CYCLOSPORINE ANALOGUE MIXTURES AND THEIR USE AS IMMUNOMODULATING AGENTS

Title:

CYCLOSPORINE ANALOGUE MIXTURES AND THEIR USE AS IMMUNOMODULATING AGENTS

Document Type and Number:

Japanese Patent JP2013136597

Kind Code:

A

Abstract:

To provide cyclosporine analogues that posse enhanced efficacy and reduced toxicity compared with presently known cyclosporine.

There are provided cis and trans-isomers of cyclosporine A analogs referred to as ISA_TX247, and derivatives thereof. ISA_TX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The stereoselective synthetic pathways utilize a Witting reaction or organometallic reagents including inorganic elements, such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 wt.% of the (E)-isomer to about 90 to 10 wt.% of the (Z)-isomer, based on the total weight of the mixture.

Inventors:

NAICKER SELVARAJ
YATSCOFF RANDALL W
FOSTER ROBERT T

Application Number:

JP2013017448A

Publication Date:

July 11, 2013

Filing Date:

January 31, 2013

Export Citation:

Click for automatic bibliography generation Help

Assignee:

ISOTECHNIKA PHARMA INC

International Classes:

A61K38/00; C07K7/00; A61K9/00; A61K9/107; A61K9/48; A61K38/13; A61K47/10; A61K47/14; A61K47/34; A61K47/42; A61P1/04; A61P1/16; A61P3/10; A61P7/00; A61P7/04; A61P7/06; A61P9/00; A61P11/00; A61P11/06; A61P13/12; A61P17/00; A61P17/04; A61P17/06; A61P17/14; A61P19/02; A61P19/08; A61P21/04; A61P25/00; A61P27/02; A61P29/00; A61P31/12; A61P37/02; A61P37/06; A61P37/08; C07K7/64; C07K11/02

Domestic Patent References:

JP2005511538A	2005-04-28
JP2009197036A	2009-09-03
JP5272140B2	2013-08-28

Foreign References:

WO1999018120A1

1999-04-15

Other References:

JPN5004001601; ＡＳＰＥＳＬＥＴ　Ｌ: ＴＲＡＮＳＰＬＡＮＴＡＴＩＯＮ　ＰＲＯＣＥＥＤＩＮＧＳＶ３３, 200102, Ｐ１０４８-１０５１
JPN6008063756; Ｔｈｅ　Ｊｏｕｒｎａｌ　ｏｆ　Ｈｅａｒｔ　ａｎｄ　Ｌｕｎｇ　ＴｒａｎｓｐｌａｎｔａｔｉｏｎＶｏｌ．２０，　Ｎｏ．２, 200102, ｐａｇｅ　１６１
JPN6008063757; モリソンボイド　有機化学（上）第６版 , 1994, 第１８６-１８８，３６２-３６６頁
JPN5004001601; ＡＳＰＥＳＬＥＴ　Ｌ: ＴＲＡＮＳＰＬＡＮＴＡＴＩＯＮ　ＰＲＯＣＥＥＤＩＮＧＳＶ３３, 200102, Ｐ１０４８-１０５１
JPN6008063756; Ｔｈｅ　Ｊｏｕｒｎａｌ　ｏｆ　Ｈｅａｒｔ　ａｎｄ　Ｌｕｎｇ　ＴｒａｎｓｐｌａｎｔａｔｉｏｎＶｏｌ．２０，　Ｎｏ．２, 200102, ｐａｇｅ　１６１

Attorney, Agent or Firm:

Taro Yaguchi

Previous Patent: USE OF c-Src INHIBITOR IN COMBINATION WITH PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR TREATMENT OF LEUKEMI...

Next Patent: DETERGENT COMPOSITION AND PRODUCTION METHOD OF THE SAME