公开(公告)号：US5418231A

公开(公告)日：1995-05-23

申请号：US78315

申请日：1993-06-28

申请人： Kaoru Shimada ,  Yuji Shishido

发明人： Kaoru Shimada ,  Yuji Shishido

IPC分类号： C07D513/04 ,  A61K31/54

CPC分类号： C07D513/04

摘要： This invention relates to novel pyrimido-benzothiazine derivative compounds. ##STR1## The compounds of the present invention inhibit the action of the lipoxygenase enzyme and are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals. This invention also relates to pharmaceutical compositions comprising such compounds.

摘要翻译： PCT No.PCT / US91 / 09161 Sec。 371日期：1993年6月28日 102（e）日期1993年6月28日PCT 1991年12月16日PCT公布。 公开号WO92 / 12161 本发明涉及新颖的嘧啶 - 苯并噻嗪衍生物化合物。 本发明化合物抑制脂氧合酶的作用，可用于治疗或减轻哺乳动物炎症性疾病，变态反应和心血管疾病。 本发明还涉及包含这些化合物的药物组合物。

公开(公告)号：US4668799A

公开(公告)日：1987-05-26

申请号：US739182

申请日：1985-05-30

申请人： Junji Yoshizawa ,  Yoshimi Tsuchiya ,  Yukio Hirayama ,  Kaoru Shimada ,  Nobuyuki Mino ,  Kyoko Nakamichi ,  Ikuo Matsumoto

发明人： Junji Yoshizawa ,  Yoshimi Tsuchiya ,  Yukio Hirayama ,  Kaoru Shimada ,  Nobuyuki Mino ,  Kyoko Nakamichi ,  Ikuo Matsumoto

IPC分类号： A61K31/381 ,  A61K31/385 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/495 ,  A61P1/16 ,  C07D333/00 ,  C07D339/00 ,  C07D339/06 ,  C07D409/06 ,  C07D401/02 ,  C07D403/04 ,  C07D409/04

CPC分类号： C07D409/06 ,  C07D339/06

摘要： A 1,3-dithiol-2-ylidene derivative of the formula: ##STR1## wherein each of R and R.sup.1 which may be the same or different, is a lower alkyl group, a lower alkenyl group, a cycloalkyl group, a lower alkoxyalkyl group, or a substituted or unsubstituted aryl, aralkyl or heterocyclic group, or R and R.sup.1 together form a substituted or unsubstituted ethylene or trimethylene group.

摘要翻译： 下式的1,3-二硫醇-2-亚基衍生物：其中R和R 1可以相同或不同的是低级烷基，低级烯基，环烷基， 低级烷氧基烷基或取代或未取代的芳基，芳烷基或杂环基，或R和R 1一起形成取代或未取代的亚乙基或三亚甲基。

公开(公告)号：US10975070B2

公开(公告)日：2021-04-13

申请号：US13580479

申请日：2011-02-28

申请人： Kaoru Shimada ,  Masaki Sudo ,  Masaomi Tajimi ,  Nobuyuki Takahashi ,  Kazuhiko Nonomura

发明人： Kaoru Shimada ,  Masaki Sudo ,  Masaomi Tajimi ,  Nobuyuki Takahashi ,  Kazuhiko Nonomura

IPC分类号： A61K31/44 ,  C07D471/04 ,  A61K31/437 ,  A61K45/06

摘要： The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease.

公开(公告)号：US20120322821A1

公开(公告)日：2012-12-20

申请号：US13580479

申请日：2011-02-28

申请人： Kaoru Shimada ,  Masaki Sudo ,  Masaomi Tajimi ,  Nobuyuki Takahashi ,  Kazuhiko Nonomura

发明人： Kaoru Shimada ,  Masaki Sudo ,  Masaomi Tajimi ,  Nobuyuki Takahashi ,  Kazuhiko Nonomura

IPC分类号： A61K31/437 ,  A61P3/00 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K45/06

摘要： The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease.

摘要翻译： 本发明涉及本发明化合物或其药学上可接受的盐或包含该化合物或其盐的药物组合物在制备用于治疗恶病质的药物中的用途。 本发明还涉及治疗恶病质的方法，其包括向人或动物施用本发明化合物或其包含该化合物的药物组合物。 本发明还涉及所述化合物或其药学上可接受的盐或包含该化合物或盐的药物组合物与一种或多种第二活性剂的组合的用途。 此外，本发明涉及药物组合物和包含本发明化合物或其药学上可接受的盐的试剂盒，用于治疗所述疾病。

公开(公告)号：US20120101105A1

公开(公告)日：2012-04-26

申请号：US13375117

申请日：2010-05-31

申请人： Tadashi Inoue ,  Shuzo Watanabe ,  Tatsuya Yamagishi ,  Yoshimasa Arano ,  Mikio Morita ,  Kaoru Shimada

发明人： Tadashi Inoue ,  Shuzo Watanabe ,  Tatsuya Yamagishi ,  Yoshimasa Arano ,  Mikio Morita ,  Kaoru Shimada

IPC分类号： A61K31/498 ,  C07D401/12 ,  C07D213/65 ,  C07D241/18 ,  A61K31/497 ,  A61K31/444 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/4439 ,  A61P29/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/00 ,  A61P1/00 ,  A61P35/00 ,  A61P25/28 ,  A61P25/02 ,  A61P25/24 ,  A61P25/08 ,  A61P25/06 ,  A61P5/00 ,  A61P19/00 ,  A61P25/22 ,  C07D413/12 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61P25/14 ,  A61P25/20 ,  A61P19/02 ,  A61P9/06 ,  A61P1/18 ,  C07D403/12

CPC分类号： A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  C07D213/65 ,  C07D215/40 ,  C07D241/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

摘要翻译： 本发明涉及式（I）的芳基取代的甲酰胺衍生物或其药学上可接受的盐，其具有T型钙通道或电压门控钠通道的阻断活性，作为河豚毒素敏感型（TTX-S）阻断剂如Nav1 3和Nav1.7，其可用于治疗或预防其中涉及T型钙通道或电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道或电压门控钠通道的疾病中的用途。

公开(公告)号：US20080069867A1

公开(公告)日：2008-03-20

申请号：US11575406

申请日：2005-08-19

申请人： Kaoru Shimada ,  Yasuhiro Matsumura ,  Toshiaki Tagawa

发明人： Kaoru Shimada ,  Yasuhiro Matsumura ,  Toshiaki Tagawa

IPC分类号： A61K9/127 ,  A61K39/395 ,  A61P37/00

CPC分类号： A61K49/0045 ,  A61K47/6869 ,  A61K47/6913 ,  C07K16/3069 ,  C07K2317/56 ,  C07K2317/565

摘要： It was found that an antibody containing the amino acid sequences described in the sequence listing as SEQ ID NOS: 1 to 6 was an antibody having reactivity also to ovarian cancer, as well as the cancer species known so far such as gastric cancer, colon cancer and breast cancer, and was useful as an ovarian cancer tissue-specific diagnostic and/or therapeutic agent.

摘要翻译： 发现含有SEQ ID NO：1至6的序列表中所述的氨基酸序列的抗体是具有对卵巢癌的反应性的抗体，以及迄今已知的癌症，例如胃癌，结肠癌 和乳腺癌，并且可用作卵巢癌组织特异性诊断和/或治疗剂。

公开(公告)号：US06222038B1

公开(公告)日：2001-04-24

申请号：US08377552

申请日：1995-01-24

申请人： Fumitaka Ito ,  Hiroshi Kondo ,  Masami Nakane ,  John Adams Lowe, III ,  Terry Jay Rosen ,  Kaoru Shimada

发明人： Fumitaka Ito ,  Hiroshi Kondo ,  Masami Nakane ,  John Adams Lowe, III ,  Terry Jay Rosen ,  Kaoru Shimada

IPC分类号： C07D45302

CPC分类号： C07D453/02

摘要： Compounds of the formula wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

摘要翻译： 甲酰基赖氨酸R1的化合物是甲氧基，R2选自甲基，乙基，异丙基，仲丁基和叔丁基; 和这些化合物的药学上可接受的盐。这些化合物是物质P拮抗剂，可用于治疗胃肠疾病，炎性疾病，中枢神经系统疾病和疼痛。

公开(公告)号：US5086062A

公开(公告)日：1992-02-04

申请号：US529971

申请日：1990-05-29

申请人： Kazuo Ando ,  Nobuko Asai ,  Fumitaka Ito ,  Takashi Mano ,  Masami Nakane ,  Kunio Satake ,  Kaoru Shimada

发明人： Kazuo Ando ,  Nobuko Asai ,  Fumitaka Ito ,  Takashi Mano ,  Masami Nakane ,  Kunio Satake ,  Kaoru Shimada

IPC分类号： C12N9/99 ,  A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/435 ,  A61K31/445 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D263/58 ,  C07D407/02 ,  C07D409/12 ,  C07D413/12 ,  C07D493/08

CPC分类号： C07D263/58 ,  C07D413/12 ,  C07D493/08 ,  Y02P20/55

摘要： This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.

公开(公告)号：US4655951A

公开(公告)日：1987-04-07

申请号：US837033

申请日：1986-03-06

申请人： Masayuki Hanazaki ,  Noriyuki Harada ,  Kaoru Shimada

发明人： Masayuki Hanazaki ,  Noriyuki Harada ,  Kaoru Shimada

IPC分类号： C09K5/00 ,  C09K5/08 ,  C09K5/06

CPC分类号： C09K5/08

摘要： A coolant, comprising an aqueous solution of potassium hydrogencarbonate, a polyhydric alcohol and, where desired, 1.0 to 20.0% by weight of saccharides, which may be additionally incorporated, for the purpose of protection against corrosion, with 0.01 to 0.5% by weight of at least one compound selected from the group consisting of alkali metal salts of silicic acid, alkali metal salts of metasilicic acid and alkali metal salts of polyphosphoric acid.The coolant has an eutectic melting point as low as -8.5.degree. C. or below and is less corrosive to metal containers. In addition, the potassium hydrogencarbonate in the coolant is quite stable, so that the bubbling phenomenon of the coolant could be prevented.

摘要翻译： 一种冷却剂，其包含碳酸氢钾的水溶液，多元醇，并且在需要时，为了防腐蚀的目的可以另外加入1.0至20.0重量％的糖，以0.01至0.5重量％ 至少一种选自硅酸的碱金属盐，偏硅酸的碱金属盐和多磷酸的碱金属盐的化合物。 冷却液的共晶熔点低至-8.5℃或更低，对金属容器的腐蚀性较差。 此外，冷却剂中的碳酸氢钾相当稳定，从而可以防止冷却剂的起泡现象。

公开(公告)号：US09101616B2

公开(公告)日：2015-08-11

申请号：US13375117

申请日：2010-05-31

申请人： Tadashi Inoue ,  Shuzo Watanabe ,  Tatsuya Yamagishi ,  Yoshimasa Arano ,  Mikio Morita ,  Kaoru Shimada

发明人： Tadashi Inoue ,  Shuzo Watanabe ,  Tatsuya Yamagishi ,  Yoshimasa Arano ,  Mikio Morita ,  Kaoru Shimada

IPC分类号： A61K31/498 ,  C07D401/12 ,  C07D213/65 ,  C07D241/18 ,  A61K31/497 ,  A61K31/444 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/4439 ,  A61K31/4709 ,  C07D413/12 ,  A61K31/4725 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4706 ,  A61K31/506 ,  C07D215/40 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  C07D213/65 ,  C07D215/40 ,  C07D241/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

摘要翻译： 本发明涉及式（I）的芳基取代的甲酰胺衍生物或其药学上可接受的盐，其具有作为河豚毒素敏感型（TTX-S）阻滞剂如NaV1的T型钙通道或电压门控钠通道的阻断活性 3和NaV1.7，其可用于治疗或预防其中涉及T型钙通道或电压门控钠通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道或电压门控钠通道的疾病中的用途。