公开(公告)号：US11312676B2

公开(公告)日：2022-04-26

申请号：US15540386

申请日：2015-12-29

Applicant: BAYLOR COLLEGE OF MEDICINE

Inventor： David Michael Lonard ,  Lei Wang ,  Bert W. O'Malley ,  Jianming Xu ,  Yongcheng Song ,  Xiaonan Li ,  Timothy Gerald Palzkill

IPC: C07C49/753 ,  A61K31/444 ,  A61K31/45 ,  A61K31/4402 ,  A61K31/351 ,  A61K31/4433 ,  A61K31/122 ,  A61K31/4545 ,  C07D401/06 ,  C07D309/38 ,  C07D405/06 ,  C07D213/68 ,  C07D405/12 ,  A61P35/00 ,  C07C49/697 ,  C07D211/86 ,  C07D213/50 ,  C07D309/32 ,  C07D401/14 ,  C07D405/14

Abstract: Small molecule stimulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing cancer. Also provided are methods for stimulating SRC family proteins in a cell.

公开(公告)号：US20210002246A1

公开(公告)日：2021-01-07

申请号：US16969530

申请日：2019-02-12

Applicant: Rutgers, the State University of New Jersey

Inventor： Richard H. Ebright ,  Yon W. Ebright

IPC: C07D309/38 ,  A01N47/12 ,  A61K9/00 ,  A61P31/04 ,  A61P31/06 ,  C07D417/06

Abstract: The invention provides compounds of formula Ia, Ib, Ic, or as well as compositions comprising a compound of formula Ia-Id, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

公开(公告)号：US10202624B2

公开(公告)日：2019-02-12

申请号：US14783375

申请日：2014-04-18

Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA

Inventor： Kechun Zhang ,  Mingyong Xiong

IPC: C07D309/30 ,  C12P17/06 ,  C07D309/32 ,  C07D309/38 ,  C12P7/42 ,  C12N9/10

Abstract: This disclosure describes biosynthesized compounds including anhydromevalonolactone and β-methyl-δ-valerolactone. This disclosure further describes biosynthetic methods for making these compounds. In some embodiments, the biosynthetic methods can include a combination of biosynthesis and chemical steps to produce β-methyl-δ-valerolactone. Finally, this disclosure described recombinant cells useful for the biosynthesis of these compounds.

公开(公告)号：US09592221B2

公开(公告)日：2017-03-14

申请号：US15064452

申请日：2016-03-08

Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  PROVID PHARMACEUTICALS INC.

Inventor： Richard H. Ebright ,  Yon W. Ebright ,  Juan Shen ,  James Bacci ,  Anne-Cecile Hiebel ,  William Solvibile ,  Christopher Self ,  Gary Olson

IPC: A01N43/16 ,  A61K31/366 ,  C07D309/38 ,  C07D405/06 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06 ,  C07D417/06 ,  C07D309/36 ,  C07D405/12 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/4433

CPC classification number: A61K31/366 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/4433 ,  C07D309/36 ,  C07D309/38 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06 ,  C07D417/06

Abstract: The invention provides compounds of formula Ia, Ib and Ic: and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

Abstract translation: 本发明提供式Ia，Ib和Ic化合物：[式Ia，Ib和Ic]及其盐，其中变量如说明书中所述，以及包含式Ia-1c化合物的组合物，制备方法 这些化合物和使用这些化合物的方法，例如作为细菌RNA聚合酶的抑制剂和作为抗菌剂。

公开(公告)号：US09532938B2

公开(公告)日：2017-01-03

申请号：US14447541

申请日：2014-07-30

Applicant: Eastman Chemical Company ,  Chanel Parfums Beaute

Inventor： Liu Deng ,  Neil Warren Boaz ,  Sabine Delaire

IPC: A61K8/67 ,  A61Q19/08 ,  C07C67/03 ,  C07C67/11 ,  C07C403/12 ,  C07C403/20 ,  C07C69/734 ,  C07D309/40 ,  C12P7/62 ,  A61Q19/00 ,  C07C67/10 ,  C07D213/80 ,  C07D213/803 ,  C07D309/38 ,  A61Q19/02

CPC classification number: A61K8/671 ,  A61Q19/00 ,  A61Q19/002 ,  A61Q19/02 ,  A61Q19/08 ,  C07C67/03 ,  C07C67/10 ,  C07C67/11 ,  C07C69/734 ,  C07C403/12 ,  C07C403/20 ,  C07C2601/16 ,  C07D213/80 ,  C07D213/803 ,  C07D309/38 ,  C07D309/40 ,  C12P7/62 ,  C07C69/63

Abstract: Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: wherein R and R1 are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C1-C22 alkyl, substituted and unsubstituted C3-C8 cycloalkyl, substituted and unsubstituted C6-C20 carbocyclic aryl, and substituted and unsubstituted C4-C20 heterocyclic; wherein the heteroatoms are selected from sulfur, nitrogen, and oxygen; and wherein n is 1-6. Process of producing esters of O-substituted hydroxy carboxylic acids are also provided.

Abstract translation: 提供O-取代的羟基羧酸的酯，其具有式1或2或两者或式2或其两者：其中R和R 1独立地选自取代和未取代的，支链和直链的饱和不饱和的 和多不饱和C 1 -C 22烷基，取代和未取代的C 3 -C 8环烷基，取代和未取代的C 6 -C 20碳环芳基和取代和未取代的C 4 -C 20杂环; 其中所述杂原子选自硫，氮和氧; 并且其中n为1-6。 还提供了生产O-取代羟基羧酸酯的方法。

公开(公告)号：US08853215B2

公开(公告)日：2014-10-07

申请号：US13264510

申请日：2010-04-16

Applicant: Shizuo Kasai ,  Kevin Francis McGee, Jr.

Inventor： Shizuo Kasai ,  Kevin Francis McGee, Jr.

IPC: A61K31/495 ,  C07D295/00 ,  C07D207/416 ,  C07D335/02 ,  C07D231/18 ,  C07D295/215 ,  C07D261/18 ,  C07D209/24 ,  C07D209/18 ,  C07D295/185 ,  C07D213/75 ,  C07D211/88 ,  C07D263/34 ,  C07D513/04 ,  C07D213/70 ,  C07D213/65 ,  C07D235/28 ,  C07D233/72 ,  C07D233/64 ,  C07D307/24 ,  C07D211/76 ,  C07D231/14 ,  C07D211/58 ,  C07D233/90 ,  C07D257/04 ,  C07D211/46 ,  C07D213/61 ,  C07D261/12 ,  C07D209/42 ,  C07D207/16 ,  C07D211/22 ,  C07D307/30 ,  C07D233/34 ,  C07D309/38 ,  C07D249/10 ,  C07D211/34 ,  C07D213/81 ,  C07D207/26

CPC classification number: C07D295/185 ,  C07D207/16 ,  C07D207/26 ,  C07D207/416 ,  C07D209/18 ,  C07D209/24 ,  C07D209/42 ,  C07D211/22 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D211/76 ,  C07D211/88 ,  C07D213/61 ,  C07D213/65 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D231/14 ,  C07D231/18 ,  C07D233/34 ,  C07D233/64 ,  C07D233/72 ,  C07D233/90 ,  C07D235/28 ,  C07D249/10 ,  C07D257/04 ,  C07D261/12 ,  C07D261/18 ,  C07D263/34 ,  C07D295/215 ,  C07D307/24 ,  C07D307/30 ,  C07D309/38 ,  C07D335/02 ,  C07D513/04

Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.

Abstract translation: 本发明涉及由下式表示的化合物，其中每个符号如本说明书中所定义，其具有优异的RBP4降低作用，并且可用作预防或治疗由下列疾病介导的疾病或病症的药物组合物： 增加RBP4。

公开(公告)号：US20130296421A1

公开(公告)日：2013-11-07

申请号：US13821804

申请日：2011-09-07

Applicant: Richard H. Ebright

Inventor： Richard H. Ebright

IPC: C07D309/38

CPC classification number: C07D309/38 ,  A61K31/351 ,  C07D309/36 ,  Y02A50/473

Abstract: The invention provides a compound of formula (I): or a salt thereof, wherein R1-R4 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.

Abstract translation: 本发明提供式（I）化合物或其盐，其中R 1 -R 4具有说明书中描述的任何值，以及包含式（I）化合物的组合物。 这些化合物可用作抗菌剂。

公开(公告)号：US20130237595A1

公开(公告)日：2013-09-12

申请号：US13822935

申请日：2011-09-16

Applicant: Richard H. Ebright ,  Yon W. Ebright

Inventor： Richard H. Ebright ,  Yon W. Ebright

IPC: C07D309/38 ,  C12N9/99

CPC classification number: C07D309/38 ,  A01N47/12 ,  A61K9/0019 ,  A61K31/366 ,  A61K47/18 ,  A61K47/44 ,  C07D309/22 ,  C12N9/99 ,  Y02A50/473

Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Ya, Yb, R1, R2, and G are as described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as inhibitors of bacterial RNA polymerase and as antibacterial agents.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其中Ya，Yb，R 1，R 2和G如说明书中所述，以及包含式（I）化合物的组合物。 该化合物可用作细菌RNA聚合酶和抗菌剂的抑制剂。

公开(公告)号：US20110178169A1

公开(公告)日：2011-07-21

申请号：US13058899

申请日：2009-08-14

Applicant: Alberdan Silva Santos ,  Edilene Oliveira Da Silva ,  Jose Luiz Martins do Nascimento ,  Claudio Naum Alves ,  Ana Paul Drumond Rodrigues ,  Antonio Sergio da Costa Carvalho

Inventor： Alberdan Silva Santos ,  Edilene Oliveira Da Silva ,  Jose Luiz Martins do Nascimento ,  Claudio Naum Alves ,  Ana Paul Drumond Rodrigues ,  Antonio Sergio da Costa Carvalho

IPC: A61K31/366 ,  C12N5/02 ,  C07D309/38 ,  A61P33/00

CPC classification number: C07D309/40 ,  A61K31/351 ,  A61K31/366 ,  Y02A50/409

Abstract: The present invention refers to the use of HMP (a secondary metabolite obtained from Aspergillus fungi) as an agent that intensifies the mechanism of macrophage activation, leading to the death of L. (Leishmania) amazonensis, the etiologic agent of cutaneous leishmaniasis. The main mechanism of action of this agent is the activation of the microbicidal activity of host cells, through increased superoxide production, number of lysosomes, actin and microtubule filament polymerization and increased spreading, typical of activated cells. Additionally, HMP represents a molecule of easy acquisition, presents an efficient combat mechanism with no adverse reactions and capacity to inhibit the development of promastigotes and amastigotes forms. Finally, results suggest HMP to be a potential candidate for use against cutaneous leishmaniasis at a minimal concentration of 50 μg/mL.

Abstract translation: 本发明涉及使用HMP（由曲霉属真菌获得的次生代谢物）作为增强巨噬细胞活化机制的药物，导致皮肤利什曼病的病原体亚马逊（Leishmania）亚马逊的死亡。 该药物的主要作用机制是通过增加超氧化物的产生，溶酶体的数量，肌动蛋白和微管丝聚合以及增加的活化细胞的典型活性来扩大宿主细胞的杀微生物活性。 另外，HMP代表一个容易获取的分子，提供了一种有效的作战机制，没有不利的反应和能力来抑制前鞭毛体和无花果的形成。 最后，结果表明，HMP在50μg/ mL的最低浓度下成为潜在的抗皮肤利什曼病的候选药物。

公开(公告)号：US07691883B2

公开(公告)日：2010-04-06

申请号：US10572639

申请日：2004-09-16

Applicant: Yoshitaka Tomigahara ,  Kiyoshi Higashi ,  Junya Takahashi ,  Chizuko Takahashi

Inventor： Yoshitaka Tomigahara ,  Kiyoshi Higashi ,  Junya Takahashi ,  Chizuko Takahashi

IPC: A61K31/44 ,  A61K31/366 ,  C07D309/38 ,  C07D405/12

CPC classification number: C07C47/55 ,  C07C235/16 ,  C07D309/26

Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):

Abstract translation: 本发明涉及由式（I）表示的肉桂酰基化合物：