公开(公告)号：US20230084263A1

公开(公告)日：2023-03-16

申请号：US17799865

申请日：2021-02-15

申请人： LUCOZADE RIBENA SUNTORY LIMITED ,  BRAIN BIOTECH AG

发明人： Alice CANCELLIERI ,  Zafer GEZGIN ,  Paul Stephen JONES ,  Caroline Jane SAUNDERS ,  Roberto VANIN ,  Juergen ECK ,  Guido MEURER ,  Claudia BORGMEIER

IPC分类号： A23L2/60 ,  A23L33/135 ,  A23L33/14 ,  A23L33/105

摘要： The present invention relates to ingredients, particularly sweetening ingredients, for example ingredients for use in reduced sugar, low-sugar, or zero-sugar beverage or food products. More specifically, the present invention relates to ingredients derived from plant infusions, in particular fermented infusions of stevia.

公开(公告)号：US20020040017A1

公开(公告)日：2002-04-04

申请号：US09871655

申请日：2001-06-04

申请人： SUNTORY LIMITED

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

IPC分类号： A61K031/554 ,  A61K031/542 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D207/36

摘要： A pyrrolesulfonamide derivative having the following formula (I): 1 wherein the ring P represented by 2 is a pyrrole ring having the following structure: 3 wherein R represents alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group 4 in which W represents CH, Cnull or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is Cnull; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

摘要翻译： 具有下式（I）的吡咯磺酰胺衍生物：其中由代表的环P是具有以下结构的吡咯环：其中R表示烷基，环烷基，环烷基烷基或芳烷基; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但当不存在键时，Z1表示H，Z2表示OH或Z1，Z2组合在一起表示O或NOR1基团，其中R1表示 H或烷基，芳烷基或芳基; l代表0或1; A表示亚烷基，亚烯基或亚炔基; Y表示W表示CH，C =或N的基团; 当W为CH或N时，m代表0或1，当W为C =时，m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基。 化合物（I）具有强的5-羟色胺-2受体拮抗作用，毒性低，副作用小，可用作循环系统疾病如缺血性心脏病，脑血管障碍和周围循环障碍

公开(公告)号：US20030078256A1

公开(公告)日：2003-04-24

申请号：US09955416

申请日：2001-09-19

申请人： SUNTORY LIMITED

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Iwamori ,  Norio Inomata

IPC分类号： C07D279/16 ,  A61K031/551 ,  A61K031/5415

CPC分类号： C07D275/06 ,  C07D279/02 ,  C07D417/06 ,  C07D513/10

摘要： Disclosed are benzothiazine derivatives represented by the following formula (I): 1 wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: 2 in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q1 and Q2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, Cnull or N; when Y is CH, m stands for 0 or 1, n stands for 1 or 2, B represents O, S, carbonyl or the like, when Y is Cnull, m stands for 1, n stands for 1 or 2, B represents: 3 in which the double bond is linked to Y, R6 represents substituted or unsubstituted aryl or the like; when Y is N, m stands for 0 or 1, n stands for 2 or 3 and B represents carbonyl, sulfonyl or the like, E1 and E2 individually represent H or lower alkyl; and D represents an aromatic hydrocarbon group or an aromatic heterocyclic group; and salts thereof. The benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent selectivity to this action against null1 blocking action and have high safety. Accordingly, the present invention has made it possible to provide pharmaceuticals making use of antagonistic action against serotonin-2 receptors, for example, therapeutics for various circulatory diseases such as ishemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

摘要翻译： 公开了由下式（I）表示的苯并噻嗪衍生物：其中虚线表示存在或不存在键; Z表示以下基团之一：其中R1和R2分别表示烷基，芳烷基等，R3表示H，烷基等，R4表示H，芳烷基等，X1，X2和X3各自表示O或S ，G表示取代或未取代的乙烯，三亚甲基等; Q1和Q2各自表示H，OH，卤素，烷氧基等; A表示亚烷基，亚烯基等; Y表示CH，C =或N; 当Y是CH时，m代表0或1，n代表1或2，B代表O，S，羰基等，当Y是C =，m代表1，n代表1或2，B代表 ：其中双键与Y连接，R​​6表示取代或未取代的芳基等; 当Y为N时，m代表0或1，n代表2或3，B代表羰基，磺酰基等，E1和E2分别代表H或低级烷基; D表示芳香族烃基或芳香族杂环基; 及其盐。 根据本发明的苯并噻嗪衍生物（I）及其盐具有强的5-羟色胺-2阻断作用，对该作用对α1阻断作用具有优异的选择性并具有高安全性。 因此，本发明使得可以提供利用针对5-羟色胺-2受体的拮抗作用的药物，例如用于各种循环系统疾病如血液性心脏病，脑血管障碍和外周循环障碍的治疗剂。

公开(公告)号：US20020137928A1

公开(公告)日：2002-09-26

申请号：US09939829

申请日：2001-08-28

申请人： SUNTORY LIMITED

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

IPC分类号： A61K031/553 ,  C07D513/00 ,  C07D267/02 ,  A61K031/554 ,  C07D281/02 ,  C07D291/08

CPC分类号： C07D513/04 ,  C07D207/36

摘要： A pyrrolesulfonamide compound having the following 1 is a pyrrole ring having the following structure: 2 wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group 3 in which W represents CH, Cnull or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is Cnull; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with null1-blocking action and serotonin-2 receptor antagonistic action in combination.

摘要翻译： 具有下列结构的吡咯磺酰胺化合物是具有下列结构的吡咯环：其中A表示亚烷基，亚烯基或亚炔基; Y表示W表示CH，C =或N的基团; 当W为CH或N时，m代表0或1，当W为C =时，m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基; l代表0或1; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但当不存在键时，Z1表示H，Z2表示OH或Z1，Z2组合在一起表示O或NOR5基团，其中R5表示 H或烷基，芳烷基或芳基; R代表H，烷基，环烷基，环烷基 - 烷基或芳烷基。 化合物（1）对迄今为止报道的并且具有α1-阻断作用和5-羟色胺-2受体拮抗作用的药物的效力，对5-羟色胺2受体以外的受体的选择性，毒性，副作用等改善 组合。

公开(公告)号：US20040261146A1

公开(公告)日：2004-12-23

申请号：US10411225

申请日：2003-04-11

申请人： SUNTORY LIMITED ,  SUNTORY FLOWERS LIMITED

发明人： Masako Mizutani ,  Yoshikazu Tanaka ,  Takaaki Kusumi ,  Shin-Ichi Ayabe ,  Tomoyoshi Akashi

IPC分类号： C12N015/82 ,  C07H021/04 ,  C12N015/87 ,  C12N015/09 ,  C12N015/63 ,  C07K014/00 ,  A01H005/00 ,  A01H005/02

CPC分类号： C12N15/8243 ,  C12N9/0077 ,  C12N15/825

摘要： DNA obtained, for example, from snapdragon or torenia, encoding an enzyme that can convert flavanones directly to flavones, and its uses; the DNA and amino acid sequences for enzymes encoded thereby are listed as SEQ.ID. No. 1 & 2 and 3 & 4, for example. Introduction of the genes into plants can, for example, alter the flower colors of the plants.

摘要翻译： 获得的DNA例如从金枪鱼或者是肾上腺素编码可以将黄烷酮直接转化成黄酮的酶及其用途; 由此编码的酶的DNA和氨基酸序列列为SEQ.ID. 例如1＆2和3和4。 将基因引入植物可以例如改变植物的花色。

公开(公告)号：US20040067525A1

公开(公告)日：2004-04-08

申请号：US10095017

申请日：2002-03-12

申请人： Suntory Limited

发明人： Hideo Naoki ,  Terumi Nakajima ,  Yasufumi Ohfune ,  Tetsuro Shinada ,  Kazuya Murata

IPC分类号： G01N033/53 ,  G06F019/00 ,  G01N033/48 ,  G01N033/50 ,  B01D059/44

CPC分类号： C07C49/753 ,  C07C45/70 ,  Y10T436/17 ,  Y10T436/24

摘要： A method for effectively causing charge-remote fragmentation (CRF) when the structural analysis of an nitrogen-containing organic compound is performed using a high-energy collisional-induced dissociation-mass/mass spectrum (CID-MS/MS spectrum), a reagent to be used in such a method, and a method for analyzing an organic compound by the induction of CRF are provided. The method for the induction of charge-remote fragmentation (CRF) using a high-energy collisional-induced dissociation-mass/mass spectrum (CID-MS/MS spectrum) has the step of: introducing a squaric acid residue into an end of a nitrogen-containing organic compound. The squaric acid residue is represented by a chemical formula (I): 1 The reagent is provided for introducing such a squaric acid residue. Furthermore, the method is provided for analyzing such an organic compound by the induction of CRF.

摘要翻译： 当使用高能碰撞诱导的解离质谱/质谱（CID-MS / MS谱）进行含氮有机化合物的结构分析时，有效地引起电荷远程碎片化（CRF）的方法， 用于这种方法，并且提供了通过诱导CRF分析有机化合物的方法。 使用高能碰撞诱导的解离 - 质谱/质谱（CID-MS / MS谱）诱导电荷远程碎裂（CRF）的方法具有以下步骤：将方酸残渣引入到 含氮有机化合物。 方酸残基由化学式（I）表示：提供用于引入方酸残基的试剂。 此外，提供了通过诱导CRF分析这种有机化合物的方法。

公开(公告)号：US20030040093A1

公开(公告)日：2003-02-27

申请号：US09961253

申请日：2001-09-25

申请人： SUNTORY LIMITED

发明人： Hideki Adachi ,  Masafumi Tsujimoto ,  Hiroyuki Arai ,  Keizo Inoue

IPC分类号： C12N009/16 ,  C07H021/04 ,  C12P021/02 ,  C12N005/06

CPC分类号： C12N9/18

摘要： A protein having activities of a human platelet activating factor acetylhydrolase, and represented by an amino acid sequence represented by the following formula (I) or an amino acid sequence having homology therewith; and a DNA encoding the protein: 1 Met Gly Val Asn Gln Ser Val Gly Phe Pro Pro Val Thr Gly Pro His Leu Val Gly Cys Gly Asp Val Met Glu Gly Gln Asn Leu Gln Gly Ser Phe Phe Arg Leu Phe Tyr Pro Cys Gln Lys Ala Glu Glu Thr Met Glu Gln Pro Leu Trp Ile Pro Arg Tyr Glu Tyr Cys Thr Gly Leu Ala Glu Tyr Leu Gln Phe Asn Lys Arg Cys Gly Gly Leu Leu Phe Asn Leu Ala Val Gly Ser Cys Arg Leu Pro Val Ser Trp Asn Gly Pro Phe Lys Thr Lys Asp Ser Gly Tyr Pro Leu Ile Ile Phe Ser His Gly Leu Gly Ala Phe Arg Thr Leu Tyr Ser Ala Phe Cys Met Glu Leu Ala Ser Arg Gly Phe Val Val Ala Val Pro Glu His Arg Asp Arg Ser Ala Ala Thr Thr Tyr Phe Cys Lys Gln Ala Pro Glu Glu Asn Gln Pro Thr Asn Glu Ser Leu Gln Glu Glu Trp Ile Pro Phe Arg Arg Val Glu Glu Gly Glu Lys Glu Phe His Val Arg Asn Pro Gln Val His Gln Arg Val Ser Glu Cys Leu Arg Val Leu Lys Ile Leu Gln Glu Val Thr Ala Gly Gln Thr Val Phe Asn Ile Leu Pro Gly Gly Leu Asp Leu Met Thr Leu Lys Gly Asn Ile Asp Met Ser Arg Val Ala Val Met Gly His Ser Phe Gly Gly Ala Thr Ala Ile Leu Ala Leu Ala Lys Glu Thr Gln Phe Arg Cys Ala Val Ala Leu Asp Ala Trp Met Phe Pro Leu Glu Arg Asp Phe Tyr Pro Lys Ala Arg Gly Pro Val Phe Phe Ile Asn Thr Glu Lys Phe Gln Thr Met Glu Ser Val Asn Leu Met Lys Lys Ile Cys Ala Gln His Glu Gln Ser Arg Ile Ile Thr Val Leu Gly Ser Val His Arg Ser Gln Thr Asp Phe Ala Phe Val Thr Gly Asn Leu Ile Gly Lys Phe Phe Ser Thr Glu Thr Arg Gly Ser Leu Asp Pro Tyr Glu Gly Gln Glu Val Met Val Arg Ala Met Leu Ala Phe Leu Gln Lys His Leu Asp Leu Lys Glu Asp Tyr Asn Gln Trp Asn Asn Leu Ile Glu Gly Ile Gly Pro Ser Leu Thr Pro Gly Ala Pro His His Leu Ser Ser Leu

公开(公告)号：US20020028809A1

公开(公告)日：2002-03-07

申请号：US09933717

申请日：2001-08-22

申请人： SUNTORY LIMITED

发明人： Masahiro Imoto ,  Tatsuya Iwanami ,  Minako Akabane ,  Yoshihiro Tani

IPC分类号： C07D417/02 ,  C07D413/02 ,  C07D41/02 ,  A61K031/541 ,  A61K031/535 ,  A61K031/4545 ,  A61K031/4439

CPC分类号： C07D401/06 ,  C07D277/18 ,  C07D277/40 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04

摘要： There is provided heterocyclic compounds of the following formula (I): 1 in which, A is optionally substituted aryl group or optionally substituted heterocyclic group; X is oxygen atom, sulfur atom, carbon atom or nitrogen atom; dotted line shows either presence or absence of bond; n is integer of 1 or 2; and Y represents alkylene bond and so on; or a pharmaceutically acceptable salt thereof. These compounds have good affinity to null4null2 nicotinic acetylcholine receptors and activate the same to thereby exert a preventive or therapeutic effect on cerebral dysfunction.

摘要翻译： 提供下式（I）的杂环化合物：其中A为任选取代的芳基或任选取代的杂环基; X是氧原子，硫原子，碳原子或氮原子; 虚线表示存在或不存在结合; n为1或2的整数; Y代表亚烷基键等; 或其药学上可接受的盐。 这些化合物对α4β2烟碱乙酰胆碱受体具有良好的亲和力，并使其活化，从而对脑功能障碍起到预防或治疗作用。

公开(公告)号：US20040003431A1

公开(公告)日：2004-01-01

申请号：US10411115

申请日：2003-04-11

申请人： SUNTORY LIMITED ,  SUNTORY FLOWERS LIMITED

发明人： Masako Mizutani ,  Yoshikazu Tanaka ,  Takaaki Kusumi ,  Shin-Ichi Ayabe ,  Tomoyoshi Akashi

IPC分类号： A01H001/00 ,  C12N009/10 ,  C12N015/82 ,  C07H021/04 ,  C07H017/00 ,  C12P021/02 ,  C12N005/04

CPC分类号： C12N15/8243 ,  C12N9/0077 ,  C12N15/825

摘要： DNA obtained, for example, from snapdragon or torenia, encoding an enzyme that can convert flavanones directly to flavones, and its uses; the DNA and amino acid sequences for enzymes encoded thereby are listed as SEQ.ID. No. 1 & 2 and 3 & 4, for example. Introduction of the genes into plants can, for example, alter the flower colors of the plants.

公开(公告)号：US20030166926A1

公开(公告)日：2003-09-04

申请号：US10188234

申请日：2002-07-03

申请人： SUNTORY LIMITED

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Iwamori ,  Tetsuo Shimamoto ,  Kyoko Nakanishi ,  Norio Inomata

IPC分类号： A61K031/55 ,  C07D487/02

CPC分类号： C07D487/04 ,  C07D207/34

摘要： A method of effecting serotonin-2-receptor antagonism in a mammal in need thereof, which includes administering to the mammal an effective amount of the compound of the formula (I), or a pharmaceutically acceptable salt thereof: 1 wherein ring P, the dashed line, A, Y, Z1 and Z2 are defined herein.

摘要翻译： 一种在有需要的哺乳动物中实现5-羟色胺-2-受体拮抗作用的方法，其包括向哺乳动物施用有效量的式（I）化合物或其药学上可接受的盐：其中环P为虚线 A，Y，Z 1和Z 2在本文中定义。