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1. 发明申请

WO1986000893A1 NOVEL AMIDINE COMPOUNDS 审中-公开
标题翻译：新型氨基化合物
公开(公告)号：WO1986000893A1
公开(公告)日：1986-02-13
申请号：PCT/JP1985000392
申请日：1985-07-12
申请人： TORII & CO., LTD. , FUJII, Setsurou , OKUTOME, Toshiyuki , NAKAYAMA, Toyoo , NUNOMURA, Shigeki , SUDO, Kimio , WATANABE, Shinichi , KURUMI, Masateru , AOYAMA, Takuo
发明人： TORII & CO., LTD.
IPC分类号： C07C129/12
CPC分类号： C07C279/18 , C07D233/50 , C07D233/88 , C07D235/30
摘要： Novel amidine compounds represented by formula (I) (wherein R1 and R2 each represents hydrogen, a straight or branched chain alkyl group containing 1 to 6 carbon atoms, R3 represents a straight or branched chain alkyl group containing 1 to 6 carbon atoms or R4-B-(VH2)n-, n represents -O- or NH-, R4 represents hydrogen, R5-CO- or $(1,7)$-CH2-, R5 represents a straight or branched chain alkyl group containing 1 to 15 carbon atoms, and R1 and R3 may optionally form a ring via 2 to 4 carbon atoms which may contain a double bond or a straight or branched alkyl substituent containing 1 to 4 carbon atoms) and medicinally acceptable acid addition salts thereof are useful as orally administrable anti-trypsin, anti-plasmin, anti-kallikrein, anti-thrombin, and anti-complement agents.

2. 发明申请

WO1982001367A1 NOVEL GUANIDINE DERIVATIVES 审中-公开
标题翻译：新的制剂衍生物
公开(公告)号：WO1982001367A1
公开(公告)日：1982-04-29
申请号：PCT/EP1981000163
申请日：1981-10-12
申请人： SCHERING CORP
发明人： SCHERING CORP , NAFISSI VARCHEI MOHAMMAD M
IPC分类号： C07C129/12
CPC分类号： C07D213/40 , C07C279/24 , C07C279/28 , C07C323/44 , C07D211/56 , C07D211/58 , C07D213/75 , C07D265/30 , C07D295/13 , C07D309/14
摘要： Guanidine derivatives of formula: (FORMULA) their isomers at the guanidine groups and pharmaceutically acceptable salts of such compounds, wherein one of X and Y is CR s and the other is CH or N; R s is hydrogen, halogen, nitro, amino, NHCOR s or NHSO uR s; R s and R s are independently selected from hydrogen, N-alkyl-piperidyl tetrahydropyranyl morpholinyl, piperidyl and alkyl substituted by one or more substituents selected from OH, SCH3, COR s, OSO uH, SO uH, COOR s, piperazinyl, pyridyl and (FORMULA) with the proviso that R s and R s cannot both be hydrogen; R s is C u to C u alkyl or alkyl substituted by alkoxy, hydroxy or amino; and their salts are useful as anthelmintics.
摘要翻译：胍（式）的胍衍生物：其胍基上的异构体和这些化合物的药学上可接受的盐，其中X和Y之一是CR 5，另一个是CH或N; R s是氢，卤素，硝基，氨基，NHCOR s或NHSO 4 s; R s和R 3独立地选自氢，N-烷基 - 哌啶基四氢吡喃基吗啉基，哌啶基和被一个或多个选自OH，SCH 3，COR 9，S O， uH，SOu，COOR，s，哌嗪基，吡啶基和（式），条件是R 2和R 3不能都是氢; R 6是C u至C u烷基或被烷氧基，羟基或氨基取代的烷基; 其盐可用作驱肠虫剂。

3. 发明申请

WO1988000583A1 SIGMA BRAIN RECEPTOR LIGANDS AND THEIR USE 审中-公开
标题翻译： SIGMA脑受体配体及其使用
公开(公告)号：WO1988000583A1
公开(公告)日：1988-01-28
申请号：PCT/US1987001545
申请日：1987-06-26
申请人： STATE OF OREGON, acting by and through the OREGON , WEBER, Eckard , SONDERS, Mark , KEANA, John, F.
发明人： STATE OF OREGON, acting by and through the OREGON
IPC分类号： C07C129/12
CPC分类号： C07C279/18
摘要： Formula (I), wherein R and R' are hydrocarbon groups, e.g., N,N'-dibutyl-guanidine, N,N'-diphenyl-guanidine, N,N'-di-o-tolyl-guanidine, N-o-tolyl-N'-p-azido-o-tolyl-guanidine and N-adamantyl-N'-o-tolyl-guanidine, are highly selective ligands for sigma brain receptors and are useful in the diagnosis and treatment of hallucination associated psychotic mental illness and chronic mental depression. Tritium labeled N,N'-di-(o-tolyl)-guanidine is useful as a screening tool for compounds having selective sigma receptor binding activity, as it is displaced from isolated mammalian brain membrane to which it is bound portionately to the activity of such a compound.
摘要翻译：式（I）其中R和R'是烃基，例如N，N'-二丁基胍，N，N'-二苯基胍，N，N'-二邻甲苯基胍，无甲苯基 -N'-对叠氮基邻甲苯基胍和N-金刚烷基-N'-邻甲苯基胍是用于σ脑受体的高选择性配体，可用于诊断和治疗与幻觉相关的精神病性精神病和慢性精神抑郁氚标记的N，N'-二（邻甲苯基） - 胍可用作具有选择性σ受体结合活性的化合物的筛选工具，因为它从分离的哺乳动物脑膜中被部分地结合到活性这样的化合物。

4. 发明申请

WO1986005782A1 GUANIDINE DERIVATIVES 审中-公开
标题翻译：胍基衍生物
公开(公告)号：WO1986005782A1
公开(公告)日：1986-10-09
申请号：PCT/JP1985000151
申请日：1985-03-28
申请人： TORAY INDUSTRIES, INC. , MORIMOTO, Hiroshi , OHURA, Akio
发明人： TORAY INDUSTRIES, INC.
IPC分类号： C07C129/12
CPC分类号： C07C279/12 , A01N47/44
摘要： Novel guanidine derivatives having a straight hydrocarbon chain as a molecular skeleton, a guanidino group, (I), on the primary carbon atoms of both ends, and an amino group on the central carbon atom possess excellent effects against various plant diseases with substantially no phytotoxicity, thus being usable as fungicides.
摘要翻译：具有直链烃链作为分子骨架的新型胍衍生物，胍基（I），两末端的碳原子和中心碳原子上的氨基对各种植物病害具有极好的效果，基本上没有植物毒性，因此可用作杀真菌剂。

5. 发明申请

WO1988007990A1 METHOD FOR THE PREPARATION OF AMIDINO-UREA DERIVATIVES 审中-公开
标题翻译：制备氨基尿素衍生物的方法
公开(公告)号：WO1988007990A1
公开(公告)日：1988-10-20
申请号：PCT/HU1988000017
申请日：1988-04-08
申请人： REANAL FINOMVEGYSZERGYAR , TÖRÖK, Sándor , NAGY, Balázs , PRIBÉK, Ferenc , BALOGH, Sándor
发明人： REANAL FINOMVEGYSZERGYAR
IPC分类号： C07C129/12
CPC分类号： C07C279/24
摘要： The invention relates to an improved method for the preparation of an amidino-urea derivative of general formula (I), wherein R , R and R each stand for hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro or optionally substituted amino, R is hydrogen or lower alkyl, and R is hydrogen or C1-10 alkyl, by reacting a lower alkyl carbamate with an appropriate guanidine derivative. According to the invention the reaction is performed in the presence of a bipolar aprotic solvent. The invention also relates to a method for preparing an adduct of 1-(2,6-dimethylphenyl)-3-(N-methylamidino)-urea and dimethyl sulphoxide, in which 1-(2,6-dimethylphenyl)-3-(N-methylamidino)-urea, prepared optionally directly in the reaction mixture, is reacted with dimethyl sulphoxide. When decomposing this aduct with water, 1-(2,6-dimethylphenyl)-3-(N-methylamidino)-urea is obtained in extremely pure state.
摘要翻译：本发明涉及制备通式（I）的脒基 - 脲衍生物的改进方法，其中R 1，R 2和R 3各自代表氢，卤素，低级烷基，低级烷氧基三氟甲基，硝基或任选取代的氨基，R 4是氢或低级烷基，R 5是氢或C 1-10烷基，通过使氨基甲酸低级烷基酯与适当的胍衍生物反应。根据本发明，反应在双极性非质子传递溶剂的存在下进行。本发明还涉及制备1-（2,6-二甲基苯基）-3-（N-甲基脒基） - 脲和二甲基亚砜的加合物的方法，其中1-（2,6-二甲基苯基）-3-（ N-甲基脒基） - 脲（任选地直接在反应混合物中制备）与二甲基亚砜反应。当用水分解该产物时，以非常纯的状态获得1-（2,6-二甲基苯基）-3-（N-甲基脒基） - 脲。

6. 发明申请

WO1988000181A1 ANTIVIRAL GUANIDINE DERIVATIVE COMPOSITIONS AND THEIR METHODS OF USE 审中-公开
标题翻译：抗病毒药物衍生物组合物及其使用方法
公开(公告)号：WO1988000181A1
公开(公告)日：1988-01-14
申请号：PCT/US1987001562
申请日：1987-06-25
申请人： HARBOR BRANCH OCEANOGRAPHIC INSTITUTION, INC.
发明人： HARBOR BRANCH OCEANOGRAPHIC INSTITUTION, INC. , HIGA, Tatsuo , SAKAI, Ryuichi
IPC分类号： C07C129/12
CPC分类号： C07D239/42 , C07C279/08
摘要： Antiviral organic guanidine derivatives compositions; a process of producing the antiviral compositions; and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are tubastrines derived from marine coral tubastrea aurea.
摘要翻译：抗病毒有机胍衍生物组合物; 制备抗病毒组合物的方法; 以及利用该组合物抑制病毒的方法。更具体地，组合物是衍生自海洋珊瑚tubastrea aurea的大麻素。

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