Abstract: Disclosed is an ozanimod addition salt crystal, which is provided with one or more improved characteristics compared with a known ozanimod solid form. Also disclosed are a preparation method for the ozanimod addition salt crystal, a pharmaceutical composition of same, and uses thereof in preparing a medicament for diseases or disorders medically requiring optional regulation, activation, excitement, inhibition or antagonism of sphingosine-1-phosphate receptor.

Abstract: This present application disclosed a method for the treatment of treating pain, opioid dependence, alcohol use disorder or autism comprising the step of administering to a mammal in need thereof a therapeutically effective amount of one or more compounds of formula (I), or a pharmaceutically acceptable salt thereof, and one or more carriers, diluents, or excipients. Those compounds are selective adenylyl cyclase 1 (AC1) inhibitors, which may provide an effective method of treatment for chronic/inflammatory pain, and prevent opioid dependence and/or reduce opioid dependence.

Abstract: Disclosed is a polymerizable compound useful for preparing a polymer that enables the production of a film, such as an optical film, which has a good balance of lightness and saturation and which can improve reverse wavelength dispersion on the short wavelength side while achieving reverse wavelength dispersion on the longer wavelength side. The polymerizable compound of the present disclosure is represented by: where in the formula (I-1), A1 and A2 each independently represent an aromatic group which may have a substituent, B1 and B2 each independently represent a cyclic aliphatic group which may have a substituent, or, an aromatic group which may have a substituent, and p and q each independently represent an integer from 0 to 2.

Abstract: The invention relates to a compound of general formula (I): wherein R1, R2, R3, R4, Q, m and n are as defined herein. The compounds are inhibitors of Bcl-3 and are useful for the treatment of cancer, particularly metastatic cancer.

Abstract: The present invention describes thymoquinone compounds formula (I): (i) These compounds have been identified as being useful in the treatment of cancer.

Abstract: The present invention describes thymoquinone compounds formula (I): (i) These compounds have been identified as being useful in the treatment of cancer.

Abstract: The present invention refers to a process for reacting an alkyl aryl ketone obtaining thereby the corresponding aryl oxirane or ?-functionalized alkyl aryl ketal, the aryl oxirane or ?-functionalized alkyl aryl ketal obtained by the process as well as the ?-functionalized ketone obtained by the process.

Abstract: The present disclosure, in at least certain embodiments, is directed to shikimate (shikimic acid) analogues and compositions thereof, devices and kits which contain the shikimate analogues or compositions thereof, and methods of use of the compounds and compositions for treating and neutralizing irritant or odoriferous compounds on animate or inanimate surfaces or in atmospheres. Examples of such irritant and odoriferous compounds include urushiols from poison ivy, oak, and sumac and mercaptans of skunk spray.

Abstract: This invention relates to a process for preparing (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (I) any of its individual enantiomers or any non-racemic mixture thereof, comprising the steps of (a) reacting (±)-2-exo-hydroxy-1-methyl-4-isopropyl-7-oxabicyclo[2.2.1]heptane of the formula (II) any of its individual enantiomers or any non-racemic mixture thereof with a 2-Methylbenzyl compound of the formula (III) wherein X is a leaving group in the presence of at least one base capable of forming water or a C1-C4 alkyl alcohol under the reaction conditions, and at least one inert organic solvent, and (b) simultaneously removing water, the C1-C4 alkyl alcohol or any mixture thereof from the reaction mixture.

Abstract: The present invention relates to the preparation of compounds of Formula I, including thapsigargin, nortrilobolide and 8-O-debutanoyl-thapsigargin from commercially available (R)-(?)-carvone via synthetic intermediate compound of formula 12 by pinacol coupling and in situ lactonization.

Abstract: The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.

Abstract: Disclosed are compounds, for example, compounds of formula I, wherein R, R0, R1-R8, n, X, Y, Y?, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

Abstract: The present invention relates to a composition comprising: (a) at least one compound of thiolactone type, and (b) one or more solvents, which may be identical or different, chosen from polar (non-)protic organic solvents; the pH of said composition being less than or equal to 7.

Abstract: Described herein arc 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein arc methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

Abstract: Benzazepine compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed benzazepine compounds are useful, among other things, in the treating of cancer and modulating TLR8. Additionally, benzazepine compounds incorporated into a conjugate with an antibody construct are described herein.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.

Abstract: Compounds having the following Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use and preparation are disclosed:

Abstract: The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein.

Abstract: The present invention relates to a selective method for carrying out the Buchwald-Hartwig coupling of biphenyl derivatives.

Abstract: Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.

Abstract: The present invention relates to 6-amido-1H-indol-2-yl compounds which can act as aryl hydrocarbon receptor (AhR) modulators and, in particular, as AhR antagonists. The invention further relates to the use of the compounds for the treatment and/or prophylaxis of diseases and/or conditions through binding of said aryl hydrocarbon receptor by said compounds.

Abstract: Provided are a pyrimidine compound represented by Formula 1, a method of preparing the compound, and a pharmaceutical use of the compound for the prevention or treatment of cancer.

Abstract: Disclosed are a small-molecule AURKB inhibitor and applications thereof. The invention is directed to a diindolylmethane compound of formula (I) or a stereoisomer, a tautomer, a solvate, a prodrug, a N-oxide or a pharmaceutically acceptable salt thereof. The invention also provides an application of the small-molecule inhibitor and a modified derivative thereof (such as a stereoisomer, a tautomer, a solvate, a prodrug, an N-oxide or a pharmaceutically acceptable salt) in the preparation of an antitumor drug. The small-molecule AURKB inhibitor identified herein is slightly toxic to those normal cells and can significantly inhibit the expression of a downstream gene E2F2 mediated in the phosphorylation of an AURKB substrate histone H3S10. Therefore, the small-molecule inhibitor, as an anti-tumor drug, can effectively inhibit the proliferation of various tumor cells and induce the apoptosis of tumor cells.

Abstract: The present invention relates to a process for synthesis of Eliglustat and intermediate compounds thereof. In particular, the present invention belongs to the field of synthesis of organic compounds, relates to a process for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and relates to the intermediate compounds used in the process and a process for preparation of the intermediate compounds. Compared with the existing synthetic processes, the process for preparing Eliglustat according to the present invention utilizes novel intermediates and steps for synthesis, has advantages of convenient operations, high yield, good purity of intermediates and desired product, and it is easy to apply the process in the industrial production.

Abstract: This invention relates to compounds which are used in the preparation of the compound of formula (II).

Abstract: The present disclosure relates to a composition for analysis of DNA sequences and a method for analysis of DNA sequences by using the same and, more particularly, to a composition comprising the compound represented by Chemical Formula 1 and a method for analysis of DNA sequences, the method comprising a step of treating a sample with the same. The compound represented by Chemical Formula 1 in which TAMRA is linked to polypyrrole specifically binds an A/T base pair (W) to fluoresce alone without causing DNA photocleavage. Therefore, the compound is useful for DNA analysis particularly at the single DNA molecule level.

Abstract: Disclosed are compounds of formula (I) wherein A is CH or N, B is CR or N; and D is CR; R represents hydrogen, OH or NH2; R1 and R2, independently of each other, represent hydrogen, N(R3)2, halogen, cyano, nitro, R4-C1-C4alkyl, R4-C1-C4halogenoalkyl, OH, R4-C1-C4alkoxy, R4-C1-C4halogenoalkoxy, SH, R4-C1-C4alkythio, R4-C1-C4halogenoalkylthio; R3 represents, independently at each occurrence, hydrogen, R4-C1-C4alkyl or R4-C1-C4halogenoalkyl; R3a represents, independently at each occurrence, hydrogen or C1-C4 alkyl; R4 represents, independently at each occurrence, hydrogen, halogen, cyano, OH, SH, NH2, NH(CH3) or N(CH3)2; X represents a group of formula -E- or -E-F—, wherein E and F are different from each other and represent a group selected from —C(R3a)2-, —(C?O)—, —NR3a- and —O— and F is linked to Y, with the proviso that if X represents -E-F— one of E or F represents —C(R3a)2— or —(C?O)—; Y represents a group selected from C1-C6alkyl, mono- or bicyclic C3-C11cycloalkyl, which may be partially unsaturated, mon

Abstract: A condensed cyclic compound represented by Formula 1: Ar1-L1-Ar2??Formula 1 wherein, in Formula 1, Ar1, Ar2, and L are the same as described in the specification.

Abstract: The invention provides compounds of the formula: (A), pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds, salts, or compositions to treat hyperphosphatemia, chronic kidney disease, and/or the cardiovascular disease associated with chronic kidney disease.

Abstract: Compounds of formula (I) as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.

Abstract: The present invention relates to novel piperazine derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially for targeted therapy treatment of hyperproliferative disorders, including benign hyperproliferative disorders, cancer and pre-cancer conditions.

Abstract: The present invention relates to a novel heteroaryl compound, an enantiomer, a diastereomer or a pharmaceutically acceptable salt thereof, and an antiviral composition comprising the same as an active ingredient. The novel compounds represented by formula (I) or formula (II) according to the present invention are remarkably superior in antiviral activity against an influenza virus, and furthermore, have low cytotoxicity and thus low adverse effects on a human body. Therefore, a pharmaceutical composition containing the same as an active ingredient can be effectively used for the prevention or treatment of diseases caused by an influenza virus infection.

Abstract: The present invention relates to compounds of formula (I) wherein A1, A2, A3, A4, R1, R2, R3, R4 and n are as defined in claim 1; or a tautomer, isomer, enantiomer, salt or N-oxide thereof; to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.

Abstract: A method of providing spatial diversity for critical data delivery in a beamformed mmWave small cell is proposed. The proposed spatial diversity scheme offers duplicate or incremental data/signal transmission and reception by using multiple different beams for the same source and destination. The proposed spatial diversity scheme can be combined with other diversity schemes in time, frequency, and code, etc. for the same purpose. In addition, the proposed spatial diversity scheme combines the physical-layer resources associated with the beams with other resources of the same or different protocol layers. By spatial signaling repetition to avoid Radio Link Failure (RLF) and Handover Failure (HOF), mobility robustness can be enhanced. Mission-critical and/or time-critical data delivery can also be achieved without relying on retransmission.

Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.

Abstract: The present invention relates to 3-carboxylic acid pyrrole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

Abstract: Compounds comprising quinazolinone derivatives and methods of identification and use of imaging agents. The compounds have the general formula I: wherein R2 is selected from halogen, halosubstituted alkyl, alkyl, hydroxyl-alkyl, and amino-alkyl; X is selected from ester, carbonyl or —CH2—; R1 is selected from mono-, or bicyclic aromatic or heteroaromatic ring systems, wherein the mono-, or bicyclic aromatic or heteroaromatic ring systems are optionally substituted by halo, alkyl, nitro, alkoxy, amino; R3 is selected from one or two halo, halosubstituted alkyl, alkyl, nitro, hydroxyl-alkyl, and alkyl tosylate; or a pharmaceutically acceptable salt thereof. The compounds of the present invention may be used for detection, diagnosis and/or staging of prostate or other forms of cancer, and may also be used for cardiac disease.

Abstract: The present invention provides Formula (1) compounds that are gamma-carbolines, Formula (1) wherein R1 a, R1 b, R1 c, R1d, R2, R3, and “-” are as defined herein; veterinary acceptable salts thereof, and stereoisomers thereof, which act as parasiticides, in particular, endoperasiticides.

Abstract: Disclosed in the present invention are a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and also disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.

Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

Abstract: Compounds of Formula I and II have been prepared for use in the treatment of diseases, disorders or conditions treatable by activation of the stimulator of interferon genes (STING) adaptor protein, such as in the treatment or prevention of cancers.

Abstract: A method of recovering a highly pure hydrocodone base from an impure hydrocodone preparation includes contacting the impure hydrocodone preparation with a weak acid in water to form a solution and adding a strong base to the solution in an amount sufficient to precipitate the pure hydrocodone base product. A highly pure hydrocodone base comprises less than 0.0025 wt % codeinone.

Abstract: The present invention describes compounds comprising at least one structural element having at least three fused aromatic or heteroaromatic rings (AR) and at least one structural element having an aromatic or heteroaromatic valerolactam (AV), especially for use in electronic devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.

Abstract: Disclosed are an azaphenalene-3-one derivative, its preparation method and its application, in the field of pharmaceutical synthesis. The derivative has the following Formula (I), wherein R is H, 2-fluoroethylamino, 2,2,2-trifluoroethylamino, diethylamino, pyrrolidinyl, imidazolyl, piperidinyl, morphinolinyl, 4-methylaminopiperidinyl, 4-dimethylaminopiperidinyl, (1-methylpiperidin-4-yl)methylamino, (1-phenylpiperidin-4-yl)methylamino, (1-benzylpiperidin-4-yl)methylamino, or 7-fluoro-3,4-dihydroisoquinoline-2(1H)-yl. The preparation method of the azaphenalene-3-one derivative is simple, the yield is high, post-treatment is easy, and purity is high. The derivative has high inhibitory activity against PARP enzyme. It establishes a foundation for researching better anti-tumor drugs using PARP inhibitors.

Abstract: Disclosed are co-crystals of 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, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the co-crystals, as well as methods of using co-crystals, 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: Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

Abstract: The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n=2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein R2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R3 is hydrogen or halogen; -( ) m - is —(CH2)m— or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-in-farct dementia, dementia pugilistica or Down syndrome.

Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection or a disease linked to impaired or abnormal autophagy.