Abstract: Molecules of general Formula (I): able to bind to native polyribosomes engaged in active protein synthesis. The disclosure relates also to the use of the molecules of general Formula (I) for isolating at least one active ribosome from a biological sample, and for ribosome profiling, as well as kits for isolating at least one active ribosome from a biological sample.

Abstract: The present invention provides crystalline forms of Ibrutinib. Specific crystalline forms provided by the present invention include Ibrutinib Form APO-I, an anhydrous form; APO-II, a methyl benzoate solvate of Ibrutinib; and APO-IV, a methyl salicylate solvate of Ibrutinib.

Abstract: Phosphodiesterase-4 (PDE4) inhibiting compositions comprising a Sceletium and an activity enhancer are disclosed and described. Methods and systems for inhibiting PDE4, as well as, dosage forms comprising a Sceletium extract and an activity enhancer are also disclosed. Additionally disclosed are methods for enhancing the potency or PDE4 inhibitory activity of a Sceletium extract by addition of an activity enhancer.

Abstract: The disclosure is directed to compounds and pharmaceutically acceptable salts thereof for the treatment and/or prevention of neurodegenerative and/or mitochondrial diseases, such as Parkinson's disease and Leigh's disease. The compounds and pharmaceutically acceptable salts thereof are of the class of nitrogenous bases, for example, pyrimidines, purines, pteridines and pharmaceutically acceptable salts thereof.

Abstract: The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R2, and X are as defined in the specification; or a salt thereof.

Abstract: Pyrazolopyrimidine compounds for inhibition of isoprenoid biosynthesis have a formula (I) or a pharmaceutically acceptable salt thereof. In formula (I), R1 includes an alkyl group and R2 includes an optionally substituted moiety selected from the group consisting of an optionally substituted benzyl group, an optionally substituted phenethyl group, an optionally substituted ethanol group, an optionally substituted ethyl acetate group, an optionally substituted methyl furan group, an optionally substituted 3-ethyl indole group, and a lower alkyl group. Compositions containing pyrazolopyrimidine compounds and methods for using pyrazolopyrimidine compounds are described.

Abstract: The present invention refers to the use of theobromine or its derivatives as an inhibitor of the crystallization of uric acid to avoid the formation of uric acid crystals in urine and as a consequence renal lithiasis or specifically uric acid renal lithiasis.

Abstract: Disclosed herein are pharmaceutical compositions, methods and kits for lowering the serum uric acid level of a subject and for the treatment of a condition associated with elevated serum uric acid levels comprising administering a composition comprising a first urate-lowering agent and a second urate-lowering agent. In some aspects the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salts thereof. In some aspects the second urate-lowering agent is an inhibitor of uric acid production, a uricosuric agent, a uricase, or a pharmaceutically acceptable salt thereof.

Abstract: A preparation method of PCI-32765 crystalline form A, which comprises the following steps: 1) dissolving free base of PCI-32765 in a good solvent; 2) the solution prepared by Step 1) is dropwise added into an anti-solvent, stirred and added seed crystal of PCI-32765 Form A; Or the solution prepared by Step 1) is dropwise added into the suspension containing seed crystal of PCI-32765 Form A; 3) solution obtained by step 2) is continuously stirred and aged until crystal transformation is completed, then the crystal slurry is obtained; 4) crystal slurry in step 3) is filtered, washed, and dried to obtain the powder of PCI-32765 Form A. The preparation method of crystalline Form A provided by the present disclosure is a simple process and can be easily controlled, scaled up stably and conducted reliably. The process has high yield, good impurity removing capacity and is environmentally friendly.

Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.

Abstract: The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.

Abstract: The present invention relates to acid addition salts of ibrutinib, a pharmaceutical composition comprising the same as well as a method of preparing the same.

Abstract: The present invention encompasses solid state forms of Ibrutinib, including forms G, J and K, and pharmaceutical compositions thereof.

Abstract: Disclosed are chemical entities of formula (I) wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.

Abstract: Compounds of formula (I) and salts thereof: wherein R1 is n-C1-6alkyl or C1-2alkoxyC1-2alkyl-, R2 is halo, OH or C1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.

Abstract: This disclosure relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants, such as compounds of Formula (I):

Abstract: The present invention relates to BTK occupancy assays.

Abstract: A compound represented by the general Formula I: a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a deuterated radio-labeled analog thereof, and mixtures of any of the foregoing, wherein: A-K are individually selected from carbon or nitrogen; X?—O, —NR1, or —S; R1-11 are individually selected from the group consisting of —H, C1-C6 alkyl, C6-C14 aryl, substituted C6-C14 aryl, C1-C14-alkoxy, halogen, hydroxyl, carboxy, cyano, C1-C6-alkanoyloxy, C1-C6-alkylthio, C1-C6-alkylsulfonyl, trifluoromethyl, hydroxy, C2-C6-alkoxycarbonyl, C2-C6-alkanoylamino, —O—R12, S—R12, —SO2—R12, —NHSO2R12 and —NHCO2R12, wherein R12 is phenyl, naphthyl, or phenyl or naphthly substituted with one to three groups selected from C1-C6-alkyl, C6-C10 aryl, C1-C6-alkoxy and halogen, and C4-C20 hydroxyheteroaryl wherein the heteroatoms are selected from the group consisting of sulfur, nitrogen, and oxygen.

Abstract: The present disclosure provides compounds of Formula (II) as disclosed herein, and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK inhibitors, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

Abstract: A pharmaceutical composition comprising: (a) a liquid carrier comprising water and at least 20% of at least one alcohol; and (b) sildenafil citrate dissolved in said liquid carrier at a concentration of at least 7 mg/ml.

Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III? (PI4KIII?) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.

Abstract: Described herein are compositions having a nanoparticle that is conjugated to at least one bone targeting moiety, wherein the bone targeting moiety is bonded to the nanoparticle by a linker, wherein the nanoparticle contains iron, and wherein the compositions are neutral or pharmaceutically acceptable salts or esters. Also described herein are methods of making these compositions. In one aspect, the nanoparticles serve as contrast agents for magnetic resonance imaging of bone metabolism. The compounds, compositions, and methods described herein can be used in a number of therapeutic applications including diagnosing or monitoring fracture and/or the progress of conditions associated with bone loss, which include, but are not limited to, osteoporosis, Paget's disease, osteolytic tumors, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, osteoarthritis, osteopenia, and hypercalcemia.

Abstract: In some embodiments, the present invention relates to novel small molecule inhibitors that block the CXCR4-SDF-1 signaling pathway by directly inhibiting members of the Tec family of kinases, namely Bruton's tyrosine kinase (BTK), and their use in treating diseases in which pathogenesis is mediated by the CXCR4/SDF-1 signaling pathway.

Abstract: To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 inhibitory effect. The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, Z3, Z4, W, n, R1, R2, and R3 have meanings as defined in the present specification, or a salt thereof.

Abstract: A method comprising the step of: administering an effective amount of a topical dipyridamole to a subject in need thereof due to an eye disorder selected from the group consisting of pterygium and pinguecula.

Abstract: Presented herein are novel therapeutic compounds and methods of using the same for the treatment of cancers.

Abstract: The present invention relates to intranasally administered pharmaceutical compositions for the treatment of headaches, such as migraines. Such pharmaceutical compositions comprise benzyl alcohol or a combination of benzyl alcohol and tetracaine. The invention also relates to methods for treating headaches, such as migraines, using these pharmaceutical compositions.

Abstract: The present disclosure relates to cyclic sulfones and sulfoximines that are HIF-2a inhibitors and methods of making and using them for treating cancers. In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound described herein and a pharmaceutically acceptable carrier or excipient. The compound may exist in an amorphous form, a crystalline form, or as a salt, solvate, or hydrate. In another aspect, the present disclosure provides a method of treating renal cell carcinoma by administrating a therapeutically effective amount of a compound described herein or a pharmaceutical composition thereof to a subject in need of such treatment.

Abstract: Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.

Abstract: The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

Abstract: Disclosed are methods of treating fibrosis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of an ACK inhibitor (e.g., a BTK inhibitor, such as for example an irreversible BTK inhibitor, such as for example, ibrutinib).

Abstract: The present invention provides efficient, economical, and improved methods for synthesizing ibrutinib and intermediates thereof. The invention involves a unique biphasic acylation reaction system which advantageously allows for easy separation of ibrutinib from the reaction mixture without additional extraction and wash steps. The isolated ibrutinib formed using the methods described herein can be useful in the preparation of an amorphous form of ibrutinib. In some embodiments, the isolated ibrutinib produced by the processes described herein is a homogenous solution of ibrutinib and DMSO which may be directly used in the formation of the amorphous polymorph. In some embodiments, the isolated ibrutinib is solid ibrutinib. The solid ibrutinib may also be used in the formation of amorphous ibrutinib.

Abstract: The present invention relates to a nanoformulated self-assembled pharmaceutical composition for photodynamic therapy. More particularly, the present invention is directed to a self-assembled pharmaceutical composition for photodynamic therapy comprising a photosensitizer, a ligand A which is separated at a specific pH range, and a ligand B of which surface charge changes at a specific pH range and a method for manufacturing the same.

Abstract: The invention relates to the treatment and prevention of cancers, including blood-based cancers and breast cancers, by administering agents that inhibit the activity of microRNAs, including miR-22. Inhibitors can include oligonucleotides that are at least partially complementary to these miRNAs. In some embodiments, these inhibitors are chemically modified oligonucleotides, including locked nucleic acids (LNAs).

Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.

Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

Abstract: Disclosed herein are pharmaceutical compositions, methods and kits for lowering the serum uric acid level of a subject and for the treatment of a condition associated with elevated serum uric acid levels comprising administering a composition comprising a first urate-lowering agent and a second urate-lowering agent. In some aspects the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salts thereof. In some aspects the second urate-lowering agent is an inhibitor of uric acid production, a uricosuric agent, a uricase, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

Abstract: Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.

Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: The invention relates to the combined use of a PDE4 inhibitor with a HMG-CoA reductase inhibitor for the prevention and curative treatment of an inflammatory pulmonary disease.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: Disclosed are pharmaceutical compositions comprising, bucillamine, including bucillamine and allopurinol or colchicine, or pharmaceutically acceptable salts or solvates thereof, together with one or more pharmaceutically acceptable carriers, diluents and excipients. Methods for use of the said compositions in the treatment of gout and metabolic syndrome are also disclosed.

Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: There is provided inter alia 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide in the form of a solid crystalline hydrate and in solid crystalline anhydrous form. There are also provided dry powder pharmaceutical compositions for inhalation containing such solid crystalline forms.

Abstract: The present invention relates to the compound of formula (I) and to compositions comprising the same and to the use of the compound and to compositions of the compound in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compound.

Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.