ii) one or more cells harvested from an animal or organism subsequent to the administration of a composition comprising a compound of (i); or (iii) any combination of (i) and (ii). The invention can be useful in treating decreases in neuronal function, for example from injury or disease.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.