公开(公告)号：US20120295848A1

公开(公告)日：2012-11-22

申请号：US13564928

申请日：2012-08-02

Applicant: Kazumichi Yamamoto ,  Akiko YAMADA ,  Yoshio HATA

Inventor： Kazumichi Yamamoto ,  Akiko YAMADA ,  Yoshio HATA

IPC: A61K47/34 ,  A61K38/09 ,  C08G63/08 ,  A61P13/08 ,  A61P15/00 ,  A61P15/18 ,  A61K38/02 ,  A61P35/00

CPC classification number: A61K38/09 ,  A61K9/1647

Abstract: Present invention is to provide a sustained-release composition which contains a physiologically active substance in high content even when gelatin is not included, and suppresses its initial excessive release and, thus, can achieve a stable release rate over about one month. A sustained-release composition containing a lactic acid-glycolic acid polymer having a ratio or weight average molecular weight and number average molecular weight of about 1.90 or lower, or a salt thereof, and a physiologically active substance.

Abstract translation: 本发明提供即使在不含明胶时也含有高含量的生理活性物质的缓释组合物，抑制其初始过度释放，从而能够在约1个月内达到稳定的释放速度。 一种缓释组合物，其含有比例或重均分子量和数均分子量为约1.90以下的乳酸 - 乙醇酸聚合物或其盐和生理活性物质。

公开(公告)号：US08299261B2

公开(公告)日：2012-10-30

申请号：US13156216

申请日：2011-06-08

Applicant: Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

Inventor： Masahiro Kajino ,  Atsushi Hasuoka ,  Haruyuki Nishida

IPC: C07D401/02

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/04

Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.

Abstract translation: 本发明提供具有优异的酸分泌抑制作用并显示出抗溃疡活性等的化合物。 本发明提供由式（I）表示的化合物，其中R 1是任选与苯环或杂环稠合的含氮单环杂环基，任选地与苯环或杂环稠合的含氮单环杂环基 具有取代基，R 2为任选取代的C 6-14芳基，任选取代的噻吩基或任选取代的吡啶基，R 3和R 4各自为氢原子，或者R 3和R 4中的一个为氢原子， 另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，R 5是烷基或其盐。

公开(公告)号：US08293901B2

公开(公告)日：2012-10-23

申请号：US12520247

申请日：2007-12-18

Applicant: Qing Dong ,  Nicholas Scorah ,  Steven W Kaldor

Inventor： Qing Dong ,  Nicholas Scorah ,  Steven W Kaldor

IPC: C07D471/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Compounds of the following formula are provided for use with MEK (I): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 提供下式的化合物用于MEK（I）：其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US20120264967A1

公开(公告)日：2012-10-18

申请号：US13421421

申请日：2012-03-15

Applicant: David Paul Provencal ,  Todd Miller ,  Yuxin Zhao ,  Jonathon S. Salsbury

Inventor： David Paul Provencal ,  Todd Miller ,  Yuxin Zhao ,  Jonathon S. Salsbury

IPC: C07C255/23

CPC classification number: C07D471/04 ,  C07C255/23 ,  C07D213/82 ,  C07D213/85

Abstract: The present invention relates generally to processes of making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, intermediates thereof, and a process for making a particular polymorph of (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione.

Abstract translation: 本发明一般涉及制备（R）-3-（2,3-二羟基丙基）-6-氟-5-（2-氟-4-碘苯基氨基）-8-甲基吡啶并[2,3-d]嘧啶 -4,7（3H，8H） - 二酮及其中间体，以及制备（R）-3-（2,3-二羟基丙基）-6-氟-5-（2-氟-4- - 碘苯基氨基）-8-甲基吡啶并[2,3-d]嘧啶-4,7（3H，8H） - 二酮。

公开(公告)号：US08278450B2

公开(公告)日：2012-10-02

申请号：US12103882

申请日：2008-04-16

Applicant: Jason W. Brown ,  Qing Dong ,  Bheema R. Paraselli ,  Nicholas Scorah ,  Jeffrey A. Stafford ,  Michael B. Wallace ,  Hasanthi Wijesekera

Inventor： Jason W. Brown ,  Qing Dong ,  Bheema R. Paraselli ,  Nicholas Scorah ,  Jeffrey A. Stafford ,  Michael B. Wallace ,  Hasanthi Wijesekera

IPC: C07D471/00 ,  C07D209/88

CPC classification number: C07D471/14 ,  C07D241/18 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 提供化合物用于与包含选自以下的化合物的激酶一起使用：其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US08273761B2

公开(公告)日：2012-09-25

申请号：US12448094

申请日：2007-12-07

Applicant: Osamu Uchikawa ,  Tatsuki Koike ,  Takafumi Takai ,  Yasutaka Hoashi

Inventor： Osamu Uchikawa ,  Tatsuki Koike ,  Takafumi Takai ,  Yasutaka Hoashi

IPC: C07D491/048 ,  A61K31/4355

CPC classification number: C07D491/04 ,  C07D491/14

Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa to Xe are each a carbon atom or a nitrogen atom, m is 0 to 2, and ring A to ring C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.

Abstract translation: 本发明提供由下式表示的化合物，其中R 1是任选具有取代基的烃基，任选具有取代基的氨基，任选具有取代基的羟基或任选具有取代基的杂环基，R2是 氢原子或任选具有取代基的烃基，R 3是氢原子，卤素原子，任选具有取代基的烃基，任选具有取代基的氨基，任选具有取代基的羟基或任选具有取代基的巯基， 取代基，Xa〜Xe各自为碳原子或氮原子，m为0〜2，环A〜环C各自为任选具有取代基的环，或其盐，可用作试剂 用于预防或治疗与褪黑素的作用相关的疾病等。

公开(公告)号：US08252814B2

公开(公告)日：2012-08-28

申请号：US12219198

申请日：2008-07-17

Applicant: Yuji Ishihara ,  Takayuki Doi ,  Hiroshi Nagabukuro ,  Yuji Ishichi

Inventor： Yuji Ishihara ,  Takayuki Doi ,  Hiroshi Nagabukuro ,  Yuji Ishichi

IPC: A01N43/40 ,  A61K31/445

CPC classification number: A61K31/00 ,  A61K31/343 ,  A61K31/382 ,  A61K31/395 ,  A61K31/404 ,  A61K31/435 ,  A61K31/445 ,  A61K31/452 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D211/26 ,  C07D211/32 ,  C07D273/06 ,  C07D401/06 ,  C07D471/06 ,  C07D487/04 ,  A61K2300/00

Abstract: Agents for improving potency of the urinary bladder which comprise an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholinesterase and an action to improve the excretory potency of the urinary bladder. As an example, crystals of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.

Abstract translation: 用于提高膀胱效能的药剂，其包含具有乙酰胆碱酯酶抑制作用的非氨基甲酸酯型胺化合物。 特别地，提供三环，缩合，杂环衍生物的结晶，其具有抑制乙酰胆碱酯酶的优异作用和提高膀胱排泄能力的作用。 例如，8- [3- [1 - [（3-氟苯基） - 甲基] -4-哌啶基] -1-氧代丙基] -1,2,5,6-四氢-4H-吡咯并[ 2,1-ij]喹啉-4-酮或其盐和含有它们的药物组合物。

公开(公告)号：US20120214855A1

公开(公告)日：2012-08-23

申请号：US13347302

申请日：2012-01-10

Applicant: Masanori OKANIWA ,  Terufumi TAKAGI ,  Masaaki HIROSE

Inventor： Masanori OKANIWA ,  Terufumi TAKAGI ,  Masaaki HIROSE

IPC: A61K31/428 ,  A61P35/00

CPC classification number: C07D277/82 ,  C07D417/12

Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity.A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.

Abstract translation: 提供显示出强的Raf抑制活性的稠合杂环衍生物。 由下式表示的化合物，其中每个符号如本说明书中所定义，或其盐。

公开(公告)号：US08222411B2

公开(公告)日：2012-07-17

申请号：US12066769

申请日：2006-09-15

Applicant: Jun Feng ,  Stephen L. Gwaltney ,  Jeffrey A. Stafford ,  Zhiyuan Zhang ,  Paul R. Brodfuahrer ,  Bruce Elder ,  Paul Isbester ,  Richard S. Fornicola ,  Philip B. Kisanga ,  Bingidimi I. Mobele ,  Grant J. Palmer ,  Maxwell M. Reeve ,  Jonathon S. Salsbury ,  Luckner Ulysse ,  Sripathy Venkatraman

Inventor： Jun Feng ,  Stephen L. Gwaltney ,  Jeffrey A. Stafford ,  Zhiyuan Zhang ,  Paul R. Brodfuahrer ,  Bruce Elder ,  Paul Isbester ,  Richard S. Fornicola ,  Philip B. Kisanga ,  Bingidimi I. Mobele ,  Grant J. Palmer ,  Maxwell M. Reeve ,  Jonathon S. Salsbury ,  Luckner Ulysse ,  Sripathy Venkatraman

IPC: C07D239/02

CPC classification number: C07D239/553 ,  C07D239/545 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14

Abstract: Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.

Abstract translation: 制备式（I）化合物的方法，其中变量如本文所定义。 另外，制备可用于抑制二肽基肽酶的化合物的方法。

公开(公告)号：US20120178924A1

公开(公告)日：2012-07-12

申请号：US13429865

申请日：2012-03-26

Applicant: Bohan Jin ,  Nicholas Scorah ,  Qing Dong

Inventor： Bohan Jin ,  Nicholas Scorah ,  Qing Dong

IPC: C07D498/14

CPC classification number: C07D498/14

Abstract: The present invention relates to intermediates of the formula wherein G1 is N; G2 is selected from the group consisting of C═O and CH2; X is a halogen; and the other groups are defined herein.

Abstract translation: 本发明涉及下式的中间体，其中G1是N; G2选自C = O和CH 2; X是卤素; 并且其他组在本文中定义。