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公开(公告)号:US11028056B2
公开(公告)日:2021-06-08
申请号:US16616596
申请日:2018-05-30
发明人: Shun Tanimura , Masaya Tanimoto , Koji Hagiya
IPC分类号: C07D239/42 , C07C67/347 , C07C231/12 , C07C269/00 , C07C69/612 , C07C233/08 , C07C271/14
摘要: The present invention provides a method for industrially producing: a pyrimidine compound having pest control efficacy; 2-[4-(trifluoromethyl)phenyl]ethylamine which is a production intermediate of the pyrimidine compound; a phenylethylamine compound useful as a pharmaceutical and agrochemical intermediate; and further a 3-arylpropionamide compound and a 3-arylpropionic acid ester compound useful as production intermediates of the phenylethylamine compound. The 3-arylpropionamide compound or the 3-arylpropionic acid ester compound can be efficiently and industrially produced in a single step by reacting a compound represented by formula (1) (wherein X represents a chlorine atom or a bromine atom; and Y represents an alkyl group optionally substituted with fluorine atom(s), a hydrogen atom, a fluorine atom, a cyano group, an alkylcarbonyl group, a dialkylamino group, or the like) with acrylamide or an acrylic acid ester in the presence of a metal catalyst and a reducing agent.
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公开(公告)号:US07253194B2
公开(公告)日:2007-08-07
申请号:US10333871
申请日:2001-07-24
申请人: Robert C Reid , Christopher I Clark , Karl Hansford , Martin J Stoermer , Ross P McGeary , David P Fairlie , Karl Schafer
发明人: Robert C Reid , Christopher I Clark , Karl Hansford , Martin J Stoermer , Ross P McGeary , David P Fairlie , Karl Schafer
IPC分类号: A61K31/44 , A61K31/165 , A61K31/351 , C07C233/08 , C07C213/46
CPC分类号: C07D213/30 , C07C233/51 , C07C235/12 , C07C271/22 , C07D209/20 , C07D213/55 , C07D213/56 , C07D233/64 , C07D257/04 , C07F9/4006 , C07F9/4075
摘要: The present invention relates generally to amino acid derivatives and to methods of making the same. In particular, the invention relates to compounds bearing a stereochemical identity, that is, the same stereochemistry, with the chiral α-carbon of D-α-amino acids and their use in methods of therapy, including the treatment of inflammatory diseases, and to compositions and enantiomeric mixtures containing them.
摘要翻译: 本发明一般涉及氨基酸衍生物及其制备方法。 特别地,本发明涉及具有立体化学特征的化合物,即与D-α-氨基酸的手性α-碳相同的立体化学结构,以及它们在治疗方法中的应用,包括治疗炎性疾病,以及 组合物和含有它们的对映体混合物。
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3.
公开(公告)号:US5719170A
公开(公告)日:1998-02-17
申请号:US763364
申请日:1996-12-11
IPC分类号: C07D235/08 , A61K31/215 , A61K31/33 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61P3/08 , A61P3/10 , C07C65/36 , C07C69/02 , C07C233/08 , C07C233/90 , C07C255/50 , C07C311/01 , C07C311/02 , C07C311/50 , C07C327/20 , C07C327/38 , C07C327/56 , C07C329/04 , C07C329/14 , C07C333/02 , C07D233/02 , C07D235/04 , C07D235/06 , C07D277/22 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D417/04 , C07D417/12 , C07D491/10 , C07D491/113 , C07D493/10 , A61K31/42 , A61K31/425 , C07D413/12
CPC分类号: C07D235/06 , C07D403/12 , C07D405/04 , C07D405/14 , C07D417/04 , C07D417/12 , C07D491/10 , C07D493/10
摘要: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.
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公开(公告)号:US5643925A
公开(公告)日:1997-07-01
申请号:US837491
申请日:1992-02-18
IPC分类号: A61K31/16 , A61K31/135 , A61K31/165 , A61K31/38 , A61K31/381 , A61K31/47 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P25/28 , A61P43/00 , C07C57/03 , C07C205/06 , C07C233/07 , C07C233/08 , C07C235/32 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07D215/14 , C07D215/38 , C07D295/18 , C07D295/185 , C07D333/56 , C07D333/68 , A01N43/42
CPC分类号: C07D215/38 , C07C235/34 , C07C235/36 , C07C237/20 , C07C237/22 , C07D295/185 , C07D333/68 , C07C2102/08 , C07C2103/74
摘要: Novel benzene derivatives are provided of the general formula (I): ##STR1## [wherein R.sup.1 represents an amino group, a substituted amino group, a protected amino group, or a nitro group; R.sup.2 represents an amino group, a substituted amino group, a protected amino group, a hydroxy group, a substituted hydroxy group, or a protected hydroxy group; R.sup.3 represents an amino group, a substituted amino, a heterocyclyl group having a ring nitrogen atom as the point of binding, or a substituted heterocyclyl group having a ring nitrogen atom as the point of binding; m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n represents an integer from 2 to 6] and salts thereof.Compounds of formula (I) except those wherein R.sup.1 is a nitro group have activity in promoting production of nerve growth factor. Compounds of formula (I) wherein R.sup.1 is a nitro group are intermediates for compounds of formula (I) wherein R.sup.1 is an amino group.
摘要翻译: 提供通式(I)的新型苯衍生物:其中R1表示氨基,取代氨基,被保护的氨基或硝基; R2表示氨基,取代氨基,保护氨基,羟基,取代羟基或被保护的羟基; R3表示氨基,取代氨基,具有环氮原子作为结合点的杂环基或具有环氮原子作为结合点的取代的杂环基; m为0〜2; n为0〜6; 条件是当m为0时,n表示2至6的整数]及其盐。 式(I)的化合物除了其中R1是硝基之外,具有促进神经生长因子产生的活性。 其中R 1是硝基的式(I)化合物是其中R 1是氨基的式(I)化合物的中间体。
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公开(公告)号:US5580893A
公开(公告)日:1996-12-03
申请号:US211904
申请日:1994-07-25
申请人: Sadao Ishihara , Fujio Saito , Mitsuru Kataoka , Hiroyuki Koike , Shigeki Miyake , Hiroshi Mizuno
发明人: Sadao Ishihara , Fujio Saito , Mitsuru Kataoka , Hiroyuki Koike , Shigeki Miyake , Hiroshi Mizuno
IPC分类号: A61K31/16 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/41 , A61P9/08 , A61P9/10 , C07C233/08 , C07C233/13 , C07C235/20 , C07C235/22 , C07C271/48 , C07C323/60 , C07C323/62 , C07C333/04 , C07D261/08 , C07D261/10 , C07D261/12 , C07D307/54 , C07D307/68 , C07D307/71 , C07D319/20 , C07D333/38 , C07D261/06
CPC分类号: C07D261/10 , C07C235/20 , C07C271/48 , C07C323/60 , C07D261/08 , C07D261/12 , C07D307/68 , C07D307/71 , C07D319/20 , C07D333/38
摘要: Nitroxyalkylamide compounds having the formula: R.sup.1 --(A).sub.n --CONH--B'--ONO.sub.2 wherein R.sup.1 is an optionally substituted furyl, furyloxy, thienyl, thienyloxy, isoxazolyl, phenoxy, phenylthio or 1,4-dibenzodioxanyl, A is a C.sub.1 -C.sub.4 alkylene group; B' is a C.sub.1 -C.sub.4 alkylene group; and n is 0 or 1. The compounds of the present invention have a desirable vasodilator action for collateral vessels and an anti-anginal action, and are useful as therapeutic agents for treating angina pectoris.
摘要翻译: PCT No.PCT / JP92 / 01419 Sec。 371日期:1994年7月25日 102(e)日期1994年7月25日PCT提交1992年11月2日PCT公布。 公开号WO93 / 09085 日期:1993年5月13日具有下式的硝基烷基酰胺化合物:R1-(A)n-CONH-B'-ONO2其中R1是任选取代的呋喃基,呋喃氧基,噻吩基,噻吩氧基,异恶唑基,苯氧基,苯硫基或1,4-二苯并二恶烷, 是C1-C4亚烷基; B'是C1-C4亚烷基; 本发明化合物对侧支血管具有期望的血管舒张作用和抗心绞痛作用,可用作治疗心绞痛的治疗剂。
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公开(公告)号:US5532266A
公开(公告)日:1996-07-02
申请号:US453811
申请日:1995-05-30
申请人: Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk , Frank Mauler , Manfred Stohrer , Andrew Barber
发明人: Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk , Frank Mauler , Manfred Stohrer , Andrew Barber
IPC分类号: A61K31/435 , A61K31/165 , A61K31/17 , A61K31/35 , A61K31/40 , A61K31/4025 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61P7/10 , A61P11/08 , A61P11/14 , A61P25/04 , A61P25/08 , A61P25/28 , A61P29/00 , A61P43/00 , C07C233/00 , C07C233/05 , C07C233/08 , C07D207/08 , C07D207/09 , C07D207/12 , C07D215/00 , C07D217/06 , C07D217/14 , C07D295/12 , C07D295/135 , C07D311/84 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D207/36 , C07D207/325
CPC分类号: C07D405/06 , C07D207/09 , C07D207/12 , C07D217/14 , C07D311/84 , C07D405/12
摘要: Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.
摘要翻译: 其中Q为R4-CH(CH2Z)-NA-,R1为Ar,具有3-7个C原子的环烷基或C 4 -C 8 - 环烷基-C 1 -C 4烷基的新的芳基乙酰胺, C7-烷基,R2是Ar,R3是H,OH,OA或A,R4是A或可以被F,Cl,Br,I,OH,OA,CF3,NO2,NH2等任意取代一次或两次的苯基, NHA,NHCOA,NHSO2A或NA2,R5和R6各自独立地为H,F,Cl,Br,I,OH,OA,CF3,NH2,NHA,NA2,NHCOA,NHCONH2, 亚甲二氧基,A是具有1-7个C原子的烷基,以及其生理上可接受的盐。
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公开(公告)号:US5411989A
公开(公告)日:1995-05-02
申请号:US168163
申请日:1993-12-17
申请人: Helmut Michel , Wolfgang Bartsch
发明人: Helmut Michel , Wolfgang Bartsch
IPC分类号: A61K31/16 , A61K31/04 , A61K31/18 , A61K31/19 , A61K31/21 , A61K31/215 , A61K31/265 , A61K31/275 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07C203/02 , C07C203/08 , C07C233/12 , C07C233/19 , C07C233/23 , C07C233/60 , C07C235/08 , C07C235/14 , C07C235/40 , C07C237/22 , C07C255/19 , C07C259/08 , C07C271/24 , C07C311/07 , C07C311/14 , C07D207/26 , C07D207/28 , C07D213/81 , C07D213/82 , C07D213/89 , C07D257/00 , C07D257/04 , C07D257/06 , C07D295/185 , C07C233/08 , C07C309/26
CPC分类号: C07D213/81 , C07C233/19 , C07C233/23 , C07C235/08 , C07C235/14 , C07C235/40 , C07C237/22 , C07C255/19 , C07C259/08 , C07C271/24 , C07C311/07 , C07D207/28 , C07D213/82 , C07D295/185 , C07C2101/14
摘要: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.
摘要翻译: 本发明涉及式I的环己醇的硝酸酯,其中A表示价键或C1-C6-亚烷基链,B表示基团-NR1-CO-Z,-NR1-SO2-Z或 -CO-NR 2 -Z,其中R 1表示氢或C 1 -C 6烷基烷基R 2氢,羟基,羟基-C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷基,C 2 -C 6 - 烯基或C 2 -C 6 - 炔基,Z表示氢,C 1 -C 6 - 烷基,C 2 -C 6 - 烯基或C 2 -C 6 - 炔基,其可以任选地取代B为-NR 1 -CO-Z基团的情况 Z也可以表示C1-C6-烷氧基。
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公开(公告)号:US5260478A
公开(公告)日:1993-11-09
申请号:US986646
申请日:1992-12-08
申请人: Edward R. Bacon , Sol J. Daum , Carl R. Illig
发明人: Edward R. Bacon , Sol J. Daum , Carl R. Illig
IPC分类号: A61K49/04 , A61K31/16 , C07C233/01 , C07C233/06 , C07C233/07 , C07C233/08 , C07C233/43 , C07C233/54 , C07C233/56 , C07C69/76
CPC分类号: C07C233/43
摘要: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;n is an integer from 0 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently a substituent as defined for R.sup.1 and R.sup.2 above, halogen, hydroxy or acylamino;and R.sup.5 and R.sup.6 are independently H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, alkoxyalkyl, or acetamidoalkyl;or R.sup.5 and R.sup.6, taken together with the nitrogen atom to which they are attached, represent a 4 to 7-membered nitrogen containing ring, are useful as contrast agents in x-ray imaging compositions and methods.
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公开(公告)号:US4666943A
公开(公告)日:1987-05-19
申请号:US514799
申请日:1983-07-19
申请人: Hiroshi Noguchi , Toshiro Kato , Junya Takahashi , Yukio Ishiguri , Shigeo Yamamoto , Naonori Hirata
发明人: Hiroshi Noguchi , Toshiro Kato , Junya Takahashi , Yukio Ishiguri , Shigeo Yamamoto , Naonori Hirata
IPC分类号: A01N37/18 , A01N37/08 , A01N37/22 , A01N37/24 , A01N37/32 , A01N37/34 , A01N37/36 , A01N37/40 , A01N37/46 , A01N39/02 , A01N39/04 , A01N43/24 , A01N47/34 , A01N53/00 , A01N53/04 , A01N53/12 , A01N57/30 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/02 , C07C233/07 , C07C233/08 , C07C233/09 , C07C233/11 , C07C233/12 , C07C233/15 , C07C233/25 , C07C233/27 , C07C233/28 , C07C233/29 , C07C233/43 , C07C233/46 , C07C233/55 , C07C233/58 , C07C233/65 , C07C235/24 , C07C235/56 , C07C237/06 , C07C239/00 , C07C251/48 , C07C253/00 , C07C255/27 , C07C255/44 , C07C255/60
摘要: Use of an anilide of the formula: ##STR1## as a fungicidal agent against phytophatogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.
摘要翻译: 使用下式的酰苯胺:作为杀真菌剂的植物致病真菌,特别是其对苯并咪唑硫氮菌素杀真菌剂和/或环状酰亚胺杀真菌剂有抗性的菌株。
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公开(公告)号:US4533749A
公开(公告)日:1985-08-06
申请号:US349122
申请日:1982-02-16
申请人: Paul A. Aristoff , John C. Sih
发明人: Paul A. Aristoff , John C. Sih
IPC分类号: C07C69/675 , A61K31/557 , A61P7/02 , A61P11/00 , A61P35/00 , C07C27/00 , C07C31/27 , C07C31/44 , C07C33/05 , C07C33/44 , C07C35/31 , C07C35/52 , C07C51/00 , C07C51/353 , C07C57/18 , C07C59/01 , C07C59/42 , C07C67/00 , C07C69/732 , C07C213/00 , C07C215/20 , C07C215/26 , C07C215/42 , C07C231/00 , C07C233/08 , C07C233/10 , C07C233/11 , C07C233/65 , C07C233/70 , C07C233/72 , C07C233/73 , C07C235/06 , C07C235/26 , C07C235/30 , C07C235/32 , C07C239/00 , C07C253/00 , C07C255/31 , C07C281/14 , C07C405/00 , C07D309/12 , C07F9/38 , C07F9/40 , C07C177/00 , C07C57/26
CPC分类号: C07C405/0083 , C07C51/353 , C07C57/18 , C07F9/4015
摘要: Novel compounds of the following general formula: ##STR1##
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