公开(公告)号：US11649218B2

公开(公告)日：2023-05-16

申请号：US16976012

申请日：2019-03-08

Applicant: The USA, as represented by the Secretary, Dept. of Health and Human Services ,  Pontificia Universidad Católica de Chile

Inventor： Juan J. Marugan ,  Marc Ferrer ,  Noel T. Southall ,  Andres E. Dulcey ,  Xin Hu ,  Christopher R. Dextras ,  Daniel C. Talley ,  Alejandra Alvarez ,  Silvana Zanlungo ,  Rommy M. Von Bernhardi

IPC: A61K31/553 ,  A61P25/08 ,  A61P25/28 ,  A61P33/06 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  C07D267/20 ,  C07D413/10 ,  C07D413/14 ,  C07D243/38 ,  A61K31/5513 ,  A61K31/554 ,  C07C201/12 ,  C07C227/22 ,  C07C319/14 ,  C07D267/18 ,  C07D281/16 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07F5/02 ,  C07F7/08

CPC classification number: C07D243/38 ,  A61K31/553 ,  A61K31/554 ,  A61K31/5513 ,  A61P25/08 ,  A61P25/28 ,  A61P33/06 ,  A61P35/02 ,  C07C201/12 ,  C07C227/22 ,  C07C319/14 ,  C07D267/18 ,  C07D267/20 ,  C07D281/16 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07F5/025 ,  C07F7/0812

Abstract: Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

公开(公告)号：US20230113948A1

公开(公告)日：2023-04-13

申请号：US17787089

申请日：2020-12-17

Applicant: ARBUTUS BIOPHARMA CORPORATION

Inventor： Mahesh PALLERLA ,  Ganapati Reddy PAMULAPATI ,  Jan SPINK

IPC: A61K47/54 ,  C07D491/048 ,  C07D207/08 ,  C07C213/08 ,  C07H1/00 ,  C07H15/08 ,  C07C231/12 ,  C07C231/02 ,  C07D207/46 ,  C07C201/12 ,  C07C227/04 ,  C07C231/10 ,  C07C237/06 ,  C07C237/16 ,  C12N15/113 ,  A61K45/06

Abstract: The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.

公开(公告)号：US11623913B2

公开(公告)日：2023-04-11

申请号：US16830037

申请日：2020-03-25

Applicant: Sichuan University

Inventor： Fener Chen ,  Lin Dong ,  Yingqi Xia ,  Pei Tang ,  Youcai Xiao

IPC: C07C201/12 ,  C07C205/16 ,  B01J31/18

Abstract: Disclosed is a method of synthesizing a (1R,2R)-nitroalcohol compound of formula (I), as shown in the following reaction scheme, including: subjecting a compound of formula (II) and a compound of formula (III) to a condensation reaction in an organic solvent in the presence of a copper complex generated in situ from a chiral (1S,2R)-amino alcohol ligand and a cupric salt to produce the (1R,2R)-nitroalcohol compound of formula (I), where R1 and R2 are defined in the same manner as that in the specification. The method involves mild reaction conditions, excellent diastereoselectivity and high chemical yield, and thus it is suitable for industrial applications.

公开(公告)号：US20230091355A1

公开(公告)日：2023-03-23

申请号：US17797536

申请日：2021-02-02

Applicant: BASF AGRO B.V.

Inventor： Timo Frassetto ,  Florian Vogt ,  Christiane Alznauer ,  Sebastian Illies ,  Philip Muelheims ,  Swapnil Yerande ,  Daniel Saelinger ,  Robin Thiele ,  Heinz Rriedrich Sutoris ,  Marcel Hofrichte

IPC: C07C201/12 ,  C07C45/64

Abstract: The present invention relates to a process for the preparation of 1-[4-nitro-2-(trifluoromethyl)-phenyl]-alkanones and substituted phenoxyphenyl ketones.

公开(公告)号：US20230057608A1

公开(公告)日：2023-02-23

申请号：US17972220

申请日：2022-10-24

Applicant: MannKind Corporation

Inventor： Kelly Sullivan Kraft ,  John J. Freeman ,  Paul Serwinski ,  Vincent Pavia ,  Otto Phanstiel ,  Navneet Kaur

IPC: C07D241/08 ,  C07C201/12 ,  C07C67/39 ,  C07C67/30

Abstract: Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.

公开(公告)号：US11577233B2

公开(公告)日：2023-02-14

申请号：US17673220

申请日：2022-02-16

Applicant: UNIVERSITA DEGLI STUDI DI UDINE ,  INNOVATION FACTORY S.R.L.

Inventor： Walter Baratta ,  Salvatore Baldino ,  Steven Giboulot

IPC: B01J31/24 ,  C07B41/02 ,  C07F15/00 ,  C07C29/143 ,  C07C29/145 ,  C07C41/26 ,  C07C201/12 ,  C07C29/14 ,  B01J31/18

Abstract: The invention relates to monocarbonyl complexes of ruthenium and osmium with bi- and tridentate nitrogen and phosphine ligands. The invention relates to methods for preparing these complexes and the use of these complexes, isolated or prepared in situ, as catalysts for reduction reactions of ketones and aldehydes both via transfer hydrogenation or hydrogenation with hydrogen.

公开(公告)号：US11465958B2

公开(公告)日：2022-10-11

申请号：US16517546

申请日：2019-07-20

Applicant: Fujian Yongjing Technology Co., Ltd.

Inventor： Hongjun Du ,  Wenting Wu

IPC: C07C45/46 ,  B01J27/08 ,  C07C17/269 ,  C07C201/12 ,  C07C22/08 ,  C07C49/813 ,  C07C205/12

Abstract: The invention relates to a new process for the manufacture of fluoroaryl compounds and derivatives thereof, in particular of fluorobenzenes and derivatives thereof, and especially wherein said manufacture relates to an environmentally friendly production of the said compounds. Thus, the present invention overcomes the disadvantages of the prior art processes, and in a surprisingly simple and beneficial manner, and as compared to the prior art processes, in particular, the invention provides a more efficient and energy saving processes, and also provides a more environmentally friendly process, for the manufacture of nuclear fluorinated aromatics, and preferably of nuclear fluorinated fluorobenzenes. Accordingly, in one aspect of the invention, an industrially beneficial process for preparing fluorobenzenes from halobenzene precursors using HF to form hydrogen halide is provided by the present invention. A beneficial and surprisingly simple use of chlorobenzene as an industrially interesting starting material in the manufacture of fluorobenzene is provided.

公开(公告)号：US20220168723A1

公开(公告)日：2022-06-02

申请号：US17608589

申请日：2020-04-22

Applicant: ORGANO CORPORATION

Inventor： Shinji NAKAMURA ,  Hitoshi TAKADA ,  Hironao SAJIKI ,  Yoshinari SAWAMA ,  Tsuyoshi YAMADA

IPC: B01J35/04 ,  B01J41/07 ,  B01J41/05 ,  B01J39/04 ,  B01J23/44 ,  B01J35/02 ,  B01J35/10 ,  C07C45/68 ,  C07C201/12 ,  C07C253/30 ,  C07C17/263 ,  C07F7/08 ,  C07C67/343 ,  C07C1/32 ,  C07C2/86

Abstract: A method for forming a carbon-carbon bond, wherein a reaction is performed by filling a platinum group metal-supported catalyst into a filling container, and passing a raw material liquid through the platinum group metal-supported catalyst in a continuous circulation manner, and wherein the platinum group metal-supported catalyst is a platinum group metal-supported catalyst in which nanoparticles of a platinum group metal with an average particle diameter of 1 to 100 nm are supported on a non-particulate organic porous ion exchanger formed of a continuous framework phase and a continuous pore phase.

公开(公告)号：US11174211B2

公开(公告)日：2021-11-16

申请号：US16696790

申请日：2019-11-26

Applicant: Nevada Research & Innovation Corporation

Inventor： Wesley A. Chalifoux ,  Kyle C. Sproul ,  Wenlong Yang

IPC: C07C43/205 ,  C07C22/08 ,  C07C25/24 ,  C07C15/38 ,  C07C201/12 ,  C07C205/06 ,  C07C209/68 ,  C07C211/50 ,  C07C43/21 ,  C07D333/18 ,  C07C13/28 ,  C07C5/09 ,  C07C17/354 ,  C07C25/22 ,  C07C41/20 ,  C07C303/30 ,  C07C309/68 ,  C07D333/08 ,  C07F7/08 ,  C08G61/10

Abstract: Disclosed herein are embodiments of aryl compounds and polymers thereof that are made using methods that do not require harsh conditions or expensive reagents. The methods disclosed herein utilize precursor compounds that can be polymerized to form polycyclic aromatic hydrocarbons and polymers, such as carbon-based polymers like nanostructures (e.g., graphene or graphene-like nanoribbons).

公开(公告)号：US20210276954A1

公开(公告)日：2021-09-09

申请号：US17212514

申请日：2021-03-25

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Fujie TANAKA ,  Feng YIN

IPC: C07D209/54 ,  C07C201/12 ,  C07C205/51 ,  C07D207/16

Abstract: The present invention relates to a process for preparing 3-pyrrolidine carboxylic acid derivatives, and particularly a simple process for preparing 5-substituted 3-pyrrolidine carboxylic acid derivatives. In addition, the present invention relates to a novel pyrrolidine carboxylic acid derivative, its manufacture, pharmaceutical compositions containing it and its use as a catalyst.