C07D487/12

Methods of treating lymphoma using thienotriazolodiazepine compounds
09968620 · 2018-05-15 · ·

A method of treating lymphoma in a mammal comprises the step of: administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R.sup.1 is alkyl having a carbon number of 1-4, R.sup.2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R.sup.3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; NR.sup.5(CH.sub.2).sub.mR.sup.6 wherein R.sup.5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R.sup.6 is phenyl or pyridyl optionally substituted by a halogen atom; or NR.sup.7CO(CH.sub.2).sub.qR.sup.8 wherein R is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R.sup.8 is phenyl or pyridyl optionally substituted by a halogen atom, and R.sup.4 is (CH.sub.2).sub.aCONHR.sup.9 wherein a is an integer of 1-4, and R.sup.9 is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or (CH.sub.2).sub.bCOOR.sup.10 wherein b is an integer of 1-4, and R.sup.10 is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof. The lymphoma to be treated is diffuse large B-cell lymphom (DLBCL) specifically selected from activated B-cell DLBCL (ABC-DLBCL) and germinal B-cell DLBCL (GBC-DLBCL). ##STR00001##

Processes for making alkylated arylpiperazine and alkylated arylpiperidine compounds including novel intermediates

Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively ##STR00001##
wherein, R.sub.1 and R.sub.2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR.sub.3R.sub.4, OR.sub.5, or SR.sub.5, where R.sub.3 and R.sub.4 are individually selected from acyl or sulfonyl, and where R.sub.5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Processes for making alkylated arylpiperazine and alkylated arylpiperidine compounds including novel intermediates

Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively ##STR00001##
wherein, R.sub.1 and R.sub.2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR.sub.3R.sub.4, OR.sub.5, or SR.sub.5, where R.sub.3 and R.sub.4 are individually selected from acyl or sulfonyl, and where R.sub.5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

PROCESSES FOR MAKING ALKYLATED ARYLPIPERAZINE AND ALKYLATED ARYLPIPERIDINE COMPOUNDS INCLUDING NOVEL INTERMEDIATES

Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively

##STR00001##

wherein, R.sub.1 and R.sub.2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR.sub.3R.sub.4, OR.sub.5, or SR.sub.5, where R.sub.3 and R.sub.4 are individually selected from acyl or sulfonyl, and where R.sub.5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

PROCESSES FOR MAKING ALKYLATED ARYLPIPERAZINE AND ALKYLATED ARYLPIPERIDINE COMPOUNDS INCLUDING NOVEL INTERMEDIATES

Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively

##STR00001##

wherein, R.sub.1 and R.sub.2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR.sub.3R.sub.4, OR.sub.5, or SR.sub.5, where R.sub.3 and R.sub.4 are individually selected from acyl or sulfonyl, and where R.sub.5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

IL-15 Conjugates and Uses Thereof
20240383957 · 2024-11-21 · ·

Disclosed herein are interleukin (IL)-15 conjugates and use in the treatment of one or more indications. Also described herein include pharmaceutical compositions and kits comprising one or more of IL-15 conjugates. In some embodiments, at least one amino acid residue in the IL-15 conjugate is replaced by the structure of Formula (I) described herein.

IL-15 Conjugates and Uses Thereof
20240383957 · 2024-11-21 · ·

Disclosed herein are interleukin (IL)-15 conjugates and use in the treatment of one or more indications. Also described herein include pharmaceutical compositions and kits comprising one or more of IL-15 conjugates. In some embodiments, at least one amino acid residue in the IL-15 conjugate is replaced by the structure of Formula (I) described herein.

N-type dopants for efficient solar cells

Triazabicylodecene can effectively n-dope a variety of organic semiconductors, including PCBM, thus increasing in-plane conductivities. We synthesized a series of TBD-based n-dopants via an N-alkylation reaction and studied the effect of various alkyl chains on the physical and device properties of the dopants. Combining two TBD moieties on a long alky chain gave a solid dopant, 2TBD-C10, with high thermal stability above 250 C. PCBM films doped by 2TBD-C10 were the most tolerant to thermal annealing and reached in-plane conductivities of 6.510.sup.2 S/cm. Furthermore, incorporating 2TBD-C10 doped PCBM as the electron transport layer (ETL) in methylammonium lead triiodide (MAPbI.sub.3) based photovoltaics led to a 23% increase in performance, from 11.8% to 14.5% PCE.

N-type dopants for efficient solar cells

Triazabicylodecene can effectively n-dope a variety of organic semiconductors, including PCBM, thus increasing in-plane conductivities. We synthesized a series of TBD-based n-dopants via an N-alkylation reaction and studied the effect of various alkyl chains on the physical and device properties of the dopants. Combining two TBD moieties on a long alky chain gave a solid dopant, 2TBD-C10, with high thermal stability above 250 C. PCBM films doped by 2TBD-C10 were the most tolerant to thermal annealing and reached in-plane conductivities of 6.510.sup.2 S/cm. Furthermore, incorporating 2TBD-C10 doped PCBM as the electron transport layer (ETL) in methylammonium lead triiodide (MAPbI.sub.3) based photovoltaics led to a 23% increase in performance, from 11.8% to 14.5% PCE.

SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF

Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.