Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: A combination of a muscarinic cholinergic receptor agonist with a non-anticholinergic antiemetic agent, and the optional addition of an acetyl choline esterase inhibitor, for the treatment of hypocholinergic disorder of the central nervous system.

Abstract: A pharmaceutical composition comprises at least one integrase inhibitor or its salt, solvate, complex, hydrate, isomer, ester, tautomer, anhydrate, enantiomer, polymorph or prodrug and at least one antiretroviral or anti-HIV agent or its salt, solvate, complex, hydrate, isomer, ester, tautomer, anhydrate, enantiomer, polymorph or prodrug.

Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (1) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.

Abstract: The invention relates to antibacterial compounds of formula I wherein M is one of the groups MA, MB and MC represented below wherein R1, MA, MB and MC are as defined in the specification; and to salts thereof.

Abstract: The present invention relates to a pharmaceutical composition for the treatment of primary biliary cirrhosis (PBC), in which containing a therapeutically effective amount of (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy] butyric acid, a salt thereof, or a solvate thereof.

Abstract: Described herein is a genetic modifier of cystic fibrosis (CF), which may serve as a predictor of the efficacy of a CFTR-directed therapy. SNPs rs7512462 or rs2869027 in non-coding regions of SLC26A9 are shown to correlate with CF lung disease severity in patients having CFTR mutations that leave protein at the cell surface, e.g. gating mutations such as G551D. It is also shown that patient response to Ivacaftor correlates with SLC26A9 genotype. Given the biology of SLC26A9, risk alleles of LC26A9 should correlate with reduced SLC26A9. SLC26A9 activity (marked by e.g. genotype or expression level) is therefore a predictor of treatment efficacy for any CFTR-directed therapeutic, such as Ivacaftor or Lumacaftor. Associated methods of selecting and treating patients are described, along with related kits, uses, and drug discovery platforms.

Abstract: Compounds of Formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, their preparation, pharmaceutical compositions comprising such compounds and their use in treating and/or preventing bacterial infections are disclosed.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.

Abstract: Provided are in vitro and in vivo methods for determining whether a patient with Fabry disease will respond to treatment with a specific pharmacological chaperone.

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract: Pharmaceutical compositions for simultaneous transdermal delivery of Doxylamine and Pyridoxine comprising Doxylamine or its salts, Pyridoxine or its salts or its active metabolites and a vehicle system wherein pharmaceutical compositions are liquid formulations, semisolid formulations and polymer matrices. Further pharmaceutical compositions can be incorporated into transdermal delivery systems or transdermal patches. The invention provides a method for treatment of nausea and vomiting in general, and for pregnant women in particular by continuous and simultaneous transdermal delivery of Doxylamine and Pyridoxine. This is to be accomplished through topical application of pharmaceutical compositions or by application of a transdermal delivery system or transdermal patch to the surface of the skin wherein the duration of application is once in a day, once every two days, once every three days, once every four days, once every five days, once every six days, or once in a week.

Abstract: The present invention provides compounds of Formula 1, or a pharmaceutically acceptable salt thereof, where R, R1, and G are as described herein; methods of preparing the compounds; and use of the compounds to treat pain and/or inflammation associated with arthritis or osteoarthritis.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract: The present invention relates in a first aspect to compounds for use in the treatment of leukodystrophy whereby these compounds are quinoline derivatives, e.g. laquinimod. In a further aspect, the present invention relates to methods for the treatment of Leukodystrophy, in particular, peroxisomal disorders including Zellweger syndrome.

Abstract: This invention provides a method of treating a patient afflicted with a neurodegenerative disorder, e.g., Huntington's disease (HD), comprising administering to the patient laquinimod as an add-on therapy to or in combination with pridopidine. This invention also provides a package and a pharmaceutical composition comprising laquinimod and pridopidine for treating a patient afflicted with a neurodegenerative disorder, e.g., HD. This invention also provides laquinimod for use as an add-on therapy or in combination with pridopidine in treating a patient afflicted with a neurodegenerative disorder, e.g., HD. This invention further provides use of laquinimod and pridopidine in the preparation of a combination for treating a patient afflicted with a neurodegenerative disorder, e.g., HD.

Abstract: A depot precursor formulation comprising: a) a controlled-release matrix; b) at least oxygen containing organic solvent; c) at least 12% by weigh of at least one active agent selected from buprenorphine and salts thereof, calculated as buprenorphine free base. Corresponding depot compositions and methods of treatment in pain management, by opioid maintenance and related methods are provided.

Abstract: An abuse deterrent opioid formulation for rectal use. The formulation contains a therapeutically effective amount of the opioid buprenorphine or salts and homologs thereof; and either a gel with a diminishing agent or a suppository base with a diminishing agent into which the opioid buprenorphine is mixed.

Abstract: The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to the opioid oxymorphone, in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal use, and overdose. When delivered at the proper dosage, the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.

Abstract: Compositions and methods for the treatment of Charcot-Marie-Tooth disease and related disorders. Also provided are combination therapies for treating this disease by decreasing PMP22 expression in a subject.

Abstract: The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders.

Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

Abstract: Antibiotic gel formulations for use in dental applications are disclosed. More particularly, the present disclosure is directed to antibiotic gel formulations including low concentrations of antibiotics that are capable of killing root canal pathogens without harming the stem cells inside the root canal. Additionally, the present disclosure is directed to delivery systems and methods for applying the antibiotic gel formulations into a subject's intracanal region.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: The present invention relates to compounds for the treatment of chronic obstructive airway diseases such as chronic obstructive pulmonary disease (COPD) or asthma or bronchiectasis. The present invention further relates to drug delivery devices suitable to be used in the treatment of chronic obstructive airway diseases such as a nebulizer comprising the present compounds. Specifically, the present invention relates to (6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)(piperazin-1-yl)methanone or N,6-dihydroxy-2,5,7,8-tetramethylchroman-2-carboxamide or a pharmaceutically acceptable salt or base thereof for use in the treatment of chronic obstructive airway diseases, preferably chronic obstructive pulmonary disease (COPD) or asthma or bronchiectasis, more preferably chronic obstructive pulmonary disease (COPD).

Abstract: This invention provides methods of treating motor disorder side effects associated with the administration of levodopa to a subject having Parkinson's disease, by administering a dose of eltoprazine or a pharmaceutically acceptable acid addition salt thereof. In particular, the invention provides methods for reducing dyskinesia associated with Parkinson's disease treatments, and effective doses of eltoprazine or a pharmaceutically acceptable acid addition salt thereof.

Abstract: Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.

Abstract: The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.

Abstract: Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the ?- and ?-isoforms and selective for both ?- and ?-isoforms (PI3K-?,?, PI3K-?, and PI3K-?), a Janus kinase-2 (JAK-2) inhibitor, a Bruton's tyrosine kinase (BTK) inhibitor, and/or a B-cell lymphoma-2 (BCL-2) inhibitor are described. In some embodiments, the invention provides therapeutic combinations of a PI3K-? inhibitor and a BTK inhibitor, a JAK-2 and a BTK inhibitor, and a BCL-2 and BTK inhibitor.

Abstract: This disclosure relates to the use of kinase inhibitor to treat or prevent infectious diseases such as tuberculosis. In certain embodiments, this disclosure relates to treating or preventing an infectious disease comprising administering an effective amount of a kinase inhibitor or other compound disclosed herein to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing tuberculosis comprising administering a kinase inhibitor to a subject in need thereof. In certain embodiments, the subject is diagnosed with Mycobacterium tuberculosis (Mtb) that is resistant to multiple antibiotic agents.

Abstract: The present invention describes novel methods for the treatment of sexual dysfunction.

Abstract: The present invention is directed to compositions and methods for treating hepatitis B virus infection. In particular, the present invention is directed to a combination therapy comprising administration of an HBV capsid assembly inhibitor and an interferon for use in the treatment of hepatitis B virus infections.

Abstract: The present disclosure relates to pharmaceutical combinations comprising a cyclin dependent kinase 4/6 (CDK4/6) inhibitor compound, (b) a B-Raf inhibitor compound, and optionally (c) an alpha-isoform specific phosphatidylinositol 3-kinase (PI3K) inhibitor compound, for the treatment or prevention of cancer, as well as related pharmaceutical compositions, uses, and methods of treatment or prevention of cancer.

Abstract: The invention relates generally to compounds of formula (I) that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: Pharmaceutical compositions comprising an antidiabetic agent as an active agent are provided. The present invention relates to pharmaceutical compositions comprising linagliptin or a pharmaceutically acceptable salt thereof as an active agent. The present invention also relates to process of preparation of pharmaceutical compositions comprising linagliptin or a pharmaceutically acceptable salt thereof. The present invention also relates to method of administering the compositions comprising linagliptin to a subject in need thereof.

Abstract: Provided are a type of compounds that can be used for treating cardiovascular diseases and compositions containing the compounds. The compounds and the compositions can improve lipid metabolism disorders by increasing high-density lipoprotein cholesterol in blood; in addition, the compounds and the compositions can also release nitric oxide, and reduce the onset risk of cardiovascular diseases by means of relaxing blood vessels, lowering blood pressure, inhibiting platelet adhesion and aggregation and maintaining vascular tension, and thus play an important role in preventing and treating the occurrence and development of cardiovascular diseases.

Abstract: The present invention provides compounds and methods of use thereof for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.

Abstract: The present application relates to a-substituted amino acid compounds of the Formula (I), compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with the hypercitrullination of proteins by peptidyl arginine deiminase (PAD) enzymes.

Abstract: The present invention provides novel means and methods for treatment auf immunemediated inflammatory diseases.

Abstract: Certain embodiments are directed to composition and methods related to 23 hydroxy ursolic acid and it use in attenuating the effects to monocyte hypersensitivity or hyper-reactivity

Abstract: This document provides methods and materials involved in reducing suppression of immune function in mammals. For example, methods and materials for (a) identifying a mammal as having an elevated level of CD14+/DR? cells (e.g., CD14+/DR? monocytes) and (b) administering RU486 (mifepristone; or drugs with a similar functional profile) to the identified mammal under conditions that change the ratio of CD14+/HLA-DR? cells to CD14+/HLA-DR? cells as well as methods and materials for (a) identifying a mammal as being likely to experience an elevated level of CD14+/DR? cells (e.g., CD14+/DR? monocytes) and (b) administering RU486 (mifepristone; or drugs with a similar functional profile) to the identified mammal under conditions that reduce the degree to which the mammal develops CD14+/DR? cells are provided.

Abstract: An intraocular active agent delivery device can include an active agent homogenously combined with a biodegradable active agent matrix such that the entire delivery device is homogenous. The homogenous delivery device can have a shape and size to fit within a lens capsule or ciliary sulcus of an eye and provide a therapeutically effective amount of the active agent to the eye. The biodegradable active agent matrix can be formulated to provide sustained release of the therapeutically effective amount of the active agent during a release period. In some examples, the active agent can include dexamethasone.

Abstract: Compositions for the topical administration of an active agent comprise a corticosteroid and a fatty alcohol as a skin penetration enhancer, in the form of topical sprays. Processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders, are described.

Abstract: The present disclosure is directed to compositions, formulations and methods of use thereof in the treatment and prevention of ocular conditions including cataract and presbyopia.

Abstract: A system for skin treatment including first, second, third, fourth, and fifth formulations that each include glycolic acid in an amount that ranges between 6 to 13 wt %, and salicylic acid in an amount that ranges between 1.3 to 2 wt %, wherein each of the first, second, third, fourth, and fifth formulations are free of ethanolamine, paraben, propylene glycol, and sulfate.

Abstract: A method for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant irritable bowel syndrome or other non-specific bowel disorder is disclosed comprising administering to a patient in need of such treatment or prophylaxis an effective amount of balsalazide, or a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or a derivative thereof, or a composition comprising balsalazide the modified compound, or a salt or a derivative thereof together with a suitable carrier. Use of balsalazide, a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or derivative thereof, for the manufacture of a medicament for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-pre-dominant irritable Bowel Syndrome or other non-specific bowel disorder is also disclosed.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the NR2B NMDA receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract: Muparfostat for use in reducing intrahepatic tumor recurrence and increasing disease-free survival period in a hepatocellular carcinoma patient with microvascular invasion after curative liver resection, while excluding HCC patients with no vascular invasion and HCC patients with macrovascular invasion, is disclosed. The hepatocellular carcinoma patient with microvascular invasion is identified by examining a resected liver tumor sample from the HCC patient for the presence of microvascular invasion in the sample.

Abstract: The present invention relates to compositions, particularly compositions useful in maintaining and supporting healthy microflora in the female urogenital tract which could lead to inhibition of vaginal infections, as well as methods of treating and preventing vaginal infections. Compositions useful in supporting healthy microflora, disclosed herein, generally comprise a therapeutic amount of a first saccharide and a therapeutic amount of a second saccharide or an organic acid. The saccharides may be, for example, a pentose, a disaccharide, a cyclodextrin, a pectic substance or a non-digestible polysaccharide. The organic acid may be, for example, malic acid.