公开(公告)号：US08232282B2

公开(公告)日：2012-07-31

申请号：US12311335

申请日：2007-09-28

申请人： Keiji Nakamura ,  Hiroyuki Nakagawa ,  Yoko Kan

发明人： Keiji Nakamura ,  Hiroyuki Nakagawa ,  Yoko Kan

IPC分类号： A01N43/00

CPC分类号： C07D471/04

摘要： The present invention relates to a bicyclic pyrimidine compound of the following formula (I) or a salt thereof. wherein R1 is lower alkyl, cyclic lower alkyl. etc.; R2 is H, lower alkyl, lower alkenyl, etc.; R3 is H, lower alkyl, lower alkenyl, etc.; X is O, S or —N(R4)—; R4 is H or lower alkyl; or R2 and R4 may combine each other to form cyclic amino; Y is amido, keto, sulfonyl, etc.; R5 is H or lower alkyl; Z is O or S; m and n are 1 or 2. Said compound (I) or a salt thereof have MGAT inhibitory activity, and are useful as an agent for treatment or prophylaxis of adiposity, metabolic syndromes, hyperlipidemia, hyper neutral lipemia, hyper VLDL-mia, hyper fatty acidemia, diabetes mellitus, arteriosclerosis.

摘要翻译： 本发明涉及下式（I）的双环嘧啶化合物或其盐。 其中R1是低级烷基，环状低级烷基。 等等。; R2是H，低级烷基，低级烯基等; R3是H，低级烷基，低级烯基等; X是O，S或-N（R 4） - ; R4是H或低级烷基; 或者R 2和R 4可以相互结合形成环状氨基; Y是酰胺基，酮基，磺酰基等; R5是H或低级烷基; Z是O或S; m和n为1或2.所述化合物（I）或其盐具有MGAT抑制活性，可用作治疗或预防肥胖，代谢综合征，高脂血症，高中性脂肪血症，超VLDL-mia，hyper 脂肪酸血症，糖尿病，动脉硬化。

公开(公告)号：US20120178911A1

公开(公告)日：2012-07-12

申请号：US13423734

申请日：2012-03-19

申请人： Shinya YAMANAKA ,  Eiko KAIHO

发明人： Shinya YAMANAKA ,  Eiko KAIHO

IPC分类号： C07K16/18

CPC分类号： C12Q1/6881 ,  C12N5/0606 ,  C12Q2600/158

摘要： The invention provides an antibody that specifically binds to (a) a protein having an amino acid sequence depicted in SEQ ID NO:16 or 32 or (b) a protein which has an amino acid sequence of (a), wherein one to several amino acids are deleted, substituted, or added, and which is specifically expressed in an ES cell.

摘要翻译： 本发明提供了特异性结合（a）具有SEQ ID NO：16或32所示氨基酸序列的蛋白质的抗体或（b）具有氨基酸序列（a）的蛋白质，其中一至几个氨基 酸被删除，取代或添加，并且其在ES细胞中特异性表达。

公开(公告)号：US20120178743A1

公开(公告)日：2012-07-12

申请号：US13402850

申请日：2012-02-22

申请人： Yoshiaki ISOBE ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

发明人： Yoshiaki ISOBE ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

IPC分类号： A61K31/52 ,  A61K31/5377 ,  A61P37/08 ,  A61P37/00 ,  A61P31/12 ,  A61P17/00 ,  C07D473/18 ,  A61K31/55

CPC分类号： A61K31/5377 ,  A61K31/522 ,  A61K31/55

摘要： An antiallergic agent for topical administration containing an adenine compound of general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

摘要翻译： 一种用于局部给药的抗过敏剂，其含有通式（1）的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳烃或5至10元单或双环芳族杂环， 选自0至2个氮原子，0或1个氧原子和0或1个硫原子的3个杂原子; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。

公开(公告)号：US20120172347A1

公开(公告)日：2012-07-05

申请号：US13395429

申请日：2010-09-08

申请人： Keiji Aachi ,  Yoko Nakai ,  Tomoyuki Furuta ,  Yuki Fujii

发明人： Keiji Aachi ,  Yoko Nakai ,  Tomoyuki Furuta ,  Yuki Fujii

IPC分类号： A61K31/522 ,  A61K31/55 ,  A61K31/5377 ,  A61P25/22 ,  A61P29/00 ,  C07D473/00 ,  A61P25/24

CPC分类号： A61K31/52 ,  A61K31/5377 ,  A61K31/55 ,  C07D473/00

摘要： The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like.

摘要翻译： 本发明提供由式（1）表示的化合物或其药学上可接受的盐（其中W表示氢原子，卤素原子等），A表示任选被芳基取代的烷基等， 芳基或其它基团; X和Y之一表示二取代的烷基氨基羰基等，另一个表示氢原子，烷基，烷基羰基等）。 用于治疗或预防FAAH相关疾病如抑郁症，焦虑症或疼痛的药物或药物组合物，其包含化合物等作为活性成分; 化合物等的用途; 以及使用该化合物等进行治疗或预防的方法。

公开(公告)号：US08148379B2

公开(公告)日：2012-04-03

申请号：US12140927

申请日：2008-06-17

申请人： Yukihiro Ohno ,  Takeo Ishiyama

发明人： Yukihiro Ohno ,  Takeo Ishiyama

IPC分类号： A61K31/497

CPC分类号： C07D417/12

摘要： A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: wherein Z is a group of the formula [2]: D is a group of —(CH2)p-A-(CH2)q—; G is ═N—, —CH—, etc.; and Ar is an aromatic heterocyclic group, etc.

摘要翻译： 一种用于认知功能障碍的治疗/预防剂，其包含作为活性成分的下式[1]的酰亚胺衍生物：其中Z是式[2]的基团：D是 - （CH 2）p -A（ CH2）q-; G是= N - ， - CH-等; Ar为芳香族杂环基等。

公开(公告)号：US20110263550A1

公开(公告)日：2011-10-27

申请号：US13084503

申请日：2011-04-11

申请人： Toshinari Sugasawa ,  Takashi Nakajima ,  Hitoshi Fujita ,  Toshio Kanai

发明人： Toshinari Sugasawa ,  Takashi Nakajima ,  Hitoshi Fujita ,  Toshio Kanai

IPC分类号： A61K31/56 ,  A61P11/00 ,  A61K31/5377

CPC分类号： A61K31/56 ,  A61K9/10 ,  A61K31/5377 ,  C07D277/42

摘要： Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.

摘要翻译： 本发明公开了一种预防和/或治疗慢性阻塞性肺疾病的方法，该方法是通过给予由下式表示的5元环状化合物：或化合物的药学上可接受的盐或其化合物或盐的前体药物：其中X 表示氧或硫原子; R1表示氢原子，取代或未取代的烷基等; R 2表示氢原子，取代或未取代的烷基等; Y1表示单键，取代或未取代的亚烷基等; 波浪线表示（E）或（Z）配位; R3表示氢原子，取代或未取代的芳基等; Y2表示取代或未取代的亚烷基或亚烯基; R4表示氢原子，取代或未取代的烷酰基等; 并且R 5表示氢原子或取代或未取代的烷基。

公开(公告)号：US20110262566A1

公开(公告)日：2011-10-27

申请号：US13127362

申请日：2009-11-02

申请人： Natsuko Goto ,  Setsuko Yamamoto

发明人： Natsuko Goto ,  Setsuko Yamamoto

IPC分类号： A61K31/517 ,  A61P13/02 ,  A61P13/00 ,  A61P13/10 ,  A61K31/56 ,  A61K31/495

CPC分类号： A61K31/517 ,  A61K45/06 ,  C07D401/04 ,  A61K2300/00

摘要： Provided is a therapeutic agent for lower urinary tract symptom consisting of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof or a combination of (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof and a compound selected from the group consisting of α1-adrenergic receptor blockers, 5-α reductase inhibitors, antiandrogen drugs, β3-adrenergic receptor agonists, phosphodiesterase V inhibitors, plant preparations, amino acid preparations, herbal medicines and the like. Also provided is a method of using in combination the above-described therapeutic agent and a surgical treatment such as bladder distention or surgery.

摘要翻译： 本发明提供由（+） - 3- {1- [3-（三氟甲氧基）苄基]哌啶-4-基} -4-苯基-3,4-二氢-2（1H） - - 喹唑啉酮或其药学上可接受的盐或（+） - 3- {1- [3-（三氟甲氧基）苄基]哌啶-4-基} -4-苯基-3,4-二氢-2（1H） 喹唑啉酮或其药学上可接受的盐和选自α1-肾上腺素能受体阻断剂，5-α还原酶抑制剂，抗雄激素药物，β-肾上腺素能受体激动剂，磷酸二酯酶V抑制剂，植物制剂，氨基酸制剂 ，草药等。 还提供了组合使用上述治疗剂和手术治疗如膀胱膨胀或手术的方法。

公开(公告)号：US20110217366A1

公开(公告)日：2011-09-08

申请号：US13109949

申请日：2011-05-17

申请人： Keiji FUJIOKA ,  Akihiko Sano ,  Shunji Nagahara ,  Malcolm Roy Brandon ,  Andrew Donald Nash ,  Shari Lofthouse

发明人： Keiji FUJIOKA ,  Akihiko Sano ,  Shunji Nagahara ,  Malcolm Roy Brandon ,  Andrew Donald Nash ,  Shari Lofthouse

IPC分类号： A61K39/12 ,  A61K39/00 ,  A61K39/02 ,  A61K39/002 ,  A61K9/00 ,  A61K9/127 ,  C07K16/00 ,  A61P31/12 ,  A61P31/04 ,  A61P31/00 ,  A61P33/00 ,  A61P37/04

CPC分类号： A61K39/39 ,  A61K9/0024 ,  A61K9/0092 ,  A61K9/70 ,  A61K47/42

摘要： The present invention provides an immunopotentiating composition which comprises an antigen or antigen-inducing substance, and a carrier comprising a biocompatible material for effectively increasing an immune response derived from an antigen. The present invention further provides a method of producing an antibody by administering said immunopotentiating composition to a mammal or bird, thereby modulating the immune response in said mammal or bird and recovering the antibody produced.

摘要翻译： 本发明提供一种免疫增强组合物，其包含抗原或抗原诱导物质，和包含生物相容性物质的载体，用于有效增加源自抗原的免疫应答。 本发明进一步提供了通过向哺乳动物或鸟施用所述免疫增强组合物从而调节所述哺乳动物或鸟类中的免疫应答并回收产生的抗体来产生抗体的方法。

公开(公告)号：US20110200629A1

公开(公告)日：2011-08-18

申请号：US13125044

申请日：2009-10-19

申请人： Noriyuki Sato ,  Tomohide Tsukahara ,  Satoshi Kawaguchi ,  Takuro Wada

发明人： Noriyuki Sato ,  Tomohide Tsukahara ,  Satoshi Kawaguchi ,  Takuro Wada

IPC分类号： A61K39/00 ,  C12N15/63 ,  C12N5/0783 ,  C07K7/06 ,  G01N33/574 ,  C07H21/00 ,  C12N5/10 ,  C07K16/44 ,  C12Q1/02 ,  C12Q1/68 ,  A61P37/04 ,  A61P35/00

CPC分类号： C07K14/4748 ,  A61K39/00 ,  A61K39/0011 ,  G01N33/57407 ,  G01N33/57438 ,  G01N33/57484 ,  G01N2333/70539

摘要： Disclosed is a peptide consisting of the identical amino acid sequence or a substantially identical amino acid sequence to the amino acid sequence depicted in SEQ ID NO:4, wherein the peptide binds to an HLA antigen and is recognized by cytotoxic T cells. The peptide of the present invention can be used in vivo or in vitro as an agent for inducing CTL, that is, cancer vaccine, and exerts therapeutic or ameliorating effects on tumors such as osteosarcoma, renal cancer, and others. The peptide of the present invention is also useful as a tumor marker directed to tumors such as sarcoma, renal cancer, and others.

摘要翻译： 公开了由与SEQ ID NO：4所示的氨基酸序列相同的氨基酸序列或基本相同的氨基酸序列组成的肽，其中所述肽结合HLA抗原并被细胞毒性T细胞识别。 本发明的肽可以在体内或体外用作诱导CTL的药剂，即癌症疫苗，对骨肉瘤，肾癌等肿瘤发挥治疗或改善作用。 本发明的肽也可用作针对诸如肉瘤，肾癌等肿瘤的肿瘤标志物。

公开(公告)号：US20110166469A1

公开(公告)日：2011-07-07

申请号：US13048337

申请日：2011-03-15

申请人： Shinya Nagata ,  Ryuji Nagai ,  Kenji Kouchi

发明人： Shinya Nagata ,  Ryuji Nagai ,  Kenji Kouchi

IPC分类号： A61B5/0402

CPC分类号： G06T11/206 ,  A61B5/0432 ,  A61B5/044 ,  A61B5/742 ,  G06T11/203 ,  G09G5/20 ,  G09G5/24

摘要： An electrocardiogram (ECG) chart device and method capable of easily assisting with the diagnosis of heart disease. Hexagonal radar charts displayed on a screen act as indicators of feature values corresponding to data obtained from each of 12 electrode leads and correlated with the related portions of the heart. For example, a (V1, V2) lead is an indicator of a right ventricle. Each of the radar charts is schematically arranged to correspond with the related portion of the heart. Each vertex of the hexagonal radar charts acts as an indicator of the recognized value. More specifically, each vertex of the radar chart is based on a value obtained by extracting a waveform critical point, a waveform start point, a waveform end point, or the like, of constituent elements of the ECG waveform as the P wave, the Q wave, the R wave, the S wave, the ST segment, the T wave, or the like. Therefore, a user of the ECG radar chart device can intuitively and easily carry out interpretation of ECG data.

摘要翻译： 一种心电图（ECG）图表装置和方法，能够容易地协助诊断心脏病。 显示在屏幕上的六角形雷达图用作与从12个电极引线中的每一个获得的数据对应的特征值的指标，并与心脏的相关部分相关联。 例如，（V1，V2）引线是右心室的指标。 每个雷达图表被示意性地布置成与心脏的相关部分相对应。 六角形雷达图的每个顶点都作为识别值的指标。 更具体地，雷达图的每个顶点基于通过提取作为P波的ECG波形的组成元素的波形临界点，波形起始点，波形终点等获得的值，Q 波，R波，S波，ST段，T波等。 因此，ECG雷达图表设备的用户可以直观，轻松地对ECG数据进行解释。