Patent classifications
C07C229/50
Compositions And Methods of Synthesizing Shape Shifting Cyclic Peptides (Sscp) And Their Use in The Identification of Novel Therapeutic Compounds
The invention described herein includes a novel platform for the development of novel shapeshifting drug-like compounds that overcome physical mass limitations as they possess the ability to interconvert internally and spontaneously, i.e., shapeshift, between multiple chemical structures with varying pharmacophore properties. In one preferred embodiment, the invention include systems, methods, and compositions for the synthesis of novel bullvalene amino acid (Bvas) compounds that may further be incorporated into Shape Shifting Cyclic Peptides (SSCP) with varying pharmacophore properties and their use as novel therapeutic compounds.
SPIROCYCLOHEXANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USES AS ANTI-APOPTOTIC INHIBITORS
- Stephen STOKES ,
- Simon BEDFORD ,
- l-Jen CHEN ,
- James Edward Paul DAVIDSON ,
- Nicholas DAVIES ,
- Christopher John Graham ,
- Sean Martin MCKENNA ,
- Johannes W.G. MEISSNER ,
- James Brooke Murray ,
- Rachel Jane PARSONS ,
- Stuart RAY ,
- Emma SANDERS ,
- Claire Louise WALMSLEY ,
- Paul Andrew BROUGH ,
- Andr?s KOTSCHY ,
- ?gnes PROSZENY?K ,
- ?d?m SINAI ,
- Bal?zs K?roly B?LINT ,
- M?rton CS?KEI ,
- M?rton ZWILLINGER ,
- Rita GARAMV?LGYI ,
- Szabolcs Sipos ,
- Vilibald KUN ,
- Zolt?n SZAB? ,
- Ma?a CHANRION ,
- Francesca ROCCHETTI ,
- Fr?d?ric COLLAND ,
- Ana Leticia MARAGNO ,
- Laura Bresson
Compounds of Formula (I):
##STR00001##
wherein R.sub.1, R.sub.3, R.sub.11, R.sub.12, X, Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4 and are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring anti-apoptotic inhibitors.
SPIROCYCLOHEXANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USES AS ANTI-APOPTOTIC INHIBITORS
- Stephen STOKES ,
- Simon BEDFORD ,
- l-Jen CHEN ,
- James Edward Paul DAVIDSON ,
- Nicholas DAVIES ,
- Christopher John Graham ,
- Sean Martin MCKENNA ,
- Johannes W.G. MEISSNER ,
- James Brooke Murray ,
- Rachel Jane PARSONS ,
- Stuart RAY ,
- Emma SANDERS ,
- Claire Louise WALMSLEY ,
- Paul Andrew BROUGH ,
- Andr?s KOTSCHY ,
- ?gnes PROSZENY?K ,
- ?d?m SINAI ,
- Bal?zs K?roly B?LINT ,
- M?rton CS?KEI ,
- M?rton ZWILLINGER ,
- Rita GARAMV?LGYI ,
- Szabolcs Sipos ,
- Vilibald KUN ,
- Zolt?n SZAB? ,
- Ma?a CHANRION ,
- Francesca ROCCHETTI ,
- Fr?d?ric COLLAND ,
- Ana Leticia MARAGNO ,
- Laura Bresson
Compounds of Formula (I):
##STR00001##
wherein R.sub.1, R.sub.3, R.sub.11, R.sub.12, X, Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4 and are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring anti-apoptotic inhibitors.
FUSED TRICYCLIC GAMMA-AMINO ACID DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
Disclosed are a fused tricyclic -amino acid derivative and a medical use thereof, in particular, the present invention relates to a fused cyclic -amino acid derivative as shown in general formula (I), or a stereoisomer, solvate, metabolite, prodrug, pharmaceutically acceptable salt or eutectic thereof, a pharmaceutical composition containing same, and the use of a compound or the composition in the field of analgesia, wherein the definitions of each substituent in general formula (I) are the same as the definitions in the description.
##STR00001##
FUSED TRICYCLIC GAMMA-AMINO ACID DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
Disclosed are a fused tricyclic -amino acid derivative and a medical use thereof, in particular, the present invention relates to a fused cyclic -amino acid derivative as shown in general formula (I), or a stereoisomer, solvate, metabolite, prodrug, pharmaceutically acceptable salt or eutectic thereof, a pharmaceutical composition containing same, and the use of a compound or the composition in the field of analgesia, wherein the definitions of each substituent in general formula (I) are the same as the definitions in the description.
##STR00001##
THERAPEUTIC AMINOINDANE COMPOUNDS AND COMPOSITIONS
The present invention discloses therapeutic compounds of the aminoindane class, including certain short-acting ester and lactone derivatives, and pharmaceutical compositions made therewith, as well as methods of their use in the treatment of alcohol and other substance use disorders, behavioral addictions, and CNS and mental health disorders, and for the improvement of mental health and psychological functioning.
THERAPEUTIC AMINOINDANE COMPOUNDS AND COMPOSITIONS
The present invention discloses therapeutic compounds of the aminoindane class, including certain short-acting ester and lactone derivatives, and pharmaceutical compositions made therewith, as well as methods of their use in the treatment of alcohol and other substance use disorders, behavioral addictions, and CNS and mental health disorders, and for the improvement of mental health and psychological functioning.
Therapeutic compounds and uses thereof
Provided herein are compounds of formula I: ##STR00001##
and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.
Therapeutic compounds and uses thereof
Provided herein are compounds of formula I: ##STR00001##
and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.
Fused (hetero)cyclic compounds as S1P modulators
The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.