Lin Chen

US Patent:

8227571, Jul 24, 2012

Filed:

Dec 11, 2008

Appl. No.:

12/316309

Inventors:

Lin Chen - Superior CO, US
Yeun-Kwei Han - Louisville CO, US
Christopher R. Roberts - Berthoud CO, US

Assignee:

Roche Palo Alto LLC - South San Francisco CA

International Classification:

C07K 14/00

US Classification:

530324, 530308, 530338

Abstract:

The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.

US Patent:

20060160201, Jul 20, 2006

Filed:

Oct 14, 2005

Appl. No.:

11/251643

Inventors:

Lin Chen - Boulder CO, US
Aidong Han - Boulder CO, US
Ju He - Boulder CO, US

International Classification:

G06F 19/00
C12N 9/16
A61K 31/404

US Classification:

435196000, 514419000, 702019000

Abstract:

Disclosed are the three-dimensional structures of two complexes: a Cabin1/MEF2B/DNA complex and a MITR/MEF2B/DNA complex. Also disclosed are methods of using such structures and models derived therefrom in structure-based design methods to identify regulators of the interaction of MEF2 with its cognate ligands/corepressors, to compounds that can be designed or identified based on the knowledge of such structures and models, and to methods of using such compounds in therapeutic methods. Also disclosed are peptide and non-peptide regulatory compounds that regulate, and preferably inhibit, MEF2.

US Patent:

20080004429, Jan 3, 2008

Filed:

Jun 21, 2007

Appl. No.:

11/821017

Inventors:

Christopher Roberts - Berthoud CO, US
Lin Chen - Superior CO, US
Yeun-Kwei Han - Louisville CO, US

International Classification:

C07K 1/10
C07K 1/00
C07K 5/00

US Classification:

530330000, 530333000

Abstract:

The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to one of the fragments. The fragments are then coupled together in the solid solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.

US Patent:

20080287649, Nov 20, 2008

Filed:

Dec 20, 2007

Appl. No.:

12/004265

Inventors:

Lin Chen - Superior CO, US
Yeun-Kwei Han - Louisville CO, US
Christopher R. Roberts - Berthoud CO, US

International Classification:

C07K 2/00
C07C 69/616
C07K 5/12

US Classification:

530317, 560 39

Abstract:

Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.

US Patent:

20100137561, Jun 3, 2010

Filed:

Dec 3, 2009

Appl. No.:

12/630002

Inventors:

Lin Chen - Superior CO, US

International Classification:

C07K 14/435
C07K 7/08
C07K 7/06
C07K 5/103

US Classification:

530324, 530326, 530327, 530330

Abstract:

This application discloses processes for synthesizing human relaxin Chain B for treatment of diseases mediated by relaxin. This application in particular discloses processes of synthesizing the Chain B of human relaxin using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to couple the fragments.

US Patent:

20100292435, Nov 18, 2010

Filed:

Apr 30, 2010

Appl. No.:

12/770907

Inventors:

LIN CHEN - SUPERIOR CO, US
YEUN-KWEI HAN - LOUISVILLE CO, US
CHRISTOPHER R. ROBERTS - BETHOUD CO, US

International Classification:

C07K 14/00
C07K 7/08

US Classification:

530324, 530326, 530327, 530328

Abstract:

The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to couple the second fragment and the first fragment. Alternatively, a different second fragment is coupled to a first fragment in the solid phase. Then, solution phase chemistry is then used to add the third fragment, whereby the third fragment is coupled to the coupled first and second fragments in the solution phase. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.

US Patent:

20110213082, Sep 1, 2011

Filed:

May 11, 2011

Appl. No.:

13/105435

Inventors:

Christopher R. Roberts - Berthoud CO, US
Lin Chen - Superior CO, US
Yeun-Kwei Han - Louisville CO, US

International Classification:

C08G 61/00
C07K 7/08

US Classification:

525 541, 530327, 530326

Abstract:

The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid”) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to one of the fragments. The fragments are then coupled together in the solid solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.