Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: The present invention relates to a heterocyclic compound, a pharmaceutical composition containing the same, a preparation method thereof, and use thereof as a fibroblast growth factor receptor (FGFR) inhibitor. The compound is a heterocyclic compound as shown in Formula I, or a pharmaceutically acceptable salt, prodrug, solvent compound, polymorph, isomer or stable isotopic derivative thereof. The present invention further relates to use of the compound for the treatment or prevention of related diseases which are FGFR-mediated such as cancer, and a method for applying the compound to treat said diseases.

Abstract: The invention is concerned with the compounds of formula I: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Abstract: The present invention provides compounds, pharmaceutical compositions, methods of inhibiting ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.

Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Abstract: The present application relates to a novel and improved process for preparing 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives of the formula (I) in which R1A and R1B are independently selected from the group consisting of hydrogen, fluorine, chlorine, methyl, monofluoromethyl, difluoromethyl, trifluoromethyl, ethyl, methoxy, difluoromethoxy and trifluoromethoxy, to novel precursors for preparation thereof, and to the preparation and use of the crystalline polymorph I of (5-(4-chlorophenyl)-2-({1-(3-chlorophenyl)-5-[(1S)-1-hydroxyethyl]-1H-1,2,4-triazol-3-yl}methyl)-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one of the formula (I-A-1).

Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.

Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

Abstract: The present invention provides halogenated quinazolin-THF-amines as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Abstract: Disclosed herein are compositions and methods of treating osteroporosis, bone fracture, bone loss, and increasing bone density by administration of compounds of formula (I) or compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier, wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification.

Abstract: A compound of formula (I) where R1, R2, X, Y, n, m, R3, R4, R5, R6 and R7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.

Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein which exhibit strong inhibition effects on various cancer cell lines. The compounds disclosed herein are useful for the treatment of proliferative diseases, including neoplastic diseases such as cancer and non-neoplastic disorders such as rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing compounds of Formula I and at least one carrier, diluent or excipient and optionally one or more additional therapeutically active agents, including anticancer agents. This application also discloses methods for treating a proliferative disease, including neoplastic diseases such as cancer and non-neoplastic disorders such as rheumatoid arthritis.

Abstract: Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like: (wherein R1 represents furyl, R4, R5 and R6 are the same or different and each represents lower alkyl or aryl, R2 represents pyridyl or tetrahydropyranyl, and X1 represents halogen).

Abstract: Disclosed are compounds of Formula (I?), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

Abstract: Disclosed herein are compounds and compositions for treating or inhibiting RSV and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus, and methods of treatment or prevention thereof.

Abstract: Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

Abstract: The invention relates to compound of formula (I): A-X1-L-X2—B?? (I) and salts, solvates and tautomers thereof, which are useful as medicaments, in particular as anti-proliferative agents and for use as a drug in an antibody-drug conjugate; wherein A is a group selected from: X1 and X2 are independently selected from O, S, NR28, CR28R29, CR28R29O, C(?O), C(?O)NR28, NR28C(?O), C(O)—RA—C(O)—NH, C(O)—RA—NH—C(O), C(O)—NH—RA—C(O), NH—C(O)—RA—C(O), NH—C(O)—RA—C(O)—NH, NH—C(O)—RA—NH—C(O), C(O)—NH—RA—NH—C(O), C(O)—NH—RA—C(O)—NH, O—C(O) and C(O)—O or is absent; L is selected from an amino acid, a peptide chain having from 2 to 12 amino acids, a paraformaldehyde chain —(OCH2)1-24—, a polyethylene glycol chain —(OCH2CH2)1-12— and —(CH2)m—Y6—(CH2)n— wherein Y6 is selected from —(CH2)z— and a group (L1) a group (L1) that is selected from arylene, monocyclic heteroarylene, monocyclic cycloalkylene, monocyclic cycloalkenylene and monocyclic heterocyclylene groups optionally substituted with up to three optional subst

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

Abstract: Polycyclic derivatives of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Provided are certain fused tricyclic urea compounds and salts thereof, compositions thereof, and methods of use therefor.

Abstract: Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

Abstract: Compounds of formula (I): wherein R1, R2, R3, n and W are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring pro-apoptotic and/or anti-proliferative agents.

Abstract: Compounds of formula (I): wherein R1, R2, J, K, L, n and W are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring pro-apoptotic and/or anti-proliferative agents.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, 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 an improved process of preparation of idelalisib using a solid form of intermediate of formula (2); characterized by XRPD pattern having 2? values 5.5°, 10.9°, 14.3°, 16.9° (±0.2) the process comprising steps a. Reacting of compound of formula (1); ?with a chlorinating agent to obtain a product; b. Reacting of the product with (S)-2-((tert-butoxycarbonyl)amino)butanoic acid and a base, wherein pH of the reaction mixture is set between 7.5 and 10 to obtain compound of formula (2); c. Isolating a solid form of compound of formula (2); d. Transforming the compound of formula (2) into idelalisib.

Abstract: The present invention relates to novel quinazolinone derivatives inhibiting PI3K; a method for preparing the derivatives; and a pharmaceutical composition for treating hematologic neoplasms or liver diseases, containing the quinazolinone derivatives, wherein the novel quinazolinone derivatives according to the present invention have a beneficial effect in the treatment of hematologic neoplasms or liver diseases. Particularly, the quinazolinone derivatives inhibit PI3K? with high selectivity compared to that of a conventional anticancer drug of PI3K? inhibitors, thereby significantly reducing immunotoxicity, or simultaneously inhibit PI3K? and PI3K?, thereby enabling the treatment of autoimmune diseases, and anticancer therapy for blood cancer and the like. These targeted drugs have an advantage of enabling the problem of side effects of a conventional highly toxic anticancer therapy to be resolved.

Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.

Abstract: The present invention relates to new compounds of general formula (I) that show great affinity and activity towards the subunit ?2? of voltage-gated calcium channels (VGCC), especially ?2?-1 subunit of voltage-gated calcium channels or dual activity towards subunit ?2? of voltage-gated calcium channels (VGCC), especially ?2?-1 subunit of voltage-gated calcium channels, and noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

Abstract: The present invention provides novel CDK7 inhibitors and pharmaceutical compositions thereof: or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.

Abstract: The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.

Abstract: The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.

Abstract: The subject matter generally relates to compounds and methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

Abstract: The present invention provides a process for the preparation of darunavir or solvates or a pharmaceutically acceptable salt thereof substantially free of bisfuranyl impurities, particularly darunavir propionate solvate. The present invention also provides a process for preparation amorphous darunavir using the darunavir propionate solvate.

Abstract: Methods of making low odor choline salts of an organic compound, for example, choline ellagate compound(s), and uses and formulations thereof.

Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.

Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.

Abstract: The present disclosure provides for compounds of formula (I) wherein A2, A3, A4, A6, A7, A8, R15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.

Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

Abstract: The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

Abstract: The present invention relates to a method for preparing difluoroallylboronate and application thereof, and it belongs to a field of compound preparation. A method for preparing difluoroallyl borate ester is using a compound of the formula II and bis (pinacolato) diboron as raw materials in a solvent and in the presence of an iron catalyst and a base according to the following reaction formula, to obtain a compound of the formula I, The method of the present invention directly use an inexpensive, commercially available metal iron salt as a catalyst to provide a convenient, low-cost method for preparing difluoroallyl borate ester, and provide a new and effective approach for the synthesis of ?-aminobutyric acid receptor agonist (III).

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: A novel method and system for using certain tin compounds as dopant sources for ion implantation are provided. A suitable tin-containing dopant source material is selected based on certain attributes. Some of these attributes include stability at room temperature; sufficient vapor pressure to be delivered from its source supply to an ion chamber and, the ability to produce a suitable beam current for ion implantation to achieve the required implant Sn dosage.

Abstract: A tin compound, tin precursor compound for atomic layer deposition (ALD), a method of forming a tin-containing material film, and a method of synthesizing a tin compound, the tin compound being represented by Chemical Formula (I): wherein R1, R2, Q1, Q2, Q3, and Q4 are each independently a C1 to C4 linear or branched alkyl group.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

Abstract: This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands.