公开(公告)号：US06624313B2

公开(公告)日：2003-09-23

申请号：US10133954

申请日：2002-04-26

申请人： Keith M. DeVries ,  Michel A. Couturier ,  Brian M. Andresen ,  John L. Tucker ,  Fumitaka Ito

发明人： Keith M. DeVries ,  Michel A. Couturier ,  Brian M. Andresen ,  John L. Tucker ,  Fumitaka Ito

IPC分类号： C07D20704

CPC分类号： C07D207/12

摘要： A process of preparing compounds having the formula I: or an optical isomer or racemic or optically active mixture thereof, which are useful as selective kappa-receptor agonists.

摘要翻译： 制备具有式I化合物或其旋光异构体或外消旋或光学活性混合物的方法，其可用作选择性κ-受体激动剂。

公开(公告)号：US06423725B1

公开(公告)日：2002-07-23

申请号：US09403408

申请日：2000-03-06

申请人： Fumitaka Ito ,  Hirohide Noguchi ,  Yoriko Ohashi ,  Hiroshi Kondo ,  Tatsuya Yamagishi

发明人： Fumitaka Ito ,  Hirohide Noguchi ,  Yoriko Ohashi ,  Hiroshi Kondo ,  Tatsuya Yamagishi

IPC分类号： A61K31454

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D409/14

摘要： A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.

摘要翻译： 下式化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如上定义，可用作ORL1-受体激动剂，并且可用作哺乳动物受试者中的止痛剂等。

公开(公告)号：US06303602B1

公开(公告)日：2001-10-16

申请号：US09770512

申请日：2001-01-26

申请人： Fumitaka Ito ,  Hiroshi Kondo

发明人： Fumitaka Ito ,  Hiroshi Kondo

IPC分类号： A61K31401

CPC分类号： C07D213/82 ,  C07D207/10 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

摘要： A compound of the following formula: or a salt thereof, wherein A is hydrogen, halo, hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, furanyl or thienyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

摘要翻译： 下式的化合物或其盐，其中A是氢，卤素，羟基; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基; Ar 2是选自苯基，萘乙基，呋喃基或噻吩基的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基或C1-C4烷基; 并且R 2和R 3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基或R 2和R 3与它们所连接的氮原子一起形成任选取代的 吡咯烷，哌啶或吗啉环。 这些化合物可用作κ激动剂。

公开(公告)号：US06294557B1

公开(公告)日：2001-09-25

申请号：US09771030

申请日：2001-01-26

申请人： Fumitaka Ito ,  Hiroshi Kondo

发明人： Fumitaka Ito ,  Hiroshi Kondo

IPC分类号： A61K314439

CPC分类号： C07D213/82 ,  C07D207/10 ,  C07D207/12 ,  C07D207/20 ,  C07D207/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

摘要： A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

摘要翻译： 下式的化合物及其盐，其中A是氢，卤素，羟基等; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基等; Ar 2是选自苯基，萘乙基，吡啶基等的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基，C1-C4烷基等; 并且R2和R3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基等，或者R 2和R 3与它们所连接的氮原子一起形成 任选取代的吡咯烷，哌啶或吗啉环。 这些化合物可用作κ激动剂。

公开(公告)号：US6110947A

公开(公告)日：2000-08-29

申请号：US302097

申请日：1999-04-29

申请人： Fumitaka Ito

发明人： Fumitaka Ito

IPC分类号： C07D295/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/00 ,  A61P7/00 ,  A61P7/10 ,  A61P23/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D207/12 ,  C07D213/54 ,  C07D295/13 ,  C07D307/79 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  A61K31/4439 ,  C07D407/12

CPC分类号： C07D213/54 ,  C07D207/12 ,  C07D295/13 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

摘要： A compound of the formula: ##STR1## and it pharmaceutically acceptable salt, wherein A is hydrogen, hydroxy or OY, where Y is a hydroxy protecting group;Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, C.sub.1 -C.sub.4 alkyloxy, and carboxy-C.sub.1 -C.sub.4 alkyloxy;X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiopheny, 1-tetralone-6-yl, C.sub.1 -C.sub.4 alkylenedioxy, pyridyl, furyl and thienyl, these groups optionally being substituted with up to three substituents selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, NO.sub.2, CF.sub.3 and SO.sub.2 CH.sub.3 ; andR is hydrogen, C.sub.1 -C.sub.4 alkyl or a hydroxy protecting group.These compounds and pharmaceutical compositions containing them are useful as analgesic, antiinflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for stroke or treatment of functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject. Further, the present invention provides processes for producing the hydroxamic compounds of formula (I) and their intermediate compounds of formula (II).

摘要翻译： 下式的化合物及其药学上可接受的盐，其中A是氢，羟基或OY，其中Y是羟基保护基; Ar是任选被一个或多个选自卤素，羟基，C 1 -C 4烷基，C 1 -C 4烷氧基，CF 3，C 1 -C 4烷氧基和羧基-C 1 -C 4烷氧基的取代基取代的苯基; X是苯基，萘基，联苯基，茚满基，苯并呋喃基，苯并噻吩并，1-四氢萘酮-6-基，C 1 -C 4亚烷基二氧基，吡啶基，呋喃基和噻吩基，这些基团任选被至多三个选自卤素，C 1 -C 4 烷基，C 1 -C 4烷氧基，羟基，NO 2，CF 3和SO 2 CH 3; 和R是氢，C 1 -C 4烷基或羟基保护基。 含有它们的这些化合物和药物组合物可用作止痛剂，抗炎剂，利尿剂，麻醉剂或神经保护剂，或用于中风或治疗功能性肠病如腹痛的药剂，用于治疗哺乳动物受试者，特别是人类受试者。 此外，本发明提供了制备式（I）的异羟肟酸化合物及其中间体式（II）的化合物的方法。

公开(公告)号：US5984764A

公开(公告)日：1999-11-16

申请号：US861200

申请日：1997-05-21

申请人： Hideo Saito ,  Hiromi Nishihara ,  Fumitaka Ito ,  Hironobu Hirata

发明人： Hideo Saito ,  Hiromi Nishihara ,  Fumitaka Ito ,  Hironobu Hirata

IPC分类号： B24B37/04 ,  B24B53/007 ,  B24D7/06 ,  B24B1/00

CPC分类号： B24B53/017 ,  B24B37/042 ,  B24D7/06

摘要： The present invention relates to a method of discovering optimal conditions such as the rotational speed ratio of an abrasive cloth and a dresser, to improve the flatness of the abrasive cloth after it has been dressed. A narrow annular dresser having an inner diameter of at least the width of a wide annular utilization region of the abrasive cloth is pressed while rotating against the abrasive cloth which is fixed onto a turn table. A rotational motion is imparted to the abrasive cloth in the same direction as the rotation of the dresser and at a predetermined rotational speed. The abrasive cloth is dressed thereby in such a manner that there is a uniform distribution of distances through which the grindstone slides over various points within the utilization region of the abrasive cloth.

摘要翻译： 本发明涉及一种发现最佳条件的方法，例如研磨布和修整器的转速比，以提高研磨布整修后的平整度。 具有至少宽度大的研磨布的环形利用区域的内径的窄环形修整器在被固定到转台上的研磨布上旋转时被按压。 旋转运动以与修整器的旋转相同的方向并以预定的转速传递给研磨布。 研磨布以这样一种方式穿着，使磨石在研磨布的利用区域内的各个点上滑动穿过该距离的均匀分布。

公开(公告)号：US4675325A

公开(公告)日：1987-06-23

申请号：US622790

申请日：1984-06-21

申请人： Larry E. Overman ,  Fumitaka Ito

发明人： Larry E. Overman ,  Fumitaka Ito

IPC分类号： A61K31/445 ,  C07D471/04 ,  A61K31/475 ,  C07D221/02

CPC分类号： C07D471/04 ,  A61K31/445

摘要： A method of making dendrobatid alkaloids with the formula ##STR1## in which A is either CH.sub.3 or H, and n is an integer from 1-9, and R is CH.sub.2 OH, CHO, ##STR2## and R.sub.1 and R.sub.2 are alkyl groups; and the use of such alkaloids to treat cardiovascular illness.

摘要翻译： 制备式为“IMAGE”的生物碱，其中A为CH 3或H，n为1-9的整数，R为CH 2 OH，CHO， 并使用这些生物碱来治疗心血管疾病。