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1. 发明申请

WO2005084687A2 BORONIC ACID THROMBIN INHIBITORS 审中-公开
标题翻译：硼酸抑制剂
公开(公告)号：WO2005084687A2
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000918
申请日：2005-03-09
申请人： TRIGEN LIMITED , WANG, Shouming
发明人： WANG, Shouming
IPC分类号： A61K31/69
CPC分类号： C07F5/025 , Y02P20/55
摘要： A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH 2 ) or an amino-protecting group; aal is an amino acid residue having a side chain selected from formula (A) and (B)-(CO) a -(CH 2 ) b -D c -(CH 2 )d-E (A), -(CO) a -(CH 2 ) b -D c -C e (E 1 )(E 2 )(E 3 ) wherein E 1 , E 2 and E 3 ore 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E 1 , E 2 and E 3 is hydrogen and the other two are a said hydrocarbyl ring, E, E 1 , E 2 and E 3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa 2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R 9 is a straight chain alkyl group interrupted by one or more ether linkages or R 9 is -(CH2)m W and W is -OH or halogen.
摘要翻译：选自式（I）的硼酸的凝血酶抑制剂及其盐，前药和前药盐：其中X为H（形成NH 2）或氨基保护基; aAL是具有选自式（A）和（B） - （CO）a-（CH2）b-Dc-（CH2）dE（A）， - （CO）a-（CH2） b-Dc-Ce（E 1）（E 2）（E 3）（E 3）其中E 1，E 2和E 3为5-6元饱和或不饱和烃基环，或 E 1，E 2和E 3之一是氢，另外两个是所述烃基环，E，E 1，E 2和E 3任选在饱和时卤化，当不饱和时，强制卤化，特定的卤素为氟; aa 2是与凝血酶S2亚位点结合的氨基酸残基; 并且R 9是被一个或多个醚键中断的直链烷基，或者R 9是 - （CH 2）m W且W是-OH或卤素。

2. 发明申请

WO1995009150A1 CHIRAL NITRILES, THEIR PREPARATION AND THEIR USE FOR THE MANUFACTURE OF VERAPAMIL AND ANALOGUES 审中-公开
标题翻译：氯吡格雷，他们的制备及其制备维生素和类似物的用途
公开(公告)号：WO1995009150A1
公开(公告)日：1995-04-06
申请号：PCT/GB1994002091
申请日：1994-09-26
申请人： CHIROSCIENCE LIMITED , MCCAGUE, Raymond , WANG, Shouming
发明人： CHIROSCIENCE LIMITED
IPC分类号： C07C255/43
CPC分类号： C07C255/43 , C07C253/34
摘要： A process for preparing a substantially single enantiomer (R &cir& _ or S &cir& _) of R'-NH-(CH2)3-C(Ar) (CN)-R, the process comprising reacting together R-CH(Ar)-CN and X-(CH2)3-A to give X-(CH2)3-CH(Ar) (CN)-R, reacting that with methylamine to give R'-NH-(CH2)3-C(Ar) (CN)-R, and resolving that into a substantially single enantiomer thereof, wherein Ar is aryl, R and R' are each independently C1-20 alkyl, X is a halo atom and A is a leaving group and the resolution is carried out using a chiral acid. The process is particularly useful for preparing verapamil, and analogues thereof, in single enantiomeric form.
摘要翻译：一种制备R'-NH-（CH2）3-C（Ar）（CN）-R的基本上单一对映异构体（R 1和R 3）的方法，该方法包括使R-CH（Ar） - CN和X-（CH 2）3 -A，得到X-（CH 2）3 -CH（Ar）（CN）-R，使其与甲胺反应，得到R'-NH-（CH 2）3 -C（Ar）（ CN）-R，并将其拆分成基本上单一的对映异构体，其中Ar是芳基，R和R'各自独立地是C 1-20烷基，X是卤素原子，A是离去基团，分辨率是使用手性酸。该方法特别可用于以单一对映体形式制备维拉帕米及其类似物。

3. 发明申请

WO2012131396A1 3 -DESCLADINOSYL-O- CARBAMOYL FUNCTIONALIZED DERIVATIVES OF AZITHROMYCIN 审中-公开
标题翻译：三氧嘧啶的3 -DESCLADINOSYL-O-碳酰胺官能化衍生物
公开(公告)号：WO2012131396A1
公开(公告)日：2012-10-04
申请号：PCT/GB2012/050728
申请日：2012-03-30
申请人： NORBROOK LABORATORIES LIMITED , DAUVERGNE, Jerome , WANG, Shouming
发明人： DAUVERGNE, Jerome , WANG, Shouming
IPC分类号： C07D413/12 , C07D413/14 , A61P31/00 , A61P31/04 , A61K31/7052
CPC分类号： C07D413/14 , C07D413/12
摘要： The present invention relates to novel compounds from the class of azalide antibiotics. Particularly the invention relates to novel 3-descladinosyl-0-carbamoyl-9-deoxo-9a-aza- 9a-homoerythromycin compounds and to their pharmaceutically acceptable derivatives. The present invention also relates to the use of such compounds as anti-microbial agents, to pharmaceutical compositions comprising such compounds, as well as to methods of manufacturing such compounds.
摘要翻译：本发明涉及来自氮杂类抗生素类的新化合物。特别地，本发明涉及新的3-去二脱氧谷氨酰基-O-氨基甲酰基-9-脱氧-9a-氮杂-9a-高红霉素化合物及其药学上可接受的衍生物。本发明还涉及这种化合物作为抗微生物剂，包含这些化合物的药物组合物的用途以及制备这些化合物的方法。

4. 发明申请

WO2006059083A1 NEUTRALISING AGENTS FOR BORONIC ACID DRUGS 审中-公开
标题翻译：中性酸药物中和剂
公开(公告)号：WO2006059083A1
公开(公告)日：2006-06-08
申请号：PCT/GB2005/004565
申请日：2005-11-30
申请人： TRIGEN LIMITED , CHAHWALA, Suresh, Babubhai , WANG, Shouming , RUSSELL, Patric, Russell
发明人： CHAHWALA, Suresh, Babubhai , WANG, Shouming , RUSSELL, Patric, Russell
IPC分类号： A61K31/19
CPC分类号： A61K31/19
摘要： The use of specified compounds for the manufacture of a medicament for therapeutically neutralising an organoboronate drug. The specified compounds are typically hydroxy fatty acids or hydroperoxy fatty acids, for example 9(S)-HODE, 8(S)-HETRE or 8(S)-HEPE, or their salts or prodrugs. The organoboronate drug may be TRI 50c or a salt or prodrug thereof. Also disclosed are intravenous formulations containing the specified compounds.
摘要翻译：使用指定的化合物来制造用于治疗中和有机硼酸盐药物的药物。指定的化合物通常是羟基脂肪酸或氢过氧脂肪酸，例如9（S）-HODE，8（S）-HETRE或8（S）-HEPE，或其盐或前药。有机硼酸盐药物可以是TRI 50c或其盐或前药。还公开了含有特定化合物的静脉内制剂。

5. 发明申请

WO1994013828A1 CHIRAL ARYLPROPIONATES AND THEIR USE 审中-公开
标题翻译： CHIRAL ARYLPROPIONATES及其使用
公开(公告)号：WO1994013828A1
公开(公告)日：1994-06-23
申请号：PCT/GB1993002530
申请日：1993-12-10
申请人： CHIROSCIENCE LIMITED , McCAGUE, Raymond , WANG, Shouming , TAYLOR, Stephen, John, Clifford
发明人： CHIROSCIENCE LIMITED
IPC分类号： C12P41/00
CPC分类号： C07D281/10 , C07C69/732 , C07D303/48 , C12P7/62 , C12P41/004
摘要： Compounds having the formula: Ar-CHOR -CHHal-COOR are useful as chiral synthons, for example in the synthesis of the anti-hypertensive agent diltiazem, and related calcium channel blocking agents. The synthons can be prepared in enantiomerically-purified form without wastage of the unwanted enantiomer.
摘要翻译：具有下式的化合物：Ar-CHOR 1 -CHHal-COOR 2可用作手性合成子，例如在抗高血压剂地尔硫卓的合成中以及相关的钙通道阻断剂。合成子可以以对映体纯化的形式制备而不浪费不需要的对映异构体。

6. 发明申请

WO2005084687A3 BORONIC ACID THROMBIN INHIBITORS 审中-公开
标题翻译：硼酸抑制剂
公开(公告)号：WO2005084687A3
公开(公告)日：2006-04-20
申请号：PCT/GB2005000918
申请日：2005-03-09
申请人： TRIGEN LTD , WANG SHOUMING
发明人： WANG SHOUMING
IPC分类号： A61K31/69 , C07F5/02 , A61P7/02
CPC分类号： C07F5/025 , Y02P20/55
摘要： A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH
摘要翻译：选自式（I）的硼酸的凝血酶抑制剂及其盐，前药和前药盐：其中X是H（以形成NH

7. 发明申请

WO2004065389A1 PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS MODULATORS OF MULTIDRUG RESISTANCE 审中-公开
标题翻译：用作多抗电荷调节剂的吡咯烷酮衍生物
公开(公告)号：WO2004065389A1
公开(公告)日：2004-08-05
申请号：PCT/GB2004/000274
申请日：2004-01-23
申请人： XENOVA LIMITED , MILTON, John , WREN, Stephen , WANG, Shouming , FOLKES, Adrian , CHUCKOWREE, Irina , HANCOX, Timothy , MILLER, Warren , SOHAL, Sukhjit
发明人： MILTON, John , WREN, Stephen , WANG, Shouming , FOLKES, Adrian , CHUCKOWREE, Irina , HANCOX, Timothy , MILLER, Warren , SOHAL, Sukhjit
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound which is a pyrrolopyrimidine of formula (I) wherein: R 1 is selected from R 9 and halogen; R 2 is NR 6 R 7 ; R 3 is selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted and -(CH2) n Ar; R 4 is selected from H, C 1 -C 6 alkyl and -(CH 2 )„ Ar; or R 3 and R 4 form, together with the N and C atoms to which they are attached, a fused five-, six-, seven- or eight-membered N-containing saturated ring which is unsubstituted or substituted; R 5 is selected from CN, C0 2 R 9 , C(O)NR 10 R 11 , -(CH 2 ) n OH, -(CH 2 ) n R 10 R n , -C = CH, -C(S)NR 10 R 11 , -C(NH 2 )=NOR 9 , -C(R 9 )=NOR 9 , -C(NH 2 )NH, -C(O)R 9 and an unsaturated 5- or 6-membered heterocyclic group which contains 1, 2 or 3 heteroatoms selected from N, O and S and which is unsubstituted or substituted; R 6 and R 7 , which are the same or different, are selected from C 1 -C 6 alkyl which is unsubstituted or substituted, -(CH 2 ) n X and -(CH 2 ) n Ar; or R 6 and R 7 form, together with the nitrogen atom to which they are attached, a saturated five-, six-, seven- or eight-membered heterocyclic group which contains one nitrogen atom and 0 or from 1 to 3 additional heteroatoms selected from N, O and S, which is unsubstituted or substituted and which optionally contains one or two bridgehead atoms; R 10 and R 11 , which are the same or different, are selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted, -(CH 2 ) n C 3 -C 10 cycloalkyl and -(CH 2 ) n Ar; or R 10 and R 11 form, together with the nitrogen atom to which they are attached, a saturated five or six membered heterocyclic group which contains a nitrogen atom and 0 or from to 3 additional heteroatoms selected from O, S and N, which is unsubstituted or substituted and which is optionally fused to a benzene ring which is unsubstituted or substituted; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of from 1 to 6; X is selected from -CN, -C0 2 R 9 and -NR 10 R 11 ; R 9 is the same or different when more than one is present within a given substituent group and is selected from -H, -QAr, -(CH 2 ) n Ar, C 1 -C 6 alkyl which is unsubstituted or substituted and -(CH 2 ) n C 3 -C 10 cycloalkyl, wherein the cycloalkyl moiety is optionally fused to a benzene ring which is unsubstituted or substituted; Q is C 2 -C 6 alkenylene or alkynylene; and Ar is an unsaturated C 6 -C 10 membered carbocyclic group or an unsaturated 5-11 membered heterocyclic group, which groups are unsubstituted or substituted; or a pharmaceutically acceptable salt thereof. These compounds have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
摘要翻译：化合物，其是式（I）的吡咯并嘧啶，其中：R 1选自R 9和卤素; R 2是NR 6 R 7; R 3选自H，未取代或取代的C 1 -C 6烷基和 - （CH 2）n Ar; R 4选自H，C 1 -C 6烷基和 - （CH 2）“Ar;或R 3和R 4形式，与它们所连接的N和C原子一起，未取代或取代的六元，七元或八元的含N饱和环; R 5选自CN，CO 2 R 9，C（O）NR 10 R 11， - （ CH 2）n OH， - （CH 2）n R 10 R n，-C = CH，-C（S）NR 10 R 11，-C（NH 2）= NOR 9，-C（ R 9）= NOR 9，-C（NH 2）NH，-C（O）R 9和不饱和的5-或6-元杂环基，其含有1,2或3个选自N， O和S是未取代或取代的; R 6和R 7相同或不同，选自未取代或取代的C 1 -C 6烷基， - （CH 2）n X和 - （CH 2） nAr;或R 6和R 7与它们所连接的氮原子一起形成饱和的五元，六元，七元或八元杂环基，其含有一个氮原子且为0或从 1至3个选自N，O和S的杂原子，其是未取代的或取代的并且其任选地包含一个或两个桥头原子; R 10和R 11相同或不同，选自H，未取代或取代的C 1 -C 6烷基， - （CH 2）n C 3 -C 10环烷基和 - （CH 2）n Ar; 或R 10和R 11与它们所连接的氮原子一起形成饱和的五或六元杂环基，其含有氮原子和0或至少3个选自O，S的另外的杂原子， N是未取代或取代的，并且任选地与未被取代或取代的苯环稠合; 当给定的取代基中存在多于一个时，n相同或不同，为0或1-6的整数; X选自-CN，-CO 2 R 9和-NR 10 R 11; R 9在给定的取代基中存在多于一个且选自-H，-QAr， - （CH 2）nAr，未取代或取代的C 1 -C 6烷基和 - （CH 2） nC 3 -C 10环烷基，其中环烷基部分任选地与未被取代或取代的苯环稠合; Q是C 2 -C 6亚烯基或亚炔基; 和Ar是不饱和的C 6 -C 10的碳环基团或不饱和的5-11元杂环基团，这些基团是未取代的或取代的; 或其药学上可接受的盐。这些化合物具有作为MRP（多药耐药蛋白）的抑制剂的活性

8. 发明申请

WO2007096362A1 HETEROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CARDIOVASCULAR DISEASE 审中-公开
标题翻译：杂环化合物及其在治疗心血管疾病中的应用
公开(公告)号：WO2007096362A1
公开(公告)日：2007-08-30
申请号：PCT/EP2007/051626
申请日：2007-02-20
申请人： TRIGEN LIMITED , WANG, Shouming , BLENCH, Toby Jonathan , MARLIN, Frederic , BECK, Richard , DICKINSON, Roger Peter
发明人： WANG, Shouming , BLENCH, Toby Jonathan , MARLIN, Frederic , BECK, Richard , DICKINSON, Roger Peter
IPC分类号： A61K31/381 , C07D333/70 , A61P9/10
CPC分类号： A61K31/381 , C07D333/70 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , Y, m, n and q are as defined herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.
摘要翻译：提供式（I）的杂环化合物：其中环A，环B，R 1，R 2，R 3，R 3， SUP，4，Y，m，n和q如本文所定义。 R1特别是脒基。本发明还提供特定的苯并噻吩化合物。本发明的化合物可用作因子IXa的抑制剂和用于心血管疾病和疾病的治疗。血栓形成。

9. 发明申请

WO2004111052A1 PYRROLOPYRIMIDINE DERIVATIVES AS MODULATORS OF MULTI-DRUG RESISTANCE (MDR) 审中-公开
标题翻译：作为多药耐药（MDR）的调节剂的吡咯烷酮衍生物
公开(公告)号：WO2004111052A1
公开(公告)日：2004-12-23
申请号：PCT/GB2004/002523
申请日：2004-06-11
申请人： XENOVA LIMITED , WANG, Shouming , HANCOX, Timothy , MILLER, Warren , HARRISON, John , CHUCKOWREE, Irina , BAKER, Stewart , FOLKES, Adrian , WAN, Nan, Chi
发明人： WANG, Shouming , HANCOX, Timothy , MILLER, Warren , HARRISON, John , CHUCKOWREE, Irina , BAKER, Stewart , FOLKES, Adrian , WAN, Nan, Chi
IPC分类号： C07D487/04
CPC分类号： C07D471/14 , C07D487/04
摘要： A compound which is a pyrrolopyrimidine of formula (I) wherein R 1 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n Ar 1 , (CH 2 ) p NR 4 R 5 , halogen and (CH 2 ) p X; R 2 is CH 2 ) p Ar l ; R 3 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) p Z and (CH 2 ) p Ar l ; P is an unsaturated 5, 6, or 7 membered carbocyclic or heterocyclic ring which is unsubstituted or substituted; R 4 and R 5 which are the same or different are selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n C 3 -C 10 cycloalkyl, (CH 2 ) n Ar 1 , and (CH 2 ) n OR 6 , or R 4 and R 5 together with the nitrogen atom to which they are attached, form a saturated five or six membered nitrogen containing heterocyclic ring which may contain one extra heteroatom selected from 0, N and S and which is unsubstituted or substituted; R 6 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, C 3 -C 10 cycloalkyl, (CH 2 ) n OC 1 -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n O(CH 2 ) n Ar 1 , (CH 2 ) n CO 2 C 1 -C 6 ,alkyl which is unsubstituted or substituted and (CH 2 ) n Ar 1 ; X is selected from CN, azide, (CH 2 ) n NHSO 2 R 6 and (CH 2 ) n NHCOR 6 ; Z is selected from CN, CO 2 R 6 and CONR 4 R 5 ; Ar 1 is the same or different when more than one is present within a given substituent group and is an unsaturated C 6 -C 10 membered carbocylic group or an unsaturated 5-11 membered heterocycle, either of which is unsubstituted or substituted; p is an integer of 1 to 6; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of 1 to 6; with the proviso that the pyrrolepyrimidine compound of formula (I) is other than 1-(4-benzyl-piperazin-1-yl)-9H-2,4,9-triaza-fluorene; and the pharmaceutically acceptable salts thereof, have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
摘要翻译：化合物，其是式（I）的吡咯并嘧啶，其中R 1选自H，未取代或取代的C 1 -C 6烷基，（CH 2）n Ar 1，（CH 2）p NRR 5 R 5，，卤素和（CH 2）pX; R 2是CH 2）pAr 1; R 3选自H，未被取代或取代的C 1 -C 6烷基，（CH 2）pZ和（CH 2）p Ar 1; P是未取代或取代的不饱和5,6或7元碳环或杂环; （CH 2）n C 3 -C 10环烷基，（CH 2）n Ar 1和（CH 2）n C 3 -C 10环烷基，C 1 -C 4烷基， nOR 6或R 4和R 5与它们所连接的氮原子一起形成饱和的五或六元含氮杂环，其可含有一个选自0，N和S的杂原子并且其是未取代或取代的; R 6选自未取代或取代的C 1 -C 6烷基，C 3 -C 10环烷基，未取代或取代的（CH 2）n O（CH 2）n Ar 1（CH 2）n OC 1 -C 6烷基，）nCO2C1-C6，未取代或取代的烷基和（CH2）nAr 1; X选自CN，叠氮化物，（CH 2）n NHSO 2 R 6和（CH 2）n NHCOR 6; Z选自CN，CO 2 R 6和CONR 4 R 5; 当在给定的取代基中存在多于一个时，Ar 1是相同或不同的，并且是不饱和的C 6 -C 10元碳环基或不饱和5-11元杂环，其中任一个是未取代的或取代的; p为1〜6的整数。当给定取代基中存在多于一个时，n相同或不同，为0或1〜6的整数; 条件是式（I）的吡咯嘧啶化合物不是1-（4-苄基 - 哌嗪-1-基）-9H- 2,4,9-三氮杂芴; 和其药学上可接受的盐具有作为MRP（多药耐药性蛋白）的抑制剂的活性，因此可用于调节多药耐药性，例如增强化学治疗剂的细胞毒性。

10. 发明申请

WO1998025932A1 ANTIBACTERIAL AGENTS 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1998025932A1
公开(公告)日：1998-06-18
申请号：PCT/US1997022356
申请日：1997-12-05
申请人： WARNER-LAMBERT COMPANY , DOMAGALA, John, Michael , ELLSWORTH, Edmund, Lee , STIER, Michael, Andrew , HUANG, Liren , MICETICH, Ronald, George , SINGH, Rajeshwar , WRIGLEY, Stephen, Keith , WANG, Shouming , ROE, Michael , THORNTON, David, Michael
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D498/04
CPC分类号： C07D487/04 , C07D513/04
摘要： Described are antibacterial agents of formula (I): X is O, S or N-R8; R1, R2, R3 and R8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, CO2R, COR, CON(R)2, CON(R")2, SR, SON, SCO2R or SCON(R)2; R4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, CN, NO2, N(R)2, NRCOR, NRCOR", COR, CO2R, CON(R)2, CON(R")2, NRCON(R)2, NRCO2R; R5 is 1-6 straight or branched alkyl, a cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR2, NR'COR', CN, CO2R' or CONR2', halogen, OR, N(R)2, NRCOR, NRCOR", COR, CON(R)2, CON(R")2, SR or SO2R; R6, R7 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, COR, COR", SO2NR2, CONR2 and these may be optionally substituted by any of the groups listed for R5; R is H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or pheny, all of which may be optionally substituted by halogen, OR', NR'2, NR'COR', CN, CO2R', CONR'2; R' is H, alkyl of from 1-3 carbon atoms or Ph; R" is part of a naturally occurring amino acid connected via an amide or acyl bond as determined by the formula; halogen is any one of fluoro, chloro, bromo or iodo; or a pharmaceutically acceptable salt.
摘要翻译：描述了式（I）的抗菌剂：X是O，S或N-R8; R1，R2，R3和R8独立地为H，1-6个碳的直链或支链烷基，3-6个碳原子的环烷基，2-6个碳原子的烯基或炔基，5-8个原子的杂环，1-3个杂原子作为氮，氧或硫或苯基，所有这些环可以任选被卤素，OR，NR 2，NR'COR'，CN，CO 2 R'或CONR 2'，卤素，CN，CO 2 R，COR ，CON（R）2，CON（R“）2，SR，SON，SCO 2 R或SCON R 2; R 4是H，1-6个碳原子的直链或支链烷基，2至6的烯基或炔基原子，5-8个原子与1-3个杂原子作为氮原子的杂环，氧或硫或苯基，所有这些环可以任选地被卤素OR，NR 2，NR'COR'，CN， CO 2 R，CONR 2，CON（R“）2，NRCON（R）2，NRCO 2 R; R 5是 1-6个直链或支链烷基，3-6个碳原子的环烷基，2-6个碳原子的烯基或炔基，5-8个原子的杂环和1-3个杂原子作为氮，氧或硫或苯基，所有这些环可以任选被卤素，OR，NR 2，NR'COR'，CN，CO 2 R'或CONR 2'，卤素，OR，N（R） 2，NRCOR，NRCOR“，COR，CON（R）2，CON（R”）2，SR或SO2R; R 6，R 7独立地是H，1-6个碳的直链或支链烷基，3-6个碳的环烷基，COR，COR“，SO2NR2，CONR2，并且它们可以任选被R5所列的任何基团取代; R是H ，1-6个碳原子的直链或支链烷基，3-6个碳原子的环烷基，5-8个原子的杂环，1-3个杂原子作为氮，氧或硫或苯基，所有这些可以是任选的被卤素取代，OR'，NR'2，NR'COR'，CN，CO2R'，CONR'2; R'是H，1-3个碳原子的烷基或Ph; R“是天然存在的氨基通过由式决定的酰胺或酰基键连接酸; 卤素是氟，氯，溴或碘中的任何一种; 或药学上可接受的盐。

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