Abstract: Water- and lipid-soluble cannabinoid compounds that are agonists for CB1 and CB2 receptors are provided. The cannabinoid compounds are useful for the treatment of retinal neurodegenerative disorders such as glaucoma, diabetic retinopathy and macular degeneration.

Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.

Abstract: The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.

Abstract: A compound of the following formula: wherein X, Y, and Z are as defined herein. Also disclosed are methods for inhibiting TNF? expression, IL-1? expression, iNOS expression, and NF-?B activity and methods for treating autoimmune disease, cancer, or atherosclerosis with such a compound.

Abstract: The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.

Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract: The present invention relates to methods useful for treating or preventing anemia or thrombocytopenia, comprising administrating an effective amount of a Triheterocyclic Compound to a subject in need thereof. The present invention also relates to methods useful for preventing anemia or thrombocytopenia in a subject, comprising administrating an effective amount of a Triheterocyclic Compound to the subject, wherein the subject is at heightened risk of developing anemia or thrombocytopenia.

Abstract: The invention concerns pyrimidine derivatives of Formula (I) wherein each of p, R1, R2, q, R3, r, R4, X1 and Q1 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.

Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.

Abstract: This invention provides the combination of a growth hormone secretagogue and a p38 kinase inhibitor for use in treatment or prevention of a disease associated with deposition of A? in the brain.

Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

Abstract: The present invention provides compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, type II diabetes, Metabolic syndrome and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea, Alzheimer's disease, and pain related disorders, and to pharmaceutical compositions containing them.

Abstract: Disclosed herein are compositions containing brimonidine and timolol. Therapeutic methods and medicaments related thereto are also disclosed.

Abstract: Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.

Abstract: The invention relates to the use of PDE5 inhibitors, preferably sildenafil or tadalafil, optionally in combination with a further active ingredient, for treating and/or preventing hypopigmentary disorders.

Abstract: The present invention concerns neuroreceptor-active carboxamide-substituted indolizine derivatives of general formula I wherein X represents a group of general formula X1

Abstract: The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or casein kinase (CK) pathways (e.g., CK1?, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or CK pathways (e.g., CK1?, and upstream and downstream protein kinases).

Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.

Abstract: The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.

Abstract: The effects of KMUP-3, (7-[2-[4-(4-Nitrobezene)peperazinyl]ethyl]-1,3-dimethylxanthine) on tracheal smooth muscle are provided. Intratracheal instillation of KMUP-3 avoids bronchoconstriction, decreases of lung resistance, and increases of dynamic lung compliance. These merits provide insightful benefits for the treatment in asthma and COPD (chronic obstructive pulmonary disease).

Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

Abstract: Disclosed are novel piperazine 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: The present invention is directed to novel compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: The present invention discloses effect of non-selective COX1 inhibitor such as aspirin, statins, thiazolidinediones or combinations thereof on COX2. Also disclosed herein is a method to avoid the adverse effects that the non-selective COX1 inhibitor may have when administered with statins and/or thiazolidinediones.

Abstract: A compound represented by the formula (I): wherein Ar is an optionally substituted aromatic ring; Xa, Xc, Ya, Yc, Z1 and Z2 are each a bond, O, S, —CO—, —CS—, —CR3(OR4)—, —NR5—, —SO—, —SO2—, —CONR6— or —NR6CO— (wherein R3, R4, R5 and R6 are as defined in the specification); Xb and Yb are each a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R1 is an optionally substituted hydrocarbon group; ring A is an optionally further substituted aromatic ring, provided that the ring should not be benzimidazole; n is an integer of 1 to 8; ring B is an optionally further substituted aromatic ring, provided that the ring should not be oxazole; W is a divalent saturated hydrocarbon group having 1 to 20 carbon atoms; and R2 is —OR8 or —NR9R10 (wherein R8, R9 and R10 are as defined in the specification) or a salt thereof, is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein: A is a moiety of formula: and to pharmaceutically acceptable salts and solvates thereof, wherein X, Z, D, E, V, W, Y, R1, R2, R5, R6, L, and u are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula I to a patient in need thereof, and to compositions for treating such disorders which contain the compounds of formula I. The invention also relates to methods of making the compounds of formula I.

Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

Abstract: The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula I wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined hereinabove. The present invention also relates to a process for their preparation, a pharmaceutical composition containing said derivatives and a method of treating or preventing acute or chronic neurological disorder comprising administering to a patient in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of at least one such derivatives.

Abstract: This invention relates to novel 4-aminoquinazolines, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2.

Abstract: Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: are disclosed.

Abstract: The invention relates to nonadepsipeptides and methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial infectious diseases.

Abstract: The present invention relates to novel vinorelbine derivatives. Pharmaceutical compositions containing these compounds as well as processes of preparation and processes of use for treatment of various conditions are also disclosed.

Abstract: Various calcium channel blockers and pharmaceutical compositions containing these compounds are disclosed. Calcium channel blockers are compounds capable of inhibiting calcium ion channels. Methods for preparing calcium channel blockers and their use as calcium channel antagonists are also disclosed.

Abstract: A pharmaceutical composition is provided that comprises a solid dispersion of implitapide. Such solid dispersions may include implitapide and least one pharmaceutically acceptable excipient. In some embodiments, the disclosed solid dispersions comprise substantially amorphous implitapide.

Abstract: The invention includes compositions comprising substantially purified pyrroloquinoline quinone, that are useful in methods for the treatment and prevention of cardiac injury caused by hypoxia or ischemia. The invention also includes methods for the treatment and prevention of cardiac injury comprising contacting a composition of the invention with a human patient.

Abstract: Inverse agonists and antagonists of serotonin receptors are disclosed for use in treating sleep disorders such as insomnia, and specifically sleep maintenance insomnia. The compound increase slow wave sleep, decrease the number of awakenings after sleep onset, and decrease the time awake after sleep onset.

Abstract: Certain novel N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract: Provided herein are compositions comprising one or more immunomodulatory compounds and valproic acid, hydroxyurea or trichostatin A, methods for their use in CD34+ hematopoietic stem cell expansion in vitro and in vivo for bone marrow reconstitution and bone marrow transplantation, increasing fetal hemoglobin expression, and methods for treating, preventing and/or managing cancer, tumors and hematological diseases and disorders.

Abstract: This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNF? releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): wherein n represents 1, 2, 3, 4, 5 or 6; R1 represents from one to four of the same or different substituents selected from F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents OR3, NR3R4, N(R3)COR4, O2CR5; R3 and R4 represent independently and at each occurrence H or C1-4 alkyl; R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, a heterocycle W or CHR6NR9C(O)W; R6, R9, R10 represent independently and at each occurrence H, or C1-4 alkyl; R7 and R8 represent independently and at each occurrence H, C1-4 alkyl, or R7 and R8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-

Abstract: The present invention relates to compounds of Formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.

Abstract: The present invention provides 24 new forms of tiagabine, including 22 new crystalline forms of tiagabine and its salts, an amorphous form of tiagabine free base, and a cocrystal form of tiagabine hydrochloride with 2-furancarboxylic acid. The present invention further provides a process for preparing each of the new tiagabine forms. The present invention further provides a pharmaceutical composition containing at least one of the new tiagabine forms, and a process for the preparation thereof. The present invention further provides a method of treating a disease related to GABA uptake in a mammal, comprising the step of administering to the mammal a therapeutically effective amount of at least one of the new tiagabine forms.

Abstract: This invention discloses and claims a method of treatment of a disease as defined herein using a compound conforming to the general formula (I): Wherein R1, R2, R?2, R3, R4 and R5 are as described herein. Specifically, the compounds of the present invention exhibit an inhibitory effect on the production of ?-amyloid peptide (?-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.

Abstract: The present invention provides methods of improving cognitive and motor deficits associated with central nervous system (CNS) disorder or condition in an animal. The methods comprise a general administration of phosphodiesterase 4 inhibitors and optionally training the animal under conditions sufficient to produce an improvement in performance.

Abstract: The present invention provides compositions that exert a superior hypotensive action while inhibiting an increase in heart rate. The present invention provides antihypertensives and preventive/therapeutic compositions useful in the treatment of cardiovascular diseases, which contain cilnidipine and at least one angiotensin II receptor blocker(s). The present invention also provides methods for treating cardiovascular diseases by administration of said compositions.

Abstract: Methods for regulating food intake in a human subject; for improving a compliance of a human subject to caloric restriction; and for reducing a desire of a human subject to consume fats, utilizing H1-receptor agonists that have a pharmacological half-life that allows an efficient treatment regime thereof are disclosed. The methods can be efficiently used for treating conditions such as overeating, overweight, obesity, binge eating disorder, night eating syndrome, obsessive eating, compulsive eating and bulimia, as well as conditions associated with metabolic derangement such as dyslipidemia.

Abstract: Methods and compositions for regulating food intake in a human subject; for improving a compliance of a human subject to caloric restriction; and for reducing a desire of a human subject to consume fats, utilizing H1-receptor agonists that have a pharmacological half-life that allows am efficient treatment regime thereof are disclosed. The methods and compositions can be efficiently used for treating conditions such as overeating, overweight, obesity, binge eating disorder, night eating syndrome, obsessive eating, compulsive eating and bulimia, as well as conditions associated with metabolic derangement such as dyslipidemia and for preventing or reducing weight gain due to factors such as drug use, cessation of smoking, and the like in a human subject.

Abstract: Compounds of Formula I: wherein R1, R2, R3, R4, R5 Ar1 and X are as described in the specification, pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission.

Abstract: Disclosed herein is an agent for preventing and treating cancer comprising an oxadiazole urea compound represented by Chemical Formula 1, below, as an effective ingredient. The oxadiazole urea compound effectively inhibits the growth of cancer cell lines and the activity of STAT3, and may be thus useful in the prevention and treatment of cancer.