Abstract: The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III), wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.

Abstract: A process of making Roxadustat of the following formula: comprising converting a compound of formula VI: to Roxadustat, wherein R is a C1-C20 alkyl group, and PG is a protective group.

Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.

Abstract: The present application relates to crystalline form 04, crystalline form 06, crystalline form D-1, and crystalline form D-2 of an antidepressant drug SAGE-217 and a preparation method therefor and a pharmaceutical composition containing same. The crystalline form 04 has an XRPD pattern with characteristic peaks at 2theta values of 11.6±0.2°, 13.5±0.2°, 16.2±0.2°, 16.5±0.2°, and 23.2±0.2°; the crystalline form 06 has an XRPD pattern with characteristic peaks at 2theta values of 8.7±0.2°, 10.0±0.2°, 13.2±0.2°, 15.0±0.2°, 15.8±0.2°, and 17.3±0.2°; the crystalline form D-1 has an XRPD pattern with characteristic peaks at 2theta values of 7.2±0.2°, 8.6±0.2°, 13.3±0.2°, 19.6±0.2°, and 23.0±0.2°; and the crystalline form D-2 has an XRPD pattern with characteristic peaks at 2theta values of 7.3±0.2°, 8.6±0.2°, 13.4±0.2°, 19.7±0.2°, and 23.3±0.2°. The novel crystalline forms provided by the present application have good stability, and provide more choices for drug development.

Abstract: The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.

Abstract: The present application provides a upadacitinib salt compound and a preparation method therefor. The salt involved in the method in the present application has an easy preparation operation, a cheap raw material easy to get, and a good purification effect on upadacitinib, and is beneficial to industrial production.

Abstract: The present invention relates to a method for preparing the compound of formula IV, compound of formula XI, and acalabrutinib, a new generation of bruton tyrosine kinase (BTK) inhibitor.

Abstract: The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III), wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.

Abstract: The present invention relates to amorphous and crystalline forms of valbenazine salt and the methods for their preparation.

Abstract: The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.

Abstract: The present invention relates to a method for preparing the compound of formula IV, compound of formula XI, and acalabrutinib, a new generation of bruton tyrosine kinase (BTK) inhibitor.

Abstract: Novel crystalline forms of lesinurad and its sodium salt, processes for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transporter 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.

Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.

Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.

Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.

Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.

Abstract: Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.

Abstract: Novel crystalline Forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3?-methyl-T-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.

Abstract: Novel crystalline Forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3?-methyl-T-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.

Abstract: Crystalline Form I of ibrutinib, processes for its preparation, pharmaceutical compositions comprising the new Form, and use of Form I of ibrutinib for treating or delaying diseases or disorders related to activity of Bruton's tyrosine kinase (BTK) proteins are disclosed. The novel Form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. It can be readily prepared and is suitable for use in the preparation of solid dosage forms.