C07D207/273

BRIVARACETAM INTERMEDIATE, PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR BRIVARACETAM

The present invention relates to a brivaracetam intermediate, a preparation method therefor, and a preparation method for brivaracetam. The steps of the method for preparing brivaracetam described in the present invention are short and the raw materials are cheap, moreover, the method is simple and highly effective without requiring isomer separation by means of column chromatography or asymmetric synthesis, being suitable for industrial large-scale production. In addition, disclosed by the present invention is a compound as shown in formula (II), which may be used for the synthesis of brivaracetam.

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BRIVARACETAM INTERMEDIATE, PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR BRIVARACETAM

The present invention relates to a brivaracetam intermediate, a preparation method therefor, and a preparation method for brivaracetam. The steps of the method for preparing brivaracetam described in the present invention are short and the raw materials are cheap, moreover, the method is simple and highly effective without requiring isomer separation by means of column chromatography or asymmetric synthesis, being suitable for industrial large-scale production. In addition, disclosed by the present invention is a compound as shown in formula (II), which may be used for the synthesis of brivaracetam.

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QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

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comprising treating a compound of Formula (I):

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with a transition metal catalyst and under alkylation conditions as valence and stability permit.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

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comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

Urea Derivative Or Pharmacologically Acceptable Salt Thereof

Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect.

The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.

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Urea Derivative Or Pharmacologically Acceptable Salt Thereof

Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect.

The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.

##STR00001##

METHODS FOR TREATING DIABETES USING VDAC1 INHIBITORS
20210130291 · 2021-05-06 ·

The present invention relates to compositions and methods for treating prediabetes and diabetes and delaying progression of the disease. The present invention uses molecules that specifically bind to and inhibit Voltage Dependent Anion Channel (VDAC1) that is expressed on the beta cells of diabetic subjects. Particularly, the present invention discloses the use of substituted piperazine and piperidine derivatives as specific inhibitors of VDAC1 for preventing the progression of and treating prediabetes and diabetes.

METHODS FOR TREATING DIABETES USING VDAC1 INHIBITORS
20210130291 · 2021-05-06 ·

The present invention relates to compositions and methods for treating prediabetes and diabetes and delaying progression of the disease. The present invention uses molecules that specifically bind to and inhibit Voltage Dependent Anion Channel (VDAC1) that is expressed on the beta cells of diabetic subjects. Particularly, the present invention discloses the use of substituted piperazine and piperidine derivatives as specific inhibitors of VDAC1 for preventing the progression of and treating prediabetes and diabetes.

Chemical Compounds as ATF-4 Pathway Inhibitors

The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ:

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wherein X.sup.6′, a, b, C.sup.8′, D.sup.8′, L.sup.82′, L.sup.83′, R.sup.81′, R.sup.82′, R.sup.83′, R.sup.84′, R.sup.85′, R.sup.86′, z.sup.82′, z.sup.84′, z.sup.85′, and z.sup.86′ are as defined herein; or salts thereof.

The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Chemical Compounds as ATF-4 Pathway Inhibitors

The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ:

##STR00001##

wherein X.sup.6′, a, b, C.sup.8′, D.sup.8′, L.sup.82′, L.sup.83′, R.sup.81′, R.sup.82′, R.sup.83′, R.sup.84′, R.sup.85′, R.sup.86′, z.sup.82′, z.sup.84′, z.sup.85′, and z.sup.86′ are as defined herein; or salts thereof.

The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.