Abstract: Provided are telomerase inhibitor compounds. Some compounds include a lactone or lactam group that is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In other cases, a sulfonamide-containing moiety is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In some embodiments, the telomerase inhibitor compound has a vinyl sulfonamide group bonded to an amide moiety and an aromatic group. In other cases, the inhibitor compound has an isothiazolidine 1,1-dioxide core that is bonded to a phenyl group. Aspects of the invention also include pharmaceutical compositions comprising the subject telomerase inhibitor compounds, as well as methods of treating telomerase-related diseases or conditions.

Abstract: Solid forms of a dual RAF/MEK inhibitor, pharmaceutical compositions thereof, oral dosage forms thereof, and methods of treating cancer are described herein. Also provided herein are processes for preparing solid forms of a dual RAF/MEK inhibitor and pharmaceutical compositions and oral dosage forms thereof.

Abstract: Disclosed are organic compounds including a structure of formula (I). Also provided are mixtures containing a first organic compound (H1) and a second organic compound (H2), the first organic compound (H1) includes at least one of the organic compound. Further provided are organic electronic devices containing the organic compounds or the mixtures. By means of device structure optimization, improved device performance can be achieved, specifically, a high-performance OLED device can be implemented, improved material and manufacturing technical options are provided for full-color display and lighting applications.

Abstract: The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being: where: R independently represents a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a —NR1R2 group, or a (C1-C3)alkoxy group; R? is a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —NO2 group, a (C1-C3)alkoxy group, or a —NR1R2 group; and R1 and R2 are a hydrogen atom or a (C1-C3)alkyl group.

Abstract: A compound of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, which can be used as fungicides.

Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1X2 and X3 are N; Y is N or CH; R1 and R2 are independently of each other (iii) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fhioroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(0)0-C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6- selected from Ci-C3alkylene optionally substituted with 1 to 4 F, —CH2-0-CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (iv) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence Ci-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3 alkyl, C3-C

Abstract: Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.

Abstract: A compound of formula (I) and a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, or a pharmaceutical composition containing same, and the use thereof as an AAK1 inhibitor in the preparation of a drug for treating related diseases.

Abstract: The present invention provides a heterocyclic compound having a HDAC6 inhibitory action, which is useful for the treatment of central nervous system diseases including neurodegenerative diseases, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.

Abstract: The invention relates to novel compounds of the general formula (1-A) as defined in the application and pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders leading to increased iron levels or increased iron absorption, and/or iron overload.

Abstract: Provided are novel crystalline forms of Lanifibranor (Referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline forms, and uses of the crystalline forms for preparing pan-PPAR agonists drugs and drugs for treating NASH. Compared with prior arts, the provided crystalline forms of Compound I have one or more improved properties, which solve the problems of the prior art and is of great value to the optimization and development of the drugs.

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

Abstract: The present invention provides a process for the preparation of compound of Formula I, The present invention also provides intermediates formed during the preparation of the compound of Formula I.

Abstract: N-(3-substituted thiazaheterocyclylidene)-1H-pyrrolo[2,3-b]pyridine-3-carboxamides, N-(3-substituted thiazaheterocyclylidene)-1H-pyrrolo[2,3-b]pyridine-4-carboxamides and N-(3-substituted thiazaheterocyclylidene)-1H-pyrrolo[3,2-b]pyridine-1-carboxamides wherein the ring designated Q or Q? is a five-, six-, or seven-membered heterocycle containing one sulfur and one nitrogen are disclosed. The compounds activate Yap and inhibit Lats kinases. They are therefore useful for treating hearing loss.

Abstract: Provided herein are novel compounds, for example, compounds having a Formula (I), or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising the same. Also provided herein are methods of preparing the compounds and methods of using the compounds, for example, in treating cancer.

Abstract: This disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3K?). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) PI3K? activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

Abstract: The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, optical isomer, and/or N-oxide thereof. The invention also relates to the processes for the preparation of those compounds, pharmaceutical compositions comprising those compounds, and the uses of those compounds in treating diseases or conditions associated with inflammatory bowel disease (IBD), in particular ulcerative colitis (UC) and Crohn's disease (CD).

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R1 is C1-C3alkyl optionally substituted with F, C3-C6cycloalkyl, C1-C3alkoxy; X represents a bond or C1-C3alkylene optionally substituted with OH, ONO, ONO2; R2 is H, OH, ONO, ONO2, C(O)OH, C(O)OC1-C3alkyl, CHO, CN, C1-C3alkoxy, OC(O)H, OC(O)—C1-C3alkyl, C(O)N(R6)OR7, OC1-C3alkylene-C(O)OH, OC1-C3alkylene-C(O)OC1-C3alkyl, OC1-C3alkylene-C(O)N(R6)OR7, S(O0-2)C1-C3alkyl, CR8?N—OR9, CR8?N—NR10R11, CR8?NR12 or CR8?N—ONO2; R3 is C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, C1-C3alkoxy, C3-C6cycloalkyl; C3-C6cycloalkyl, C2-C6alkenyl, C2-C6alkynyl; R4 is C1-C6alkyl optionally substituted with C3-C6cycloalkyl, C1-C6alkoxy, F, ONO, ONO2; C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl; R5 is H, SO2N—R13R14, NHSO2NR13R14; R6 is H or C1-C3alkyl; R7 is H, C1-C3alkyl, C1-C3alkoxy, C1-C3alkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or said het

Abstract: Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide, including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the compound, as well as methods of using the compound, 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 present invention relates to compounds for degradation of cyclin-dependent kinase 7 (CDK7). The present invention also relates to pharmaceutical compositions comprising such compound(s). Furthermore, the present invention also relates to uses of such compound(s) or of such pharmaceutical compositions in a method of prevention and/or treatment of a disease associated with inhibition of apoptosis, abnormal transcriptional activity and/or cell cycle arrest by aberrant activity and/or overexpression of one or several cyclin-dependent kinases (CDKs), in particular cyclin-dependent kinase 7 (CDK7). Moreover, the present invention relates to methods of preventing and/or treating a disease which is associated with inhibition of apoptosis, abnormal transcriptional activity and/or cell cycle arrest by aberrant activity and/or overexpression of one or several cyclin-dependent kinases (CDKs), in particular cyclin-dependent kinase 7 (CDK7).

Abstract: This disclosure relates to compounds of Formula (A): IRAK-L-DSM (A), or a pharmaceutically acceptable salt thereof, wherein DSM is a degradation signaling moiety that is covalently attached to the linker L, L is a linker that covalently attaches IRAK to DSM; and IRAK is an IRAK4 binding moiety represented by Formula (I) that is covalently attached to linker L; in which all of the variables are as defined in the application. Compounds or pharmaceutically acceptable salts thereof as described herein are capable of activating the selective ubiqitination of IRAK4 proteins via the ubiquitin-proteasome pathways (UPP) and cause degradation of IRAK4 proteins. The present disclosure also provides methods of treating disorders responsive to modulation of IRAK4 activity and/or degradation of IRAK4 with at least one compound described herein.

Abstract: Disclosed herein are, inter alia, compounds inhibiting activity of pseudouridine synthase (PUS) and methods of use thereof for treating PUS associated conditions or disorders.

Abstract: A hydrochloride salt of inupadenant, pharmaceutical compositions thereof, methods of making pharmaceutical compositions of a hydrochloride salt of inupadenant (e.g., crystalline hydrochloride salt of inupadenant) and methods of using the pharmaceutical compositions in combination with carboplatin and pemetrexed in the treatment of non-small cell lung cancer (NSCLC), including squamous NSCLC and nonsquamous NSCLC.

Abstract: The present invention provides compounds of the formula: wherein A, Z, G, R1, R2, and R4 are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and pharmaceutically acceptable salts thereof for treating patients for cancer.

Abstract: The present invention relates to radiolabelled 4-(furo[3,2-c]pyridin-4-yl) derivatives and their use as radioactive tracers, and in particular their use as imaging agents.

Abstract: The present invention belongs to the field of medicine and relates to a method for preparing pranoprofen. The present invention also relates to a composition containing pranoprofen and impurities, a quality control method, an intermediate compound for synthesizing pranoprofen and a preparation method thereof. The method of the present invention overcomes the deficiencies of the prior art, shortens the synthetic route, lowers the requirements of process conditions, simplifies the process operation, improves labor safety, is more suitable for industrial production, is more environmentally friendly and has higher yield.

Abstract: The present application provides two dimensional benzo[4,5]imidazo[2,1-a]isoindole incorporated non-fullerene electron acceptors having the structure of Formula I (I), and processes for the synthesis and manufacture thereof. Also provided are semiconductor materials, polymers, oligomers, films and membranes incorporating the non-fullerene acceptor of Formula (I), and the optoelectronic devices made therefrom.

Abstract: In an embodiment, the present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type II diabetes mellitus.

Abstract: The present invention is directed to compounds of formula IIa These compounds are considered useful for the treatment of diseases associated with leucine-rich repeat kinase 2 (LRRK2) such as Parkinson's disease. Furthermore, the invention relates to pharmaceutical compositions comprising said compounds.

Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Abstract: Embodiments provide a polycyclic compound and a light emitting element that includes the polycyclic compound. The light emitting element includes a first electrode, a second electrode facing to the first electrode, and at least one functional layer disposed between the first electrode and the second electrode, wherein the at least one functional layer includes the polycyclic compound. The polycyclic compound is represented by Formula 1, which is explained in the specification.

Abstract: There is provide herein a compound of Formula (3): wherein R1, R2, R3, R4, R5, R6, and R7 are each independently H or an organic group.

Abstract: A phosphorus-containing flame retardant is produced by reacting at a reaction temperature a mixture including a metal or suitable metal compound and a stoichiometric excess relative to the metal or suitable metal compound of an unsubstituted or alkyl or aryl substituted phosphonic or pyrophosphonic acid, wherein the phosphonic or pyrophosphonic acid is in a molten state at the reaction temperature. The chemical composition of the resulting flame retardant product leads to excellent flame retardancy and exhibits high thermal stability. The presently disclosed flame retardants are useful, for example, in polymer compositions, particularly thermoplastics processed at high temperatures, over a wide range of applications.

Abstract: This invention relates to a compound comprising a structure of formula (I): cyclic disulfide moiety-phosphorus coupling group (I). The cyclic disulfide moiety has the structure of (C-I), (C-II), or (C-III). This invention also relates to an oligonucleotide comprising one or more compounds that comprise the structure of formula (I), wherein at least one phosphorus coupling group contains a nucleoside or oligonucleotide. The invention also relates to a pharmaceutical composition comprising the oligonucleotide described herein and a method of reducing or inhibiting the expression of a target gene by administering to the subject a therapeutically effective amount of the oligonucleotide described herein.

Abstract: The present disclosure provides phosphonate-containing heterocycle compounds with TYK2 kinase inhibitory activity, pharmaceutical compositions comprising the same, and applications thereof. The present disclosure provides compounds of Formula (I), as inhibitors of TYK2 kinase. These compounds can be used for preventing and/or treating TYK2 kinase-related diseases and/or conditions.

Abstract: Molybdenum(0) coordination complexes comprising ligands which each coordinate to the metal center by nitrogen or phosphorous are described. Methods for depositing molybdenum-containing films on a substrate are described. The substrate is exposed to a molybdenum precursor and a reactant to form the molybdenum-containing film (e.g., elemental molybdenum, molybdenum oxide, molybdenum carbide, molybdenum silicide, molybdenum nitride). The exposures can be sequential or simultaneous.

Abstract: Provided are organometallic compounds wherein a boron containing group bridges two monocyclic or fused polycyclic ring systems each independently comprised of one or more 5-membered or 6-membered rings. Also provided are formulations comprising these organometallic compounds. Further provided are organic light emitting devices (OLEDs) and related consumer products that utilize these organometallic compounds.

Abstract: The present disclosure relates to ansa-metallocene catalyst compounds, catalyst systems comprising such compounds, and uses thereof. In some embodiments, a catalyst compound is represented by Formula (I): TyLAMXn-2 ??(I), wherein: M is a group 3-6 metal; n is the oxidation state of M; A is a monocyclic or polycyclic arenyl ligand bonded to M and is substituted by at least one phenanthridin-5-yl substituent; L is a monocyclic or polycyclic arenyl ligand bonded to M; T is a bridging group; y is 1 or 0; and each X is independently a univalent anionic ligand, or two Xs are joined and bound to M to form a metallocycle ring, or two Xs are joined to form a chelating ligand, a diene ligand, or an alkylidene ligand.

Abstract: A new method for producing D-allulose crystals that allows for a continuous production process and ensures a high yield. Also, new D-allulose crystals. Further, the use of a nanofiltration unit in a method for producing D-allulose crystals to improve the yield and/or quality of the resulting crystals.

Abstract: Oligomers prepared from a bicyclic nucleoside having the formula (I) shown below: in which each of T1 and T2 is independently OR1 or OR2; R1 is H or a hydroxyl protecting group, R2 is a phosphorus moiety; and Bx is a nucleobase. The compounds, bicyclic nucleosides and oligomers are useful for the prevention, treatment or diagnosis of muscular dystrophy.

Abstract: The invention provides a compound of formula (I): or a salt thereof, wherein R1, R2, R3, B, X, and Y have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as TET inhibitors, epigenetic modulators, and for treating cancer, eating disorders, and as adjuvants in cancer immunotherapy.

Abstract: The invention provides 7-substituted 7-deazaadenine-containing 2?,3?-cyclic dinucleotides of general formula I, wherein R is selected from the group comprising C1-C5 alkyl; C6-C16 aryl, optionally substituted by at least one substituent selected from C6-C16 aryl or (C6-C16 aryloxy) C1-C5 alkyl; C4-C12 heteroaryl, comprising at least one O atom; C4-C12 heteroaryl, comprising at least one S atom, and pharmaceutically acceptable salts thereof. The compounds according to the invention show strong activation of protein STING (stimulator of interferon genes) and, consequently, stimulation of the signal transduction pathway that induces interferons and other cytokines/chemokines.

Abstract: Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. These compounds are conjugates of glucocorticoids with rho-kinase inhibitors. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.

Abstract: Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R19, R5, R3a, R1a, R1b, R2a, R2b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R12a, R12b, R18, RD, and q are defined herein. L is selected from the group consisting of: wherein A indicates the point of attachment at C17 and wherein X is selected from the group consisting of —C(0)N(R55a)(R55b), —N(R55a)(R55b), —N(R55b)C(O)(R55a), and R55C wherein R55c is carbon-bound substituted or unsubstituted heteroaryl or substituted or unsubstituted aryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Abstract: The present invention relates to a new process for the preparation of budesonide 21-phosphate and its disodium salt.

Abstract: The present invention relates to purification process of pharmacologically active IgG1 containing protein comprising at least affinity chromatography followed by mixed-mode chromatography. The present invention provides cytotoxic T-lymphocyte-associated 4-immunoglobulin (CTLA4-Ig) fusion protein by using at least affinity chromatography, mixed-mode chromatography and optionally one or more suitable purification steps that provides purified composition of the fusion protein, substantially free of impurities selected from Pre-Peak, product and process related impurities. Further, the present invention provides highly purified CTLA4-Ig fusion protein with reduced heterogeneity.

Abstract: The present invention discloses a method of preparing procollagen from freshwater fish. The method comprises the following steps: pressure treatment, physical crushing, mixing and emulsification, homogenization, refrigeration, cleaning, extraction, homogenization, inactivation, homogenization, and filtration. In the mixing and emulsification step, freshwater fish tissue containing collagen is mixed with a surfactant to remove endotoxins to below 0.25 EU/ml. The procollagen is extracted following the step of adding enzymes and an acid solution of pH 3 to 6 to the pretreated tissue. The pretreatment of freshwater fish tissue in this invention can effectively reduce the endotoxins to below 0.25 EU/ml. The extraction technique of this invention can extract and retain greater amounts of procollagen while increasing its denaturation temperature and preserving the intact, tightly twisted triple-helix bonds of type I procollagen.

Abstract: Disclosed herein are peptides useful for targeting the retina, and may be useful for targeting specific cells in the retina. The peptides may have a Formula I or V: R1—X1—X2—(X3)n—X4—X5—X6—X7—R2?? Formula I R1-Asn-Val-Ser-Ala-Tyr-Pro-Thr-R2?? Formula V. Also disclosed are conjugates and compositions comprising the peptides. The compositions may comprise a desired agent to be delivered to the retina, such as a therapeutic agent and/or an imaging agent. Methods for administering the peptide, conjugates, and/or composition to a subject also are disclosed.

Abstract: Aperlinergic macrocyclic compounds are provided. In particular, a compound of formula (II): or a stereoisomer or a mixture thereof, or a pharmaceutically acceptable salt, ester or solvate thereof is provided. Also provided is a method of using aperlinergic macrocyclic compounds of the disclosure for treating a cardiovascular disease in a subject in need thereof, comprising administering an effective amount of the compound to the subject.

Abstract: A proton pump modulator, and a use of the proton pump modulator in preparing a reagent. The reagent is used for improving learning ability, treating cognitive impairment, and/or treating neurodegenerative diseases. Also involved are an ATP6V1B2 modulator and a use thereof in preparing a reagent used for improving learning ability, treating cognitive impairment, and/or treating neurodegenerative diseases.