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41. 发明申请

WO1997041124A1 PROCESS FOR THE PREPARATION OF TETRAHYDRO-INDOLIZINES 审中-公开
标题翻译：制备四氢吲哚类化合物的方法
公开(公告)号：WO1997041124A1
公开(公告)日：1997-11-06
申请号：PCT/JP1997001428
申请日：1997-04-24
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , KAMIHARA, Shinji , KANAI, Kazuaki , NOGUCHI, Shigeru
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D491/10
CPC分类号： C07D471/04
摘要： A process for the preparation of compounds (7), which comprises reacting a compound (5) with ethylene glycol in the presence of a Lewis acid in a solvent to form a compound (6) and reacting the compound (6) with a carbonic diester in the presence of a metal alkoxide in a solvent, as represented by the following reaction scheme wherein R and R are each C1-C6 alkyl or the like; or R is H or C1-C5 alkyl. The compounds (7) are useful as intermediates for the preparation of camptothecins useful as antitumor agents.
摘要翻译：一种制备化合物（7）的方法，其包括使化合物（5）与乙二醇在路易斯酸存在下在溶剂中反应以形成化合物（6）并使化合物（6）与碳酸二酯在溶剂中存在金属醇盐的情况下，如下列反应路线所示，其中R 1和R 6各自为C 1 -C 6烷基等; 或R 5为H或C 1 -C 5烷基。化合物（7）可用作制备用作抗肿瘤剂的喜树碱的中间体。

42. 发明申请

WO1997040037A1 CYCLOALKYLAMINOMETHYLPYRROLIDINE DERIVATIVES 审中-公开
标题翻译：环丙基氨基甲基吡咯烷衍生物
公开(公告)号：WO1997040037A1
公开(公告)日：1997-10-30
申请号：PCT/JP1997001446
申请日：1997-04-24
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , KAWAKAMI, Katsuhiro , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Compounds of general formula (I) and salts thereof, giving quinolone derivatives which exhibit high antibacterial activity against various bacteria including resistant ones and high safety, wherein R is cycloalkyl; R is hydrogen, amino, hydroxyl, mercapto, halogenomethyl, alkyl, alkenyl, alkynyl or alkoxy; R is amino, halogenomethyl, halogenomethoxy, alkyl, alkenyl, alkynyl or alkoxy; R is hydrogen or C1-C6 alkyl; R is C3-C6 cycloalkyl; and X is halogeno or hydrogen, with the proviso that these substituents may be further substituted; and Y is hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, choline, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, C1-C6 alkyl, C2-C7 alkoxymethyl or phenylalkyl composed of C1-C6 alkylene and phenyl.
摘要翻译：给出通式（I）的化合物及其盐，得到喹诺酮衍生物，其对包括耐药性的各种细菌具有高抗菌活性，高安全性，其中R 1为环烷基; R 2是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; R 3是氨基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; R 4是氢或C 1 -C 6烷基; R 5是C 3 -C 6环烷基; 且X为卤素或氢，条件是这些取代基可进一步被取代; 并且Y是氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆碱，二甲基氨基乙基，5-二氢化茚基，邻苯二基苯基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，3-乙酰氧基-2-氧代丁基，C1 -C 1-6烷基，C 2 -C 7烷氧基甲基或由C 1 -C 6亚烷基和苯基组成的苯基烷基。

43. 发明申请

WO1997029764A1 BRAIN ACTIVATORS 审中-公开
标题翻译：脑激活剂
公开(公告)号：WO1997029764A1
公开(公告)日：1997-08-21
申请号：PCT/JP1997000390
申请日：1997-02-14
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , SAITO, Hiroshi , NISHIYAMA, Nobuyoshi , ISHIHARA, Masanao
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K35/84
CPC分类号： A61K36/09 , A61K36/076
摘要： Brain activators and anti-demential drugs containing as the active ingredient(s) one or more saccharides selected from among low-molecular weight pachyman originating in hoelen, lichenan, isolichenan, dextrans, curdlan and pustulan, derivatives thereof and salts thereof. Use of these drugs makes it possible to inhibit or treat lowering of learning and memory functions caused by various factors.
摘要翻译：脑活化剂和抗痴呆药物含有一种或多种选自源自于hoelen，lichenan，isolichenan，葡聚糖，凝乳球和脓疱兰的低分子量异丙基梭菌，其衍生物及其盐的糖类作为活性成分。使用这些药物可以抑制或治疗各种因素引起的学习和记忆功能的降低。

44. 发明申请

WO1997010261A1 PEPTIDE DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：WO1997010261A1
公开(公告)日：1997-03-20
申请号：PCT/JP1996002572
申请日：1996-09-10
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , FUJI CHEMICAL INDUSTRIES, LTD. , SAKURADA, Shinobu , OKAYAMA, Toru , NUKUI, Eriko , HONGO, Kazuya , OGAWA, Tadashi , HONGO, Tomoko , TAKESHIMA, Satoko , TAKE, Nobuhiro , NAKANO, Masaharu
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , FUJI CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07K05/087
CPC分类号： C07K7/02 , A61K38/00 , C07K5/0202
摘要： Compounds represented by the following general formula and salts thereof: Y-L-Tyr-Q-NR -CH(R )-CO-X, wherein R represents hydrogen or C1-6 alkyl; R represents optionally substituted benzyl; Q represents D- or L-Arg; Y represents two hydrogen atoms in the N-terminal amino group of L-Tyr or substituent(s) of the same, for example, C1-6 alkyl optionally having amino or carboxy; and X represents N-methyl- beta -alanine, etc. Because of having an analgetic effect, the compounds are usable in the treatment of cancer pain, etc.
摘要翻译：由以下通式表示的化合物及其盐：Y-L-Tyr-Q-NR 1 -CH（R 2）-CO-X，其中R 1表示氢或C 1-6烷基; R 2表示任选取代的苄基; Q表示D-或L-Arg; Y表示L-Tyr的N-末端氨基中的两个氢原子或相同的取代基，例如任选具有氨基或羧基的C 1-6烷基; X代表N-甲基-β-丙氨酸等。由于具有止痛作用，该化合物可用于治疗癌症疼痛等。

45. 发明申请

WO1997008128A1 PROCESS FOR PRODUCING HALOGENATED CYCLOPROPANE DERIVATIVES 审中-公开
标题翻译：生产羟基环丙基衍生物的方法
公开(公告)号：WO1997008128A1
公开(公告)日：1997-03-06
申请号：PCT/JP1996002417
申请日：1996-08-29
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , SUMITOMO CHEMICAL CO., LTD. , EBATA, Tsutomu , AKIBA, Toshifumi , IKEYA, Takanobu , WAKITA, Ryuhei , SASAKI, Mikio
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , SUMITOMO CHEMICAL CO., LTD.
IPC分类号： C07C69/74
CPC分类号： C07C327/24 , C07C67/347 , C07C231/12 , C07C231/18 , C07C2601/02 , C07C69/74
摘要： A process for producing compounds represented by general formula (1) which comprises reacting a compound represented by the general formula CH2 = CXF with a compound represented by the general formula N2CHCOR in the presence of a catalyst containing an atom of a transition metal of the group 8, etc., and an optically active ligand of carboxylic acid or amide type to thereby form preferentially a stereoisomer of the compound of formula (1) having the S-configuration at the 1-position, wherein X represents chloro, etc.; and R represents alkyloxy, amino, etc.
摘要翻译：一种制备由通式（1）表示的化合物的方法，该方法包括使通式为CH2 = CXF的化合物与通式为N 2 CHCOR的化合物在含有该基团过渡金属原子的催化剂存在下反应 8等，以及羧酸或酰胺型的光学活性配位体，从而优选形成在1-位具有S-构型的式（1）化合物的立体异构体，其中X表示氯等。 R表示烷氧基，氨基等

46. 发明申请

WO1997001532A1 KETONITRILE DERIVATIVES AND ANTIBACTERIAL AGENT AND DRUG CONTAINING THE SAME 审中-公开
标题翻译：酮类衍生物和抗菌药物及含有其的药物
公开(公告)号：WO1997001532A1
公开(公告)日：1997-01-16
申请号：PCT/JP1995002751
申请日：1995-12-28
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TOKUYAMA CORPORATION , KATO, Shozo , ITAHANA, Hidenobu , YAMAGUCHI, Masao , FURUKI, Makiko , NAGATA, Seiji , KITAJIMA, Toshio
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , TOKUYAMA CORPORATION
IPC分类号： C07C255/40
CPC分类号： C07D213/643 , C07C255/21 , C07C255/40 , C07C259/06 , C07D213/57 , C07D263/58 , C07D295/185 , C07D307/20 , C07D309/12 , C07D333/32 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： A ketonitrile derivative represented by general formula (1) or a salt thereof and an antibacterial agent and a drug containing the same, wherein R represents hydrogen or lower alkyl; R , R , R and R are the same or different and each represents hydrogen, halogeno, nitro, lower alkyl, lower alkoxy or optionally substituted phenoxy; X represents an optionally substituted aromatic hydrocarbon group or an optionally substituted heterocyclic group; and Y represents an optionally substituted aromatic hydrocarbon group, an optionally substituted heterocyclic group, carbonyl substituted by an optionally substituted aromatic hydrocarbon group, carbonyl substituted by an optionally substituted aromatic heterocyclic group, N,N-disubstituted carbamoyl or heterocycle-substituted alkyl. The compound is excellent in antibacterial activity on Gram-positive and Gram-negative bacteria.
摘要翻译：由通式（1）表示的酮腈衍生物或其盐和抗菌剂以及含有它们的药物，其中R 1表示氢或低级烷基; R 2，R 3，R 4和R 5相同或不同，各自表示氢，卤代，硝基，低级烷基，低级烷氧基或任意取代的苯氧基; X表示任选取代的芳族烃基或任选取代的杂环基; Y表示任意取代的芳香族烃基，可以具有取代基的杂环基，被任意取代的芳香族烃基取代的羰基，被任意取代的芳香族杂环基取代的羰基，N，N-二取代的氨基甲酰基或杂环取代的烷基。该化合物对革兰氏阳性和革兰氏阴性菌的抗菌活性优良。

47. 发明申请

WO1996023782A1 HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO1996023782A1
公开(公告)日：1996-08-08
申请号：PCT/JP1996000208
申请日：1996-02-01
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , KAWAKAMI, Katsuhiro , KIMURA, Kenichi , OHKI, Hitoshi , MATSUHASHI, Norikazu , KAWATO, Haruko
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： N1-(Halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by general formula (I), heterocyclic compounds useful as antibacterial agents, wherein X represents halo or hydrogen; X represents halo; R represents hydrogen, hydroxy, thiol, halomethyl, amino, alkyl or alkoxy; R represents a group of general formula (II) (wherein R and R represent each hydrogen or alkyl; and n represents an integer of 1 or 2); A represents nitrogen or a group of general formula (III), (wherein X represents halo, cyano, amino, alkyl, halomethyl, alkoxy or halomethoxy); and R represents hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, choline, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1, 3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl or phenylalkyl.
摘要翻译：由通式（I）表示的N1-（卤代环丙基）取代的吡啶酮羧酸衍生物，可用作抗菌剂的杂环化合物，其中X 1表示卤素或氢; X 2表示卤素; R 1表示氢，羟基，硫醇，卤代甲基，氨基，烷基或烷氧基; R 2表示通式（II）的基团（其中R 3和R 4各自代表氢或烷基; n表示1或2的整数）; A表示氮或通式（III）的基团（其中X 3表示卤素，氰基，氨基，烷基，卤代甲基，烷氧基或卤代甲氧基）; 并且R表示氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆碱，二甲基氨基乙基，5-二氢化茚基，邻苯二基苯基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，3-乙酰氧基-2-氧代丁基，，烷氧基甲基或苯基烷基。

48. 发明申请

WO1996000571A1 ANTIBACTERIAL AGENT 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1996000571A1
公开(公告)日：1996-01-11
申请号：PCT/JP1995001290
申请日：1995-06-28
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TOKUYAMA CORPORATION , ISHIZAKI, Shigeyo +hf , ISHIZAKI, Masayo +hf , ISHIZAKI, Yoshihiko +hm , ISHIZAKI, Yumi +hf , KATO, Shozo , ITAHANA, Hidenobu , FURUKI, Makiko , YAMAGUCHI, Masao , OHMURO, Fumio , NAGATA, Seiji , OHARA, Eiji , KITAJIMA, Toshio
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , TOKUYAMA CORPORATION , ISHIZAKI, Shigeyo +hf , ISHIZAKI, Masayo +hf , ISHIZAKI, Yoshihiko +hm , ISHIZAKI, Yumi +hf , ISHIZAKI, Masahiko +di
IPC分类号： A61K31/275
CPC分类号： C07D213/64 , A61K31/275 , A61K31/277 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/423 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/495 , A61K31/498 , A61K31/505 , A61K31/506 , A61K31/5375 , A61K31/55 , C07C255/21 , C07D213/57 , C07D239/30 , C07D241/44 , C07D263/58 , C07D277/68 , C07D295/15 , C07D295/185 , C07D307/54 , C07D333/24
摘要： An antibacterial for animals containing a ketonitrile derivative represented by general formula (1) or a salt thereof as the active ingredient and having an excellent antibacterial activity against Gram-positive and Gram-negative bacteria, wherein R represents hydrogen or lower alkyl; R , R , R and R represent each independently hydrogen, halogen, nitro, lower alkyl, lower alkoxy or (un)substituted phenoxy; X represents (un)substituted aromatic hydrocarbyl or (un)substituted heterocycle; Y represents (un)substituted aromatic hydrocarbyl, (un)substituted heterocycle, carbonyl substituted by (un)substituted aromatic hydrocarbyl, carbonyl substituted by (un)substituted heterocycle, or N,N-disubstituted carbamoyl.
摘要翻译：含有通式（1）表示的酮腈衍生物或其盐作为活性成分，对革兰氏阳性菌和革兰氏阴性菌具有优异抗菌活性的动物的抗菌剂，其中R 1表示氢或低级烷基; R 2，R 3，R 4和R 5各自独立地表示氢，卤素，硝基，低级烷基，低级烷氧基或（取代的）取代的苯氧基; X表示（un）取代的芳族烃基或（un）取代的杂环; Y代表（取代的）取代的芳族烃基，（取代的）取代的杂环，由（未）取代的芳族烃基取代的羰基，被（未）取代的杂环取代的羰基或N，N-二取代的氨基甲酰基。

49. 发明申请

WO1995026978A1 CYCLIC PEPTIDE AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：循环肽及其生产方法
公开(公告)号：WO1995026978A1
公开(公告)日：1995-10-12
申请号：PCT/JP1995000611
申请日：1995-03-30
申请人： MERCIAN CORPORATION , DAIICHI PHARMACEUTICAL CO., LTD. , AGEMATSU, Hitoshi , CHIBA, Hiroyuki , KANETO, Rei , OHTA, Toshiharu , NAKAYAMA, Kiyoshi
发明人： MERCIAN CORPORATION , DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07K05/08
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0806
摘要： A cyclic tetrapeptide or a corresponding depsipeptide represented by general formula (I) and a salt thereof, wherein R , R and R represent each independently, together with the alpha -amino acid units to which they are bonded, an appropriate alpha -amino acid residue; Q represents NR or oxygen; and Q represents an optionally substituted bonding group. These peptides have an antifungal activity and are useful for treating infectious diseases.
摘要翻译：由通式（I）表示的环状四肽或相应的缩酚酸肽及其盐，其中R 5，R 6和R 7各自独立地表示与它们所属的α-氨基酸单元键合，合适的α-氨基酸残基; Q 1表示NR 4或氧; 并且Q 2表示任选取代的键合基团。这些肽具有抗真菌活性，可用于治疗感染性疾病。

50. 发明申请

WO1994025015A1 DIGESTIVE SYMPTOM AMELIORANT 审中-公开
标题翻译：消极症状特征
公开(公告)号：WO1994025015A1
公开(公告)日：1994-11-10
申请号：PCT/JP1994000721
申请日：1994-04-28
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , ASANO, Masahide , NAKAJIMA, Kazuhiko , FURUHAMA, Kazuhisa , HATANAKA, Satoshi , KAWARABAYASHI, Keiko
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/165
CPC分类号： C07D295/192 , A61K31/165 , A61K31/166 , A61K31/185 , A61K31/215 , A61K31/535 , C07C237/30 , C07C237/44 , C07C309/14
摘要： A digestive symptom ameliorant or a digestive tract movement modulator comprising an aminobenzamide compound represented by general formula (1) or a salt thereof wherein R and R represent each independently lower alkoxy; R represents hydrogen, lower acyl, lower alkyl, lower alkoxycarbonyl or -X-SO3M, wherein X represents lower alkylene and M represents alkali or alkaline earth metal; R represents hydrogen, halogen or lower alkoxy; R represents amino, morpholino or lower alkylamino wherein the alkyl group may be hydroxylated; and n represents an integer of 1 to 6.
摘要翻译：消炎症改善剂或消化道运动调节剂，其包含由通式（1）表示的氨基苯甲酰胺化合物或其盐，其中R 1和R 2各自独立地为低级烷氧基; R 3表示氢，低级酰基，低级烷基，低级烷氧基羰基或-X-SO 3 M，其中X表示低级亚烷基，M表示碱金属或碱土金属; R 4表示氢，卤素或低级烷氧基; R 5表示氨基，吗啉代或低级烷基氨基，其中烷基可被羟基化; n表示1〜6的整数。

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