公开(公告)号：US20190241531A1

公开(公告)日：2019-08-08

申请号：US16303646

申请日：2017-05-23

Applicant: Institute of Materia Medica, Chineses Academy of Medical Sciences

Inventor： Zhiqiang Feng

IPC: C07D295/155 ,  A61P35/00 ,  C07C271/64 ,  C07C269/02 ,  C07C229/36 ,  C07C227/12 ,  C07D207/08 ,  C07D309/14 ,  C07D319/16

CPC classification number: C07D407/12 ,  A61K31/165 ,  A61K31/277 ,  A61K31/36 ,  A61P35/00 ,  C07C211/29 ,  C07C227/12 ,  C07C229/36 ,  C07C233/36 ,  C07C235/34 ,  C07C255/54 ,  C07C269/02 ,  C07C271/64 ,  C07C311/05 ,  C07D207/08 ,  C07D221/00 ,  C07D265/30 ,  C07D295/155 ,  C07D309/14 ,  C07D319/16 ,  C07D319/18 ,  C07D405/12

Abstract: The present invention discloses a benzyl phenyl ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to benzyl phenyl ether derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.

公开(公告)号：US20180343870A1

公开(公告)日：2018-12-06

申请号：US15755231

申请日：2016-08-26

Applicant: NANO SAFE COATINGS INCORPORATED (A FLORIDA CORPORATION 3 P 14000024914)

Inventor： Daniel Foucher ,  Gideon Wolfaardt ,  Alexander Gabriel Caschera ,  Aman Ullah Khan ,  Kamiesh Mistry ,  Evan Lindsay Gilmore Ronan ,  Lukasz Porosa

IPC: A01N57/22 ,  C07C311/18 ,  C07C311/05 ,  C07C307/06 ,  C07F7/18 ,  C07F9/40 ,  A01N41/06 ,  A01N55/00 ,  B05D3/06

CPC classification number: A01N57/22 ,  A01N41/06 ,  A01N55/00 ,  B05D3/065 ,  C07C307/06 ,  C07C311/05 ,  C07C311/18 ,  C07C2602/42 ,  C07F7/1804 ,  C07F9/4006

Abstract: A quaternary ammonium sulfonamide compound of formula (I): wherein R=(II), C1-C3 linear or branched alkyl, R1 and R2 are the same or different and selected from C1 to C18 linear or branched alkyl, R3 and R4 are the same or different and selected from C1 to C4 linear or branched alkyl, CF3, OR5 where R5 is C1 to C8 linear or branched alkyl or polyethylene oxide, l is 1, 2, 3, 4, 5, 6, 7 or 8, m is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 or 17, n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 or 18, wherein the aryl groups of R may be substituted or unsubstituted, X=halogen, and Y=(III) wherein R6, R7, R8, R9 and R10 are the same or different and selected from C1 to C6 linear or branched alkyl and the benzophenone is selected from the group consisting of substituted benzophenone and unsubstituted benzophenone, process for preparing the compound and antimicrobial surface coating compositions of the compound.

公开(公告)号：US09867888B2

公开(公告)日：2018-01-16

申请号：US15493281

申请日：2017-04-21

Applicant: MODERNATX, Inc.

Inventor： Kerry E. Benenato

IPC: A61K48/00 ,  A61K9/51 ,  A61K31/7105 ,  C07C229/16 ,  C07C227/18 ,  A61K38/17 ,  A61K38/18

CPC classification number: C07C229/12 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1272 ,  A61K9/1617 ,  A61K9/1641 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/7105 ,  A61K38/1725 ,  A61K38/1816 ,  A61K47/543 ,  A61K47/6911 ,  A61K48/00 ,  A61K48/0033 ,  A61K48/005 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C235/10 ,  C07C255/24 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/091 ,  C07K14/505

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US09758492B2

公开(公告)日：2017-09-12

申请号：US14914184

申请日：2014-08-26

Applicant: Bristol-Myers Squibb Company

Inventor： Jay A. Markwalder ,  Steven P. Seitz ,  James Aaron Balog ,  Audris Huang ,  Sunil Kumar Mandal ,  Shefali Srivastava ,  David K. Williams ,  Libing Chen

IPC: C07D257/04 ,  A61K31/17 ,  A61K31/18 ,  A61K31/381 ,  A61K31/41 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/50 ,  A61K31/506 ,  A61K31/5375 ,  A61K45/06 ,  C07D211/14 ,  C07D237/20 ,  C07D333/38 ,  C07D401/10 ,  C07D407/12 ,  C07D417/12 ,  C07D403/12 ,  C07D309/14 ,  C07D215/06 ,  C07D231/12 ,  C07D333/10 ,  C07D401/12 ,  C07D409/12 ,  C07D411/12 ,  C07D413/12 ,  C07D277/22 ,  C07C275/42 ,  C07C311/05 ,  C07C311/09 ,  C07C317/44 ,  C07B59/00

CPC classification number: C07D257/04 ,  A61K31/17 ,  A61K31/18 ,  A61K31/381 ,  A61K31/41 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/50 ,  A61K31/506 ,  A61K31/5375 ,  A61K45/06 ,  C07B59/002 ,  C07C275/42 ,  C07C311/05 ,  C07C311/09 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07D211/14 ,  C07D215/06 ,  C07D231/12 ,  C07D237/20 ,  C07D277/22 ,  C07D309/14 ,  C07D333/10 ,  C07D333/38 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention.

公开(公告)号：US20160200674A1

公开(公告)日：2016-07-14

申请号：US14914184

申请日：2014-08-26

Applicant: Bristol-Myers Squibb Company

Inventor： Jay A. Markwalder ,  Steven P. Seitz ,  James Aaron Balog ,  Audris Huang ,  Sunil Kumar Mandal ,  Shefali Srivastava ,  David K. Williams ,  Libing Chen

IPC: C07C275/42 ,  A61K31/41 ,  A61K45/06 ,  C07C311/09 ,  A61K31/18 ,  A61K31/17 ,  C07D417/12 ,  A61K31/427 ,  C07D333/38 ,  A61K31/381 ,  C07D401/10 ,  A61K31/4439 ,  C07D407/12 ,  C07D211/14 ,  A61K31/451 ,  C07D403/12 ,  A61K31/506 ,  C07D413/12 ,  A61K31/422 ,  A61K31/497 ,  A61K31/4709 ,  C07D237/20 ,  A61K31/50 ,  A61K31/5375 ,  C07D257/04

CPC classification number: C07D257/04 ,  A61K31/17 ,  A61K31/18 ,  A61K31/381 ,  A61K31/41 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/50 ,  A61K31/506 ,  A61K31/5375 ,  A61K45/06 ,  C07B59/002 ,  C07C275/42 ,  C07C311/05 ,  C07C311/09 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07D211/14 ,  C07D215/06 ,  C07D231/12 ,  C07D237/20 ,  C07D277/22 ,  C07D309/14 ,  C07D333/10 ,  C07D333/38 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention.

Abstract translation: 公开了调节或抑制吲哚胺2,3-双加氧酶（IDO）的酶活性的化合物，含有所述化合物的药物组合物和治疗增殖性疾病的方法，例如癌症，病毒感染和/或自身免疫疾病，其利用 发明。

公开(公告)号：US20160002183A1

公开(公告)日：2016-01-07

申请号：US14792493

申请日：2015-07-06

Applicant: President and Fellows of Harvard College

Inventor： Andrew G. Myers ,  David A. Kummer ,  Derun Li ,  Evan Hecker ,  Amelie Dion ,  Peter M. Wright

IPC: C07D261/20 ,  C07D261/18 ,  C07C45/67 ,  C07C45/00 ,  C07C29/32 ,  C07C45/29 ,  C07F7/18

CPC classification number: C07D261/20 ,  C07B2200/07 ,  C07C29/32 ,  C07C45/00 ,  C07C45/29 ,  C07C45/67 ,  C07C45/673 ,  C07C45/69 ,  C07C49/637 ,  C07C237/26 ,  C07C311/05 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2603/46 ,  C07C2603/66 ,  C07D207/16 ,  C07D209/58 ,  C07D213/30 ,  C07D213/74 ,  C07D233/61 ,  C07D261/18 ,  C07D277/24 ,  C07D277/64 ,  C07D295/15 ,  C07D295/155 ,  C07D498/04 ,  C07F7/0814 ,  C07F7/188

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

Abstract translation: 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够高效合成以前从未制备的新型四环素类似物。 本发明提供了更有效的制备烯酮中间体的途径，并允许四环素环体系的4a，5,5a和12a位置的取代基。

公开(公告)号：US09073827B2

公开(公告)日：2015-07-07

申请号：US14111828

申请日：2012-04-27

Applicant: Taichiro Touge ,  Tomohiko Hakamata ,  Hideki Nara

Inventor： Taichiro Touge ,  Tomohiko Hakamata ,  Hideki Nara

IPC: C07C303/40 ,  C07C311/05 ,  C07C311/18 ,  C07C309/73

CPC classification number: C07C303/40 ,  C07C309/73 ,  C07C311/05 ,  C07C311/18 ,  C07C2601/16

Abstract: The present invention provides a method for producing a compound represented by general formula (1) (wherein R1, R2, R3, R10-R14, A1-A3, n1 and n2 are as defined in the description), which is characterized by reacting a compound represented by general formula (2) (wherein R10-R14, A1-A3, n1, n2 and B are as defined in the description) with a diamine compound represented by general formula (3) (wherein R1-R3 are as defined in the description). The present invention is a method for producing a diamine compound, which is useful for the formation of a ruthenium-diamine complex, under mild conditions, said method being able to be put in industrial practice.

Abstract translation: 本发明提供由通式（1）表示的化合物（其中R1，R2，R3，R10-R14，A1-A3，n1和n2如说明书中所定义）的制备方法，其特征在于使 由通式（2）表示的化合物（其中R10-R14，A1-A3，n1，n2和B如说明书中所定义）与通式（3）表示的二胺化合物（其中R 1 -R 3如 说明）。 本发明是一种在温和条件下可用于形成钌二胺络合物的二胺化合物的制造方法，所述方法能够在工业实践中进行。

公开(公告)号：US09051280B2

公开(公告)日：2015-06-09

申请号：US13546434

申请日：2012-07-11

Applicant: Udo Lange ,  Wilhelm Amberg ,  Michael Ochse ,  Berthold Behl ,  Frauke Pohlki ,  Charles W. Hutchins

Inventor： Udo Lange ,  Wilhelm Amberg ,  Michael Ochse ,  Berthold Behl ,  Frauke Pohlki ,  Charles W. Hutchins

IPC: A61K31/135 ,  C07D231/00 ,  C07D233/00 ,  C07C211/16 ,  A61K31/131 ,  C07D233/84 ,  C07C311/05 ,  C07C311/10 ,  C07C311/14 ,  C07D403/12 ,  C07D205/04

CPC classification number: C07D233/84 ,  C07C311/05 ,  C07C311/10 ,  C07C311/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D403/12

Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.

Abstract translation: 本发明涉及式（I）的四氢化萘和二氢化茚衍生物或其生理上耐受的盐。 本发明涉及包含这种四氢化萘和二氢化茚衍生物的药物组合物，以及这些四氢化萘和二氢化茚衍生物用于治疗目的的用途。 四氢化萘和茚满衍生物是GlyT1抑制剂。

公开(公告)号：US20140256701A1

公开(公告)日：2014-09-11

申请号：US14282712

申请日：2014-05-20

Applicant: AbbVie Deutschland GmbH & Co. KG ,  Abbott Laboratories

Inventor： Frauke Pohlki ,  Udo Lange ,  Wilhelm Amberg ,  Michael Ochse ,  Berthold Behl ,  Wilfried Hornberger ,  Mario Mezler ,  Charles W. Hutchins ,  Sean Turner

IPC: C07D403/12 ,  C07D231/18 ,  C07D401/12 ,  C07D295/135 ,  C07C311/05 ,  C07C311/06 ,  C07D233/84 ,  C07C311/10

CPC classification number: C07C311/06 ,  C07C311/04 ,  C07C311/05 ,  C07C311/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07D205/04 ,  C07D207/08 ,  C07D207/267 ,  C07D231/18 ,  C07D233/42 ,  C07D233/84 ,  C07D295/135 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Abstract translation: 本发明涉及式（I）的苯烷基胺衍生物或其生理上耐受的盐。 本发明涉及包含这种苯烷基胺衍生物的药物组合物，以及这种苯烷基胺衍生物用于治疗目的的用途。 酚烷基胺衍生物是GlyT1抑制剂。

公开(公告)号：US08779195B2

公开(公告)日：2014-07-15

申请号：US12514540

申请日：2007-11-12

Applicant: Muneharu Miyake ,  Tadashi Kusama ,  Takashi Masuko

Inventor： Muneharu Miyake ,  Tadashi Kusama ,  Takashi Masuko

IPC: C07C303/00 ,  C07C307/00 ,  C07C309/00 ,  C07C311/00

CPC classification number: C07C311/18 ,  C07C311/05

Abstract: A compound having the general formula (I) or a pharmacologically acceptable salt thereof: X—NH—Y—NH—R1  (I) [wherein X represents R2—SO2— in which R2 represents an optionally substituted lower alkyl group or phenyl group; Y represents a group selected from the group consisting of —R3—NH—R4—, —R5—NH—R6—NH—R7—, —R8—NH—R9—NH—R10—NH—R11—and —R12—NH—R13—NH—R14—NH—R15— in which R3 to R15 each independently represent a C3 to C5 alkylene group; and R1 represents hydrogen or an optionally substituted lower alkyl group, with the proviso that the case where X represents a tosyl group, Y represents —(CH2)3—NH—(CH2)4—NH—(CH2)3—and R1 represents hydrogen is excepted].

Abstract translation: 具有通式（I）的化合物或其药学上可接受的盐：X-NH-Y-NH-R1（I）[其中X表示R2-SO2-，其中R2表示任选取代的低级烷基或苯基; Y表示选自-R 3 -NH-R 4 - ，-R 5-NH-R 6 -NH-R 7 - ， - R 8 -NH-R 9 -NH-R 10 -NH-R 11 - 和-R 12-NH -R13-NH-R14-NH-R15-，其中R3至R15各自独立地表示C3至C5亚烷基; 并且R 1表示氢或任选取代的低级烷基，条件是X表示甲苯磺酰基，Y表示 - （CH 2）3 -NH-（CH 2）4 -NH-（CH 2）3 - 并且R 1表示 氢除外]。