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1. 发明授权

US06787543B2 Benzhydryl derivatives 失效
标题翻译：二苯甲基衍生物
公开(公告)号：US06787543B2
公开(公告)日：2004-09-07
申请号：US10297937
申请日：2002-12-20
申请人： Kazuhiko Take , Chiyoshi Kasahara , Shinji Shigenaga , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Masataka Morita
发明人： Kazuhiko Take , Chiyoshi Kasahara , Shinji Shigenaga , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Masataka Morita
IPC分类号： A61K31495
CPC分类号： C07D265/30 , C07C45/71 , C07D241/04 , C07D241/08 , C07D403/10 , C07D487/04 , C07C47/575
摘要： A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.
摘要翻译：式（I）的化合物：其中Z，R 1，R 2，R 8，R 10，R 11，R 12，R 13和R 13， 14>各自如说明书中所定义，或其盐。本发明的目的化合物具有速激肽拮抗作用等药理活性，可用于制备治疗或预防速激肽介导的疾病的药物。

2. 发明授权

US07166598B2 Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US07166598B2
公开(公告)日：2007-01-23
申请号：US10968473
申请日：2004-10-20
申请人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
发明人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
IPC分类号： A61K31/5355 , C07D413/06 , A61K31/496 , C07D401/06
CPC分类号： C07D401/06 , C07D241/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/08 , C07D495/04 , C07D498/04 , C07D498/08 , C07F7/1804
摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
摘要翻译：本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途速激肽介导的人类或动物疾病。

3. 发明申请

US20070123532A1 PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：US20070123532A1
公开(公告)日：2007-05-31
申请号：US11562149
申请日：2006-11-21
申请人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
发明人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
IPC分类号： A61K31/5377 , A61K31/496
CPC分类号： C07D401/06 , C07D241/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/08 , C07D495/04 , C07D498/04 , C07D498/08 , C07F7/1804
摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
摘要翻译：本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途速激肽介导的人类或动物疾病。

4. 发明申请

US20060014948A1 Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US20060014948A1
公开(公告)日：2006-01-19
申请号：US10968473
申请日：2004-10-20
申请人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
发明人： Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
IPC分类号： A61K31/5377 , C07D413/02 , C07D43/02
CPC分类号： C07D401/06 , C07D241/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/08 , C07D495/04 , C07D498/04 , C07D498/08 , C07F7/1804
摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
摘要翻译：本发明涉及下式的哌嗪衍生物：其中每个符号如说明书中所定义，及其药学上可接受的盐，其制备方法，包含其的药物组合物及其用于治疗或预防的用途速激肽介导的人类或动物疾病。

5. 发明申请

US20100168159A1 HETERO COMPOUND 有权
标题翻译： HETERO化合物
公开(公告)号：US20100168159A1
公开(公告)日：2010-07-01
申请号：US12696327
申请日：2010-01-29
申请人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Masataka Morita , Sunao Imada , Yoshito Abe , Hiromichi Itani , Tatsuaki Morokata , Hideo Tsutsumi
发明人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Masataka Morita , Sunao Imada , Yoshito Abe , Hiromichi Itani , Tatsuaki Morokata , Hideo Tsutsumi
IPC分类号： A61K31/4439 , A61K31/4709 , C07D471/04 , C07D413/14 , A61P35/02 , A61P37/06 , A61P29/00 , A61P9/10 , A61P35/00
CPC分类号： C07D413/04 , C07D417/04 , C07D471/04
摘要： [Problems]To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.[Means for solving]Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.
摘要翻译： [问题]提供一种有用的化合物作为活性成分，用于预防和/或治疗移植器官，骨髓或组织，自身免疫疾病等中的排斥反应，其具有优异的S1P1激动剂活动。 [解决方法]由于本发明的化合物具有S1P1激动剂活性，因此可用作由不利的淋巴细胞浸润引起的疾病的治疗或预防剂的活性成分，例如自身免疫性疾病如移植排斥反应器官移植，骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化，系统性红斑狼疮，肾病综合征，脑炎，重症肌无力，胰腺炎，肝炎，肾炎，糖尿病，肺功能障碍哮喘，特应性皮炎，炎症性肠病，动脉粥样硬化，局部缺血再灌注损伤，炎症性疾病等疾病，以及癌症，白血病等细胞异常生长或积累引起的疾病。

6. 发明申请

US20070043084A1 1,2-Diarylimidazoles useful as inhibitors of cox 审中-公开
标题翻译：可用作cox的抑制剂的1,2-二芳基咪唑
公开(公告)号：US20070043084A1
公开(公告)日：2007-02-22
申请号：US10555656
申请日：2004-04-26
申请人： Fumie Takahashi , Tadashi Terasaka , Masataka Morita , Nobukiyo Konishi , Katsuya Nakamura
发明人： Fumie Takahashi , Tadashi Terasaka , Masataka Morita , Nobukiyo Konishi , Katsuya Nakamura
IPC分类号： A61K31/444 , A61K31/4439 , C07D403/04
CPC分类号： C07D401/12 , C07D233/90 , C07D417/12
摘要： A compound of the formula (1): wherein R1 is cyano, and the like; R2 is hydroxy, and the like; R3 is (lower)alkoxy, and the like; X and Y are each CH or N; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
摘要翻译：式（1）的化合物：其中R 1是氰基等; R 2是羟基等; R 3是（低级）烷氧基等; X和Y各自为CH或N; 或其药学上可接受的盐，其可用作药物。

7. 发明申请

US20060276521A1 Thiazole derivatives 失效
公开(公告)号：US20060276521A1
公开(公告)日：2006-12-07
申请号：US11505321
申请日：2006-08-17
申请人： Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
发明人： Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
IPC分类号： A61K31/427 , A61K31/426 , C07D417/02
CPC分类号： C07D417/06 , C07D277/46 , C07D277/48 , C07D277/56 , C07D417/12
摘要： A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.

8. 发明申请

US20060128770A1 Thiazole derivatives 审中-公开
标题翻译：噻唑衍生物
公开(公告)号：US20060128770A1
公开(公告)日：2006-06-15
申请号：US11345492
申请日：2006-02-02
申请人： Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
发明人： Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
IPC分类号： A61K31/427 , A61K31/426 , C07D417/02
CPC分类号： C07D417/06 , C07D277/46 , C07D277/48 , C07D277/56 , C07D417/12
摘要： A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.
摘要翻译：式（I）化合物：其中各符号如说明书中所定义，或其药学上可接受的盐可用作血管粘附蛋白-1（1R） VAP-1）抑制剂，药物组合物，预防或治疗VAP-1相关疾病，尤其是黄斑水肿的方法，该方法包括将有效量的化合物或其药学上可接受的盐给予哺乳动物等。

9. 发明申请

US20080212085A1 METHOD OF EVALUATING NON-LINEAR OPTICAL CRYSTAL AND DEVICE THEREFOR, AND WAVELENGTH CONVERSION METHOD AND DEVICE THEREFOR 审中-公开
标题翻译：评估非线性光学晶体及其器件的方法和波长转换方法及其器件
公开(公告)号：US20080212085A1
公开(公告)日：2008-09-04
申请号：US12111046
申请日：2008-04-28
申请人： Satoshi WADA , Hideo Tashiro , Masataka Morita
发明人： Satoshi WADA , Hideo Tashiro , Masataka Morita
IPC分类号： G01N21/00
CPC分类号： G01N21/636 , G01M11/00 , G02F1/3501 , G02F1/37
摘要： A method of evaluating a non-linear optical crystal used for non-linear wavelength conversion of laser beam which enables the non-linear optical crystal to be evaluated before the crystal is actually used as a wavelength conversion element in order for the crystal to be constantly used for an extended time with a high conversion efficiency retained and without lowering in output when non-linear optical crystals for various non-linear wavelength conversions such as a CLBO crystal are used to convert laser beams, wherein the non-linear optical crystal is moved to changed a laser beam incident position to detect the output of a laser beam emitted from the non-linear optical crystal for each changing position.
摘要翻译：一种评估用于激光束的非线性波长转换的非线性光学晶体的方法，其使得在晶体实际用作波长转换元件之前能够评估非线性光学晶体以使晶体恒定用于延长的时间，保持高的转换效率，并且当用于各种非线性波长转换的非线性光学晶体（例如CLBO晶体）用于转换激光束时，输出不降低，其中非线性光学晶体被移动以改变激光束入射位置，以检测对于每个改变位置从非线性光学晶体发射的激光束的输出。

10. 发明申请

US20080015202A1 Thiazole Derivatives Having Vap-1 Inhibitory Activity 审中-公开
标题翻译：具有Vap-1抑制活性的噻唑衍生物
公开(公告)号：US20080015202A1
公开(公告)日：2008-01-17
申请号：US11574946
申请日：2005-09-08
申请人： Takayuki Inoue , Takashi Tojo , Masataka Morita
发明人： Takayuki Inoue , Takashi Tojo , Masataka Morita
IPC分类号： A61K31/426 , A61K31/445 , A61K31/497 , A61P27/02 , C07D411/00
CPC分类号： C07D417/10 , C07D277/46 , C07D417/06 , C07D417/12
摘要： A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is —CONH— or —NR1CO— wherein R1 is a hydrogen or lower alkyl; W is a bond or lower alkylene; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond or lower alkylene; and Z is a group of the formula: wherein R2 is a group of the formula: -A-B-D-E-F-G wherein A is a bond or lower alkylene; B is a bond, —NH— or D is a bond, —CS— or —CO—; E is a bond or —NH—; F is a bond, —CO—, —O— or —SO2—; and G is lower alkyl, optionally protected amino, —OH, phenyl, R3 is lower alkyl, provided that when Z is a group of the formula: then G should not be amino, when Z is a group of the formula: then G should not be when Z is a group of the formula: and G is optionally protected amino, then D should be —CS—, or then A should be lower alkylene, B or E should be —NH— and F should be —CO—; or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor as well as a pharmaceutical composition and a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.
摘要翻译：式（I）的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> UVWXYZ（I）<？in-line-formula description =“In-line Formulas” end =“tail”？>其中U是低级烷基; V是-CONH-或-NR 1 CO-，其中R 1是氢或低级烷基; W是键或低级亚烷基; X是衍生自任选取代的噻唑的二价残基; Y是键或低级亚烷基; 并且Z是下式的基团：其中R 2是下列基团：-A-B-D-E-F-G其中A是键或低级亚烷基; B是键，-NH-或D是键，-CS-或-CO-; E是键或-NH-; F是键，-CO - ， - O-或-SO 2 - 。并且G为低级烷基，任意保护的氨基，-OH，苯基，R 3为低级烷基，条件是当Z为下式基团时，则G不应为氨基，当Z为组式为：那么G不应该是当Z是下式的基团时：G是任意保护的氨基，那么D应该是-CS-，或者A应该是低级亚烷基，B或E应该是-NH- 而F应为-CO-; 或其药学上可接受的盐可用作血管粘附蛋白-1（VAP-1）抑制剂，以及用于预防或治疗VAP-1相关疾病，特别是黄斑水肿的药物组合物和方法，该方法包括施用有效的化合物或其药学上可接受的盐对受试者的量等。

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