C07C237/12

DIPEPTIDOMIMETICS AS INHIBITORS OF HUMAN IMMUNOPROTEASOMES
20220080022 · 2022-03-17 ·

The compounds of the present invention are represented by the following compounds having Formula I:

##STR00001##

where the substituents R.sup.1, R.sup.4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic):

##STR00002##

where the substituents R.sup.1-R.sup.4, R.sup.x, R.sup.y, X, Y, and s are as defined herein.

These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

DIPEPTIDOMIMETICS AS INHIBITORS OF HUMAN IMMUNOPROTEASOMES
20220080022 · 2022-03-17 ·

The compounds of the present invention are represented by the following compounds having Formula I:

##STR00001##

where the substituents R.sup.1, R.sup.4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic):

##STR00002##

where the substituents R.sup.1-R.sup.4, R.sup.x, R.sup.y, X, Y, and s are as defined herein.

These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

MYC-MAX INHIBITOR COMPOUND THERAPEUTICS FOR CANCER TREATMENT, METHODS AND USES ASSOCIATED THEREWITH

Provided herein are Myc-Max inhibitory compounds having the structure of Formula (I) and compositions thereof for use in the treatment of cancer. In particular, the Myc-Max inhibitory compounds may be useful for the treatment of cancers selected from one or more of: prostate cancer, breast cancer, colon cancer, cervical cancer, small-cell lung carcinomas, neuroblastomas, osteosarcomas, glioblastomas, melanoma and myeloid leukaemia.

##STR00001##

AGENTS FOR IMPROVED DELIVERY OF NUCLEIC ACIDS TO EUKARYOTIC CELLS
20210189433 · 2021-06-24 ·

New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes.

AGENTS FOR IMPROVED DELIVERY OF NUCLEIC ACIDS TO EUKARYOTIC CELLS
20210189433 · 2021-06-24 ·

New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes.

AN IMPROVED PROCESS FOR THE PREPARATION OF (2S)-2-[(4R)-2-OXO-4-PROPYLTETRAHYDRO-1H-PYRROL-1-YL] BUTANAMIDE AND ITS INTERMEDIATES THEREOF

The present invention relates to an improved process for the preparation of (2S)-2-[(4R)-2-oxo-4-propyltetrahydro-1H-pyrrol-1-yl] butanamide compound of formula-1, its intermediates, novel salt compounds of intermediates of the compound of formula-1. Further the use of novel salts in the preparation of the compound of formula-1. The present invention also relates to the novel process for the preparation of the compound of formula-1.

AN IMPROVED PROCESS FOR THE PREPARATION OF (2S)-2-[(4R)-2-OXO-4-PROPYLTETRAHYDRO-1H-PYRROL-1-YL] BUTANAMIDE AND ITS INTERMEDIATES THEREOF

The present invention relates to an improved process for the preparation of (2S)-2-[(4R)-2-oxo-4-propyltetrahydro-1H-pyrrol-1-yl] butanamide compound of formula-1, its intermediates, novel salt compounds of intermediates of the compound of formula-1. Further the use of novel salts in the preparation of the compound of formula-1. The present invention also relates to the novel process for the preparation of the compound of formula-1.

Method For Preparing Novel Crystalline Forms Of 1-(4-Benzyloxy-Benzyl)-3-Methyl-Thiourea

The present disclosure relates to a method for preparing 1-(4-benzyloxy-benzyl)-3-methyl-thiourea and a method for preparing a novel stable crystalline form A of 1-(4-benzyloxy-benzyl)-3-methyl-thiourea.

SURFACTANT COMPOUNDS-CLIPS FOR EXTRACTION AND STABILIZATION IN SOLUTION OF MEMBRANE PROTEINS

The present invention relates to a compound of formula (I): (I) as defined in the description. The present invention also relates to a method for extracting biological membrane-associated membrane proteins, comprising a step of bringing an aqueous solution of biological membrane-associated membrane proteins into contact with at least one compound of the invention. The present invention also relates to a method for stabilizing membrane proteins in solution in an aqueous solution, comprising a step (i) consisting in bringing an aqueous solution of a membrane protein in solution into contact with at least one compound of the invention.

COMPOSITIONS AND METHODS RELATING TO SALTS OF SPECIALIZED PRO-RESOLVING MEDIATORS

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both. Provided are pharmaceutical compositions adapted to deliver the compounds the lower gastrointestinal tract and methods of using same as monotherapy in the treatment of inflammatory diseases or disorders of the lower gastrointestinal tract, and in combination therapy with 5-aminosalicylate.