公开(公告)号：US12110263B2

公开(公告)日：2024-10-08

申请号：US17740260

申请日：2022-05-09

Applicant: CORTEXYME, INC.

Inventor： Andrei W. Konradi ,  Robert A. Galemmo, Jr. ,  Stephen S. Dominy ,  Casey C. Lynch ,  Leslie J. Holsinger

IPC: C07C233/62 ,  A61K31/165 ,  A61K31/167 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/655 ,  A61K45/06 ,  A61P25/00 ,  A61P31/04 ,  C07B59/00 ,  C07C233/78 ,  C07C235/10 ,  C07C235/50 ,  C07C237/42 ,  C07C245/08 ,  C07C247/16 ,  C07C247/18 ,  C07C317/28 ,  C07C323/40 ,  C07C323/42 ,  C07C381/00 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D257/04 ,  C07D261/12 ,  C07D401/12 ,  C07D413/12 ,  C07F5/02

CPC classification number: C07C233/62 ,  A61K31/165 ,  A61K31/167 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/655 ,  A61K45/06 ,  A61P25/00 ,  A61P31/04 ,  C07B59/001 ,  C07C233/78 ,  C07C235/10 ,  C07C235/50 ,  C07C237/42 ,  C07C245/08 ,  C07C247/16 ,  C07C247/18 ,  C07C317/28 ,  C07C323/40 ,  C07C323/42 ,  C07C381/00 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D257/04 ,  C07D261/12 ,  C07D401/12 ,  C07D413/12 ,  C07F5/02 ,  C07C2601/08

Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

公开(公告)号：US11998531B1

公开(公告)日：2024-06-04

申请号：US18539688

申请日：2023-12-14

Applicant: William Allen Boulanger ,  Zongbo Tong

Inventor： William Allen Boulanger ,  Zongbo Tong

IPC: A61K31/42 ,  C07D261/12

CPC classification number: A61K31/42 ,  C07D261/12

Abstract: Pharmaceutical intermediates and methods for efficiently preparing muscimol mono-BOC and derivatives thereof in the synthesis of muscimol and congeners and derivatives thereof.

公开(公告)号：US20230286904A1

公开(公告)日：2023-09-14

申请号：US18013431

申请日：2021-07-02

Applicant: BRIDGENE BIOSCIENCES, INC.

Inventor： Chao ZHANG ,  Michael J. BISHOP ,  Hang CHEN ,  Ping CAO

IPC: C07C233/25 ,  A61K45/06 ,  C07C233/27 ,  C07C251/42 ,  C07D333/32 ,  C07D333/36 ,  C07D213/643 ,  C07D311/68 ,  C07D215/38 ,  C07D213/64 ,  C07D261/08 ,  C07D231/12 ,  C07D231/54 ,  C07D261/20 ,  C07D271/06 ,  C07D249/06 ,  C07D309/14 ,  C07D261/12 ,  C07D217/24 ,  C07D213/40 ,  C07D237/08 ,  C07D275/02 ,  C07D205/04 ,  C07C233/23

CPC classification number: C07C233/25 ,  A61K45/06 ,  C07C233/23 ,  C07C233/27 ,  C07C251/42 ,  C07D205/04 ,  C07D213/40 ,  C07D213/64 ,  C07D213/643 ,  C07D215/38 ,  C07D217/24 ,  C07D231/12 ,  C07D231/54 ,  C07D237/08 ,  C07D249/06 ,  C07D261/08 ,  C07D261/12 ,  C07D261/20 ,  C07D271/06 ,  C07D275/02 ,  C07D309/14 ,  C07D311/68 ,  C07D333/32 ,  C07D333/36 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/50

Abstract: Disclosed herein are synthesis and use of covalent inhibitors selective for Transcriptional Enhancer Factor TEF-1 (TEAD1), which can be used for treatment of cancers such as glioblastoma, gastric cancer, colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and malignant pleural mesothelioma (MPM). Further disclosed herein are pharmaceutical compositions including the TEAD1 inhibitor and methods of treating cancers using the same.

公开(公告)号：US20230142714A1

公开(公告)日：2023-05-11

申请号：US17740260

申请日：2022-05-09

Applicant: CORTEXYME, INC.

Inventor： Andrei W. Konradi ,  Robert A. Galemmo, JR. ,  Stephen S. Dominy ,  Casey C. Lynch ,  Leslie J. Holsinger

IPC: C07C233/62 ,  C07D401/12 ,  A61K31/655 ,  A61K31/165 ,  C07C245/08 ,  C07C323/42 ,  C07C247/18 ,  C07D261/12 ,  C07C237/42 ,  C07D213/82 ,  A61K31/513 ,  C07D239/34 ,  C07D239/36 ,  A61P31/04 ,  C07F5/02 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/4409 ,  C07D413/12 ,  C07C323/40 ,  A61K31/4406 ,  A61K31/505 ,  C07C233/78 ,  C07C235/50 ,  A61K31/44 ,  C07D257/04 ,  A61K45/06 ,  C07D239/38 ,  C07C317/28 ,  A61K31/42 ,  C07C381/00 ,  C07D213/81 ,  A61K31/41 ,  C07D213/65 ,  C07C247/16 ,  C07D213/70 ,  C07B59/00 ,  A61K31/167 ,  C07C235/10 ,  C07D213/68 ,  A61P25/00

CPC classification number: C07C233/62 ,  C07D401/12 ,  A61K31/655 ,  A61K31/165 ,  C07C245/08 ,  C07C323/42 ,  C07C247/18 ,  C07D261/12 ,  C07C237/42 ,  C07D213/82 ,  A61K31/513 ,  C07D239/34 ,  C07D239/36 ,  A61P31/04 ,  C07F5/02 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/4409 ,  C07D413/12 ,  C07C323/40 ,  A61K31/4406 ,  A61K31/505 ,  C07C233/78 ,  C07C235/50 ,  A61K31/44 ,  C07D257/04 ,  A61K45/06 ,  C07D239/38 ,  C07C317/28 ,  A61K31/42 ,  C07C381/00 ,  C07D213/81 ,  A61K31/41 ,  C07D213/65 ,  C07C247/16 ,  C07D213/70 ,  C07B59/001 ,  A61K31/167 ,  C07C235/10 ,  C07D213/68 ,  A61P25/00 ,  C07C2601/08

Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

公开(公告)号：US20180194776A1

公开(公告)日：2018-07-12

申请号：US15806680

申请日：2017-11-08

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D249/08 ,  C07D263/56 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D237/04 ,  C07D213/80 ,  C07D213/79 ,  C07D277/46 ,  C07D333/40 ,  C07D261/12 ,  C07D249/12 ,  C07D213/81 ,  C07D231/14

CPC classification number: C07D498/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/04 ,  C07D237/24 ,  C07D239/34 ,  C07D239/36 ,  C07D241/24 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/12 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D263/56 ,  C07D271/06 ,  C07D277/46 ,  C07D277/56 ,  C07D307/68 ,  C07D333/40 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US09795139B2

公开(公告)日：2017-10-24

申请号：US15092641

申请日：2016-04-07

Applicant: Dow AgroSciences LLC

Inventor： Joseph D. Eckelbarger ,  Daniel I. Knueppel ,  Ronald J. Heemstra ,  Ronald Ross, Jr. ,  Kyle A. Dekorver ,  Kaitlyn Gray ,  Peter Vednor ,  Timothy P. Martin ,  Ricky Hunter ,  David A. Demeter ,  Tony K. Trullinger ,  Erich Baum ,  Zoltan L. Benko ,  Nakyen Choy ,  Gary Crouse ,  John F. Daeuble, Sr. ,  Fangzheng Li ,  Jeff Nissen ,  Michelle Riener ,  Tom Sparks ,  Frank Wessels ,  Maurice Yap

IPC: A01N53/00 ,  A01N43/90 ,  C07D207/273 ,  A01N43/82 ,  C07D307/33 ,  C07D277/36 ,  C07D263/26 ,  C07D261/12 ,  C07D333/48 ,  C07D307/52 ,  C07D277/30 ,  C07D213/56 ,  C07C237/22 ,  C07D333/60 ,  C07D233/80 ,  C07D487/04 ,  A01N43/707 ,  A01N43/653 ,  A01N43/60 ,  A01N43/40 ,  A01N41/10 ,  A01N37/34 ,  A01N37/22 ,  C07D253/07 ,  C07D241/20 ,  C07C317/14 ,  C07C233/65 ,  C07C233/63 ,  C07D209/49 ,  C07C381/10 ,  C07D205/04 ,  C07C237/42 ,  C07D207/10 ,  C07D207/452 ,  C07C255/29 ,  C07C255/57 ,  C07D285/06 ,  C07D295/32 ,  C07D305/08 ,  C07C255/46 ,  C07D213/75 ,  C07C255/60 ,  C07C259/10 ,  C07D213/81 ,  C07D213/84 ,  C07D309/14 ,  C07D213/89 ,  C07D215/227 ,  C07C271/28 ,  C07C271/66 ,  C07D215/38 ,  C07D231/12 ,  C07D331/04 ,  C07D231/56 ,  C07D333/36 ,  C07D233/36 ,  C07C311/08 ,  C07C311/46 ,  C07D235/30 ,  C07C317/28 ,  C07C317/40 ,  C07C317/50 ,  C07C323/41 ,  C07C323/42 ,  C07C323/59 ,  C07D249/08 ,  C07C331/12

CPC classification number: A01N53/00 ,  A01N37/22 ,  A01N37/34 ,  A01N41/10 ,  A01N43/40 ,  A01N43/60 ,  A01N43/653 ,  A01N43/707 ,  A01N43/82 ,  A01N43/90 ,  C07C233/63 ,  C07C233/65 ,  C07C237/22 ,  C07C237/42 ,  C07C255/29 ,  C07C255/46 ,  C07C255/57 ,  C07C255/60 ,  C07C259/10 ,  C07C271/28 ,  C07C271/66 ,  C07C311/08 ,  C07C311/46 ,  C07C317/14 ,  C07C317/28 ,  C07C317/40 ,  C07C317/50 ,  C07C323/41 ,  C07C323/42 ,  C07C323/59 ,  C07C331/12 ,  C07C381/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/10 ,  C07D207/273 ,  C07D207/452 ,  C07D209/49 ,  C07D213/56 ,  C07D213/75 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/227 ,  C07D215/38 ,  C07D231/12 ,  C07D231/56 ,  C07D233/36 ,  C07D233/80 ,  C07D235/30 ,  C07D241/20 ,  C07D249/08 ,  C07D253/07 ,  C07D261/12 ,  C07D263/26 ,  C07D277/30 ,  C07D277/36 ,  C07D285/06 ,  C07D295/32 ,  C07D305/08 ,  C07D307/33 ,  C07D307/52 ,  C07D309/14 ,  C07D331/04 ,  C07D333/36 ,  C07D333/48 ,  C07D333/60 ,  C07D487/04

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

公开(公告)号：US09737534B2

公开(公告)日：2017-08-22

申请号：US14840118

申请日：2015-08-31

Applicant: LUPIN LIMITED

Inventor： Nageswara Rao Irlapati ,  Gokul Keruji Deshmukh ,  Vijay Pandurang Karche ,  Santosh Madhukar Jachak ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC: C07D271/113 ,  A61K31/4245 ,  A61P19/02 ,  A61K31/497 ,  C07D261/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/423 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/496

CPC classification number: A61K31/497 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/496 ,  C07D261/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds of Formula (I), along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).

公开(公告)号：US09688692B2

公开(公告)日：2017-06-27

申请号：US15173870

申请日：2016-06-06

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D405/12 ,  C07D403/06 ,  C07D239/34 ,  C07D261/12 ,  C07D249/04 ,  C07D271/06 ,  C07D241/24 ,  C07D257/04 ,  C07D231/14 ,  C07D213/81 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D249/10 ,  C07D249/18 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

CPC classification number: C07D498/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/04 ,  C07D237/24 ,  C07D239/34 ,  C07D239/36 ,  C07D241/24 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/12 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D263/56 ,  C07D271/06 ,  C07D277/46 ,  C07D277/56 ,  C07D307/68 ,  C07D333/40 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US20170174672A1

公开(公告)日：2017-06-22

申请号：US15388516

申请日：2016-12-22

Applicant: AbbVie Deutschland GmbH & Co. KG

Inventor： Wilhelm Amberg ,  Udo Lange ,  Herve Geneste ,  Michael Ochse ,  Ralf Biesinger ,  Frank Oellien

IPC: C07D413/12 ,  C07D205/04 ,  C07C229/48 ,  C07C229/46 ,  C07D211/62 ,  C07D261/12 ,  C07D209/52 ,  C07D207/16 ,  C07D207/08 ,  C07D265/36 ,  C07C59/72 ,  C07D405/04 ,  C07D311/04

CPC classification number: C07D413/12 ,  C07C59/72 ,  C07C229/30 ,  C07C229/36 ,  C07C229/46 ,  C07C229/48 ,  C07C229/50 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/10 ,  C07C2602/38 ,  C07D205/04 ,  C07D207/06 ,  C07D207/08 ,  C07D207/16 ,  C07D209/52 ,  C07D209/94 ,  C07D211/32 ,  C07D211/62 ,  C07D261/12 ,  C07D265/36 ,  C07D265/38 ,  C07D311/04 ,  C07D311/58 ,  C07D405/04 ,  C07D405/14

Abstract: The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

公开(公告)号：US09670150B2

公开(公告)日：2017-06-06

申请号：US13863934

申请日：2013-04-16

Applicant: Allergan, Inc.

Inventor： Richard L. Beard ,  Tien Duong ,  John E. Donello ,  Veena Viswanath ,  Michael E. Garst

IPC: C07C309/15 ,  C07F9/40 ,  C07D257/04 ,  C07D261/12 ,  C07F9/38

CPC classification number: C07C309/15 ,  C07D257/04 ,  C07D261/12 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/4021

Abstract: The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.