Abstract: The present invention provides a novel chemical process for the synthesis of the compound N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxpyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide.

Abstract: The present disclosure relates to amorphous and crystalline forms of (R)-N-(4-chlorophenyl)-2-((1S,4S)-4-(6-fluoro-quinolin-4-yl) cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.

Abstract: The present invention is directed to 6,5-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl.

Abstract: The present invention provides for novel co-crystals of lenalidomide. The present invention particularly provides for novel cocrystals of lenalidomide with Resorcinol, Methyl paraben and Saccharin. The present invention also provides for the processes for the production of cocrystals of lenalidomide with Resorcinol, Methyl paraben and Saccharin. The present invention further provides for processes for the preparation of crystalline anhydrous lenalidomide Form IV.

Abstract: A method for preparing a tyrosine kinase inhibitor and a derivative thereof are described. In particular, the present method has a short synthesis route, low costs, easy operation, and is suitable for large-scale production.

Abstract: The present disclosure provides compounds represented by Formula I-A: A1-L1-B1 I-A and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein A1, B1, and L1 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a condition or disorder responsive to degradation of MDM2 protein such as cancer.

Abstract: The present invention relates to a co-crystal of roxadustat with L-proline and to a process for its preparation. Furthermore, the invention relates to a pharmaceutical composition comprising said roxadustat L-proline co-crystal, at least one pharmaceutically acceptable excipient and optionally at least one photostabilizing agent. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prevention of anemia in patients with end-stage renal disease (ESRD) and/or chronic kidney disease (CKD).

Abstract: The present disclosure relates to salts and crystalline forms of a compound having the formula (I): Also described are processes for the production of the salts and crystalline forms described herein.

Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.

Abstract: A compound represented by a formula (I), or a salt thereof: wherein Ar1 is a substituted or unsubstituted C6-10 aryl group, or the like; the number of X1 groups that can be substituted on Ar1 is 5 or less; X1 is a halogeno group, a substituted or unsubstituted C1-6 alkyl group, or the like; Z is a single bond, a sulfur atom, or an oxygen atom; A is a nitrogen atom or a carbon atom; X2 is a halogeno group, a substituted or unsubstituted C1-6 alkyl group, or the like; m is an integer of 0 to 2 when A is a nitrogen atom and is an integer of 0 to 3 when A is a carbon atom; R1 to R4 and R6 to R9 each independently represent a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or the like; R5 is a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or the like; k represents the number of CR6R7 moieties in a parenthesis and is 0 or 1; h represents the number of CR3R4 moieties in a parenthesis and is 0 or 1; and Ar is a substituted or unsubstituted C6-10 aryl group, or the like.

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract: An improved chemical process for the manufacture of the compound of Formula (I), which is useful, for example, as a late-stage chemical intermediate in the production of osimertinib (AZD9291) and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a method for producing 2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1,2,4-triazol-1-yl)propan-2-ol in high purity. Especially it relates to a method in which this compound is effectively separated from its 1,2,4-triazol-4-yl isomer.

Abstract: The present disclosure discloses substituted quinazoline compounds having a capacity to cross the blood-brain barrier. The compound has the structural formula represented by formula (I): The quinazoline compounds, derivatives and pharmaceutically acceptable salts thereof of the present disclosure have the ability to cross the blood-brain barrier and are capable of acting as a drug characteristic of a protein kinase inhibitor, in particular for the expression of a protein through a epidermal growth factor receptor and can be used to treat or prevent disorders associated with abnormal protein kinase activity, such as cancer, cancer with brain metastases, cancer with meningeal metastases, and neuroprotective diseases, and the like.

Abstract: Methods for synthesizing oleo-furan surfactants from fatty aldehydes and compositions of furan based surfactants synthesized from such methods are disclosed. One method of forming a surfactant can include a hydroxyalkylation reaction of two methylfuran molecules with a fatty aldehyde molecule to form a di-furan product. This method can also include forming a surfactant from the di-furan product formed from the hydroxyalkylation. In particular, this di-furan product can be a surfactant precursor that is functionalized to form a surfactant.

Abstract: The present invention provides crystalline Roxadustat Form-?, crystalline Roxadustat Form-?, process for the preparation of crystalline Roxadustat Form-?, crystalline Roxadustat Form-? and its pharmaceutical compositions thereof. The present invention also provides co-crystals of Roxadustat Form RLP, Roxadustat Form RNM and Roxadustat Form RU, process for their preparation and pharmaceutical composition thereof.

Abstract: Substituted -3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.

Abstract: The present invention relates to a coumarin (keto) oxime ester compound of formula (I), wherein n and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification. The compound has strong ultraviolet absorption in the range of 300 to 450 nm. After absorbing light energy, it can quickly transfer energy and continuously initiate polymerization. It has obvious advantages in terms of photosensitivity and pattern integrity, and is very suitable for radiation curing by UV-LED light source. In addition, the compound of formula (I) also has good thermal stability. The present invention also relates to a method for preparing the compound of formula (I) and use of the compound. The compound is suitable as a photoinitiator in a UV-LED light curing system and is suitable for the radiation wavelength of UV-LED light curing.

Abstract: Provided herein are novel monomethyl fumarate prodrugs.