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51. 发明申请

WO2009083134A1 VERFAHREN ZUM HERSTELLEN VON 2-FLUORACYL-3-AMINO-ACRYLSÄURE-DERIVATEN 审中-公开
标题翻译：方法制备2-酰基氟3-氨基丙烯酸衍生物
公开(公告)号：WO2009083134A1
公开(公告)日：2009-07-09
申请号：PCT/EP2008/010689
申请日：2008-12-16
申请人： BAYER CROPSCIENCE AG , LUI, Norbert , WOLLNER, Thomas , WIESCHEMEYER, Jürgen , DOCKNER, Michael , HEINRICH, Jens-Dietmar
发明人： LUI, Norbert , WOLLNER, Thomas , WIESCHEMEYER, Jürgen , DOCKNER, Michael , HEINRICH, Jens-Dietmar
IPC分类号： C07C227/16 , C07C229/30
CPC分类号： C07C227/16 , C07C253/30 , C07C229/30 , C07C255/30
摘要： Die vorliegende Erfindung betrifft ein Verfahren zum Herstellen von 2-Fluoracyl-3-amino- acrylsäure-Derivaten durch Umsetzung von fluorierten Carbonsäuren mit Dialkylaminoacrylsäure- Derivaten und Säurehalogeniden.
摘要翻译：本发明涉及用于通过具有Dialkylaminoacrylsäure-衍生物和酰基卤氟化的羧酸反应来制备2-氟酰基-3-氨基丙烯酸衍生物的方法。

52. 发明申请

WO2008019690A1 SUBSTITUTED ACETYLENIC COMPOUNDS USEFUL FOR THE TREATMENT OF DISEASES 审中-公开
标题翻译：替代乙酰化合物可用于治疗疾病
公开(公告)号：WO2008019690A1
公开(公告)日：2008-02-21
申请号：PCT/DK2007/000375
申请日：2007-08-16
申请人： LEO PHARMA A/S , LIANG, Xifu , HØYER, Thomas , FENSHOLDT, Jef , HAVEZ, Sophie Elisabeth , NØRREMARK, Bjarne
发明人： LIANG, Xifu , HØYER, Thomas , FENSHOLDT, Jef , HAVEZ, Sophie Elisabeth , NØRREMARK, Bjarne
IPC分类号： A61K31/137 , A61K31/381 , A61K31/4045 , A61K31/357 , C07C211/30 , C07C215/24 , C07C215/28 , C07C229/30 , C07C255/58 , C07D209/20 , C07D231/38 , C07D317/58 , C07D333/58 , C07F7/08 , C07F7/18
CPC分类号： C07F7/0818 , C07B2200/07 , C07C211/29 , C07C211/30 , C07C211/49 , C07C215/24 , C07C215/28 , C07C215/30 , C07C215/50 , C07C215/54 , C07C217/46 , C07C217/58 , C07C217/62 , C07C229/30 , C07C229/34 , C07C229/38 , C07C233/36 , C07C233/38 , C07C233/62 , C07C235/10 , C07C235/60 , C07C237/16 , C07C255/30 , C07C255/58 , C07C271/20 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C311/05 , C07C311/18 , C07C311/29 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/12 , C07D209/08 , C07D211/46 , C07D211/58 , C07D211/62 , C07D213/40 , C07D231/12 , C07D263/32 , C07D295/13 , C07D295/182 , C07D309/08 , C07D309/10 , C07D317/28 , C07D317/58 , C07D333/20 , C07D333/58 , C07F7/1852 , C07F7/1856
摘要： The invention relates to novel compounds according to formula Ia and Ib; (Formula Ia and Ib) wherein A represents substituted or unsubstituted C 1-10 heteroaryl, C 6-14 aryl or C 6- 10 heterocycloalkylaryl; R 1 is C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 amino, C 3-6 cycloalkyl, or C 1-6 heterocycloalkyl, each of which are optionally substituted; X represents -CR 3 R 4 -(CR 5 R 6 ) n -(CR 7 =CR 8 ) m -(C 6-14 aryl) r -(C 1-10 heteroaryl) s -(CR 9 R 10 ) p - (CR 11 = CR 12 ) q , R 2 represents C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 amino, C 1-12 alkylsilyl, C 6-30 alkylarylsilyl, C 1-10 heteroaryl, C 6-14 aryl, C 1-10 heterocycloalkyl, C 1-10 heterocycloalkenyl, C 1-8 cycloalkyl, C 1-18 cycloalkenyl, each of which is optionally substituted, or R 2 represents hydrogen, carboxy, or hydroxy; or a pharmaceutically acceptable salt, solvate, or ester thereof; to processes for the preparation thereof, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, wherein said compounds being useful, e.g. in the treatment of diseases associated with disturbances of CaSR activity, such as hyperparathyroidism.
摘要翻译：本发明涉及根据式Ia和Ib的新化合物; （式Ia和Ib）其中A表示取代或未取代的C 1-10 - 杂芳基，C 6-14芳基或C 6-10 - 杂环烷基芳基 ; R 1是C 1-6烷基，C 2-6链烯基，C 2-6炔基，C 1-6个羟基烷基，C 1-6卤代烷基，C 1-6 1-6氨基，C 3-6环烷基或C 1-6 - 杂环烷基，其各自为任选取代的; X表示-CR 3 R 4 - （CR 5 R 6）n 7 = CR _{8 ）_{米 - （C _{6-14 芳基）_{- [R < / SUB> - （C _{1-10 杂芳基）_{取值 - （CR _{9 - [R _{10 ）_{（CR 11）其中R 2表示C 1 -C 12烷基， 1-6个C 1-6烷基，C 2-6链烯基，C 2-6亚烷基，C 1-6烷基，C 1-6烷基， C 1-6卤代烷基，C 1-6氨基，C 1-12烷基甲硅烷基，C 6-30-30烷基芳基甲硅烷基， C 1-10杂芳基，C 6-14芳基，C 1-10 1-10杂环烷基，C 1-10烷基，杂环烯基，C 1-8环烷基，C 1-18环烯基，其各自任选被取代，或R 2代表氢，羧基，或羟基; 或其药学上可接受的盐，溶剂化物或酯; 涉及用于制备其的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，其中所述化合物是有用的。治疗与CaSR活动相关的疾病，如甲状旁腺功能亢进。}}}}}}}}}

53. 发明申请

WO2006127205A2 METHODS OF PREPARING 3-CYANO-QUINOLINES AND INTERMEDIATES MADE THEREBY 审中-公开
标题翻译：制备3-氰基喹啉及其中间体的方法
公开(公告)号：WO2006127205A2
公开(公告)日：2006-11-30
申请号：PCT/US2006/016019
申请日：2006-04-27
申请人： WYETH , CHEW, Warren , PAPAMICHELAKIS, Maria
发明人： CHEW, Warren , PAPAMICHELAKIS, Maria
IPC分类号： C07C251/50 , C07D209/48 , C07D213/30 , C07D215/54 , C07D401/12
CPC分类号： C07D209/48 , C07C217/84 , C07C255/23 , C07C255/30 , C07C257/06 , C07D213/30 , C07D215/38 , C07D215/54 , C07D401/12 , C07D401/14 , C07D403/02 , C07D413/02
摘要： The present invention relates to methods for preparing substituted 3-cyanoquinolines and intermediates obtained by the methods of the present invention. The methods of the invention comprise reacting an N-aryl-2-propanimide with phosphoryl chloride to produce the substituted 3-cyanoquinolines. The methods further comprise reacting arylamines, orthoformates and active methylenes to produce the N-aryl-2-propenamide.
摘要翻译：本发明涉及制备取代的3-氰基喹啉的方法和通过本发明的方法获得的中间体。本发明的方法包括使N-芳基-2-丙酰亚胺与磷酰氯反应以产生取代的3-氰基喹啉。所述方法还包括使芳基胺，原甲酸酯和活性亚甲基反应以产生N-芳基-2-丙烯酰胺。

54. 发明申请

WO2004048315A1 FUNGICIDES 审中-公开
标题翻译：杀菌剂
公开(公告)号：WO2004048315A1
公开(公告)日：2004-06-10
申请号：PCT/GB2003/004832
申请日：2003-11-10
申请人： SYNGENTA LIMITED , SALMON, Roger , CROWLEY, Patrick, Jelf , BACON, David, Philip
发明人： SALMON, Roger , CROWLEY, Patrick, Jelf , BACON, David, Philip
IPC分类号： C07C235/20
CPC分类号： C07D249/08 , A01N39/04 , C07C235/20 , C07C255/30 , C07C317/28 , C07C323/41
摘要： Fungicidal compounds of the general formula (1): wherein X, Y and Z are independently H, halogen, C l-4 alkyl, halo(C 1-4 )alkyl, C 2-4 alkenyl, halo(C 2 - 4 )alkenyl, C24 alkynyl, halo(C 2-4 )alkynyl, C 1 _ 4 alkoxy, halo(C 1-4 )alkoxy, -S(O) n (C 1-4 )alkyl where n is 0, 1 or 2 and the alkyl group is optionally substituted with fluoro, -OS0 2 (C 1-4 )alkyl where the alkyl group is optionally substituted with fluoro, cyano, nitro, C, 1-4 alkoxycarbonyl, -CONR'R", -COR', -NR'COR" or -NR'COOR"' where R' and R" are independently H or C 1-4 alkyl and R"' is C l-4 alkyl, provided that at least one of X and Z is other than H; R 1 is C l - 4 alkyl, C 2-4 alkenyl or C 2-4 alkynyl in which the alkyl, alkenyl and alkynyl groups are optionally substituted on their terminal carbon atom with one, two or three halogen atoms, with a cyano group, with a C 1-4 alkylcarbonyl group, with a C 1-4 alkoxycarbonyl group or with a hydroxy group; R 2 is H, C 1-4 alkyl, C 1-4 alkoxymethyl or benzyloxymethyl in which the phenyl ring of the benzyl moiety is optionally substituted with CI-4 alkoxy; R 3 and R 4 are independently H, C 1-3 alkyl, C 2-3 alkenyl or C 2-3 alkynyl provided that both are not H and that when both are other than H their combined total of carbon atoms does not exceed 4, or R 3 and R 4 join with the carbon atom to which they are attached to form a 3 or 4 membered carbocyclic ring optionally containing one 0, S or N atom and optionally substituted with halo or C 1-4 alkyl; and R 5 is unsubstituted C 3-4 alkyl, unsubstituted C 3-6 cycloalkyl or C l-4 alkyl or C 3-6 cycloalkyl in which the alkyl and cycloalkyl groups are substituted with halo, hydroxy, C 1-6 alkoxy, cyano, C 1-4 alkylcarbonyloxy, aminocarbonyloxy, mono- or di(C 1 _ 4 )alkylaminocarbonyloxy, -S(O)"(C 1-6 )alkyl where n is 0, 1 or 2, triazolyl, tri(C 1-4 )alkylsilyloxy, optionally substituted phenoxy, optionally substituted thienyloxy, optionally substituted benzyloxy or optionally substituted thienyl-methoxy, in which the optionally substituted phenyl and thienyl rings of phenoxy, thienyloxy, benzyloxy and thienylmethoxy are optionally substituted with one, two or three substituents selected from halo, hydroxy, mercapto, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C1-4 alkoxy, C 2-4 alkenyloxy, C 2-4 alkynyloxy, halo(C 1-4 )alkyl, halo(C 1-4 )alkoxy, C 1-4 alkylthio; halo(C 1-4 )alkylthio, hydroxy(C 1-4 )alkyl, C 1-4 alkoxy(C 1-4 )alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl(C 1-4 )alkyl, phenoxy, benzyloxy, benzoyloxy, cyano, isocyano, thiocyanato, isothiocyanato, nitro, -NR - R', -NHCOR m , -NHCONR m R", -CONRmR", -S02R m , -OS02R m , -COR M , -CR'=NR" or -N=CR m R", in which R"' and R" are independently hydrogen, CI-4 alkyl, halo(C 1-4 )alkyl, C1-4 alkoxy, halo(C 1-4 )alkoxy, C 1-4 alkylthio, C 3-6 cycloalkyl, C 3-6 cycloalkyl(C 1-4 )alkyl, phenyl or benzyl, the phenyl and benzyl groups being optionally substituted with halogen, C 1-4 alkyl or C 1-4 alkoxy.
摘要翻译：通式（1）的杀真菌化合物：其中X，Y和Z独立地为H，卤素，C 1-4烷基，卤代（C 1-4）烷基，C 2-4烯基，卤代（C 2-4）烯基，C 24炔基，卤素（C 2-4）炔基，C 1-4烷氧基，卤代（C 1-4）烷氧基，-S（O）n（C 1-4）烷基，其中n为0,1或2，烷基任选被氟取代， -OCO 2（C 1-4）烷基，其中烷基任选被氟，氰基，硝基，C 1-4烷氧基羰基，-CONR'R“，-COR'，-NR'COR”或-NR'COOR“ 其中R'和R“独立地是H或C 1-4烷基，R”'是C 1-4烷基，条件是X和Z中的至少一个不是H; R 1是C 1-4烷基，C 2-4烯基或C2-4炔基，其中烷基，烯基和炔基在其末端碳原子上任选被一个，两个或三个卤素原子与氰基，C 1-4烷基羰基和C 1-4烷氧基羰基基团或羟基; R 2是H，C 1-4烷基，C 1-4烷氧基甲基或苄氧基甲基，其中苄基部分任选被C 1-4烷氧基取代; R3和R4分别是H，C1-3烷基，C2-3烯基或C2-3炔基，条件是两者都不是H，当两者都不是H时，它们的总碳原子数不超过4，或者R3和R4 与它们所连接的碳原子一起形成任选含有一个O，S或N原子并任选被卤素或C 1-4烷基取代的3或4元碳环; R5是未取代的C3-4烷基，未取代的C3-6环烷基或C1-C4烷基或C3-6环烷基，其中烷基和环烷基被卤素，羟基，C1-6烷氧基，氰基，C1-4烷基羰基氧基，氨基羰基氧基，单或二（C 1-4）烷基氨基羰基氧基，-S（O）“（C 1-6）烷基，其中n为0,1或2，三唑基，三（C 1-4）烷基甲硅烷氧基，任选取代的苯氧基，任选取代的噻吩氧基，任选取代的苄氧基或任选取代的噻吩基 - 甲氧基，其中苯氧基，噻吩氧基，苄氧基和噻吩基甲氧基的任选取代的苯基和噻吩环任选被一个，两个或三个选自卤素，羟基，巯基，C 1-4烷基， C 2-4烷氧基，C 2-4烷氧基，C 2-4烷氧基，卤代（C 1-4）烷基，卤代（C 1-4）烷氧基，C 1-4烷硫基;卤代（C1- 4）烷硫基，羟基（C 1-4）烷基，C 1-4烷氧基（C 1-4）烷基，C 3-6环烷基，C 3-6环烷基（C 1-4）烷基，苯氧基，苄氧基，苯甲酰氧基，氰基，异氰酸，硫氰酸酯，异硫氰酸酯，硝基，-NR'R'，-NHCOR m，-NHCONR m R“，-CONRmR”，-SO 2 R m，-OSO 2 R m，-COR M >，-CR'= NR“或

55. 发明申请

WO2003051824A1 α-CYANOACRYLATES 审中-公开
标题翻译：阿尔法 - 氰基丙烯酸酯
公开(公告)号：WO2003051824A1
公开(公告)日：2003-06-26
申请号：PCT/EP2002/014353
申请日：2002-12-17
申请人： BASF AKTIENGESELLSCHAFT , PLATH, Peter , GÖTZ, Norbert , RACK, Michael , LANDES, Andreas , ZAGAR, Cyrill , WITSCHEL, Matthias , GROSSMAN, Klaus
发明人： PLATH, Peter , GÖTZ, Norbert , RACK, Michael , LANDES, Andreas , ZAGAR, Cyrill , WITSCHEL, Matthias , GROSSMAN, Klaus
IPC分类号： C07C255/30
CPC分类号： C07D295/185 , A01N37/44 , A01N43/08 , A01N43/16 , C07C255/30 , C07C323/60 , C07C327/22 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D305/08 , C07D307/18 , C07D307/20 , C07D307/22 , C07D309/14 , C07D319/06 , C07D331/04
摘要： α-Cyanoacrylates of the formula (I), where: R 1 is OR a wherein R a is hydrogen, substituted alkyl, branched alkyl, branched alkenyl, cycloloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; is NR b R c wherein R b is hydrogen, alkyl which may be substituted, alkenyl, alkynyl; R c is hydrogen, alkyl which may be substituted alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; or R b and R c form an alkandiyl-chain which may be substituted; or is SR d wherein R d is hydrogen, alkyl which may be substituted, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; R 2 is alkyl which may be substituted; is alkenyl or alkynyl; R 3 is alkyl may be substituted; is alkenyl or alkynyl; R 4 is hydrogen, halogen, cyano or alkyl; and their agriculturally useful salts, processes and intermediates for their preparation; and the use of these compounds or of compositions comprising these compounds for controlling undesirable plants are described.
摘要翻译：式（I）的烷基丙烯酸酯，其中：R 1是其中R a a是氢的取代的烷基，支链烷基，支链烯基，环烷基，杂环基，芳基，苯基烷基或烷基亚氨基; 其中R b是氢，可以被取代的烷基，烯基，炔基; 烯基，炔基，环烷基，杂环基，芳基，苯基烷基或烷基亚氨基; 或者R c和R c形成可以被取代的烷撑二链; 或者是其中R d为氢的烷基，可被取代的烷基，烯基，炔基，环烷基，杂环基，芳基，苯基烷基或烷基亚氨基; R 2是可被取代的烷基; 是烯基或炔基; R 3是烷基可以被取代; 是烯基或炔基; R 4是氢，卤素，氰基或烷基; 及其农业上有用的盐，其制备方法和中间体; 并且描述了这些化合物或包含这些化合物的组合物用于防治不期望的植物的用途。

56. 发明申请

WO02048111A2 METHOD FOR PRODUCING 4-HALOALKYL NICOTINE NITRILES 审中-公开
标题翻译：用于生产4-HALOALKYLNICOTINNITRILEN
公开(公告)号：WO02048111A2
公开(公告)日：2002-06-20
申请号：PCT/EP2001/014584
申请日：2001-12-12
IPC分类号： C07B61/00 , C07C255/24 , C07C255/27 , C07C255/30 , C07D211/78 , C07D211/90 , C07D213/82 , C07D213/85 , A01N43/42
CPC分类号： C07C255/24 , C07C255/27 , C07C255/30 , C07D211/78 , C07D211/90 , C07D213/85
摘要： 4-haloalkyl nicotine nitriles (I) are suitable for use as intermediate products in the production of pesticides and can be obtained by means of a method which provides that a) 3-amino-1-haloalkyl-2-propen-1-one R -C(O)-CH=CH-NH2 (II) is reacted with a compound of formula (III) to (VII), (R Z)CH=CH-CN (III) (R Z)2CH-CH2-CN (IV) Hal-CH=CH-CN (V) Hal2CH-CH2CN (VI) HC=C-CN (VII) in a condensation reaction, R meaning (C1-C4)-haloalkyl R alkyl, Hal Cl or Br and Z meaning O, S, NR or OCO, and in the case of formula (IV), the two radicals Z being able to have the aforementioned meanings, independently of each other; to produce a compound of formula (VIII), (IX) and/or (X), R -C(O)-CH=CH-NH-CH=CH-CN (VIII) R -C(O)-CH=CH-NH-CH(ZR)-CH2-CN (IX) R -C(O)-CH=CH-NH-CH(Hal)-CH2-CN (X), R, Z and Hal having the meanings given above, and subjecting the product of the reaction b) to a ring closure reaction.
摘要翻译： 4- Haloalkylnicotinnitrile（I）是如农药的制备中用作中间体，并且其可通过一种方法，其包括：a）将3-氨基-1-卤代烷基-2-丙烯-1-一个R -C（O） -CH = CH-NH 2（II）在与式（III）至（VII）的化合物，（R <1> Z）CH = CH-CN（III）（R <1> Z）2 CH-CH 2的缩合反应 -CN（IV）哈尔-CH = CH-CN（V）Hal2CH-CH 2 CN（VI）HC = C-CN（VII），其中R （C1-C4） - 卤烷基，R <1>是烷基，哈尔CI 或Br，Z为O，S，NR <1>或OCO装置，其中，在式（IV）的两个基团Z可以假定上述含义彼此独立的情况下，向式（VIII），（IX）的化合物和 /或（X）反应，R C（O）-CH = CH-NH-CH = CH-CN（VIII）中，R C（O）-CH = CH-NH-CH（ZR ）-CH2-CN（IX）R C（O）-CH = CH-NH-CH（哈尔）-CH 2 CN（X），其中R，Z和Hal具有上面给出的含义，并且将反应产物 b）中闭环反应的受试者。式（I）

57. 发明申请

WO02038536A1 PROCESSES FOR THE PREPARATION OF UNSATURATED 3-AMINONITRILES 审中-公开
标题翻译：制备不饱和3-氨基甲酸酯的方法
公开(公告)号：WO02038536A1
公开(公告)日：2002-05-16
申请号：PCT/GB2001/004918
申请日：2001-11-05
IPC分类号： C07C253/30 , C07C255/30
CPC分类号： C07C253/30 , C07C255/30
摘要： A process for the preparation of a compound of formula (I): wherein R is hydrogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C1-6 alkoxy, optionally substituted C1-6 alkylthio or optionally substituted C3-7 cycloalkyl; and R is hydrogen, halogen, optionally substituted C1-6 alkyl, optionally substituted C2-6 alkenyl, optionally substituted C2-6 alkynyl, optionally substituted C1-6 alkoxy, optionally substituted C1-6 alkylthio, optionally substituted C1-6 alkylsulfinyl, optionally substituted C1-6 alkylsulfonyl, cyano, nitro formyl, optionally substituted C1-6 alkylcarbonyl, optionally substituted C1-6 alkoxycarbonyl or SF5; or R and R together with the atoms to which they are attached may be joined to form a five, six or seven-membered saturated or unsaturated ring carbocylic or heterocyclic ring which may contain one or two heteroatoms selected from O, N or S and which may be optionally substituted by C1-6 alkyl, C1-6 haloalkyl or halogen; the process comprising reacting aqueous ammonia with a compound of formula (II): or a metal salt derived therefrom where R1 and R2 are as defined in relation to formula (I).
摘要翻译：制备式（I）化合物的方法：其中R 1是氢，任选取代的C 1-6烷基，任选取代的C 2-6烯基，任选取代的C 2-6炔基，任选取代的C 1-6烷氧基，任选取代的C 1-6烷硫基或任选取代的C 3-7环烷基; 并且R 2是氢，卤素，任选取代的C 1-6烷基，任选取代的C 2-6烯基，任选取代的C 2-6炔基，任选取代的C 1-6烷氧基，任选取代的C 1-6烷硫基，任选取代的C 1-6 烷基亚磺酰基，任选取代的C 1-6烷基磺酰基，氰基，硝基甲酰基，任选取代的C 1-6烷基羰基，任选取代的C 1-6烷氧基羰基或SF 5; 或R 1和R 2与它们连接的原子一起可以连接形成五，六或七元饱和或不饱和环的碳环或杂环，其可以含有一个或两个选自O ，N或S，并且其可任选被C 1-6烷基，C 1-6卤代烷基或卤素取代; 该方法包括使氨水与式（II）化合物反应：或其衍生的金属盐，其中R 1和R 2如关于式（I）所定义。

58. 发明申请

WO02022559A2 2-AMINO-2-ALKYL-4 HEXENOIC AND HEXYNOIC ACID DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：作为氮氧化物合成酶抑制剂有用的2-氨基-2-烷基-4-异丙酸和二异氰酸酯衍生物
公开(公告)号：WO02022559A2
公开(公告)日：2002-03-21
申请号：PCT/US2001/028733
申请日：2001-09-15
IPC分类号： C07D271/06 , A61K31/198 , A61K31/4245 , A61P19/02 , A61P29/00 , C07C229/30 , C07C251/08 , C07C251/16 , C07C251/24 , C07C255/30 , C07C257/14 , C07C259/14 , C07C271/22 , C07D209/48 , C07D271/07 , C07D413/06 , C07C251/00
CPC分类号： C07D209/48 , A61K31/198 , C07C229/30 , C07C251/08 , C07C251/16 , C07C255/30 , C07C257/14 , C07C271/22 , C07D271/07 , C07D413/06
摘要： The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
摘要翻译：本发明涉及2-氨基-2-烷基-4-己烯酸和己酸衍生物及其在治疗中的用途，特别是其用作一氧化氮合酶抑制剂。

59. 发明申请

WO9615102A3 2-cyanoacrylic acid esters 审中-公开
标题翻译： 2-氰基丙烯酸酯
公开(公告)号：WO9615102A3
公开(公告)日：1996-07-25
申请号：PCT/EP9504312
申请日：1995-11-03
申请人： BASF AG , HOLDERBAUM MARTIN , AUNMUELLER ALEXANDER , TRAUTH HUBERT , VOIT GUIDO , SPERLING KARIN , KRAUSE ALFRED
发明人： HOLDERBAUM MARTIN , AUMUELLER ALEXANDER , TRAUTH HUBERT , VOIT GUIDO , SPERLING KARIN , KRAUSE ALFRED
IPC分类号： C07D211/14 , C07B63/04 , C07C253/30 , C07C255/19 , C07C255/23 , C07C255/30 , C07C255/41 , C07C255/42 , C07D211/46 , C08K5/315 , C08K5/3435 , C09D7/12 , C09K3/00 , C09K15/16 , C09K15/20
CPC分类号： C07C255/41 , C07B63/04 , C07C255/19 , C07C255/30 , C07C255/42 , C07D211/46 , C08K5/315 , C08K5/3435 , C09D7/48
摘要： 2-Cyanoacrylic esters (I) of alpha , omega -bis(4-hydroxy-2,2,6,6-tetramethylpiperid-1-yl)alkanes or (cyclo)aliphatic polyols of the given formula (I) are new. R , R = the radical of an iso- or heterocyclic ring system with at least one iso- or heteroaromatic ring and ≥ 1 of R and R is not H, n = 2-10, if n = 2, X = a gp. of formula (II), m = 2-8; if n = 3-10, X = the radical of an n-hydric 3-20C (cyclo)aliphatic polyol, opt. with 1 or 2 heteroatoms in the cycloaliphatic gp. and up to 8 non-adjacent O or S atoms or -NH- or 1-4C alkylimino gps. in the aliphatic chain. Also claimed are various materials stabilised against the action of light, O2 and heat with (I).

60. 发明申请

WO1995023787A1 PROCESS FOR PRODUCING 5,7-DICHLORO-4-HYDROXYQUINOLINE 审中-公开
标题翻译：生产5,7-二氯-4-羟基喹啉的方法
公开(公告)号：WO1995023787A1
公开(公告)日：1995-09-08
申请号：PCT/JP1995000293
申请日：1995-02-27
申请人： ISHIHARA SANGYO KAISHA, LTD. , YOSHIZAWA, Hiroshi , HAMAGUCHI, Motohiko , FUJINO, Tomizo
发明人： ISHIHARA SANGYO KAISHA, LTD.
IPC分类号： C07D215/22
CPC分类号： C07D215/233 , C07C219/20 , C07C255/30 , C07D215/56
摘要： An industrially advantageous process for producing 5,7-dichloro-4-hydroxyquinoline (DCHQ) useful as an intermediate for agrohorticultural bactericides. The process comprises hydrolyzing 3-cyano- or 3-ethoxycarbonyl-5,7-dichloro-4-hydroxyquinoline into 5,7-dichloro-3-carboxy-4-hydroxyquinoline (DCQA) in the presence of hydrochloric, sulfuric or phosphoric acid and decarboxylating the formed DCQA into DCHQ in the presence of sulfuric or phosphoric acid. In particular, this process comprises continuously conducting the hydrolysis of 5,7-dichloro-3-ethoxycarbonyl-4-hydroxyquinoline and the decarboxylation of the hydrolyzate in the presence of sulfuric acid having a specified concentration. The invention also relates to a process for producing DCQA by hydrolyzing 3-cyano- or 3-ethoxycarbonyl-5,7-dichloro-4-hydroxyquinoline in the presence of hydrochloric, sulfuric or phosphoric acid and a process for producing DCHQ by decarboxylating DCQA in the presence of sulfuric or phosphoric acid.
摘要翻译：用于生产作为农业园艺杀菌剂中间体的5,7-二氯-4-羟基喹啉（DCHQ）的工业上有利的方法。该方法包括在盐酸，硫酸或磷酸存在下将3-氰基或3-乙氧基羰基-5,7-二氯-4-羟基喹啉水解成5,7-二氯-3-羧基-4-羟基喹啉（DCQA），和在硫酸或磷酸存在下将形成的DCQA脱羧成DCHQ。特别地，该方法包括连续进行5,7-二氯-3-乙氧基羰基-4-羟基喹啉的水解和水解产物在具有特定浓度的硫酸存在下的脱羧作用。本发明还涉及通过在盐酸，硫酸或磷酸的存在下水解3-氰基或3-乙氧基羰基-5,7-二氯-4-羟基喹啉来生产DCQA的方法，以及通过使DCQA脱羧制备DCHQ的方法存在硫酸或磷酸。

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