公开(公告)号：US12208071B2

公开(公告)日：2025-01-28

申请号：US16969521

申请日：2019-02-13

Applicant: LIGAND PHARMACEUTICALS INCORPORATED

Inventor： Lin Zhi ,  Ian Henderson ,  Joseph Kaloko ,  Martin Osterhout

IPC: A61K31/185 ,  A61K31/155 ,  A61K31/366 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/455 ,  A61K31/64 ,  A61K31/702 ,  A61K31/7032 ,  A61K38/28 ,  A61K38/31 ,  A61K45/06 ,  C07C67/00 ,  C07C67/343 ,  C07C201/12 ,  C07C209/36 ,  C07C231/02 ,  C07C231/12 ,  C07C309/24 ,  C07C315/04 ,  C07C315/06

Abstract: Provided herein are solid state forms of compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions and methods of treating, preventing, ameliorating, delaying the time to onset or reducing the risk for the development or progression of at least one condition, disease, or disorder for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance, hyperglycemia, ketoacidosis, or ketosis.

公开(公告)号：US12162854B2

公开(公告)日：2024-12-10

申请号：US17054397

申请日：2019-05-10

Applicant: DAIKIN INDUSTRIES, LTD. ,  SAGA UNIVERSITY

Inventor： Masahiro Higashi ,  Yosuke Kishikawa ,  Tsugio Kitamura

IPC: C07C49/233 ,  C07C45/67 ,  C07C201/12 ,  C07C231/12 ,  C07D333/22 ,  C07C49/813 ,  C07C205/45 ,  C07C233/33

Abstract: A method for producing a fluoromethyl derivative represented by formula (1), the method including step A of reacting an alkene compound represented by formula (2) with a fluorine source represented by formula MFn, in the presence of a hypervalent-iodine aromatic compound (1a), or in the presence of an aromatic iodine compound (1b) and an oxidant (A) to fluorinate the alkene compound.

公开(公告)号：US20240294496A1

公开(公告)日：2024-09-05

申请号：US18292731

申请日：2022-08-29

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Mitsuo NAGAI ,  Takashi FUKUYAMA ,  Yasuaki KAMADA ,  Jun NIIJIMA ,  Hirofumi KURODA ,  Yuki KAROJI ,  Keiichi MURAKAMI ,  Masayuki OMORI ,  Yusuke MIYASHITA ,  Atsushi KAMADA ,  Masaaki MATSUDA

IPC: C07D401/12 ,  C07C201/12 ,  C07C253/30 ,  C07D209/08

CPC classification number: C07D401/12 ,  C07C201/12 ,  C07C253/30 ,  C07D209/08

Abstract: The invention provides a production process allowing more high-yield and efficient synthesis of key intermediates (compound (2i) or a salt thereof, and compound (1g)) for production of E7090, which is useful as an FGFR inhibitor.

公开(公告)号：US20240270677A1

公开(公告)日：2024-08-15

申请号：US18562130

申请日：2022-05-10

Applicant: BASF SE

Inventor： Thomas Schaub ,  Desislava Slavcheva Petkova ,  Jochen Dietz ,  Roland Goetz ,  A. Stephen K. Hashmi ,  Patrizio Orecchia

IPC: C07C201/12 ,  B01J31/24 ,  C07D213/82 ,  C07D231/40

CPC classification number: C07C201/12 ,  B01J31/24 ,  C07D213/82 ,  C07D231/40

Abstract: A process for preparing substituted biphenyls of the formula (I) which comprises reacting a compound of the formula (II) in the presence of a base and of a palladium catalyst, with an organoboron compound of the formula (IV).

公开(公告)号：US11970436B2

公开(公告)日：2024-04-30

申请号：US17749293

申请日：2022-05-20

Applicant: NEONC Technologies, Inc.

Inventor： Thomas Chen ,  Daniel Levin ,  Satish Puppali

IPC: C07C29/92 ,  A61K31/045 ,  A61K31/4188 ,  A61K45/06 ,  A61N5/10 ,  C07C29/78 ,  C07C29/86 ,  C07C29/88 ,  C07C67/14 ,  C07C201/12 ,  C07C201/16

CPC classification number: C07C29/92 ,  A61K31/045 ,  A61K31/4188 ,  A61K45/06 ,  A61N5/10 ,  C07C29/78 ,  C07C29/86 ,  C07C29/88 ,  C07C67/14 ,  C07C201/12 ,  C07C201/16 ,  C07B2200/07 ,  C07C2601/16 ,  C07C29/92 ,  C07C33/14 ,  C07C201/12 ,  C07C205/57 ,  C07C67/14 ,  C07C69/76 ,  C07C67/14 ,  C07C69/92

Abstract: The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.

公开(公告)号：US20230226228A1

公开(公告)日：2023-07-20

申请号：US17997908

申请日：2021-05-04

Applicant: The Research Foundation for the State University of New York

Inventor： Peter J. Tonge ,  Yong Li ,  Fareidoon Daryaee ,  Peter Michael Smith-Jones ,  Labros Meimetis

IPC: A61K51/04 ,  C07C201/12 ,  A61P31/04

CPC classification number: A61K51/0402 ,  C07C201/12 ,  A61P31/04

Abstract: This invention provides a composition comprising the compound having the structure:




ethyl 2-[19F]F-4-nitrobenzoate, and at least one acceptable carrier.
This invention also provides a method of detecting the presence of or location of bacteria cells in a subject which comprises determining if an amount of the compound or determining where an amount of the compound having the structure:




is present in the subject at a period of time after administration of the compound or salt thereof to the subject, thereby detecting the presence of or location of the bacteria cells based on the amount of the compound determined to be present in the subject or detecting the location of the bacteria cells based on the location of the compound determined to be present in the subject.

公开(公告)号：US20230086746A1

公开(公告)日：2023-03-23

申请号：US17490108

申请日：2021-09-30

Applicant: Zhen Ding Technology Co., Ltd.

Inventor： KUAN-WEI LEE ,  SZU-HSIANG SU ,  SHOU-JUI HSIANG ,  CHING-HSUAN LIN ,  WAN-LING HSIAO ,  REN-YU YEH

IPC: C08G73/16 ,  C07C229/60 ,  C07C41/09 ,  C07C201/12 ,  C07C227/04 ,  C08J5/18 ,  H05K1/03

Abstract: A diamine monomer compound with a structural formula of wherein n1 is an integer greater than 1, forms the basis of a dielectric material with reduced dielectric losses for improved signals transmission. A method for preparing the compound, a polyimide resin made from the compound, a flexible film, and an electronic device including the polyimide resin are also disclosed. The compound has a long but flexible even numbered carbon chain and a liquid crystal unit structure. The reduced regularity and rigidity of the molecular chain make the polyimide resin convenient for film-forming. Dimensional stability is improved, the coefficient of thermal expansion of the materials is reduced, and the materials have good mechanical and thermal properties, the electron loss factor and coefficient of thermal expansion of the materials being reduced.

公开(公告)号：US11542232B2

公开(公告)日：2023-01-03

申请号：US16798160

申请日：2020-02-21

Applicant: Journey Medical Corporation

Inventor： Anthony Adrian Shaw ,  Enrico Vigano ,  Renato Molteni

IPC: C07D207/12 ,  C07C309/73 ,  C07C303/22 ,  C07C201/12 ,  C07C309/30 ,  B01D9/00 ,  C07C63/24 ,  C07C67/08 ,  C07C69/608 ,  C07F11/00

Abstract: Provided herein are methods for the production of glycopyrronium tosylate and glycopyrronium tosylate compositions. Also provided herein are compositions useful in the production of glycopyrronium tosylate. Additionally provided herein are glycopyrronium tosylate compositions. Glycopyrronium tosylate is useful for the treatment of, among other conditions, hyperhidrosis.

公开(公告)号：US11479535B2

公开(公告)日：2022-10-25

申请号：US17113540

申请日：2020-12-07

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：US11447446B2

公开(公告)日：2022-09-20

申请号：US16907188

申请日：2020-06-20

Applicant: Fujian Yongjing Technology Co., Ltd

Inventor： Changyue Zhou ,  Hongjun Du ,  Wenting Wu

IPC: C07C253/30 ,  C01B21/083 ,  C07C67/307 ,  C07C201/12 ,  C07C303/22 ,  C07D317/42 ,  C07B39/00

Abstract: The invention relates to a use of a fluorination gas, and the elemental fluorine (F2) is present in a high concentration, for example, in a concentration of elemental fluorine (F2), especially of equal to much higher than 15 or even 20% by volume, and to a process for the manufacture of a fluorinated compound by direct fluorination employing a fluorination gas, wherein the elemental fluorine (F2) is present in a high concentration. The process of the invention is directed to the manufacture of a fluorinated compound, for the exception of fluorinated benzene, by direct fluorination. Especially the invention is of interest in the preparation of fluorinated organic compounds, final products and as well intermediates, for usage in agro-, pharma-, electronics-, catalyst, solvent and other functional chemical applications. The fluorination process of the invention may be performed batch-wise or in a continuous manner.