公开(公告)号：US10174008B2

公开(公告)日：2019-01-08

申请号：US15545858

申请日：2015-12-03

Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION

Inventor： Weiping Tang ,  Xiaoxun Li

IPC: B01J31/22 ,  B01J31/40 ,  C07B37/10 ,  C07B51/00 ,  C07D209/08 ,  C07D405/08

Abstract: Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(1)-containing catalyst.

公开(公告)号：US09969686B2

公开(公告)日：2018-05-15

申请号：US14818960

申请日：2015-08-05

Applicant: Wisconsin Alumni Research Foundation

Inventor： Weiping Tang ,  Xiaoxun Li ,  Dongxu Shu ,  Gabrielle N. Winston-McPherson

IPC: C07D403/06 ,  C07D209/14 ,  C07D405/14

CPC classification number: C07D209/14 ,  C07D209/12 ,  C07D403/06 ,  C07D405/14

Abstract: Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.

公开(公告)号：US20160039754A1

公开(公告)日：2016-02-11

申请号：US14818960

申请日：2015-08-05

Applicant: Wisconsin Alumni Research Foundation

Inventor： Weiping Tang ,  Xiaoxun LI ,  Dongxu Shu ,  Gabrielle N. Winston-McPherson

IPC: C07D209/14 ,  C07D405/14 ,  C07D403/06

CPC classification number: C07D209/14 ,  C07D209/12 ,  C07D403/06 ,  C07D405/14

Abstract: Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.

Abstract translation: 描述了制备二吲哚基甲烷和吲哚基/吡咯基甲烷的方法。该方法包括以下步骤：将包含芳基炔丙基部分和胺保护的，取代或未取代的苯胺部分的醚与取代或未取代的吲哚或取代或未取代的吡咯， 含金属催化剂的存在一段时间和在一定温度下引起产生二吲哚基甲烷或吲哚基/吡咯基甲烷的环状/芳基化级联反应。 所得化合物有效调节芳基烃受体的活性，抑制PCSK9的活性，并刺激哺乳动物中胰高血糖素样肽1的分泌。

公开(公告)号：US20220251071A1

公开(公告)日：2022-08-11

申请号：US17610896

申请日：2020-05-13

Applicant: Wisconsin Alumni Research Foundation

Inventor： Weiping Tang ,  Bo Wang ,  Suzhen Wu ,  Ka Yang

IPC: C07D401/14 ,  A61K31/496 ,  A61P35/00

Abstract: Compounds of the formula: pharmaceutical compositions containing the compounds, and methods of inhibiting neoplastic cell growth using the compounds and compositions.

公开(公告)号：US20200262819A1

公开(公告)日：2020-08-20

申请号：US16789887

申请日：2020-02-13

Applicant: Wisconsin Alumni Research Foundation

Inventor： Weiping Tang ,  Gabrielle N. Winston McPherson ,  Haibo Xie ,  Alan D. Attie ,  Mark Patrick Keller ,  Ka Yang

IPC: C07D403/06 ,  C07D401/14 ,  C07D413/14 ,  C07D409/06

Abstract: Described are benzoimidazole indolyl methane compounds, pharmaceutical compositions containing them, and use of the compounds to inhibit PCSK9-mediated ailments. The compounds have the structure:

公开(公告)号：US20180002318A1

公开(公告)日：2018-01-04

申请号：US15545858

申请日：2015-12-03

Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION

Inventor： Weiping Tang ,  Xiaoxun Li

IPC: C07D405/08 ,  B01J31/40 ,  B01J31/22 ,  C07B37/10 ,  C07D209/08 ,  C07B51/00

CPC classification number: C07D405/08 ,  B01J31/2265 ,  B01J31/4046 ,  B01J2231/325 ,  C07B37/10 ,  C07B51/00 ,  C07D209/08 ,  Y02P20/55

Abstract: Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst.

公开(公告)号：US20250090520A1

公开(公告)日：2025-03-20

申请号：US18695800

申请日：2022-09-26

Applicant: Wisconsin Alumni Research Foundation

Inventor： Timothy Scott Bugni ,  Weiping Tang ,  Le Guo ,  Changgui Zhao ,  Fan Zhang ,  Douglas R. Braun ,  David Andes ,  Miao Zhao ,  Jenna Lee Fossen

IPC: A61K31/4741 ,  A61K31/4196 ,  A61K31/429 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/7048 ,  A61K38/12 ,  A61P31/10 ,  C07D491/16

Abstract: Turbinmicin analogs of Formula I are provided. Compositions including Turbinmicin analogs of Formula I, such as pharmaceutical compositions including effective amounts of Turbinmicin analogs of Formula I for treating fungal infections such as Candida and Aspergillus, including drug-resistant strains thereof, are also disclosed. Methods of treating fungal infections with Turbinmicin analogs of Formula I and compositions thereof are disclosed.

公开(公告)号：US11059815B2

公开(公告)日：2021-07-13

申请号：US16800514

申请日：2020-02-25

Applicant: Wisconsin Alumni Research Foundation

Inventor： Weiping Tang ,  Ka Yang ,  Hao Wu ,  Zhongrui Zhang

IPC: C07D417/14 ,  C07D401/14

Abstract: Histone deacetylase (“HDAC”)-selective inhibitors covalently bonded to a linker covalently bonded to an E3 ubiquitin ligase ligand, and salts thereof; pharmaceutical compositions containing them; methods of using the composition to inhibit neoplastic cell growth in mammals, including humans.

公开(公告)号：US10508092B2

公开(公告)日：2019-12-17

申请号：US15689378

申请日：2017-08-29

Applicant: Wisconsin Alumni Research Foundation

Inventor： Wei Xu ,  Weiping Tang ,  Jitian Liu ,  Jill Kolesar

IPC: C07D307/79 ,  C07D307/77

Abstract: Disclosed are unnatural analogs of Diptoindonesin G, methods to make the analogs, pharmaceutical compositions containing the analogs, and methods of using the analogs to inhibit neoplastic cell growth.

公开(公告)号：US20180065945A1

公开(公告)日：2018-03-08

申请号：US15689378

申请日：2017-08-29

Applicant: Wisconsin Alumni Research Foundation

Inventor： Wei Xu ,  Weiping Tang ,  Jitian Liu ,  Jill Kolesar

IPC: C07D307/79

CPC classification number: C07D307/79 ,  C07D307/77

Abstract: Disclosed are unnatural analogs of Diptoindonesin G, methods to make the analogs, pharmaceutical compositions containing the analogs, and methods of using the analogs to inhibit neoplastic cell growth.