Method of using dihydro-resveratrol or its stilbenoid derivatives and/or chemical variants in treatments of fibrotic and diabetic conditions

Patent metadata

Field	Value
Publication number	US-9877931-B2
Application number	US-201715633780-A
Country	US
Kind code	B2
Filing date	Jun 27, 2017
Priority date	Jun 16, 2015
Publication date	Jan 30, 2018
Grant date	Jan 30, 2018

Abstract

The present invention relates to a polyphenol derivative of the stilbenoid family, namely trans-3,5,4′-trihydroxybibenzyl, also known as dihydro-resveratrol, as a remedial agent. In particular, the present invention presents the usage of dihydro-resveratrol as an anti-fibrotic agent in suppressing the activation of pancreatic stellate cells (PSCs). One embodiment of the present invention also relates to the management of pancreatic fibrosis, which is often accompanied with chronic pancreatitis and desmoplastic reaction of pancreatic cancer. Another embodiment of the present invention also has applications in preventing or alleviating or treating pancreatic cancer or pancreatogenic diabetes.

First claim

The invention claimed is:

1. A method for treating pancreatogenic diabetes (or Type 3c diabetes milieus) in a subject in need thereof comprising using a composition comprising compounds with a formula of

wherein
R 2 and R 4 are each independently selected from —OR 11 and —OC(O)R 11 ;
R 1 , R 3 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are each independently selected from hydrogen, halogen, trifluoromethyl, —OR 11 and —OC(O)R 11 ; or R 2 and R 3 , or R 7 and R 8 are taken together with the carbon atoms to which they are attached to form a cyclic group;
R 11 is independently hydrogen or selected from hydrocarbyl and heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R 12 ;
R 12 is independently selected from halogen, trifluoromethyl, cyano, nitro, oxo, —OR 13 , —C(O)R 14 , —C(O)N(R 13 )R 14 , —C(O)OR 13 , —OC(O)R 14 , —S(O) 2 R 13 , —S(O) 2 N(R 13 )R 14 , —N(R 13 )R 14 ;
R 13 and R 14 are each independently hydrogen or selected from hydrocarbyl and heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from halogen, cyano, amino, hydroxy, C 1-6 alkyl and C 1-6 alkoxy;
or an enantiomer thereof;
or a pharmaceutically acceptable salt or prodrug thereof;
or a mixture of said compound, the derivative and/or chemical variants thereof.

2. A method for treating pancreatogenic diabetes (or Type 3c diabetes milieus) in a subject in need thereof comprising using a composition comprising compounds with a formula of

3. The method according to claim 1 wherein the composition is administered to the subject in need thereof with a dosage of at least 1.622 mg/kg/day wherein said composition consists of a compound with a formula of

4. The method according to claim 3 wherein the said subject is human.

5. The method according to claim 3 wherein the composition is administered orally to said subject in need thereof.

Assignees

• Univ Hong Kong Baptist Univ

Inventors

• Zhang Hongjie
• Tsang Siu Wai
• Chen Yegao

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07C69/753

  of polycyclic acids · CPC title

• C07C69/34

  Esters of acyclic saturated polycarboxylic acids having an esterified carboxyl group bound to an acyclic carbon atom · CPC title

• C07C69/736

  the hydroxy group of the ester being etherified with a hydroxy compound having the hydroxy group bound to a carbon atom of a six-membered aromatic ring · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title