Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.

Abstract: Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. The compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are as defined in the specification, as are A Z, Q, R1 and R2.

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.

Abstract: The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.

Abstract: Compounds of formula (I): wherein: n represents an integer of from 1 to 6 inclusive, X represents an oxygen atom or an NR6 group, Y represents a carbon atom or a nitrogen atom, Z represents a carbon atom or a nitrogen atom, R1 and R2 represent a hydrogen atom or an alkyl or arylalkyl group, R3 and R4 represent a hydrogen atom or an alkyl group, R5 represents a hydrogen atom or an alkyl, halogen, hydroxy, alkoxy, cyano, nitro, acyl, alkoxycarbonyl, trihaloalkyl, trihaloalkoxy or optionally substituted amino group, R6 represents a hydrogen atom or an alkyl or arylalkyl group, Ra, Rb, Rc, Rd and Re are as defined in the description. Medicinal products containing the same which are useful as specific nicotinic ligands of ?4?2 receptors.

Abstract: The present invention discloses a compound of formula: where Ar1, Ar2, X, Z1, Z2, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Pyridylene Compound”); compositions comprising an effective amount of a Pyridylene Compound; and methods for treating or preventing pain or other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Pyridylene Compound.

Abstract: Disclosed are novel anabaseine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.

Abstract: A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, O-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.

Abstract: The invention provides methods for treating epilepsy, mental disorders and/or deficits in sensory organ by administering to patients therapeutically effective amounts of AMPA receptor antagonists in combination with one or more other active ingredients useful for treating epilepsy, mental disorders and/or deficits in sensory organ. The invention also provides pharmaceutical combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists, and optionally, one or more other active ingredients that are useful for treating epilepsy, mental disorders and/or deficits in sensory organ.

Abstract: The present invention relates to novel 2-phenoxy-6-phenyl- and 2-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure.

Abstract: Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.

Abstract: The present disclosure is directed to surface-modified particles and to methods of making and using the same.

Abstract: The invention is related to alkylene oxide adducts of oligosaccharides, obtained by a process comprising alkoxylating at least one water-soluble oligosaccharide in aqueous solution at a temperature in the range of 90 to 160° C. The compounds are useful as adjuvants in agrochemical compositions.

Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.

Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the prolongation of time until onset of clinical symptoms in patents having an asymptomatic (occult) heart failure or for the reduction of heart size in patients having an asymptomatic (occult) heart failure of a patient suffering from asymptomatic heart disease.

Abstract: The invention provides methods for treating epilepsy by administering to patients therapeutically effective amounts of AMPA receptor antagonists in combination with zonisamide useful for treating epilepsy. The invention also provides pharmaceutical combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists, and optionally, zonisamide that are useful for treating epilepsy.

Abstract: An amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one.

Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.

Abstract: The present invention provides compounds, pharmaceutical compositions, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof.

Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.

Abstract: Disclosed herein are methods for increasing analgesic potency of TRPV1 antagonists, said methods comprise of repeated administration of the TRPV1 antagonists in a subject. Methods for treating or preventing pain by repeated administration of a TRPV1 antagonist are also discussed.

Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.

Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The invention relates to methods of treating patients who have suffered an acute myocardial infarction (AMI) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.

Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.

Abstract: The invention provides methods for treating and/or preventing neuropathic pain by administering to patients therapeutically effective amounts of AMPA receptor antagonists and zonisamide. The neuropathic pain may be diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and zonisamide. The AMPA receptor antagonist may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydropyridin-2-one.

Abstract: The invention provides methods for treating and/or preventing neuropathic pain by administering to patients in need thereof therapeutically effective amounts of AMPA receptor antagonists; and cholinesterase inhibitors and/or anti-neuropathic pain agents. The neuropathic pain may be painful diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists; and cholinesterase inhibitors and/or anti-neuropathic pain agents. The AMPA receptor antagonists may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The cholinesterase inhibitor may be, for example, 1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine (donepezil).

Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract: Methods are provided of treating renal cancer by administration of certain 3,3?,4,4?-tetrahydroxy-2,2?-bipyridine-N,N?-dioxide compounds, especially 3,3?,4,4?-tetrahydroxy-2,2?-bipyridine-N,N?-dioxide (Orellanine), using particular administration protocols and dosing regimens, as well as pharmaceutical compositions suitable for use in the treatment methods that are provided.

Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.

Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A compound of Formula: (I) or a pharmaceutically acceptable derivative thereof, where Ar1, Ar2, X, R3, and m are as disclosed herein. Compounds of Formulae (I)-(V) and pharmaceutically acceptable derivatives thereof; compositions comprising an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof; and methods for treating or preventing pain, UI, an ulcer, IBD, or IBS in an animal comprising administering to an animal in need thereof an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof are disclosed herein.

Abstract: Provided are methods of treating or reducing the risk of developing beta-amyloid production, beta-amyloid deposition, beta-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of polyhydroquinoline and dihydropyridine compounds which decrease Abeta production in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of polyhydroquinoline and dihydropyridine compounds which decrease Abeta production in cells.

Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.

Abstract: Provided are methods and compositions for the treatment of a sexual dysfunction such as premature ejaculation. In certain embodiments, a NMDA antagonist (e.g., dextromethorphan) is administered to a subject in combination with tramadol or a tramadol derivative to treat premature ejaculation. In certain embodiments, a capsaicinoid (e.g., capsaicin) and/or a phosphodiesterase type V inhibitor (e.g., sildenafil citrate) are further administered to the subject. Pharmaceutical preparations such as tablets and capsules are provided.

Abstract: The invention provides methods for treating, preventing, and delaying the onset of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Pick's disease, and the like), dementia, mild cognitive impairments, glaucoma, ocular hypertension, and pain (e.g., neuropathic pain, headaches, and the like) by administering therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists to patents in need thereof. The invention also provides combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists. Exemplary AMPA receptor antagonists include 1,2-dihydropyridine compounds, such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. Exemplary NMDA receptor antagonists include adamantane compounds, such as memantine.

Abstract: The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.

Abstract: The invention relates to 2-substituted pyridines of the formula I in which the index n and the substituents R1 to R4 and L are as defined in the description and in each case one of the two ring members X1, X2 is N, the other is C—H or C-halogen; Y is a group —CH—R1—, —N—R1—, —O— or —S— and is five- or six-membered hetaryl comprising 1 to 3 heteroatoms selected from the group consisting of O, N and S or is phenyl, and to processes for their preparation, intermediates for their preparation, pesticidal compositions and methods for controlling harmful fungi and animal pests using the compounds according to the invention.

Abstract: Compounds, compositions and methods of treating serotonin-mediated diseases and disorders are disclosed.

Abstract: The present invention is directed to bipyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

Abstract: The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the prolongation of time until onset of clinical symptoms in patients having an asymptomatic (occult) heart failure or for the reduction of heart size in patients having symptomatic or asymptomatic (occult) heart failure.

Abstract: The present invention relates to indolylamide derivatives of the general formula (I), to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP2 receptor.

Abstract: There are disclosed pharmaceutical compositions for topical administration or for use in mesotherapy, containing a PDE3 inhibitor as active ingredient, and their use in the treatment of cellulite.

Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.