67223-98-7

Upstream product

• 1191-95-3 cyclobutanone 
• 1439-36-7 1-triphenylphosphoranylidene-2-propanone 
• 1120-56-5 methylidenecyclobutane 
• 71-23-8 propan-1-ol 
• 67-56-1 methanol 

Downstream Products

• 940868-53-1 1-[1-(2-trifluoromethyl-phenyl)-cyclobutyl]-propan-2-one 
• 221342-48-9 spiro[3.5]nonane-6,8-dione 

Relevant academic research and scientific papers

COMPOSITIONS AND METHODS FOR TREATING NON-ALCOHOLIC STEATOHEPATITIS

Methods for treating non-alcoholic steatohepatitis using compounds or pharmaceutical compositions that modulate the activity of Bcl-2 family proteins are disclosed. In some methods, the patient to be treated is diagnosed with one or more additional diseases selected from cardiovascular disease, chronic kidney disease, type 2 diabetes mellitus, obesity, and metabolic syndrome, wherein the metabolic syndrome may include, but is not limited to patient presentation of one or more of hypertension, hyperglycaemia, hyperlipemia, insulin resistance (IR). In some methods, the compound or pharmaceutical composition is administered to the patient in need thereof at a therapeutically effective dose sufficient to elicit one or more effects selected from: reduced liver steatosis, reduced lobular inflammation, reduced hepatocellular ballooning, and reduced liver fibrosis.

N-(PHENYLSULFONYL)BENZAMIDES AND RELATED COMPOUNDS AS BCL-2 INHIBITORS

The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1 , X2, X3 R1a, R1b E, and = are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bc1-2 protein inhibition such as cancer.

ALDOSTERONE SYNTHASE INHIBITORS

The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation

The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.

TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION

The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.

TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION

The present invention relates to compounds defined by formula (I), wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol

Substituted tetrahydronaphthaline and analogous compounds

Substituted tetrahydro-naphthalenes and analogous compounds are prepared by reducing or condensing appropriate functional substituents in substituted tetrahydro-naphthalenes and analogous compounds by customary methods and converting functional groups in this manner into the desired groups. The compounds according to the invention are suitable for use as active compounds in pharmaceuticals, in particular in pharmaceuticals for treating arteriosclerosis and also dyslipidaemias.

Stereoselective Mukaiyama-Michael/Michael/aldol domino cyclization as the key step in the synthesis of pentasubstituted arenes: An efficient access to highly active inhibitors of cholesteryl ester transfer protein (CETP)

Seemingly heartbreaking for a stereochemist, the one-step selective construction of a stereopentad and its prompt destruction by aromatization has been proven to be an efficient strategy for the synthesis of fivefold substituted, pharmacologically highly active arenes (see scheme).

ACETYL FLUOROSULFONATE - GENERATION FROM ACETYL FLUORIDE AND SULFUR TRIOXIDE AND REACTIONS WITH OLEFINS

The acylation of methylenecyclobutane, styrene, and vinylcyclopropane by acetyl fluorosulfonate, generated in situ from acetyl fluoride and sulfur trioxide, followed by treatment with methyl or propyl alcohols leads to the products from conjugate addition (alkoxy ketones) in addition to elimination products (α,β-unsaturated ketones).The employed methods makes it possible to separate the stages of addition of the acetyl group and the external nucleophile through the intermediate formation of covalently bonded alkyl fluorosulfonates.

Acyl fluorosulfonates for the acylation of olefins

The acylation of methylenecyclobutane by acyl fluorosulfonates RCOOSO2F , generated in situ from the corresponding acyl fluorides and sulfur trioxide, with methanol as external nucleophile leads to methoxy ketones and α,β-unsaturated ketones, the ratios of which depend on the nature of the radical R.The formation of the methoxy ketones indicates substitution of the OSO2F by the methoxy group at the intermediate stage of the reaction.If triphenylphosphine is used, the OSO2F group is substituted by this nucleophile, and as a result the corresponding phosphonium salt is formed.The use of acyl fluorosulfonates for acylation makes it possible to separate the stages of direct acylation and the introduction of the external nucleophile, and this opens up the possibility of varying the nucleophiles at the concluding stage of the reaction.