公开(公告)号：US20220313624A1

公开(公告)日：2022-10-06

申请号：US17826660

申请日：2022-05-27

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Jiajia DONG ,  K. Barry SHARPLESS ,  Jeffery W. KELLY ,  Aleksandra BARANCZAK ,  Wentao CHEN

IPC: A61K31/05 ,  C07C305/26 ,  C07D277/82 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  A61K47/54 ,  C07D279/08 ,  C07D501/18 ,  A61K31/136 ,  A61K31/14 ,  A61K31/197 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4168 ,  A61K31/4245 ,  A61K31/4353 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/485 ,  A61K31/505 ,  A61K31/515 ,  A61K31/53 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/65 ,  A61K31/655 ,  A61K31/70 ,  A61K31/7048 ,  A61K38/31 ,  A61K51/04 ,  C07K1/02 ,  C07K1/113 ,  C07K2/00

Abstract: Described herein are compounds comprising a biologically active organic core group with one to five —Z—(X1—S(O)(X2)F)m groups attached thereto, wherein Z is O, NR, or N; X1 is a covalent bond or CH2CH2; m can be 1 or 2 depending on the identity of Z; and X2 is O or NR. In some embodiments, the core group is an amino acid or a protein. In some embodiments the core group is a compound that has therapeutic activity toward a therapeutic target.

公开(公告)号：US20220000799A1

公开(公告)日：2022-01-06

申请号：US17471936

申请日：2021-09-10

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Jiajia DONG ,  K. Barry SHARPLESS ,  Jeffery W. KELLY ,  Aleksandra BARANCZAK ,  Wentao CHEN

IPC: A61K31/05 ,  C07C305/26 ,  C07D277/82 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  A61K47/54 ,  C07D279/08 ,  C07D501/18 ,  A61K31/136 ,  A61K31/14 ,  A61K31/197 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4168 ,  A61K31/4245 ,  A61K31/4353 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/485 ,  A61K31/505 ,  A61K31/515 ,  A61K31/53 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/65 ,  A61K31/655 ,  A61K31/70 ,  A61K31/7048 ,  A61K38/31 ,  A61K51/04 ,  C07K1/02 ,  C07K1/113 ,  C07K2/00

Abstract: This application describes modified amino acids and polypeptides comprising a SO2F or CH2CH2SO2F group bound to the side chain of an amono acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptot sites of receptor proteins are also described herein.

公开(公告)号：US20170196985A1

公开(公告)日：2017-07-13

申请号：US15316742

申请日：2015-06-05

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Jiajia DONG ,  K. Barry SHARPLESS ,  Jeffery W. KELLY ,  Aleksandra BARANCZAK ,  Wentao CHEN

IPC: A61K47/48 ,  C07K1/02 ,  C07K2/00 ,  A61K31/56 ,  A61K31/5513 ,  A61K31/515 ,  A61K31/485 ,  A61K31/4353 ,  A61K31/65 ,  A61K31/7048 ,  A61K31/70 ,  A61K31/05 ,  A61K31/655 ,  A61K31/4245 ,  A61K31/407 ,  A61K31/4168 ,  A61K31/40 ,  A61K31/505 ,  A61K31/14 ,  A61K31/473 ,  A61K31/53 ,  A61K31/197 ,  A61K31/4745 ,  A61K31/47 ,  A61K31/397 ,  A61K31/198 ,  A61K38/31 ,  A61K31/439 ,  A61K31/4045 ,  A61K51/04 ,  A61K31/136 ,  A61K31/4709 ,  C07C305/26 ,  C07K1/113 ,  C07K19/00

CPC classification number: A61K31/05 ,  A61K31/136 ,  A61K31/14 ,  A61K31/197 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4168 ,  A61K31/4245 ,  A61K31/4353 ,  A61K31/439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/485 ,  A61K31/505 ,  A61K31/515 ,  A61K31/53 ,  A61K31/5513 ,  A61K31/56 ,  A61K31/65 ,  A61K31/655 ,  A61K31/70 ,  A61K31/7048 ,  A61K38/31 ,  A61K47/54 ,  A61K51/0497 ,  C07C305/26 ,  C07C2601/14 ,  C07C2603/18 ,  C07D277/82 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  C07K1/02 ,  C07K1/1136 ,  C07K2/00

Abstract: This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.