Compounds for inhibiting 1-deoxy-D-xylulose-5-phosphate reductoisomerase 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
US2014378418 A1 2014-12-25 [US20140378418]US9593136 B2 2017-03-14 [US9593136] / 2014-12-252017-03-14
申请号/申请日
2012US-14130384 / 2012-06-29
发明人
BOSHOFF HELENA I;DOWD CYNTHIA S;JACKSON EMILY R;KEHN-HALL KYLENE;LEE RICHARD E;LEE ROBIN;SAN JOSE GERALDINE;
申请人
GEORGE MASON UNIVERSITY;GEORGE WASHINGTON UNIVERSITY;ST JUDE CHILDRENS RESEARCH HOSPITAL;US DEPARTMENT OF HEALTH & HUMAN SERVICES;
主分类号
IPC分类号
A01N-037/46A01N-057/18A61K-031/135A61K-031/66A61K-031/662C07F-009/40C12Q-001/533
摘要
(US9593136) In particular, the compound is effective to inhibit Dxr in Mycobacterium tuberculosis (Mtb).  The present invention relates to compounds having general formula (I) or (II) where X is an acidic group, such as carboxylate, phosphonate, sulfate, and tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, preferably 2, 3, or 4.  The compounds inhibits 1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr), particularly Dxr in Mycobacterium tuberculosis (Mtb).
机翻摘要
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地址
代理人
代理机构
;
优先权号
2011US-61503736 2011-07-01 2012US-14130384 2012-06-29 2012WO-US44962 2012-06-29
主权利要求
(US9593136) What is claimed is: 1.  A compound having the chemical structure of formula (II)   wherein X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) a tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4,   wherein "n is 1" and    are not simultaneously satisfied. 2. The compound of claim 1, wherein Ar is a phenyl or a heteroaromatic group. 3. A compound having the chemical structure of formula (II)   wherein X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) a tetrazol; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and wherein n is 2, 3, or 4. 4. A compound having the chemical structure of formula (II)   wherein X is a phosphonate, an ester thereof, or a salt thereof; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, wherein "n is 1" and    are not simultaneously satisfied. 5. The compound of claim 1, selected from the group consisting of:   6. A pharmaceutical composition comprising a compound having the chemical structure of formula (II)   wherein X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, wherein "n is 1" and    are not simultaneously satisfied. 7. The composition of claim 6, wherein Ar is a phenyl or a heteroaromatic group. 8. A pharmaceutical composition comprising a compound having the chemical structure of formula (II)   where X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) a tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; wherein n is 2, 3, or 4. 9. A pharmaceutical composition comprising the compound of claim 5.
法律状态
(US9593136) LEGAL DETAILS FOR US2014378418  Actual or expected expiration date=2032-06-29    Legal state=ALIVE    Status=GRANTED     Event publication date=2012-06-29  Event code=US/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=US US14130384  Application date=2012-06-29  Standardized application number=2012US-14130384     Event publication date=2012-06-29  Event code=US/EXMR  Event type=Administrative notifications  USPTO Examiner Name Primary Examiner: OTTON, ALICIA L    Event publication date=2012-06-29  Event code=US/ART  Event type=Administrative notifications  USPTO Art Group  ART=1626     Event publication date=2012-06-29  Event code=US/ENT  Event type=Administrative notifications  Entity Status Set to Undiscounted Business Entity Status: UNDISCOUNTED    Event publication date=2012-06-29  Event code=US/AIA  Event type=Administrative notifications  First Inventor File Indicated:  AIA=No     Event publication date=2012-06-29  Event code=US/DK  Event type=Examination events  Attorney Docket Number Docket Nbr: 130761.00262    Event publication date=2012-06-29  Event code=US/CUST  Event type=Examination events  Attorney/Agent Customer Number Customer Nbr: 27557    Event publication date=2013-12-31  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2013-12-31  Event code=US/ENT  Event type=Administrative notifications  Entity Status Set to Undiscounted    Event publication date=2014-01-31  Event code=US/M905  Event type=Examination events  Event type=OAO  Notice of DO/EO Missing Requirements Mailed    Event publication date=2014-02-12  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2014-05-12  Event code=US/APE  Event type=Corrections  Preliminary amendments    Event publication date=2014-08-18  Event code=US/PTARDY  Event indicator=Pos  Event type=Examination events  Patent Term Adjustment - Ready for Examination    Event publication date=2014-09-11  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment  Effective date of the event=2014-02-04  ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNORS:LEE, RICHARD E. LEE, ROBIN REEL/FRAME:033716/0699     Event publication date=2014-09-11  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNORS:DOWD, CYNTHIA JACKSON, EMILY R. SAN JOSE, GERALDINE SIGNING DATES FROM 20120827 TO 20140826 REEL/FRAME:033716/0658     Event publication date=2014-09-11  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment  Effective date of the event=2012-07-20  ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNOR:KEHN-HALL, KYLENE REEL/FRAME:033716/0709     Event publication date=2014-09-15  Event code=US/APPFILEREC  Event type=Administrative notifications  Event type=OAO  Filing Receipt    Event publication date=2014-09-15  Event code=US/M903  Event indicator=Pos  Event type=Examination events  Event type=OAO  Notice of DO/EO Acceptance Mailed    Event publication date=2014-11-03  Event code=US/RLRCPTC  Event type=Administrative notifications  Event type=OAO  Filing Receipt - Corrected    Event publication date=2014-11-18  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2014-12-01  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment  Effective date of the event=2014-11-21  CONFIRMATORY LICENSE ASSIGNOR:GEORGE WASHINGTON UNIVERSITY REEL/FRAME:034499/0559     Event publication date=2014-12-25  Event code=US/A1  Event type=Examination events  Application published  Publication country=US  Publication number=US2014378418  Publication stage Code=A1  Publication date=2014-12-25  Standardized publication number=US20140378418     Event publication date=2014-12-29  Event code=US/PGPUBN  Event indicator=Pos  Event type=Examination events  Event type=OAO  PG-Pub Issue Notification    Event publication date=2015-03-12  Event code=US/RESTREQ  Event type=Examination events  Event type=Corrections  Event type=OAO  Restriction/Election Requirement    Event publication date=2015-05-14  Event code=US/ELC  Event type=Examination events  Event type=OAI  Response to Election / Restriction Filed    Event publication date=2015-07-07  Event code=US/CTNF  Event type=Examination events  Event type=OA  Event type=OAO  Non-Final Rejection    Event publication date=2015-10-01  Event code=US/CTNFR  Event type=Examination events  Event type=OAI  Response after Non-Final Action    Event publication date=2015-10-06  Event code=US/AS  Event type=Change of name or address  Event type=Reassignment  Assignment  Effective date of the event=2015-09-24  ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNOR:BOSHOFF, HELENA INGRID REEL/FRAME:036795/0789     Event publication date=2015-12-15  Event code=US/CTFR  Event type=Examination events  Event type=OA  Event type=OAO  Final Rejection    Event publication date=2016-03-22  Event code=US/CTFAR  Event type=Examination events  Event type=OAI  Response after Final Action    Event publication date=2016-04-09  Event code=US/CTAV  Event type=OAO  Advisory Action (PTOL-303)    Event publication date=2016-04-22  Event code=US/RCEX  Event type=Examination events  Event type=RCE  Event type=OAI  Request for Continued Examination (RCE)    Event publication date=2016-04-22  Event code=US/136G  Event type=OAO  Request for Extension of Time - Granted    Event publication date=2016-04-27  Event code=US/DRCECAP  Event type=RCE  Event type=OAO  Disposal for a RCE / CPA / R129    Event publication date=2016-08-28  Event code=US/CTNFR  Event type=Examination events  Event type=OAI  Response after Non-Final Action    Event publication date=2016-08-31  Event code=US/CTNF  Event type=Examination events  Event type=OA  Event type=OAO  Non-Final Rejection    Event publication date=2016-08-31  Event code=US/EXET  Event type=Examination events  Event type=OAO  Event type=INT  Interview Summary - Examiner Initiated - telephonic    Event publication date=2016-10-21  Event code=US/EXAC  Event type=Examination events  Event type=OAO  Examiner's Amendment Communication    Event publication date=2016-10-26  Event code=US/NOAM  Event indicator=Pos  Event type=Examination events  Event type=OAO  Mail Notice of Allowance    Event publication date=2017-01-31  Event code=US/APRDY  Event indicator=Pos  Event type=Examination events  Application Is Considered Ready for Issue    Event publication date=2017-02-22  Event code=US/PAT  Event indicator=Pos  Event type=Event indicating In Force  Patented Case    Event publication date=2017-02-22  Event code=US/ISSM  Event indicator=Pos  Event type=Examination events  Event type=OAO  Event type=Restitution or restoration  Issue Notification Mailed    Event publication date=2017-03-14  Event code=US/B2  Event indicator=Pos  Event type=Event indicating In Force  Granted patent as second publication  Publication country=US  Publication number=US9593136  Publication stage Code=B2  Publication date=2017-03-14  Standardized publication number=US9593136     Event publication date=2017-03-14  Event code=US/354  Event indicator=Pos  Event type=Extension of term of duration of protection  Patent term extended under  35 U.S.C 154(b) until/for Delays (A,B,C): 0  Overlap Delays: 0  Non Overlap Delays: 32   PTO Office Delays: 0  Applicant Delays: 141  Adjustment total:  Number of days of extension=0
专利类型码
A1B2
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