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公开(公告)号：US09346804B2
公开(公告)日：2016-05-24
申请号：US14096419
申请日：2013-12-04
Applicant: Christian Hubschwerlen , Daniel Ritz , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
Inventor： Christian Hubschwerlen , Daniel Ritz , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC: A61K31/54 , A61K31/535 , C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
CPC classification number: C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
Abstract: The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
Abstract translation: 本发明涉及式（I）的抗菌化合物，其中“----”是键或不存在，V是CH，CR 6或N; R 0是H，或者如果“----”是键，也可以是烷氧基; R1是氰基，烷基或乙炔基; 当“----”是键时，U是CH或N，或者如果不存在“----”，则U是CH 2，NH或NH 9; R2是H，烷基羰基或CH2-R3; R3是H，烷基或羟烷基; R4是H或如果n不为0且R5是H，也可以是OH; R5是H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R6是羟基烷基，羧基，烷氧基羰基或 - （CH2）q-NR7R8，q是1,2或3，R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - （CH 2）p - ， - CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - ; G是取代的苯基或G1或G2，其中Q是O或S，X是CH或N; Y1，Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - 时，n为0，当A为 - （CH 2）p - ，p为1,2,3或4时，n为0,1或2， 条件是n和p之和为2,3或4; 和这些化合物的盐。
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公开(公告)号：US20140142093A1
公开(公告)日：2014-05-22
申请号：US14096419
申请日：2013-12-04
Applicant: Christian HUBSCHWERLEN , Daniel RITZ , Georg RUEEDI , Jean-Philippe SURIVET , Cornelia ZUMBRUNN-ACKLIN
Inventor： Christian HUBSCHWERLEN , Daniel RITZ , Georg RUEEDI , Jean-Philippe SURIVET , Cornelia ZUMBRUNN-ACKLIN
IPC: C07D471/06 , C07D487/06 , C07D519/00 , C07D471/16
CPC classification number: C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
Abstract: The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
Abstract translation: 本发明涉及式（I）的抗菌化合物，其中“----”是键或不存在，V是CH，CR 6或N; R 0是H，或者如果“----”是键，也可以是烷氧基; R1是氰基，烷基或乙炔基; 当“----”是键时，U是CH或N，或者如果不存在“----”，则U是CH 2，NH或NH 9; R2是H，烷基羰基或CH2-R3; R3是H，烷基或羟烷基; R4是H或如果n不为0且R5是H，也可以是OH; R5是H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R6是羟基烷基，羧基，烷氧基羰基或 - （CH2）q-NR7R8，q是1,2或3，R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - （CH 2）p - ， - CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - ; G是取代的苯基或G1或G2，其中Q是O或S，X是CH或N; Y1，Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - 时，n为0，当A为 - （CH 2）p - ，p为1,2,3或4时，n为0,1或2， 条件是n和p之和为2,3或4; 和这些化合物的盐。
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3.发明授权公开(公告)号：US07816117B2
公开(公告)日：2010-10-19
申请号：US11411988
申请日：2006-04-26
Applicant: Jonathan Beckwith , Daniel Ritz , Melinda Faulkner , Stephanie Gon , George Georgiou
Inventor： Jonathan Beckwith , Daniel Ritz , Melinda Faulkner , Stephanie Gon , George Georgiou
CPC classification number: C12N9/0065 , C12N2500/44 , C12N2501/70 , C12N2510/02
Abstract: The invention provides composition and methods for producing proteins of interest which comprise at least one disulfide bond, include proteins which in their mature form do not contain disulfide bonds, but whose precursor molecule contained at least one disulfide bond. The methods employ a host cell modified to more efficiently produce properly folded disulfide bond containing proteins. The host cells generally contain a mutation in one or more reductase genes, and can be further genetically modified to increase their growth rate, and are further optionally modified to increase the expression of a catalyst of disulfide bond formation. Host cells, methods for u sing such to produce proteins of interest, proteins of interest produced by these methods are within the scope of the invention.
Abstract translation: 本发明提供用于产生包含至少一个二硫键的感兴趣蛋白质的组合物和方法，包括其成熟形式不含二硫键但其前体分子含有至少一个二硫键的蛋白质。 该方法使用修饰的宿主细胞以更有效地产生适当折叠的含二硫键的蛋白质。 宿主细胞通常在一个或多个还原酶基因中含有突变，并且可进行进一步遗传修饰以增加其生长速率，并进一步任选地修饰以增加二硫键形成催化剂的表达。 宿主细胞，用于产生感兴趣的蛋白质的方法，通过这些方法生产的感兴趣的蛋白质在本发明的范围内。
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公开(公告)号：US08618092B2
公开(公告)日：2013-12-31
申请号：US13123218
申请日：2009-10-06
Applicant: Christian Hubschwerlen , Daniel Ritz , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
Inventor： Christian Hubschwerlen , Daniel Ritz , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC: A61K31/54 , A61K31/535
CPC classification number: C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
Abstract: The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
Abstract translation: 本发明涉及式I的抗菌化合物，其中是一个键或不存在，V是CH，CR 6或N; R 0是H，或者如果是键，也可以是烷氧基; R1特别是H或卤素; U是CH或N，当是键时，或如果不存在，U是CH 2，NH或NR 9; R2是H，烷基羰基或-CH2-R3; R3是H，烷基或羟基烷基; R4是H或如果n不为0且R5是H，也可以是OH; R5是H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R6是羟基烷基，羧基，烷氧基羰基或 - （CH2）q-NR7R8，q是1,2或3，R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - （CH 2）p - ， - CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - ; G为取代苯基或G1或G2，其中Q为O或S，X为CH或N; Y1，Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - 时，n为0，当A为 - （CH 2）p - ，p为1,2,3或4时，n为0,1或2， 条件是n和p之和为2,3或4; 和这些化合物的盐。
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5.发明申请Methods and Compositions for Ultra-High Throughput Screening of Natural Products 审中-公开天然产物超高通量筛选的方法和组成公开(公告)号：US20080318267A1
公开(公告)日：2008-12-25
申请号：US11793168
申请日：2005-12-16
Applicant: Richard H. Baltz , Catherine Monahan , Christopher Murphy , Julia Penn , Daniel Ritz , Stephen Wrigley
Inventor： Richard H. Baltz , Catherine Monahan , Christopher Murphy , Julia Penn , Daniel Ritz , Stephen Wrigley
Abstract: The present invention provides cells having more than two drug resistance genes and at least two different resistance genes that have been recombined into the chromosome of a cell. It also teaches the processes for preparing cells by recombining two or more different drug resistance genes into the chromosome of a cell. The invention further shows a screening method using the cells of described herein that may be used to accomplish high throughput screening of, among other things, natural products and/or whole cells isolated from the environment.
Abstract translation: 本发明提供具有两个以上药物抗性基因的细胞和已经重组到细胞染色体中的至少两个不同的抗性基因。 它还教导了通过将两个或多个不同的耐药基因重组到细胞的染色体中来制备细胞的过程。 本发明还显示了使用本文所述的细胞的筛选方法，其可用于实现除了其它方面从天然产物和/或从环境分离的全细胞的高通量筛选。
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Patent Agency Ranking
6.发明授权Compositions and methods for production of disulfide bond containing proteins in host cells 有权用于在宿主细胞中生产含二硫键的蛋白质的组合物和方法公开(公告)号：US07410788B2
公开(公告)日：2008-08-12
申请号：US11058926
申请日：2005-02-16
Applicant: Jonathan Beckwith , Fredrik Aslund , Paul H. Bessette , George Georgiou , Daniel Ritz , Jackie Eun-ah Lim
Inventor： Jonathan Beckwith , Fredrik Aslund , Paul H. Bessette , George Georgiou , Daniel Ritz , Jackie Eun-ah Lim
CPC classification number: C12N9/0004 , C12P21/02
Abstract: The invention provides composition and methods for producing proteins of interest which comprise at least one disulfide bond, include proteins which in their mature form do not contain disulfide bonds, but whose precursor molecule contained at least one disulfide bond. The methods employ a host cell modified to more efficiently produce properly folded disulfide bond containing proteins. The host cells generally contain a mutation in one or more reductase genes, and can be further genetically modified to increase their growth rate, and are further optionally modified to increase the expression of a catalyst of disulfide bond formation. Host cells, methods for using such to produce proteins of interest, proteins of interest produced by these methods are within the scope of the invention.
Abstract translation: 本发明提供用于产生包含至少一个二硫键的感兴趣蛋白质的组合物和方法，包括其成熟形式不含二硫键但其前体分子含有至少一个二硫键的蛋白质。 该方法使用修饰的宿主细胞以更有效地产生适当折叠的含二硫键的蛋白质。 宿主细胞通常在一个或多个还原酶基因中含有突变，并且可进行进一步遗传修饰以增加其生长速率，并进一步任选地修饰以增加二硫键形成催化剂的表达。 宿主细胞，使用其产生感兴趣的蛋白质的方法，通过这些方法生产的感兴趣的蛋白质在本发明的范围内。
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公开(公告)号：US20080051326A1
公开(公告)日：2008-02-28
申请号：US11667645
申请日：2005-11-11
Applicant: Dylan Alexander , Richard Baltz , Paul Brian , Marie-Francoise Coeffet-Le Gal , Sascha Doekel , Xiaowei He , Vidya Kulkarni , Christopher Leitheiser , Vivian Pak Woon Miao , Kien Trung Nguyen , Ian Barrie Parr , Daniel Ritz , Yanzhi Zhang
Inventor： Dylan Alexander , Richard Baltz , Paul Brian , Marie-Francoise Coeffet-Le Gal , Sascha Doekel , Xiaowei He , Vidya Kulkarni , Christopher Leitheiser , Vivian Pak Woon Miao , Kien Trung Nguyen , Ian Barrie Parr , Daniel Ritz , Yanzhi Zhang
Abstract: The present invention relates to novel depsipeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing these novel depsipeptide compounds and intermediates used in producing these compounds.
Abstract translation: 本发明涉及新颖的三肽类化合物。 本发明还涉及这些化合物的药物组合物和使用这些化合物作为抗菌化合物的方法。 本发明还涉及生产这些新型去肽肽化合物的方法和用于制备这些化合物的中间体。
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公开(公告)号：US20110195961A1
公开(公告)日：2011-08-11
申请号：US13123218
申请日：2009-10-06
Applicant: Christian Hubschwerlen , Daniel Ritz , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
Inventor： Christian Hubschwerlen , Daniel Ritz , Georg Rueedi , Jean-Philippe Surivet , Cornelia Zumbrunn-Acklin
IPC: A61K31/5415 , C07D413/14 , A61K31/538 , C07D417/14 , C07D471/06 , A61K31/437 , A61K31/5383 , A61P31/04
CPC classification number: C07D471/06 , C07D471/16 , C07D487/06 , C07D519/00
Abstract: The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds.
Abstract translation: 本发明涉及式I的抗菌化合物，其中是一个键或不存在，V是CH，CR 6或N; R 0是H，或者如果是键，也可以是烷氧基; R1特别是H或卤素; U是CH或N，当是键时，或如果不存在，U是CH 2，NH或NR 9; R2是H，烷基羰基或-CH2-R3; R3是H，烷基或羟烷基; R4是H或如果n不为0且R5是H，也可以是OH; R5是H，烷基，羟基烷基，氨基烷基，烷氧基烷基，羧基或烷氧基羰基; R6是羟基烷基，羧基，烷氧基羰基或 - （CH2）q-NR7R8，q是1,2或3，R7和R8各自独立地是H或烷基或R7和R8与带有它们的N原子形成环; R9是烷基或羟烷基; A是 - （CH 2）p - ， - CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - ; G为取代苯基或G1或G2，其中Q为O或S，X为CH或N; Y1，Y2和Y3各自为CH或N; 当A为-CH 2 CH 2 CH（OH） - 或-COCH 2 CH（OH） - 时，n为0，当A为 - （CH 2）p - ，p为1,2,3或4时，n为0,1或2， 条件是n和p之和为2,3或4; 和这些化合物的盐。
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9.发明申请Compositions and methods for production of disulfide bond containing proteins in host cells 有权用于在宿主细胞中生产含二硫键的蛋白质的组合物和方法公开(公告)号：US20060030022A1
公开(公告)日：2006-02-09
申请号：US11058926
申请日：2005-02-16
Applicant: Jonathan Beckwith , Fredrik Aslund , Paul Bessette , George Georgiou , Daniel Ritz , Jackie Lim
Inventor： Jonathan Beckwith , Fredrik Aslund , Paul Bessette , George Georgiou , Daniel Ritz , Jackie Lim
CPC classification number: C12N9/0004 , C12P21/02
Abstract: The invention provides composition and methods for producing proteins of interest which comprise at least one disulfide bond, include proteins which in their mature form do not contain disulfide bonds, but whose precursor molecule contained at least one disulfide bond. The methods employ a host cell modified to more efficiently produce properly folded disulfide bond containing proteins. The host cells generally contain a mutation in one or more reductase genes, and can be further genetically modified to increase their growth rate, and are further optionally modified to increase the expression of a catalyst of disulfide bond formation. Host cells, methods for using such to produce proteins of interest, proteins of interest produced by these methods are within the scope of the invention.
Abstract translation: 本发明提供用于产生包含至少一个二硫键的感兴趣蛋白质的组合物和方法，包括其成熟形式不含二硫键但其前体分子含有至少一个二硫键的蛋白质。 该方法使用修饰的宿主细胞以更有效地产生适当折叠的含二硫键的蛋白质。 宿主细胞通常在一个或多个还原酶基因中含有突变，并且可进行进一步遗传修饰以增加其生长速率，并进一步任选地修饰以增加二硫键形成催化剂的表达。 宿主细胞，使用其产生感兴趣的蛋白质的方法，通过这些方法生产的感兴趣的蛋白质在本发明的范围内。
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公开(公告)号：US20100311107A1
公开(公告)日：2010-12-09
申请号：US12844046
申请日：2010-07-27
Applicant: Richard H. Baltz , Catherine Monahan , Christopher Murphy , Julia Penn , Daniel Ritz , Stephen Wrigley
Inventor： Richard H. Baltz , Catherine Monahan , Christopher Murphy , Julia Penn , Daniel Ritz , Stephen Wrigley
IPC: C12Q1/18
Abstract: The present invention provides cells having more than two drug resistance genes and at least two different resistance genes that have been recombined into the chromosome of a cell. It also teaches the processes for preparing cells by recombining two or more different drug resistance genes into the chromosome of a cell. The invention further shows a screening method using the cells of described herein that may be used to accomplish high throughput screening of, among other things, natural products and/or whole cells isolated from the environment.
Abstract translation: 本发明提供具有两个以上药物抗性基因的细胞和已经重组到细胞染色体中的至少两个不同的抗性基因。 它还教导了通过将两个或多个不同的耐药基因重组到细胞的染色体中来制备细胞的过程。 本发明还显示了使用本文所述的细胞的筛选方法，其可用于实现除了其它方面从天然产物和/或从环境分离的全细胞的高通量筛选。
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