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1. 发明申请

WO2012125746A9 TRICYCLIC GYRASE INHIBITORS 审中-公开
公开(公告)号：WO2012125746A9
公开(公告)日：2013-10-24
申请号：PCT/US2012029104
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC , BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D487/14
CPC分类号： C07D487/04 , C07D487/14
摘要： Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
摘要翻译：本文公开了具有式I结构的化合物及其药学上合适的盐，酯和前药，其可用作抗菌有效的三环类回旋酶抑制剂。还考虑了相关的药物组合物，用途和制备化合物的方法。

2. 发明专利

AU2012229997A1 Tricyclic gyrase inhibitors 未知
公开(公告)号：AU2012229997A1
公开(公告)日：2013-09-19
申请号：AU2012229997
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D487/14
摘要： Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

3. 发明专利

CA2829939A1 TRICYCLIC GYRASE INHIBITORS 未知
公开(公告)号：CA2829939A1
公开(公告)日：2012-09-20
申请号：CA2829939
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D487/14
摘要： Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

4. 发明专利

CA2829939C TRICYCLIC GYRASE INHIBITORS 未知
公开(公告)号：CA2829939C
公开(公告)日：2020-10-13
申请号：CA2829939
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D487/14
摘要： (See Formula I) Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

5. 发明专利

ZA201307583B TRICYCLIC GYRASE INHIBITORS 未知
公开(公告)号：ZA201307583B
公开(公告)日：2014-08-27
申请号：ZA201307583
申请日：2013-10-11
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
摘要： Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

6. 发明专利

AR085806A1 INHIBIDORES TRICICLICOS DE GIRASA 未知
公开(公告)号：AR085806A1
公开(公告)日：2013-10-30
申请号：ARP120100830
申请日：2012-03-14
申请人： TRIUS THERAPEUTICS INC , L LIVERMORE NAT SECURITY LLC
发明人： BENSEN DANIEL , CHEN ZHIYONG , FINN JOHN , LAM THAN TO , LEE SUK JOONG , LI XIAOMING , PHILLIPSON DOUGLAS W , TARI LESLIE WILLIAM , TRZOSS MICHAEL , ZHANG JUNHU , LIGHTSTONE FELICE , NGUYEN TOAN B , WONG SERGIO E , ARISTOFF PAUL , JUNG MICHAEL
IPC分类号： C07D487/14 , A61K31/495 , A61P31/04 , C07D487/04
摘要： Procesos de obtención, composiciones farmacéuticas y compuestos intermediarios.Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1) o sales farmacéuticamente aceptables, ésteres, y prodrogas del mismo, donde L es O ó S; R8 es H o un sustituyente interactuante con una longitud de aproximadamente 1 - 5 Å desde el punto de unión de carbono en el Anillo A hasta el átomo terminal en R8 y un ancho de aproximadamente 3,3 Å o menor; X, Y y Z se seleccionan en forma independiente entre el grupo que consiste en N, CRX, CRY, y CRZ, con la condición de que no más que dos de X, Y y Z son N, donde RX es H o un sustituyente interactuante con una longitud de aproximadamente 1 - 2 Å desde el carbono en CRX hasta el átomo terminal en RX; donde RY es H o un sustituyente interactuante con una longitud de aproximadamente 1 - 3 Å desde el carbono en CRY hasta el átomo terminal en RY; donde RZ es H o un sustituyente interactuante con una longitud de aproximadamente 1 - 2 Å desde el carbono en CRZ hasta el átomo terminal en RZ; R2 es un anillo arilo o heteroarilo de 6 miembros que contiene 0 - 3 heteroátomos O, S, o N, opcionalmente sustituido con 0 - 3 sustituyentes no interferentes, donde 2 sustituyentes no interferentes adyacentes sobre R2 pueden formar uno o más anillos fusionados con el anillo arilo o heteroarilo de 6 miembros; donde el anillo arilo o heteroarilo de 6 miembros de R2 tiene un CH en la posición inmediatamente adyacente a la posición donde R2 se une a L; R4 es: H; un ORa opcionalmente sustituido; una amina secundaria o terciaria opcionalmente sustituida unida al anillo C a través del N de la amina secundaria o terciaria; o un residuo cíclico o heterocíclico insaturado de 5 - 10 miembros opcionalmente sustituido que contiene 0 - 3 heteroátomos N, O ó S; donde el sustituyente opcional es 0 - 3 sustituyentes no interferentes; donde Ra es un arilo o heteroarilo de 5 - 6 miembros que contiene 0 - 3 heteroátomos O, S, o N opcionalmente sustituido con 0 - 3 sustituyentes no interferentes; donde el sustituyente R4 no se proyecta más que 3 Å por debajo del plano de los anillos A, B y C hacia el piso del bolsillo de unión de GyrB/ParE en el estado unido; y donde R4 no interfiere estéricamente con R2 o Z cuando el compuesto se encuentra en el estado unido.

7. 发明公开

EP3044225A4 TRICYCLIC GYRASE INHIBITORS 审中-实审转让
标题翻译：三环旋转酶抑制剂
公开(公告)号：EP3044225A4
公开(公告)日：2017-03-08
申请号：EP14844214
申请日：2014-09-10
申请人： MERCK SHARP & DOHME , L LIVERMORE NAT SECURITY LLC
发明人： FINN JOHN , TARI LESLIE WILLIAM , CHEN ZHIYONG , ZHANG JUNHU , PHILLIPSON DOUGLAS , LEE SUK JOONG , TRZOSS MICHAEL , BENSEN DANIEL , LI XIAOMING , TENG MIN , ONG VOON , BORCHARDT ALLEN JOHN , LAM THANH TO , LIGHTSTONE FELICE C , WONG SERGIO E , NGUYEN TOAN B
IPC分类号： C07D487/04 , A61K31/519 , A61P31/04 , C07D487/16 , C07D487/22 , C07D491/147 , C07D515/22
CPC分类号： C07D487/04 , C07D491/147

8. 发明专利

NZ614983A Tricyclic gyrase inhibitors 未知
公开(公告)号：NZ614983A
公开(公告)日：2016-07-29
申请号：NZ61498312
申请日：2012-03-14
申请人： MERCK SHARP & DOHME , L LIVERMORE NAT SECURITY LLC
发明人： BENSEN DANIEL , FINN JOHN , LEE SUK JOONG , CHEN ZHIYONG , LAM THANH TO , LI XIAOMING , TRZOSS MICHAEL , JUNG MICHAEL , NGUYEN TOAN B , LIGHTSTONE FELICE , TARI LESLIE WILLIAM , ZHANG JUNHU , ARISTOFF PAUL , PHILLIPSON DOUGLAS W , WONG SERGIO E
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D487/14
摘要： Disclosed are 2-(aryloxy)-4-(heterocyclyl)-9H-pyrimido[4,5-b]indole derivatives of the general formula (I) or pharmaceutically suitable salts thereof, wherein L is O or S; R8 is H, Cl, Br, OH, amino, alkylamino, aminoalkyl, aminocyclopropyl, methoxy, ethoxy, cyclopropylamino, cyclopropylmethyl, chloromethyl, dichloromethyl, trichloromethyl, CH2CH2Cl, bromomethyl, dibromomethyl, fluoromethyl, difluoromethyl, trifluoromethyl, CH2CH2F, CH2CHF2, CH2CF3, NHOH, NHNHCH3, NHOCH3, NHCD3, SCH3 or NHCOH; X, Y and Z are CRX, CRY, and CRZ, respectively, wherein RX is H, methyl, Cl, Br or F; RY is H, methyl, difluoromethyl, trifluoromethyl, cyano, ethyl, Cl, Br, or F; Rz is H, methyl, Cl, Br, or F; R2 is an optionally substituted aryl as defined herein; and R4 is an optionally substituted aryl, optionally substituted aryloxy, substituted amino, or heterocycle connected through a nitrogen atom. Representative compounds include 6-fluoro-4-[(3aR,6aR)-hexahydropyrrolo[3,4-b]pyrrol-5(1H)-yl]-N-methyl-2-[(2-methylpyrimidin-5-yl)oxy]-9H-pyrimido[4,5-b]indol-8-amine. Also disclosed are pharmaceutical compositions comprising a compound as defined above for treating bacterial infections.

9. 发明专利

ZA201601628B TRICYCLIC GYRASE INHIBITORS 未知
公开(公告)号：ZA201601628B
公开(公告)日：2017-06-28
申请号：ZA201601628
申请日：2016-03-09
申请人： L LIVERMORE NAT SECURITY LLC , MERCK SHARP & DOHME
发明人： NGUYEN TOAN B , WONG SERGIO E , LIGHTSTONE FELICE C , LAM THANH TO , BORCHARDT ALLEN JOHN , ONG VOON , TENG MIN , LI XIAOMING , BENSEN DANIEL , TRZOSS MICHAEL , LEE SUK JOONG , PHILLIPSON DOUGLAS , ZHANG JUNHU , CHEN ZHIYONG , TARI LESLIE WILLIAM , FINN JOHN

10. 发明专利

AU2014318838A1 Tricyclic gyrase inhibitors 未知
公开(公告)号：AU2014318838A1
公开(公告)日：2016-03-24
申请号：AU2014318838
申请日：2014-09-10
申请人： L LIVERMORE NAT SECURITY LLC , MERCK SHARP & DOHME
发明人： FINN JOHN , TARI LESLIE WILLIAM , CHEN ZHIYONG , ZHANG JUNHU , PHILLIPSON DOUGLAS , LEE SUK JOONG , TRZOSS MICHAEL , BENSEN DANIEL , LI XIAOMING , TENG MIN , ONG VOON , BORCHARDT ALLEN JOHN , LAM THANH TO , LIGHTSTONE FELICE C , WONG SERGIO E , NGUYEN TOAN B
IPC分类号： C07D487/04 , A61K31/519 , A61P31/04 , C07D487/16 , C07D487/22 , C07D515/22
摘要： Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

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