Daniel M Chu

US Patent:

6569867, May 27, 2003

Filed:

May 10, 2001

Appl. No.:

09/853306

Inventors:

Daniel Chu - Santa Clara CA
Maria Fardis - San Carlos CA
Chaitan Khosla - Palo Alto CA
Christopher Reeves - Orinda CA
Daniel Santi - San Francisco CA
Andreas Schirmer - Hayward CA

Assignee:

Kosan Biosciences, Inc. - Hayward CA

International Classification:

C07D49816

US Classification:

514291, 540456

Abstract:

The present invention relates to novel polyketides, host cells that produce the novel compounds, and methods fort their use. The compounds of the present invention are cyclic polyketides (also referred to as a âmacrolidesâ or âmacrolactonesâ) that include as part of their structure and bind to a FK binding protein wherein R and R are each selected from the group consisting of hydrogen, methyl, ethyl, and methoxy, provided that at least one of R and R is hydrogen, methyl, or ethyl. As will be explained in greater detail below, the compounds of the present invention have properties such as favorable P450 enzyme activity profiles that are desirable for use of these compounds as drugs.

US Patent:

6593302, Jul 15, 2003

Filed:

Feb 13, 2002

Appl. No.:

10/075466

Inventors:

Daniel Chu - Santa Clara CA
Gary Ashley - Alameda CA

Assignee:

Kosan Biosciences, Inc. - Hayward CA

International Classification:

A61K 3170

US Classification:

514 29, 536 72, 536 74

Abstract:

Compounds of the formula wherein R is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or OR is replaced by H; R is H or halogen; R is H or a protecting group; R is methyl, unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); R is H or a protecting group; L is methylene or carbonyl; T is âOâ, âN(R)â, âN(OR)â, âN(NHCOR)â, âN(N CHR)â, or âN(NHR)â wherein R is H or R as defined above, with the proviso that when L is methylene, T is âOâ; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or Z and Y together are O, NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.

US Patent:

6624302, Sep 23, 2003

Filed:

Dec 27, 2002

Appl. No.:

10/331047

Inventors:

Daniel Chu - Santa Clara CA
Maria Fardis - San Carlos CA
Chaitan Khosla - Palo Alto CA
Christopher Reeves - Orinda CA
Daniel Santi - San Francisco CA
Andreas Schirmer - Hayward CA

Assignee:

Kosan Biosciences, Inc. - Hayward CA

International Classification:

C07D49816

US Classification:

540456

Abstract:

The present invention relates to novel polyketides, host cells that produce the novel compounds, and methods fort their use. The compounds of the present invention are cyclic polyketides (also referred to as a âmacrolidesâ or âmacrolactonesâ) that include as part of their structure and bind to a FK binding protein wherein R and R are each selected from the group consisting of hydrogen, methyl, ethyl, and methoxy, provided that at least one of R and R is hydrogen, methyl, or ethyl. As will be explained in greater detail below, the compounds of the present invention have properties such as favorable P450 enzyme activity profiles that are desirable for use of these compounds as drugs.

US Patent:

6716840, Apr 6, 2004

Filed:

Apr 8, 2002

Appl. No.:

10/118730

Inventors:

Daniel Chu - Santa Clara CA
Rustum S. Boyce - San Francisco CA
David Duhl - Oakland CA
Bryan H. Chang - Concord CA

Assignee:

Chiron Corporation - Emeryville CA

International Classification:

A61K 315375

US Classification:

5142335, 544144, 544373, 546201, 548465, 51425401

Abstract:

Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH , N, NR , C O, C S, S O, SO , S, O, (CR R ) , C( O)â(CR R ) , and C( S)â(CR R ) , where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S O, SO , C(O), NC(O), NC(S), OC(O), OC(S), C(NR ), C(NOR ), and a covalent bond. Z , Z , and Z are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (âMC-4râ) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.

US Patent:

6756359, Jun 29, 2004

Filed:

Jul 3, 2002

Appl. No.:

10/190431

Inventors:

Daniel Chu - Santa Clara CA
Matthew Burger - Albany CA
Xiaodong Lin - Walnut Creek CA
Georgia Law Carroll - Walnut Creek CA
Jacob Plattner - Berkeley CA
Alice Rico - Berkeley CA

Assignee:

Chiron Corporation - Emeryville CA

International Classification:

A61K 3170

US Classification:

514 29, 536 72, 536 73, 536 74

Abstract:

Antimicrobial macrolide compounds are provided having formulas II: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

US Patent:

6794366, Sep 21, 2004

Filed:

Apr 17, 2002

Appl. No.:

10/124988

Inventors:

Daniel Chu - Santa Clara CA
Gary Ashley - Alameda CA

Assignee:

Kosan Biosciences, Inc. - Hayward CA

International Classification:

A61K 3170

US Classification:

514 29, 536 72, 536 74

Abstract:

Compounds of the formula or the 10,11-anhydro forms therefor, wherein R is H or OH; R is H or halogen; R is H or a protecting group; R is methyl; unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C) or substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); R is H or a protecting group or is mono- or disubstituted amino carbonyl; R is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (1-10C); substituted or unsubstituted alkynyl (1-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or âOR may be replaced by âH; one of Z and Y is H and the other is OH or protected OH, or is amino, mono- or dialkyl-amino, protected amino, or an aminoheterocycle or Z and Y together are O, NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.

US Patent:

7368422, May 6, 2008

Filed:

Feb 24, 2006

Appl. No.:

11/361311

Inventors:

Yaohui Lei - Hebei, CN
Yu Bai - Hebei, CN
Daniel Chu - Santa Clara CA, US
Zhi-Jie Ni - Fremont CA, US
John Jian-Xin Wang - Oakland CA, US

Assignee:

Novartis Vaccines and Diagnostics Inc. - Emeryville CA

International Classification:

A61K 38/02
A61K 38/12
A61K 31/70
C07K 7/64
C07K 9/00
C07K 5/12

US Classification:

514 8, 514 9, 514 23, 530317, 530322

Abstract:

Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

US Patent:

7456183, Nov 25, 2008

Filed:

Apr 8, 2002

Appl. No.:

10/474331

Inventors:

Daniel Chu - Santa Clara CA, US
Rustum Boyce - San Francisco CA, US
David Duhl - Oakland CA, US
Bryan Chang - Concord CA, US

Assignee:

Novartis Vaccines and Diagnostics, Inc. - Emeryville CA

International Classification:

A61K 31/47
A61K 31/425
A61K 31/415
A61K 31/40
A61P 7/00
C07D 209/02
C07D 209/44
C07D 209/46
C07D 209/48
C07D 217/22
C07D 235/24
C07D 235/28
C07D 277/62
C07D 403/02

US Classification:

51425408, 514309, 514367, 514394, 514395, 514414, 514416, 514417, 544373, 546141, 548178, 5483061, 5483064, 5483071, 5483074, 5483094, 5483097, 548466, 548467, 548470, 548471, 548472, 548473, 548476, 548477, 548480, 548481

Abstract:

Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH, N, NR, C═O, C═S, S═O, SO, S, O, (CRR), C(═O)—(CRR), and C(═S)—(CRR), where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S═O, SO, C(O), NC(O), NC(S), OC(O), OC(S), C(NR), C(NOR), and a covalent bond. Z, Z, and Zare independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.