公开(公告)号：US20040220408A1

公开(公告)日：2004-11-04

申请号：US10476856

申请日：2003-12-16

发明人： Fredrik Bjorkling

IPC分类号： C07F007/02 ,  C07D213/72

CPC分类号： C07D213/89 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12

摘要： Compounds according to formula (I) 1 wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amico, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, O, C(O), S, S(O), S(O)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring, and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.

摘要翻译： 根据式（I）的化合物，其中R 1表示氢，卤素或一个或多个直链或支链，饱和或不饱和的C 1-6烃基，任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基 氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二羟基磷酰氧基或膦酰基; X代表直链或支链饱和或不饱和的C 1 -C 12烃基，其任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基 ，羟基磺酰氧基，二羟基磷酰氧基或膦酰基; Y表示O，C（O），S，S（O），S（O）2，C（O）O，NH，C（O）NH，OC（O）或NHC（O） 羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基烷基或直链或支链，饱和或不饱和的C 1-4烃基，其中Z代表具有5-12个环原子的芳族或非芳族杂环基团 羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基或氨基烷基; 条件是R1不连接到吡啶环中的氮原子，并且公开了其药学上可接受的盐，溶剂合物，水合物，N-氧化物和前药。 这些化合物可用于治疗。

公开(公告)号：US20040176611A1

公开(公告)日：2004-09-09

申请号：US10798338

申请日：2004-03-12

申请人： TOSOH CORPORATION

发明人： Masakatsu Matsumoto ,  Nobuko Watanabe ,  Masashi Yamada

IPC分类号： C07F007/02 ,  C07D498/02

CPC分类号： C07D493/04 ,  C07D321/00 ,  C07F7/1804

摘要： A 1,2-dioxetane derivative of the formula (I): 1 wherein Ar is an aryl group which may have an alkyl group, an aryl group, a halogen atom, an alkoxyl group, a carboxyl group, a formyl group, an alkyl ester, an aryl ester, an alkylketone, an arylketone or a hetero ring bonded thereto, X is a substituent capable of labeling an organic compound or a biological molecule, or an ester, Y is a hydrogen atom, an acyl group or a group of the formula nullSi(R4R5R6) (wherein each of R4, R5 and R6 which are independent of one another, is an alkyl group or an aryl group), Z is an alkyl group, an aryl group, an oxygen atom, a sulfur atom, a carbonyl group, null(CO)nullOnull, nullOnull(CO)null, nullNHnull, nullNHnullCOnull, nullCOnullNHnull, nullOSi(R7R8)null (wherein each of R7 and R8 which are independent of each other, is an alkyl group or aryl group) or a group of the formula null(R9R10)Sionull (wherein each of R9 and R10 which are independent of each other, is an alkyl group or an aryl group), each of R1 and R2 is an alkyl group or an aryl group, and R3 is a spacer.

摘要翻译： 式（I）的1,2-二氧杂环丁烷衍生物：其中Ar是可以具有烷基，芳基，卤素原子，烷氧基，羧基，甲酰基，烷基酯的芳基 ，芳基酯，烷基酮，芳基酮或与其结合的杂环，X是能够标记有机化合物或生物分子的取代基或酯，Y是氢原子，酰基或基团的基团 式-Si（R4R5R6）（其中R4，R5和R6各自独立地为烷基或芳基），Z为烷基，芳基，氧原子，硫原子， 羰基， - （CO）-O-，-O-（CO） - ， - NH - ， - NH-CO - ， - CO-NH-，-OSi（R7R8） - （其中R7和R8各自 相互独立，为烷基或芳基）或式 - （R9R10）Sio-（其中R 9和R 10各自独立地为烷基或芳基）的基团， R 1和R 2各自是烷基或芳基，R 3 是间隔物。

公开(公告)号：US20040147744A1

公开(公告)日：2004-07-29

申请号：US10615352

申请日：2003-07-09

发明人： Klaus-Juergen Pees ,  Waldemar Pfrengle ,  Gavin Heffernan

IPC分类号： C07F007/02 ,  C07D43/02

CPC分类号： C07D239/48 ,  A01N43/54 ,  A01N47/40 ,  C07D239/38 ,  C07D401/04 ,  C07D487/04

摘要： Pyrimidines of formula I 1 in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxycarbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and x represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen atom form a heterocyclic ring; processes and intermediates for preparing these compounds, to compositions comprising them and to their use for controlling harmful fungi.

公开(公告)号：US20040029835A1

公开(公告)日：2004-02-12

申请号：US10629432

申请日：2003-07-29

发明人： Dennis P. Curran ,  Hubert Josien ,  Bom David

IPC分类号： A61K031/695 ,  C07F007/02

CPC分类号： C07D471/14 ,  A61K31/437 ,  C07F7/0812 ,  C07F7/0814 ,  C07F7/083

摘要： The present invention provides generally a compound having the following general formula (1): 1 wherein R1 and R2 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxyl group, an aryloxy group, an acyloxy group, a carbonyloxy group, a carbamoyloxy group, a halogen, a hydroxyl group, a nitro group, a cyano group, an azido group, a formyl group, a hydrazino group, an acyl group, an amino group, nullSRc, wherein, Rc is hydrogen, an acyl group, an alkyl group, or an aryl group, or R1 and R2 together form a group of the formula nullO(CH2)nOnull wherein n represents the integer 1 or 2; R3 is H, F, a halogen atom, a nitro group, an amino group, a hydroxyl group, or a cyano group; or R2 and R3 together form a group of the formula nullO(CH2)nOnull wherein n represents the integer 1 or 2; R4 is H, F, a C1-3 alkyl group, a C2-3 alkenyl group, a C2-3 alkynyl group, or a C1-3 alkoxyl group; R5 is a C1-10 alkyl group, or a propargyl group; and R6, R7 and R8 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a null(CH2)NR9 group, wherein N is an integer within the range of 1 through 10 and R9 is a hydroxyl group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group or a nitro group; and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明通常提供具有以下通式（1）的化合物：其中R 1和R 2独立地相同或不同，为氢，烷基，烯基，苄基，炔基 基团，烷氧基，芳氧基，酰氧基，羰氧基，氨基甲酰氧基，卤素，羟基，硝基，氰基，叠氮基，甲酰基，肼基， 酰基，氨基，-SR c，其中R c是氢，酰基，烷基或芳基，或者R 1和R 2一起形成一个 式-O（CH 2）n O-，其中n表示整数1或2; R 3是H，F，卤素原子，硝基，氨基，羟基或氰基; 或R 2和R 3一起形成式-O（CH 2）n O-的基团，其中n表示整数1或2; R 4是H，F，C 1-3烷基，C 2-3亚烯基，C 2-3炔基或C 1-3烷氧基; R 5是C 1-10烷基或炔丙基; 和R 6，R 7和R 8独立地是C 1-10烷基，C 2-10烯基，C 2-10炔基，芳基或 - （CH 2）NR 9 >基，其中N是1至10的整数，R 9是羟基，烷氧基，氨基，烷基氨基，二烷基氨基，卤素原子，氰基或硝基 组; 及其药学上可接受的盐。

公开(公告)号：US20030235843A1

公开(公告)日：2003-12-25

申请号：US10386403

申请日：2003-03-11

发明人： John W. Babich ,  Kevin P. Maresca

IPC分类号： C12Q001/68 ,  G01N033/53 ,  C07F007/02 ,  C07H005/04 ,  C07H021/02

CPC分类号： C07D213/38 ,  C07F13/005

摘要： One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

摘要翻译： 本发明的一个方面涉及锝（Tc）与各种杂芳族配体如吡啶基和咪唑基配体的新型复合物，以及它们在放射性药物中用于各种临床诊断和治疗应用的用途。 本发明的另一方面涉及形成上述配合物的一部分的新型吡啶基配体。 还描述了制备锝配合物的方法。 本发明的另一方面涉及基于通过固相合成方法与小肽缀合的衍生化赖氨酸，丙氨酸和双氨基酸的新型吡啶基配体。 另外，本发明涉及使用本发明复合物成像哺乳动物区域的方法。

公开(公告)号：US20030187176A1

公开(公告)日：2003-10-02

申请号：US10377793

申请日：2003-03-04

发明人： Kazuo Suga

IPC分类号： C08G077/04 ,  C07F007/02

CPC分类号： C09D183/08 ,  C07F7/1804

摘要： Disclosed is an oxazolidine compound represented by the following formula (1). 1 nullR1 represents a hydrocarbon group having 1 to 6 carbon atoms; R2 and R3 independently represent a hydrogen atom or a monovalent hydrocarbon group having 1 to 15 carbon atoms, or R2 and R3 combine to form an alicyclic ring or an aromatic ring; R4 and R5 independently represent a methyl group or an ethyl group; R6 represents a single bond or null(R7nullNHCOOnullR8nullOCONH)pnull, R7 and R8 independently represent a divalent organic group, and p represents an integer of 1 to 15; m represents 2 or 3; n represents an integer of 1 to 3null. A curable resin composition using the oxazolidine compound as a latent curing agent have excellent curability and excellent storage stability, in particular, excellent storage stability in a state where the resin composition contains only the curable ingredient(s) and the latent curing agent.

摘要翻译： 公开了由下式（1）表示的恶唑烷化合物。 [R 1]表示碳原子数1〜6的烃基。 R 2和R 3独立地表示氢原子或具有1至15个碳原子的一价烃基，或R 2和R 3结合形成脂环或芳环; R 4和R 5独立地表示甲基或乙基; R 6表示单键或 - （R 7 -NHCOO-R 8 -OCONH）p - ，R 7和R 8独立地表示二价有机基团，p表示 1至15; m表示2或3; n表示1〜3的整数]。 使用该恶唑烷化合物作为潜在性固化剂的固化性树脂组合物具有优异的固化性和优异的储存稳定性，特别是在树脂组合物仅含有可固化成分和潜在性固化剂的状态下具有良好的储存稳定性。

公开(公告)号：US20030149069A1

公开(公告)日：2003-08-07

申请号：US10254033

申请日：2002-09-24

发明人： Chao-Jun Li ,  Jianheng Zhang

IPC分类号： A61K031/695 ,  A61K031/4743 ,  A61K031/4741 ,  C07D498/02 ,  C07D491/02 ,  C07F007/02 ,  A61K009/127

CPC分类号： C07D491/04 ,  A61K47/56

摘要： The present invention provides methods for synthesizing novel tetrahydroquinoline derivatives that are useful for cancer chemotherapy and anti-viral applications. The present invention provides compounds useful for cancer chemotherapy and methods for the preparation of these compounds. The present invention also includes cancer chemotherapy methods.

摘要翻译： 本发明提供合成可用于癌症化疗和抗病毒应用的新四氢喹啉衍生物的方法。 本发明提供了可用于癌症化疗的化合物及其制备方法。 本发明还包括癌症化疗方法。

公开(公告)号：US20030139600A1

公开(公告)日：2003-07-24

申请号：US10364365

申请日：2003-02-12

申请人： SUMITOMO CHEMICAL CO., LTD.

发明人： Junichi Yoshida ,  Kenichiro Itami ,  Seiji Suga

IPC分类号： C07F007/02

CPC分类号： C07C29/48 ,  C07C2601/14 ,  C07F7/0814 ,  C07C33/20 ,  C07C33/26 ,  C07C35/08

摘要： The present invention provides a compound which can be purified by conventional acid/base extraction. There is disclosed 2-pyridylsilane of formula (1): 1 wherein R1 represents an alkyl group, etc, R2 and R3 represent an alkyl group, an alkoxy group, etc., R4, R5, R6 and R7 represent a hydrogen atom, a halogen atom, an alkyl group, etc.

摘要翻译： 本发明提供可以通过常规酸/碱提取纯化的化合物。 公开了式（1）的2-吡啶基硅烷：其中R1表示烷基等，R2和R3表示烷基，烷氧基等，R4，R5，R6和R7表示氢原子，卤素 原子，烷基等

公开(公告)号：US20030114670A1

公开(公告)日：2003-06-19

申请号：US10317720

申请日：2002-12-12

发明人： Robert L. Dow ,  Steven R. Schneider

IPC分类号： C07F007/02 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02 ,  C07D49/02 ,  C07D45/02 ,  C07D41/02

CPC分类号： C07F7/1892 ,  C07F7/1804 ,  C07F7/188 ,  Y02P20/55

摘要： A process for preparing a compound of the formula 1 wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of null-adrenergic receptor agonists.

摘要翻译： 制备下式化合物的方法其中n，R 1，R 2，R 3和X如上所定义，用作β-肾上腺素能受体激动剂合成中的中间体。

公开(公告)号：US20030100786A1

公开(公告)日：2003-05-29

申请号：US10223211

申请日：2002-08-20

申请人： SUMITOMO CHEMICAL COMPANY, LIMITED

发明人： Takahiro Ueoka ,  Hideyuki Ikehira ,  Yoshiaki Tsubata

IPC分类号： C07F007/02 ,  C07C39/73 ,  C07C255/50 ,  C07C25/06 ,  C07C043/20

CPC分类号： C07C25/24 ,  C07C43/225 ,  C07C309/65 ,  C07C309/73 ,  C07C2603/24 ,  C07F7/081

摘要： Provided is a bis(diphenylvinyl)arene compound having a reactive functional group on phenyl group, represented by below formula (1), 1 wherein, Ar is an arylene group and has one or more substituents; R1-R22 each independently represent a hydrogen atom, a halogen atom, cyano group, nitro group, etc., and at least one of R1-R20 is a halogen atom, etc. The arene compound has sufficient solubility in an organic solvent and excellent reactivity.

摘要翻译： 本发明提供一种在苯基上具有反应性官能团的双（二苯基乙烯基）芳烃化合物，由下式（1）表示，其中Ar为亚芳基并具有一个或多个取代基; R1-R22各自独立地表示氢原子，卤素原子，氰基，硝基等，R 1 -R 20中的至少一个为卤素原子等。芳族化合物在有机溶剂中具有充分的溶解性，优异的 反应性。