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公开(公告)号：US20200268683A1
公开(公告)日：2020-08-27
申请号：US16871902
申请日：2020-05-11
Applicant: THE SCRIPPS RESEARCH INSTITUTE
Inventor： Jie LI , Zilei LIU , Suhua LI , Peng WU , K. Barry SHARPLESS
IPC: A61K31/05 , A61K31/136 , C07C305/26 , C07K1/113 , C07K1/02 , A61K51/04 , A61K38/31 , A61K31/7048 , A61K31/70 , A61K31/655 , A61K31/65 , A61K31/56 , A61K31/5513 , A61K31/53 , A61K31/515 , A61K31/505 , A61K31/485 , A61K31/4745 , A61K31/473 , A61K31/4709 , A61K31/47 , A61K31/439 , A61K31/4353 , A61K31/4245 , A61K31/4168 , A61K31/407 , A61K31/4045 , A61K31/40 , A61K31/397 , A61K31/198 , A61K31/197 , A61K31/14 , C07K2/00 , C07D295/26 , C07D295/185 , C07D295/088 , C07D277/82 , A61K47/54
Abstract: A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO2F2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilyl chloride to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.
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公开(公告)号：US20220079950A1
公开(公告)日：2022-03-17
申请号：US17419904
申请日：2019-12-31
Inventor： Palmer TAYLOR , Jeremiah MOMPER , Zoran RADIC , K. Barry SHARPLESS , Rakesh SIT
Abstract: In alternative embodiments, the provided are therapeutic combinations comprising: nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nervous system (CNS); and, a brain efflux transporter inhibitor, or an inhibitor of renal tubular secretion, wherein optionally the brain efflux transporter inhibitor or the inhibitor of renal tubular secretion comprises a P-glycoprotein inhibitor, an organic anion transporter (OAT) inhibitor and/or an organic cation (OCT) transporter inhibitor.
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公开(公告)号：US20160214946A1
公开(公告)日：2016-07-28
申请号：US15085568
申请日：2016-03-30
Applicant: The Scripps Research Institute
Inventor： K. Barry SHARPLESS , Valery FOKIN , Vsevold A. ROSTOVTSEV , Luke GREEN , Fahmi HIMO
IPC: C07D249/04
CPC classification number: C07D249/04 , B01J31/1805 , B01J2231/327 , B01J2531/16 , B01J2531/96 , C07D249/06 , C07D403/06
Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Ru ion to form a 1,4-disubstituted 1,2,3-triazole.
Abstract translation: 使用铜催化的点击化学连接方法结合叠氮化物和末端炔烃以提供1,4-二取代的1,2,3-三唑三唑。 该方法包括将有机叠氮化物和末端炔烃的溶液与催化Ru离子源接触以形成1,4-二取代的1,2,3-三唑。
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公开(公告)号：US20150232432A1
公开(公告)日：2015-08-20
申请号：US14705527
申请日：2015-05-06
Applicant: The Scripps Research Institute
Inventor： K. Barry SHARPLESS , Valery FOKIN , Vsevold A. ROSTOVTSEV , Luke GREEN , Fahmi HIMO
IPC: C07D249/04
CPC classification number: C07D249/04 , B01J31/1805 , B01J2231/327 , B01J2531/16 , B01J2531/96 , C07D249/06 , C07D403/06
Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting a solution of an organic azide and a terminal alkyne with a source of catalytic Cu(I) ion to form a 1,4-disubstituted 1,2,3-triazole, wherein the source of Cu(I) ion comprises Cu(II) and a metal capable of reducing Cu(II) to Cu(I). In some embodiments, the metal capable of reducing Cu(II) to Cu(I) is selected from the group consisting of Al, Be, Co, Cr, Fe, Mg, Mn, Ni, and Zn.
Abstract translation: 使用铜催化的点击化学连接方法结合叠氮化物和末端炔烃以提供1,4-二取代的1,2,3-三唑三唑。 该方法包括将有机叠氮化物和末端炔烃的溶液与催化性Cu（I）离子源接触以形成1,4-二取代的1,2,3-三唑，其中Cu（I）离子源包括 Cu（II）和能够将Cu（II）还原为Cu（I）的金属。 在一些实施方案中，能够将Cu（II）还原为Cu（I）的金属选自Al，Be，Co，Cr，Fe，Mg，Mn，Ni和Zn。
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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.
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Patent Agency Ranking
公开(公告)号：US20150031895A1
公开(公告)日：2015-01-29
申请号：US14508552
申请日：2014-10-07
Applicant: THE SCRIPPS RESEARCH INSTITUTE
Inventor： K. Barry SHARPLESS , Valery FOKIN , Vsevold A. ROSTOVTSEV , Luke GREEN , Fahmi HIMO
IPC: C07D249/04
CPC classification number: C07D249/04 , B01J31/1805 , B01J2231/327 , B01J2531/16 , B01J2531/96 , C07D249/06 , C07D403/06
Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion in human blood plasma to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt, Cu(II) ion in the presence of a reducing agent, or copper metal.
Abstract translation: 使用铜催化的点击化学连接方法结合叠氮化物和末端炔烃以提供1,4-二取代的1,2,3-三唑三唑。 该方法包括使有机叠氮化物和末端炔与人血浆中的反应性Cu（I）离子源接触以通过环加成1,4-二取代的1,2,3-三唑接触。 反应性Cu（I）离子的来源可以是例如在还原剂存在下的Cu（I）盐，Cu（II）离子或铜金属。
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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.
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公开(公告)号：US20190167604A1
公开(公告)日：2019-06-06
申请号：US16243761
申请日：2019-01-09
Applicant: THE SCRIPPS RESEARCH INSTITUTE
Inventor： Jie LI , Zilei LIU , Suhua LI , Peng WU , K. Barry SHARPLESS
IPC: A61K31/05 , A61K47/54 , A61K31/136 , C07C305/26 , C07K1/113 , C07K1/02 , A61K51/04 , A61K38/31 , A61K31/7048 , A61K31/70 , A61K31/655 , A61K31/65 , A61K31/56 , A61K31/5513 , A61K31/53 , A61K31/515 , A61K31/505 , A61K31/485 , A61K31/4745 , A61K31/473 , A61K31/4709 , A61K31/47 , A61K31/439 , A61K31/4353 , A61K31/4245 , A61K31/4168 , A61K31/407 , A61K31/4045 , A61K31/40 , A61K31/397 , A61K31/198 , A61K31/197 , A61K31/14 , C07K2/00 , C07D295/26 , C07D295/185 , C07D295/088 , C07D277/82
Abstract: Arylfluorosulfate compounds derived from anticancer drugs are disclosed herein, which exhibit improved anti-cancer cell proliferation activities compared to their phenolic drug precursors. Among these compounds, the fluorosulfate derivative of fulvestrant showed significantly enhanced activity to down-regulate estrogen receptor (ER) expression in ER+ breast cancer cell line MCF-7, and oral availability in vivo; the fluorosulfate derivative of combretastatin A4 exhibited a 70-fold increase in potency in the drug resistant colon cancer cell line HT-29; and the fluorosulfate derivative of ABT-751 showed enhanced activity relative to ABT-751.
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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.
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公开(公告)号：US20140066632A1
公开(公告)日：2014-03-06
申请号：US14078106
申请日：2013-11-12
Applicant: The Scripps Research Institute
Inventor： K. Barry SHARPLESS , Valery FOKIN , Vsevold A. ROSTOVTSEV , Luke GREEN , Fahmi HIMO
IPC: C07D249/04
CPC classification number: C07D249/04 , B01J31/1805 , B01J2231/327 , B01J2531/16 , B01J2531/96 , C07D249/06 , C07D403/06
Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion in human blood plasma to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt, Cu(II) ion in the presence of a reducing agent, or copper metal.
Abstract translation: 使用铜催化的点击化学连接方法结合叠氮化物和末端炔烃以提供1,4-二取代的1,2,3-三唑三唑。 该方法包括使有机叠氮化物和末端炔与人血浆中的反应性Cu（I）离子源接触以通过环加成1,4-二取代的1,2,3-三唑接触。 反应性Cu（I）离子的来源可以是例如在还原剂存在下的Cu（I）盐，Cu（II）离子或铜金属。
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