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    • 2. 发明申请
    • TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS
    • 三氧化二氮唑酮类抗生素化合物
    • US20110195961A1
    • 2011-08-11
    • US13123218
    • 2009-10-06
    • Christian HubschwerlenDaniel RitzGeorg RueediJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • Christian HubschwerlenDaniel RitzGeorg RueediJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • A61K31/5415C07D413/14A61K31/538C07D417/14C07D471/06A61K31/437A61K31/5383A61P31/04
    • C07D471/06C07D471/16C07D487/06C07D519/00
    • 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.
    • 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。
    • 3. 发明授权
    • Antibiotics derivatives
    • 抗生素衍生物
    • US07981886B2
    • 2011-07-19
    • US11915179
    • 2006-05-24
    • Daniel BurChristian HubschwerlenJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • Daniel BurChristian HubschwerlenJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • C07D417/12C07D413/12C07D409/12A61K31/5415A61K31/538
    • C07D277/64C07D409/12C07D413/12C07D417/12C07D513/04
    • The invention relates to antibiotic derivatives of formula I wherein: A represents —O—, S, —C(═O)—, —C(═NOR6)—; Z—B represents NCH2CH2, NCOCH2, NCH2CO, NCH2CH(OH), CHN(R8)CH2 or CHN(R8)CO; D represents binuclear heteroaryl; Y1 represents —CR1— or —N—, Y2 represents —CR2— or —N—, Y3 represents —CR3— or —N— and Y4 represents —CR4— or —N—; U represents —NH—, —O— or —S— and V represents —N— or —CH—; W represents —CH2—, —O— or —NR7—; R1 represents H, methyl, ethyl or halogen; R2, R3 and R4 each represent independently H, C1-C4 alkyl, halogen, or C1-C4 alkoxy; R5 represents H, C1-C4 alkyl or fluorine; R6 represents H, C1-C4 alkyl or aryl-C1-C4 alkyl; R7 represents H, C1-C4 alkyl, aryl-C1-C4 alkyl or —CH2—COOH; R8 represents H, C1-C4 alkyl or —CH2—COOH; with the provisos that if Z—B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH), then W represents —CH2—; if A represents O or S, then W represents —CH2—; and only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.
    • 本发明涉及式I的抗生素衍生物,其中:A表示-O-,S,-C(= O) - , - C(= NOR 6) - ; Z-B表示NCH2CH2,NCOCH2,NCH2CO,NCH2CH(OH),CHN(R8)CH2或CHN(R8)CO; D表示双核杂芳基; Y1表示-CR1-或-N-,Y2表示-CR2-或-N-,Y3表示-CR3-或-N-,Y4表示-CR4-或-N-; U表示-NH-,-O-或-S-,V表示-N-或-CH-; W表示-CH 2 - , - O-或-NR 7 - ; R1代表H,甲基,乙基或卤素; R2,R3和R4各自独立地表示H,C1-C4烷基,卤素或C1-C4烷氧基; R5表示H,C1-C4烷基或氟; R6表示H,C1-C4烷基或芳基-C1-C4烷基; R 7表示H,C 1 -C 4烷基,芳基-C 1 -C 4烷基或-CH 2 -COOH; R8表示H,C1-C4烷基或-CH2-COOH; 条件是如果Z-B表示NCH 2 CH 2,NCOCH 2,NCH 2 CO或NCH 2 CH(OH),则W表示-CH 2 - ; 如果A表示O或S,则W表示-CH 2 - ; Y1,Y2,Y3和Y4中只有一个可以同时表示N个。
    • 6. 发明申请
    • New Piperidine Antibiotics
    • 新的哌啶抗生素
    • US20070173532A1
    • 2007-07-26
    • US11696513
    • 2007-04-04
    • Christian HUBSCHWERLENJean-Philippe SurivetComelia Zumbrunn-Acklin
    • Christian HUBSCHWERLENJean-Philippe SurivetComelia Zumbrunn-Acklin
    • A61K31/4709C07D409/14
    • C07D401/06C07D405/14C07D409/14C07D417/14
    • The invention relates to novel, antibacterially active piperidine derivatives of the formula wherein one of U and V represents N, the other represents N or CH; M represents CH2CH2, CH═CH, CH(OH)CH(OH), CH(OH)CH2, CH(NH2)CH2, COCH2 or OCH2; R1 represents alkyl, haloalkyl, alkoxy, haloalkoxy, halogen or cyano; R2 represents hydrogen or halogen; R3 represents carboxy, carboxamido, alkylaminocarbonyl, hydroxy, aminocarbonyloxy, 2-tetrazolyl or 3-methyl-1,2,4-oxadiazol-5-yl; R4 represents alkyl, (C1-C4)alkoxy-(C1-C4)alkyl, haloalkyl, alkenyl, arylalkyl, aryl-S(O)m-alkyl, heteroarylalkyl, heteroarylaminocarbonylalkyl, heteroaryl-S(O)m-alkyl, CH2—CH═CH-aryl or cycloalkyl-S(O)m-alkyl; n is an integer from 0 to 3; and m is 0 or 2.
    • 本发明涉及下式的新型抗菌活性哌啶衍生物,其中U和V中的一个代表N,另一个表示N或CH; M表示CH 2 CH 2,CH-CH,CH(OH)CH(OH),CH(OH)CH 2,CH( NH 2,CH 2,COCH 2或OCH 2; R 1表示烷基,卤代烷基,烷氧基,卤代烷氧基,卤素或氰基; R 2表示氢或卤素; R 3表示羧基,甲酰胺基,烷基氨基羰基,羟基,氨基羰基氧基,2-四唑基或3-甲基-1,2,4-恶二唑-5-基; R 4表示烷基,(C 1 -C 4 -C 4)烷氧基 - (C 1 -C 4 - 烷基,卤代烷基,烯基,芳基烷基,芳基-S(O)m - 烷基,杂芳基烷基,杂芳基氨基羰基烷基,杂芳基-S(O) 烷基,CH 2 -CH-CH-芳基或环烷基-S(O)m - 烷基; n为0〜3的整数。 m为0或2。
    • 7. 发明授权
    • Quinazoline-2,4-dione derivatives
    • 喹唑啉-2,4-二酮衍生物
    • US08916573B2
    • 2014-12-23
    • US14238415
    • 2012-08-10
    • Christian HubschwerlenGeorg RueediJean-Philippe SurivetCornelia Zumbrunn Acklin
    • Christian HubschwerlenGeorg RueediJean-Philippe SurivetCornelia Zumbrunn Acklin
    • A01N43/54A61K31/517C07D239/72C07D401/00
    • C07D471/04C07D413/14C07D417/14C07D498/04C07D513/04
    • The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.
    • 本发明涉及式(I)的抗菌化合物,其中R1是H,卤素,(C1-C3)烷基或(C1-C3)烷氧基; R2是H,卤素,(C1-C3)烷基,(C1-C3)烷氧基或吡咯烷-1-基; R 3是H,卤素,(C 1 -C 3)烷基,(C 1 -C 3)烷氧基,乙烯基或2-甲氧基羰基乙烯基,或者R 2和R 3与它们的两个碳原子一起形成苯环; R4是H,卤素,(C1-C3)烷基或(C1-C3)烷氧基; 并且R 5是H,(C 1 -C 3)烷基或环丙基,或R 4和R 5一起形成-CH 2 CH 2 CH 2 - 基; A是二价基团-CH 2 - , - CH 2 CH 2 - , - CH 2 OH,-CH 2 - , - CH 2 OH(R ​​6) - *和-CH 2 NHCH 2 - ,其中#表示与任选取代的(喹唑啉 - 2,4-二酮-3-基)甲基残基,*表示与取代的(恶唑烷酮-4-基)甲基残基的连接点; R6是H或乙酰基; Y是CH或N; Q为O或S; 和这些化合物的盐。
    • 9. 发明授权
    • Spiro antibiotic derivatives
    • 螺环类抗生素衍生物
    • US07999115B2
    • 2011-08-16
    • US12439571
    • 2007-08-29
    • Christian HubschwerlenJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • Christian HubschwerlenJean-Philippe SurivetCornelia Zumbrunn-Acklin
    • C07D263/52C07D263/58
    • C07D498/10
    • The invention relates to compounds of formula (I) wherein R1 represents H, alkyl, alkoxy, cyano or halogen; one of U and X represents CH or N and the other represents CH, or, in the case of U, may also represent CRa and, in the case of X, may also represent CRb; Ra represents halogen; Rb represents halogen or alkoxy; B represents N, D represents CH2 and A represents CH(OH)CH2 or CH2CH2, or B represents CH, D represents CH2 or O and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH═CH, CH2CH2 or NHCO, or also B represents C(OH), D represents CH2 and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH═CH, CH2CH2 Or NHCO; R2 represents H, alkyl, alkenyl, hydroxyalkyl or alkoxycarbonylalkyl; and E represents naphthyl or a binuclear heterocyclic group; and to salts of such compounds. These compounds are useful as antimicrobial agents.
    • 本发明涉及式(I)化合物,其中R 1表示H,烷基,烷氧基,氰基或卤素; U和X之一表示CH或N,另一个表示CH,或在U的情况下也可以表示CR a,在X的情况下也可以表示CRb; Ra表示卤素; Rb表示卤素或烷氧基; B表示N,D表示CH 2,A表示CH(OH)CH 2或CH 2 CH 2,或B表示CH,D表示CH 2或O,A表示OCH 2,CH 2 CH(OH),CH(OH)CH 2,CH(OH) OH),CH = CH,CH 2 CH 2或NHCO,或B表示C(OH),D表示CH 2,A表示OCH 2,CH 2 CH(OH),CH(OH)CH 2,CH(OH)CH(OH) CH,CH 2 CH 2或NHCO; R2代表H,烷基,烯基,羟基烷基或烷氧基羰基烷基; E表示萘基或双核杂环基; 和这些化合物的盐。 这些化合物可用作抗微生物剂。