Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.

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

Abstract: The present disclosure relates to polymorphic Form D of bazedoxifene acetate, pharmaceutical compositions and methods of treatment using the same, and methods of preparing the same.

Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.

Abstract: This patent describes a method and materials to treat cancer diagnosed at an early stage, particularly breast cancer. It considers that metastatic breast cancer growth includes periods of dormancy, that surgery to remove a primary tumor can induce metastatic growth, and that women with Down Syndrome rarely get breast cancer. It elevates the level of an antiangiogenic drug produced by chromosome 21 preferably Endostatin in plasma preferably at least one day prior to surgery and kept at that high level preferably indefinitely. In one embodiment, the therapy specifically excludes drugs that significantly inhibit the VEGF pathway since that is important for wound healing. This method will prevent results of surgery from stimulating tumor growth and angiogenesis of micrometastatic disease that is much easier to prevent than control after the fact. This can be done indefinitely since there is no acquired resistance that develops, as happens in most cancer therapies.

Abstract: Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein.

Abstract: The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.

Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: Bazedoxifene acetate formulations and compositions thereof having improved properties relating to reduction, elimination, or prevention of polymorphic conversion of bazedoxifene acetate, and processes for making such formulations and compositions. Components used in the formulations and compositions include a filler/diluent, an optional second filler/diluent, an optional antioxidant, a glidant/disintegrant, and a lubricant.

Abstract: The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal from drug dependency. In the latter case, the noribogaine treatment should be supplemented with the administration of an opioid antagonist such as naloxone.

Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.

Abstract: Methods for treating a mammal suffering from glucocorticoid-related diseases and conditions, comprising administering to the mammal an effective amount of a selective inhibitor of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme activity, wherein the inhibitor is a compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating neuronal degeneration, dysfunction, acute psychosis, anxiety, dementia, depression, non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention is related to tetrahydroindole derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

Abstract: The present invention relates to new triazole modulators of aromatase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Abstract: The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.

Abstract: The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.

Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: The invention relates to aza-cyclic-indole-2-carboxamide derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions.

Abstract: The invention provides a novel polymorphic form C of bazedoxifene acetate, methods of preparing the polymorphic form, and compositions and methods of treatment using the polymorphic form.

Abstract: The present invention provides compounds of general formula I: (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.

Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: This invention relates to methods, pharmaceutical compositions and kits useful in treating female sexual dysfunction and the use of an estrogen agonist/antagonist for the manufacture of a medicament for the treatment of female sexual dysfunction. The compositions are comprised of an estrogen agonist/antagonist as a first active ingredient and a cyclic guanosine 3?,5?-monophosphate elevator as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.

Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.

Abstract: The present invention relates to compounds of Formula I, 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: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating osteoporosis, acne, dysfunctional uterine bleeding, endometrial polyps, benign breast disease, adenomyosis, infertility, endometriosis, endometrial cancer, polycystic ovary syndrome, cardiovascular disease, Alzheimer's disease, cognitive decline, central nervous system disorders, central nervous system cancers, leukemia, endometrial ablations, chronic renal disease, chronic hepatic disease, coagulation diseases and disorders, hypocalcemia, hypercalcemia, Paget's disease, osteomalacia, osteohalisteresis, and multiple myeloma.

Abstract: The present invention is directed to bazedoxifene ascorbate, compositions containing the same, dispersions thereof, preparations thereof, and uses thereof.

Abstract: The present invention is directed to bazedoxifene ascorbate, compositions containing the same, dispersions thereof, preparations thereof, and uses thereof.

Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I): {wherein W represents a nitrogen atom or —CH—; X represents —C(?O)— or —CHR4— (wherein R4 represents a hydrogen atom, or the like); R1 represents a group represented by the following formula: [wherein Q1 represents a nitrogen atom or —CR8— (wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like). Q2 represents —NR15— (wherein R15 represents a hydrogen atom, or the like) and R5 and R6 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like]; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof, and the like.

Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.

Abstract: The present invention relates to novel indole derivatives such as compounds of the formula (I): which possess antagonist potency at the 5-HT6 receptor and the use of such compounds or pharmaceutically acceptable salts or solvates thereof in the treatment of Alzheimer's disease and other CNS disorders.

Abstract: Methods of treating a specific cancer or amyloidosis are disclosed. Specific methods encompass the administration of 3-(4-amino-1 oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione alone or in combination with a second active ingredient.

Abstract: Methods for treating a mammal suffering from glucocorticoid-related diseases and conditions, comprising administering to the mammal an effective amount of a selective inhibitor of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme activity, wherein the inhibitor is a compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating neuronal degeneration, dysfunction, acute psychosis, anxiety, dementia, depression, non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention relates to the use of certain aza-phenylalanine compounds of formula (I) wherein R1 denotes amino, alkylamino, dialkylamino, amidino, alkylamidino, N-hydroxyamidino, or N-alkoxyamidino, Y denotes sulfonyl or carbonyl and R2 and R4 independently represent various organic residues, in the treatment or prevention of cardiac arrhythmia and/or in treatment or prevention of diseases in association with ischemic heart conditions.

Abstract: Indole carboxamide compounds of Formula (I): are provided as inhibitors of kinase activity, in particular IKK2 activity as well as compositions and medicaments containing them, for use in inflammatory and tissue repair disorders.

Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.

Abstract: A compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.

Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.

Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor: wherein the variables are described in the specification.

Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N?N—. —NR7—, —CR7?CR8—, —CR7?N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.

Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.

Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a.

Abstract: The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders related to or associated with the 5-hydroxytryptamine-6 and 5-hydroxtryptamine-2A receptors or with norepinephrine reuptake inhibition.