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    • 7. 发明申请
    • BENZOTHIAZINO INDOLES
    • WO2005005439A1
    • 2005-01-20
    • PCT/IN2004/000200
    • 2004-07-07
    • SUVEN LIFE SCIENCES LIMITEDRAMAKRISHNA, Venkata, Satya, NirogiKAMBHAMPATI, Rama, SatriSHIRSATH, Vikas, ShreekrishnaJASTI, Venkateswarlu
    • RAMAKRISHNA, Venkata, Satya, NirogiKAMBHAMPATI, Rama, SatriSHIRSATH, Vikas, ShreekrishnaJASTI, Venkateswarlu
    • C07D513/06
    • C07D513/06
    • This invention particularly relates to novel benzothiazinoindole derivatives represented by the general formula (I), given below: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 ,, R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 and R 14 , may be same or different and each independently represent hydrogen, halogen, oxo, thio, perhaloalkyl, hydroxy, amino, nitro, cyano, formyl, amidino, guanidino, substituted or unsubstituted groups selected from linear or branched (C l -C, 12 )alkyl, (C 2 -C 12 )alkenyl, C 2 -C 12 )alkynyl, (C 3 -C 7 )cycloalkyl, (C 3 -C 7 )cycloalkenyl, bicycloalkyl, bicycloalkenyl, C 1 -C 12 )alkoxy, cyclo(C 3 -C 7 )alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heterocyclylalkyl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, heterocyclylalkyloxy, acyl, acyloxy, acylamino, monoalkylamino, dialkylamino, arylamino, diarylamino, aralkylamino, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, heterocyclylalkoxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonyamino, aryloxycarbonylamino, dialkylaminocarbonylamino, alkylamidino, alkylguanidino, dialkylguanidino, hydrazino, hydroxylamino, carboxylic acid and its derivatives, sulfonic acids and its derivatives, phosphoric acid and its derivatives; or two adjacent groups may form "cyclic structures", for example, R 1 and R 2 , R 2 and R 3 , R 5 and R 6 , R 6 , and R 7 , R 7 and R 8 together with the adjacent carbon atoms to which they are attached may form a 5, 6, or 7 membered ring, which may further optionally contain one or more double bonds and/or one or more heteroatoms such as the group "Oxygen", "Nitrogen' "Sulfur" or "Selenium" and combinations of double bond and heteroatoms; or R 9 and R 10 or R 11 and R 12 or R 13 and R 14 together represent double bond attached to "Oxygen" or "Sulfur"; or two adjacent groups may form "cyclic structures" for example, R 11 and R 12 , Ril and R 13 , R 11 and R 14 , R 13 and R 14 together with the carbon atom/s to which they are attached may form a 3, 4, 5, or 6 membered ring, which may further optionally 10 contain one or more double bonds, and/or one or more heteroatoms such as the group "Oxygen", "Nitrogen", "Sulfur" or "Selenium" and also includes combination of one or more double bonds with "heteroatoms", as above defined, R 15 and R 16 may be same or different and each independently represents hydrogen, substituted or unsubstituted groups selected from linear or branched (C 1 -C 12 )alkyl, (C 2 -C 12 )alkenyl, (C 2 -C 12 )alkynyl, (C 3 -C 7 )cycloalkyl, (C 3 -C 7 )cycloalkenyl, bicycloalkyl, bicycloalkenyl, aryl, aralkyl, heteroaryl, heterocyclylalkyl; optionally R 15 and R 16 along with the nitrogen atom may form a 3, 4, 5, 6 or 7 membered heterocyclic ring, which may further optionally contain one or more double bonds, and may include additional one or more heteroatoms such as the group "Oxygen", "Nitrogen", "Sulfur' or "Selenium" and also includes combination of one or more double bonds with "heteroatoms", as above defined; "n" ranges from 0 to 4, wherein the carbon chains which "n" represents may be either linear or branched.
    • 本发明特别涉及由下列通式(I)表示的新的苯并噻唑啉衍生物:其中R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11,R12,R13和R14, 可以相同或不同,并且各自独立地表示氢,卤素,氧代,硫代,全卤代烷基,羟基,氨基,硝基,氰基,甲酰基,脒基,胍基,取代或未取代的选自直链或支链(C 1 -C 12) ,(C 2 -C 12)炔基,(C 3 -C 7)环烷基,(C 3 -C 7)环烯基,双环烷基,双环烯基,C 1 -C 12)烷氧基,环(C 3 -C 7)烷氧基,芳基,芳氧基, 芳烷氧基,杂环基,杂芳基,杂环烷基,杂芳烷基,杂芳基氧基,杂芳烷氧基,杂环基烷氧基,酰基,酰氧基,酰氨基,单烷基氨基,二烷基氨基,芳基氨基,二芳基氨基,芳烷基氨基,烷氧基羰基,芳氧基羰基,芳烷氧基羰基,杂环基烷氧基羰基,杂芳氧基羰基,羟基烷基,氨基烷基,单烷基氨基烷基, 二烷基氨基烷基,烷氧基 烷氧基烷基,烷氧基羰基氨基,二烷基氨基羰基氨基,烷基脒基,烷基胍基,二烷基胍基,肼基,羟基氨基,羧酸及其衍生物,磺酸及其衍生物,磷酸及其衍生物; 或两个相邻的基团可以形成“环状结构”,例如,R 1和R 2,R 2和R 3,R 5和R 6,R 6和R 7,R 7和R 8与它们所连接的相邻碳原子一起形成5, 6或7元环,其可以进一步任选地含有一个或多个双键和/或一个或多个杂原子,例如“氧”,“氮”“硫”或“硒”以及双键和杂原子的组合; 或R 9和R 10或R 11和R 12或R 13和R 14一起表示与“氧”或“硫”连接的双键;或两个相邻基团可以形成例如R11和R12,R10和R13,R11和R14的“环状结构” R 13和R 14与它们所连接的碳原子一起可以形成3,4,5或6元环,其还可任选地10含有一个或多个双键,和/或一个或多个杂原子如 作为组“氧”,“氮”,“硫”或“硒”,并且还包括一个或多个双键与“杂原子”的组合,如上 (C 1 -C 12)烯基,(C 2 -C 12)炔基,(C 3 -C 12)炔基,(C 2 -C 12)炔基,(C 2 -C 12)炔基,(C 2 -C 12)炔基, )环烷基,(C 3 -C 7)环烯基,双环烷基,双环烯基,芳基,芳烷基,杂芳基,杂环基烷基; 任选地R15和R16a