701232-66-8

Upstream product

• 105640-07-1 4-(4-hydroxyphenyl)cyclohexan-1-one 
• 1067-74-9 Methyl diethylphosphonoacetate 
• 5927-18-4 trimethyl phosphonoacetate 
• 80-70-6 N,N,N',N'-tetramethylguanidine 

Downstream Products

• 701232-67-9 trans-[4-(4-hydroxyphenyl)cyclohexyl]acetic methyl ester 
• 1414867-53-0 1-O-({trans-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetyl)-β-D-glucopyranuronic acid 
• 1414867-52-9 prop-2-en-1-yl 1-O-({trans-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetyl)-β-D-glucopyranuronate 

Relevant academic research and scientific papers

Proton exchange reactions in isotope chemistry (II) synthesis of stable isotope-labeled LCQ908

The proton exchange reaction was applied to the preparation of stable isotope-labeled LCQ908. For this synthesis, a suitable intermediate with protons alpha to a carbonyl group was first subjected to the H-D exchange reaction; subsequent coupling of a car

NOVEL BETA-ALANINE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a beta-alanine derivative, pharmaceutically acceptable salts thereof, and a pharmaceutical composition including the same as an active ingredient. The novel beta-alanine derivative and pharmaceutically acceptable salts the

Development of novel benzomorpholine class of diacylglycerol acyltransferase i inhibitors

Diacylglycerol acyltransferase 1 (DGAT1) presents itself as a potential therapeutic target for obesity and diabetes for its important role in triglyceride biosynthesis. Herein we report the rational design of a novel class of DGAT1 inhibitors featuring a

DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS

The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a —CH— group; X1 represents a nitrogen atom or a —CH═CH— group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1-C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a —(C3-C10)cycloalkyl- group; Y represents a —(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1-C6)alkoxy group; Z1 is absent or represents an —NH— function; Z2 and Z3 are as defined in the description. The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.

4-AMINO-5-OXO-7,8-DIHYDROPYRIMIDO[5, 4 -F] [1, 4] OXAZEPINE COMPOUNDS AS DGAT1 INHIBITORS

Described herein are compounds of formula (I). The compounds of formula (I) act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 ((DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687)

A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low predicted dose in man. Rational design and optimization of this series led to the discovery of compound 30 (AZD7687), which met the project objectives for potency, selectivity, in particular over ACAT1, solubility, and preclinical PK profiles. This compound showed the anticipated excellent pharmacokinetic properties in human volunteers.

DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS

The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a -CH- group; X1 represents a nitrogen atom or a -CH=CH- group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1 -C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a -(C3-C10)cycloalkyl- group; Y represents a -(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1 -C6)alkoxy group; Z1 is absent or represents an -NH- function; Z2 and Z3 are as defined in the description. The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.

LACTAM DERIVATIVES AS DGAT-1 INHIBITORS

Described herein are compounds of formula I The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

COMPOSITIONS AND METHODS FOR MODULATING LPA RECEPTORS

The present invention relates to compounds of Formula (1), or pharmaceutically acceptable salts thereof and their pharmaceutical compositions, wherein variables are as defined herein, which are useful as modulators of the activity of lysophosphatidic acid (LPA).

Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1

A novel class of DGAT1 inhibitors containing a thiadiazole core has been discovered. Chemical optimization lead to inhibitors of human DGAT1 with an appropriate ADME profile and that show in vivo activity in target tissues.