公开(公告)号：US20170334838A1

公开(公告)日：2017-11-23

申请号：US15525564

申请日：2015-11-09

Applicant: Shankar Reddy Budidet ,  Jagan Mohan Reddy Sanapureddy ,  Subba Reddy Danda ,  Bhima Shankar Gangadhara ,  Somappa Somannavar Yallappa ,  Kishore Karumanchi ,  Sivakumaran Meenakshisunderam

Inventor： Shankar Reddy Budidet ,  Jagan Mohan Reddy Sanapureddy ,  Subba Reddy Danda ,  Bhima Shankar Gangadhara ,  Somappa Somannavar Yallappa ,  Kishore Karumanchi ,  Sivakumaran Meenakshisunderam

IPC: C07C253/30 ,  C07D273/02 ,  A61K31/513 ,  A61K31/506 ,  B01D11/02 ,  C07D413/12 ,  C07D239/54

CPC classification number: C07C253/30 ,  A61K31/506 ,  A61K31/513 ,  A61K2300/00 ,  B01D11/02 ,  C07C269/04 ,  C07C269/06 ,  C07D239/54 ,  C07D239/557 ,  C07D273/02 ,  C07D413/12 ,  C07C255/25 ,  C07C271/22 ,  C07C271/20

Abstract: The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

公开(公告)号：US09624220B2

公开(公告)日：2017-04-18

申请号：US15209231

申请日：2016-07-13

Applicant: Critical Outcome Technologies Inc.

Inventor： Wayne Danter ,  Clinton Threlfall ,  Sylvain Guizzetti ,  Julien Marin

IPC: C07D471/04 ,  C07D239/36 ,  C07D239/40 ,  C07D239/42 ,  C07D413/04 ,  C07D239/47 ,  C07D239/557 ,  C07D239/56 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D239/36 ,  C07D239/40 ,  C07D239/42 ,  C07D239/47 ,  C07D239/557 ,  C07D239/56 ,  C07D413/04 ,  C07D487/04

Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N═O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.

公开(公告)号：US20160333010A1

公开(公告)日：2016-11-17

申请号：US15209231

申请日：2016-07-13

Applicant: Critical Outcome Technologies Inc.

Inventor： Wayne Danter ,  Clinton Threlfall ,  Sylvain Guizzetti ,  Julien Marin

IPC: C07D471/04 ,  C07D413/04

CPC classification number: C07D471/04 ,  C07D239/36 ,  C07D239/40 ,  C07D239/42 ,  C07D239/47 ,  C07D239/557 ,  C07D239/56 ,  C07D413/04 ,  C07D487/04

Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N═O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.

Abstract translation: 和/或药学上可接受的盐，水合物，溶剂化物，互变异构体，旋光异构体，E-异构体，Z-异构体或其组合; X选自Se，N-OH，NH，NO 2，CN，N-CN，N = O，O或S，其余的取代基如本文所述; 及其组合物。 本发明还涉及其施用方法; 及其用途来治疗HIV。

公开(公告)号：US09394260B2

公开(公告)日：2016-07-19

申请号：US14390152

申请日：2013-04-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Carol Hui Hu ,  Jennifer X. Qiao ,  Tammy C. Wang

IPC: C07D401/12 ,  A61K31/513 ,  C07D239/557 ,  A61K31/5377 ,  C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D239/557 ,  A61K31/513 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides compounds of Formula (I): (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

Abstract translation: 本发明提供式（I）化合物：如本说明书中所定义的（I）和包含任何这些新化合物的组合物。 这些化合物是可用作药物的内皮脂肪酶抑制剂。

公开(公告)号：US20150361052A1

公开(公告)日：2015-12-17

申请号：US14390152

申请日：2013-04-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Carol Hui Hu ,  Jennifer X. Qiao ,  Tammy C. Wang

IPC: C07D239/557 ,  C07D401/12 ,  C07D417/14 ,  C07D413/12 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D417/12

CPC classification number: C07D239/557 ,  A61K31/513 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides compounds of Formula (I): (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

Abstract translation: 本发明提供式（I）化合物：如本说明书中所定义的（I）和包含任何这些新化合物的组合物。 这些化合物是可用作药物的内皮脂肪酶抑制剂。

公开(公告)号：US20130225596A1

公开(公告)日：2013-08-29

申请号：US13816085

申请日：2011-08-09

Applicant: Hiroyuki Kai ,  Takeshi Endoh ,  Sae Jikihara ,  Kentaro Asahi ,  Tohru Horiguchi

Inventor： Hiroyuki Kai ,  Takeshi Endoh ,  Sae Jikihara ,  Kentaro Asahi ,  Tohru Horiguchi

IPC: C07C233/75 ,  C07D239/84 ,  C07D213/74 ,  C07C217/84 ,  C07D211/72 ,  C07D405/06 ,  C07C217/80 ,  C07D413/12 ,  C07D409/12 ,  C07D409/06 ,  C07D277/28 ,  C07D401/14 ,  C07D237/04

CPC classification number: C07D239/545 ,  C07C217/80 ,  C07C217/84 ,  C07C217/92 ,  C07C233/25 ,  C07C233/75 ,  C07C2601/14 ,  C07D211/72 ,  C07D213/64 ,  C07D213/69 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D213/82 ,  C07D215/22 ,  C07D215/56 ,  C07D217/22 ,  C07D217/24 ,  C07D231/38 ,  C07D233/88 ,  C07D233/96 ,  C07D235/30 ,  C07D237/04 ,  C07D237/20 ,  C07D237/32 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/54 ,  C07D239/557 ,  C07D239/78 ,  C07D239/84 ,  C07D239/95 ,  C07D239/96 ,  C07D241/20 ,  C07D255/02 ,  C07D261/12 ,  C07D263/32 ,  C07D263/34 ,  C07D263/48 ,  C07D265/06 ,  C07D265/10 ,  C07D265/26 ,  C07D265/36 ,  C07D277/20 ,  C07D277/28 ,  C07D277/34 ,  C07D277/38 ,  C07D277/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D407/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect.A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.

Abstract translation: 本发明提供具有P2X3和/或P2X2 / 3受体拮抗作用的新化合物。 一种具有P2X3和/或P2X2 / 3受体拮抗作用的药物组合物，其包含式（I）化合物：其中环A是取代或未取代的5至7元环烷烃，取代或未取代的5至7元环烯烃或 喜欢; C是碳原子; -X-是-N（R 16） - 等; R 16是氢，取代或未取代的烷基等; R 7是取代或未取代的5元或6元杂芳基，取代或未取代的6至10元芳基; Q1和Q2各自独立地为碳原子或氮原子; -L-是-O-，-S-等; R6是取代或未取代的环烷基，取代或未取代的环烯基等; R2是氢，羟基等，或其药学上可接受的盐或其溶剂合物。

公开(公告)号：US20120123118A1

公开(公告)日：2012-05-17

申请号：US13201486

申请日：2010-02-22

Applicant: Rolf Dach ,  Xiangrui Jiang ,  Jingshan Shen ,  Jin Suo ,  Yi Zhu

Inventor： Rolf Dach ,  Xiangrui Jiang ,  Jingshan Shen ,  Jin Suo ,  Yi Zhu

IPC: C07D487/04 ,  C07D239/557

CPC classification number: C07D487/04 ,  C07D239/557

Abstract: Subject of the present invention is a new improved process for the preparation of nitroorotic acid via nitration of orotic acid.

Abstract translation: 本发明的主题是通过乳清酸硝化制备硝酸根酸的新的改进方法。

公开(公告)号：US08088783B2

公开(公告)日：2012-01-03

申请号：US13082259

申请日：2011-04-07

Applicant: Qing Dong ,  Stephen W. Kaldor

Inventor： Qing Dong ,  Stephen W. Kaldor

IPC: A61K31/505 ,  C07D401/00

CPC classification number: C07D239/545 ,  C07D239/557 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D413/06

Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.”

Abstract translation: 取代的1,3-二烷基-2,4-二氧代-6-（嘧啶基氨基）-1,2,3,4-四氢嘧啶-5-异羟肟酸的化合物如下所示：其中变量如本文所定义，药物 提供其组合物用作MEK激酶的抑制剂。

公开(公告)号：US07943626B2

公开(公告)日：2011-05-17

申请号：US12652570

申请日：2010-01-05

Applicant: Qing Dong ,  Stephen W. Kaldor

Inventor： Qing Dong ,  Stephen W. Kaldor

IPC: A61K31/505

CPC classification number: C07D239/545 ,  C07D239/557 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D413/06

Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.

Abstract translation: 取代的1,3-二烷基-2,4-二氧代-6-（芳基氨基）-1,2,3,4-四氢嘧啶-5-异羟肟酸的化合物如下所示：其中变量如本文所定义，药物 提供其组合物用作MEK激酶的抑制剂。

公开(公告)号：US20110034449A1

公开(公告)日：2011-02-10

申请号：US12884734

申请日：2010-09-17

Applicant: Benedetta Crescenzi ,  Cristina Gardelli ,  Ester Muraglia ,  Emanuela Nizi ,  Federica Orvieto ,  Paola Pace ,  Giovanna Pescatore ,  Alessia Petrocchi ,  Marco Poma ,  Michael Rowley ,  Rita Scarpelli ,  Vincenzo Summa

Inventor： Benedetta Crescenzi ,  Cristina Gardelli ,  Ester Muraglia ,  Emanuela Nizi ,  Federica Orvieto ,  Paola Pace ,  Giovanna Pescatore ,  Alessia Petrocchi ,  Marco Poma ,  Michael Rowley ,  Rita Scarpelli ,  Vincenzo Summa

IPC: A61K31/541 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/497 ,  A61K31/496 ,  A61P31/18

CPC classification number: C07D239/557 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D513/04

Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 被描述为HIV整合酶抑制剂和HIV复制抑制剂的N-取代的5-羟基嘧啶-6-酮-4-甲酰胺，其中R1，R2，R3和R4如本文所定义。 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。