Patent classifications
C07D207/08
Therapeutic compounds and methods of use thereof
The invention provides compounds having the general Formula (I); ##STR00001##
and pharmaceutically acceptable salts thereof; wherein the variables R.sup.A, R.sup.AA, subscript n, subscript q, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Therapeutic compounds and methods of use thereof
The invention provides compounds having the general Formula (I); ##STR00001##
and pharmaceutically acceptable salts thereof; wherein the variables R.sup.A, R.sup.AA, subscript n, subscript q, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
BIODEGRADABLE COMPOUND, LIPID PARTICLES, COMPOSITION AND KIT COMPRISING LIPID PARTICLES
[Problem]
To provide a biodegradable compound having a structure decomposed in a cell, lipid particles containing the compound, and a pharmaceutical composition comprising the lipid particles.
[Solution]
The compound of the embodiment is represented by the formula (1): P[XRYR-Q].sub.2 (1). In the formula, P is an alkyleneoxy having an ether bond, X is a divalent linking group having a tertiary amine structure, R is a divalent linking group, R is a single bond or a C.sub.1 to C.sub.6 alkylene, and Q is a liposoluble vitamin residue, a sterol residue, or a C.sub.12 to C.sub.22 aliphatic hydrocarbon group. The structure of the compound contains at least one biodegradable group. From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.
INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
INHIBITORS OF THE N-TERMINAL DOMAIN OF THE ANDROGEN RECEPTOR
The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
Modulators of the integrated stress pathway
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
Modulators of the integrated stress pathway
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
LIPID STRUCTURES AND COMPOSITIONS COMPRISING SAME
The disclosure relates to ionizable lipids and compositions comprising the ionizable lipids. Lipid-nanoparticle compositions comprised of an ionizable lipid, optionally in combination with other lipid components such as helper lipids, stabilization lipids and structural lipids, and a therapeutic agent, such as a nucleic acid, for delivery to mammalian cells or organs are described.
Synthesis methods for upadacitinib and intermediate thereof
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), ##STR00001## wherein, R is a protective group of nitrogen atoms, and R.sub.1 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.
Synthesis methods for upadacitinib and intermediate thereof
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), ##STR00001## wherein, R is a protective group of nitrogen atoms, and R.sub.1 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.