Abstract: Pyrido[4?,3?:5,6]pyrimido[1,2-a]indole compounds are provided. The pyrido[4?,3?:5,6]pyrimido[1,2-a]indole compounds have the general formula: where R1 represents aryl, heteroaryl, aminoaryl, aminoheteroaryl, aminoalkyl, aminocycloalkyl, aryloxy, heteroaryloxy, or alkoxy; and R2 and R3 represent hydrogen, carboxyl, ester, amide, halogen, alkyl, aryl, hydroxyl, alkoxy, aryloxy, aminoalkyl, aminocycloalkyl, aminoaryl, or aminoheteroaryl. The compounds show inhibitory activity against CK2 enzyme, and may be used as anticancer agents.

Abstract: The application relates to a compound of Formula (I): which modulates the activity of ALK or SRPK, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which ALK or SRPK plays a role.

Abstract: This disclosure relates therapeutic compositions containing a compound of Formula Im: or a pharmaceutically acceptable salt thereof, wherein R1 is as defined herein.

Abstract: 1?-Cyano nucleoside analogs of Formula I and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Abstract: In certain embodiments, this disclosure relates to methods of treating or preventing nephrogenic diabetes insipidus comprising administering an effective amount of 1,1?-(dodecane-1,12-diyl)bis(cyclopropane-1-carboxamide), pharmaceutical salts or derivatives thereof, as described herein, to a subject in need thereof. in certain embodiments, the subject has been diagnosed with nephrogenic diabetes insipidus.

Abstract: Inhibitors of CDK9 that are pyrazolo[1,5-a]pyrimidine derivatives and salts thereof, corresponding to formula (I):

Abstract: Pyrido[4?,3?:5,6]pyrazino[1,2-a]indole compounds are provided. The compounds exhibit inhibitory activity against CK2 enzyme and may be used as anticancer agents. The compounds have the following general formula I: where R1 represents aryl, heteroaryl, aminoaryl, aminoheteroaryl, aminoalkyl, aminocycloalkyl, aryloxy, heteroaryloxy, or alkoxy; and R2 and R3 represent hydrogen, carboxyl, ester, amide, halogen, alkyl, aryl, hydroxyl, alkoxy, aryloxy, aminoalkyl, aminocycloalkyl, aminoaryl, or aminoheteroaryl.

Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure relates generally to compounds of formula (I) or a pharmaceutically acceptable salt, prodrug, deuterated analog, tautomer, stereoisomer, or mixture of stereoisomers thereof and their use as LRRK2 inhibitors.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.

Abstract: The present disclosure provides a compound of Formula (I) or pharmaceutically acceptable salts thereof, a composition comprising the compound, methods of using the compound for the treatment of various disorders associated with HPK1, and methods of preparing these compounds.

Abstract: This invention relates to compounds of Formula (I): and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein L1, L2, R1, R2, R3 and n are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.

Abstract: The present disclosure provides CFTR modulator and phosphodiesterase 4 (PDE4) inhibitor compounds of the formula (Ia): and compositions including said compounds. The compounds can provide functionality for modulating CFTR, methods for treating an eye disease or disorder, and methods for treating CFTR-related indications. The present disclosure also provides methods of using said compounds and compositions for inhibiting PDE4 in a biological system or biological sample, for treating an inflammatory disease or disorder, and for treating other PDE4-related indications. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.

Abstract: The present disclosure provides small molecule drugs and pharmaceutical compositions for the treatment and prevention of diseases related to the formation of A?42 oligomers in a subject. It further provides a method of reducing formation of or disrupting A?42 oligomers in a subject, the method comprising the step of administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition.

Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.

Abstract: Compounds are provided herein. In general, the compounds are substituted pyrrolo[2,3-d]pyrimidines. The compounds can be used as inhibitors for multi-resistant cancers. Also provided herein are methods of forming the compounds, methods for inhibiting aurora kinase A and/or aurora kinase B activity and epidermal growth factor activity, methods of treating, ameliorating, or preventing cancer, and uses of the compounds for inhibiting aurora kinase A and/or aurora kinase B activity and epidermal growth factor receptor kinase activity. The compounds are generally of the formulas as illustrated herein, including those of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: X1 is N; X2 is N; X3 is —NH—; X4 is N or CR2; X5 is CH or CCH3; L1 is —NR4—R1; L2 is NH2 or H; R1 is: R2 is a 5-membered heteroaryl; R4 is H; R5 is as described herein; and m is 1, 2, 3, 4, or 5.

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I), (II) and (III). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Abstract: The present invention provides a fused heteroaryl compound having a CaMKII inhibitory action, which is expected to be useful as an agent for the prophylaxis or treatment of cardiac diseases (particularly catecholaminergic polymorphic ventricular tachycardia, postoperative atrial fibrillation, heart failure, fatal arrhythmia) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.

Abstract: Described herein are tricyclic PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors.