公开(公告)号：US20210121510A1

公开(公告)日：2021-04-29

申请号：US17047611

申请日：2019-04-17

申请人： TAKEDA GMBH ,  TAKEDA PHARMACEUTICAL COMPANY LTD.

发明人： Markus RAST ,  Sergio RODRIGUEZ-MORILLAS ,  Tomomine IIDA

IPC分类号： A61K35/76 ,  A61K9/16

摘要： The present invention relates to a bacteriophage composition comprising at least one bacteriophage species, at least one α-linked polymeric glucose and at least one polyol. In certain embodiments, the α-linked polymeric glucose has a mean molecular weight of greater than 10 kDa.

公开(公告)号：US07973163B2

公开(公告)日：2011-07-05

申请号：US12476619

申请日：2009-06-02

申请人： Masahiro Kajino ,  Yasuhiko Kawano

发明人： Masahiro Kajino ,  Yasuhiko Kawano

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/437

CPC分类号： C07D471/04

摘要： The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein R1 is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6 is (cyclic group optionally having substituent(s))-carbonyl, and the like; R7, R8, R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7 and R8, R8 and R9, and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; --- represents unsubstituted (i.e., absence) or a single bond; and represents a single bond or a double bond, or a salt thereof, and the like.

摘要翻译： 本发明旨在提供具有神经激肽2（NK2）受体拮抗作用的喹啉衍生物，其涉及式（I）表示的化合物，其中R1为氢原子等; R2是氢原子，任选具有取代基的烃基等; R3是未取代的（即不存在），氢原子等; R 4和R 5相同或不同，各自为氢原子，任选具有取代基的烃基等; R6是（任选具有取代基的环状基团） - 羰基等; R 7，R 8，R 9和R 10相同或不同，各自为氢原子，卤素等; 或R 7和R 8，R 8和R 9，并且R 9和R 10可与相邻碳原子一起形成环; n为1〜5的整数， ---表示未取代（即不存在）或单键; 并且表示单键或双键，或其盐等。

公开(公告)号：US07572574B2

公开(公告)日：2009-08-11

申请号：US10512588

申请日：2003-04-24

申请人： Takaomi Saido ,  Nobuhisa Iwata ,  Satoshi Tsubuki ,  Yoshie Takaki ,  Takashi Saito ,  Tadashi Nakaya

发明人： Takaomi Saido ,  Nobuhisa Iwata ,  Satoshi Tsubuki ,  Yoshie Takaki ,  Takashi Saito ,  Tadashi Nakaya

IPC分类号： C12Q1/00 ,  G01N33/53 ,  G01N33/567 ,  G01N33/542 ,  G01N33/537

CPC分类号： C12Q1/37 ,  G01N33/6896 ,  G01N2333/96486 ,  G01N2500/00

摘要： The present invention provides a method of measuring the activity of neprilysin, etc. More specifically, the present invention provides a method of measuring the activity of neprilysin in nerve cells; a method of screening a protein, a peptide or a compound enhancing the activity or expression of neprilysin nerve cells by measuring the activity of neprilysin; a method of enhancing the activity or expression of neprilysin; and so on. Thus, the compound enhancing the activity and/or expression of neprilysin, which is obtained by the screening method characterized by using the method of measuring the activity of neprilysin in accordance with the present invention, is useful as a preventive and/or therapeutic agent for Alzheimer's disease. The method of measuring the activity of the present invention can be used for presymptoms diagnosis of Alzheimer's disease.

摘要翻译： 本发明提供了测定尿丙氨酸等的活性的方法。更具体地，本发明提供了测定神经细胞中尿丙氨酸蛋白酶活性的方法。 通过测定尿丙氨酸的活性来筛选蛋白质，肽或增强neprilysin神经细胞活性或表达的化合物的方法; 增强头孢氨苄的活性或表达的方法; 等等。 因此，通过使用根据本发明的测定尿丙氨酸的活性的方法的筛选方法获得的增强头孢氨苄的活性和/或表达的化合物可用作预防和/或治疗剂 阿尔茨海默氏病。 测定本发明的活性的方法可用于阿尔茨海默病的症状诊断。

公开(公告)号：US20080161287A1

公开(公告)日：2008-07-03

申请号：US11978198

申请日：2007-10-25

申请人： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Lizawa

发明人： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Lizawa

IPC分类号： A61K31/55 ,  C07D401/02 ,  A61P31/18 ,  A61P19/02 ,  A61P9/00 ,  A01N1/02

CPC分类号： A61K31/4196 ,  A61K31/395 ,  A61K31/4178 ,  C07D225/06 ,  C07D313/20 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12

摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

摘要翻译： 本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。 本发明的化合物由下式表示：其中R 1为可被取代的5至6元环基团; X 1是键或类似物; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z 1是二价环状环基等; Z 2是键或类似物; R 2是氨基，可以被取代的含氮杂环基等，或其盐。

公开(公告)号：US07288654B2

公开(公告)日：2007-10-30

申请号：US10544435

申请日：2004-02-05

申请人： Mitsuru Shiraishi ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

发明人： Mitsuru Shiraishi ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

IPC分类号： C07D471/02

CPC分类号： A61K31/55 ,  C07D471/04

摘要： The present invention provides a compound represented by the formula: wherein R1 is a 5- or 6-membered ring which may be substituted; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W2-Z2b wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain which may be substituted; n is an integer of 0 to 4; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a hydrocarbon group, a heterocyclic group, or an acyl group); and R2 is (1) an amino group, in which the nitrogen atom is converted to quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as a ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, and the like, or a salt thereof. The compound has excellent CCR5 antagonist activity and is useful as a prophylactic and/or therapeutic medicine for HIV infection in human peripheral mononuclear blood cells, especially AIDS.

摘要翻译： 本发明提供由下式表示的化合物：其中R 1是可被取代的5或6元环; R 3是氢原子，低级烷基或低级烷氧基; Z 1是5或6元芳环; Z 2是由-Z 2 O 2 -W 2 -Z 2b表示的基团，其中Z 2a （O）m（其中m为0,1或2），亚氨基或键; O，S（O） 且W 2是可以被取代的亚烷基链; n为0〜4的整数。 Y是O，S（O）p（其中p是0,1或2），CH 2或NR 4（其中R' SUP> 4 是氢原子，烃基，杂环基或酰基）; 和R 2是（1）氮原子转化为季铵或氧化物的氨基，（2）可含有硫原子或氧原子的含氮杂环基 作为其中氮原子可以转化为季铵或氧化物的环构成原子等，或其盐。 该化合物具有优异的CCR5拮抗剂活性，可用作人外周血单核细胞尤其是艾滋病中HIV感染的预防和/或治疗药物。

公开(公告)号：US08373007B2

公开(公告)日：2013-02-12

申请号：US12934801

申请日：2009-03-27

申请人： Mitsuhisa Yamano ,  Yasuhiro Sawai ,  Masahiro Mizuno

发明人： Mitsuhisa Yamano ,  Yasuhiro Sawai ,  Masahiro Mizuno

IPC分类号： C07C251/00 ,  C07C211/62 ,  C07C211/63

CPC分类号： C07C251/30 ,  C07D215/38

摘要： Disclosed is a vinamidinium salt represented by the formula (I): [wherein R1 represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group or the like; R2 and R3 are the same or different and each represents a lower alkyl group, or alternatively R2 and R3 may combine together to form a ring; R4 and R5 are the same or different and each represents a lower alkyl group, or alternatively R4 and R5 may combine together to form a ring; X and Y are the same or different and each represents a bromine atom or a chlorine atom; n represents a number of not less than 2; and m represents 0 or n], and methods for synthesizing a heterocyclic ring compound using the salt.

摘要翻译： 公开了由式（I）表示的缬氨酸盐：其中R1表示氢原子，卤素原子，任选取代的烃基等; R2和R3相同或不同，各自表示低级烷基，或者R2和R3可以结合在一起形成环; R4和R5相同或不同，各自表示低级烷基，或者R4和R5可以结合在一起形成环; X和Y相同或不同，各自表示溴原子或氯原子; n表示不小于2的数; m表示0或n]，以及使用该盐合成杂环化合物的方法。

公开(公告)号：US20090298775A1

公开(公告)日：2009-12-03

申请号：US12491120

申请日：2009-06-24

申请人： Takaomi Saido ,  Nobuhisa Iwata ,  Satoshi Tsubuki ,  Yoshie Takaki ,  Takashi Saito ,  Tadashi Nakaya

发明人： Takaomi Saido ,  Nobuhisa Iwata ,  Satoshi Tsubuki ,  Yoshie Takaki ,  Takashi Saito ,  Tadashi Nakaya

IPC分类号： A61K38/31 ,  A61K38/10 ,  A61K38/12

CPC分类号： C12Q1/37 ,  G01N33/6896 ,  G01N2333/96486 ,  G01N2500/00

摘要： The present invention provides a method of measuring the activity of neprilysin, etc. More specifically, the present invention provides a method of measuring the activity of neprilysin in nerve cells; a method of screening a protein, a peptide or a compound enhancing the activity or expression of neprilysin in nerve cells by measuring the activity of neprilysin; a method of enhancing the activity or expression of neprilysin; and so on. Thus, the compound enhancing the activity and/or expression of neprilysin, which is obtained by the screening method characterized by using the method of measuring the activity of neprilysin in accordance with the present invention, is useful as a preventive and/or therapeutic agent for Alzheimer's disease. The method of measuring the activity of the present invention can be used for presymptomatic diagnosis of Alzheimer's disease.

摘要翻译： 本发明提供了测定尿丙氨酸等的活性的方法。更具体地，本发明提供了测定神经细胞中尿丙氨酸蛋白酶活性的方法。 通过测量尿丙氨酸的活性来筛选蛋白质，肽或增强神经细胞中neprilysin的活性或表达的化合物的方法; 增强头孢氨苄的活性或表达的方法; 等等。 因此，通过使用根据本发明的测定尿丙氨酸的活性的方法的筛选方法获得的增强头孢氨苄的活性和/或表达的化合物可用作预防和/或治疗剂 阿尔茨海默氏病。 测定本发明活性的方法可用于阿尔茨海默病的症状诊断。

公开(公告)号：US20090012081A1

公开(公告)日：2009-01-08

申请号：US12002273

申请日：2007-12-14

申请人： Shigenori Okawa ,  Masaomi Miyamoto ,  Masahiro Okura

发明人： Shigenori Okawa ,  Masaomi Miyamoto ,  Masahiro Okura

IPC分类号： A61K31/5377 ,  A61K31/343 ,  A61K31/438 ,  A61P25/00

CPC分类号： C07D307/79 ,  A61K31/343 ,  A61K31/36 ,  A61K31/381 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/438 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04 ,  C07D491/10

摘要： An agent for promoting the proliferation or differentiation of a stem cell and/or neural progenitor cell, comprising a compound represented by Formula: wherein each of R1 and R2 is H, a hydrocarbon group or a heterocyclic group, or taken together with the adjacent carbon atom to form a ring, R3 is H, a hydrocarbon group or a heterocyclic group, W is a group represented by Formula: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R4 is an acyl group having an aliphatic hydrocarbon group, which is substituted by an aromatic group and may have a further substitutent, or aromatic group, R5 is H, C1-6 alkyl or acyl, R4c is an aromatic group, an aliphatic hydrocarbon group or acyl, and X is O or S; Y is O, S or NH, Ring C is an optionally substituted benzene ring, or a salt or prodrug thereof is provided.

摘要翻译： 用于促进干细胞和/或神经祖细胞的增殖或分化的试剂，其包含由下式表示的化合物：其中R 1和R 2各自为H，烃基或杂环基，或与相邻碳一起 原子形成环，R 3为H，烃基或杂环基，W为由下式表示的基团：其中环A为任选取代的苯环，环B为任选取代的5-至7-元氮 - R4是具有脂肪族烃基的酰基，被芳基取代，可以具有其它的取代基或芳基，R5是H，C1-6烷基或酰基，R4c是芳基， 脂族烃基或酰基，X是O或S; Y是O，S或NH，环C是任选取代的苯环，或其盐或前药。

公开(公告)号：US20070232538A1

公开(公告)日：2007-10-04

申请号：US11647076

申请日：2006-12-27

申请人： Yoshio Matsumoto ,  Takuya Watanabe ,  Hideki Takahashi ,  Masaaki Mori

发明人： Yoshio Matsumoto ,  Takuya Watanabe ,  Hideki Takahashi ,  Masaaki Mori

IPC分类号： A61K48/00 ,  A61K38/17

CPC分类号： C07D223/16 ,  A61K31/4025 ,  A61K31/4375 ,  A61K31/4745 ,  A61K31/55 ,  A61K38/00 ,  A61K48/00 ,  C07D295/13 ,  C07D471/04 ,  C07K14/47

摘要： The present invention provides uses of a polypeptide having a ligand activity to a sensory epithelium neuropeptide-like receptor (SENR) which is a G protein-coupled receptor protein, and a DNA encoding the same. More specifically, the present invention provides an anti-attention-deficit-disorder or anti-narcolepsy agent, which comprises a polypeptide having a ligand activity for SENR or a salt thereof, as well as a method for screening compounds having an anti-attention-deficit-disorder or anti-narcolepsy activity or compounds having an anti-anxiety, anti-depression, anti-insomnia, anti-schizophrenia or anti-fear activity or salts thereof, which comprises using the above polypeptide or a precursor protein of the polypeptide or a salt thereof.

摘要翻译： 本发明提供了作为G蛋白偶联受体蛋白质的感觉上皮神经肽样受体（SENR）具有配体活性的多肽及其编码的DNA的用途。 更具体地，本发明提供了包含对SENR具有配体活性的多肽或其盐的抗注意力缺陷障碍或抗发作性睡病剂，以及用于筛选具有抗注意力缺陷型或抗发作性睡病的化合物的方法， 包括使用上述多肽或该多肽的前体蛋白，或者，具有抗焦虑，抗抑郁，抗失眠，抗精神分裂症或抗恐惧活性的化合物或抗发作性睡病活动， 其盐。

公开(公告)号：US20060258722A1

公开(公告)日：2006-11-16

申请号：US10558846

申请日：2004-05-28

申请人： Tsuneo Yasuma ,  Nobuyuki Negoro ,  Kohji Fukatsu

发明人： Tsuneo Yasuma ,  Nobuyuki Negoro ,  Kohji Fukatsu

IPC分类号： A61K31/428 ,  A61K31/381 ,  A61K31/353

CPC分类号： C07C69/734 ,  C07C59/64 ,  C07C59/68 ,  C07C59/72 ,  C07C2601/02 ,  C07C2602/10 ,  C07D277/42

摘要： The present invention aims at providing a novel fused ring compound having a GPR40 receptor function modulating action and being useful as an insulin secretagogue or a pharmaceutical agent for the prophylaxis or treatment of diabetes, more particularly, a compound represented by the formula: wherein Ar is an optionally substituted cyclic group, ring A is a ring optionally further substituted (provided that the ring is not thiazole, oxazole, imidazole and pyrazole), Xa and Xb are each independently a bond or a spacer having a main chain of 1 to 5 atom(s), Xc is O, S, SO or SO2, ring B is a 5- to 7-membered ring, Xd is a bond, CH or CH2, is a single bond when Xd is a bond or CH2, or a double bond when Xd is CH, and R1 is an optionally substituted hydroxy group, and a salt thereof.

摘要翻译： 本发明的目的在于提供一种具有GPR40受体功能调节作用的新型稠环化合物，可用作胰岛素促分泌素或用于预防或治疗糖尿病的药剂，更具体地，由下式表示的化合物：其中Ar为 任选取代的环状基团，环A为任选进一步取代的环（条件是该环不是噻唑，恶唑，咪唑和吡唑），Xa和Xb各自独立地为键或具有1至5个主链的间隔基 X是O，S，SO或SO 2，环B是5-至7-元环，Xd是键，CH或CH 2， ，是单键，或当Xd为CH时为双键，R 1为任选取代的 羟基及其盐。