公开(公告)号：US20240285584A1

公开(公告)日：2024-08-29

申请号：US18478718

申请日：2023-09-29

Applicant: Allergan, Inc.

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

IPC: A61K31/417 ,  A61K31/17 ,  A61K31/197 ,  A61K31/198 ,  A61K31/216 ,  A61K31/4045 ,  C07C275/30 ,  C07C317/42 ,  C07C317/50 ,  C07C323/44 ,  C07C323/60 ,  C07D209/20 ,  C07D233/64 ,  C07K5/062 ,  C07K5/072 ,  C07K5/078

CPC classification number: A61K31/417 ,  A61K31/17 ,  A61K31/197 ,  A61K31/198 ,  A61K31/216 ,  A61K31/4045 ,  C07C275/30 ,  C07C317/42 ,  C07C317/50 ,  C07C323/44 ,  C07C323/60 ,  C07D209/20 ,  C07D233/64 ,  C07K5/06017 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/06156 ,  Y02A50/30

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

公开(公告)号：US20230233551A1

公开(公告)日：2023-07-27

申请号：US17815256

申请日：2022-07-27

Applicant: Novartis Pharmaceuticals Corporation

Inventor： Thomas GADEK ,  John BURNIER

IPC: A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/17 ,  G01N33/50 ,  G01N33/68 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/00 ,  G01N33/566 ,  A61B3/10 ,  A61B3/14

CPC classification number: A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/6872 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  G01N33/5047 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0053 ,  G01N33/566 ,  A61B3/101 ,  A61K9/0051 ,  A61B3/145 ,  G01N2333/70525 ,  G01N2500/02 ,  G01N2500/10 ,  G01N2333/705 ,  G01N2333/70546 ,  G01N2500/20 ,  G01N2500/04 ,  G01N2800/16

Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

公开(公告)号：US20230180761A1

公开(公告)日：2023-06-15

申请号：US18166601

申请日：2023-02-09

Applicant: CORTEVA AGRISCIENCE LLC

Inventor： RONALD J. HEEMSTRA ,  RONALD ROSS, JR. ,  KYLE A. DEKORVER ,  KAITLYN GRAY ,  DANIEL I. KNUEPPEL ,  PETER VEDNOR ,  TIMOTHY P. MARTIN ,  JOSEPH D. ECKELBARGER ,  JOHN F. DAEUBLE, SR. ,  RICKY HUNTER ,  DAVID A. DEMETER ,  TONY K. TRULLINGER ,  ERICH W. BAUM ,  ZOLTAN L. BENKO ,  NAKYEN CHOY ,  GARY D. CROUSE ,  FANGZHENG LI ,  JEFFREY NISSEN ,  MONICA B. OLSON ,  MICHELLE RIENER ,  THOMAS C. SPARKS ,  FRANK J. WESSELS ,  MAURICE C. YAP

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

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

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：US20180258031A1

公开(公告)日：2018-09-13

申请号：US15758446

申请日：2016-09-16

Applicant: Boehringer Ingelheim International GmbH

Inventor： Uwe Joerg Ries ,  Nizar HADDAD ,  Bo QU

IPC: C07C269/06 ,  C07F9/6571 ,  C07D307/58 ,  C07C315/04 ,  B01J31/02

CPC classification number: C07C269/06 ,  B01J31/0258 ,  B01J2231/34 ,  C07B2200/07 ,  C07C315/04 ,  C07C319/20 ,  C07C2601/10 ,  C07C2601/16 ,  C07D307/58 ,  C07D307/66 ,  C07F9/65683 ,  C07F9/6571 ,  C07F9/65744 ,  C07C271/22 ,  C07C323/43 ,  C07C317/50

Abstract: The invention relates to a method for the stereoselective preparation of compounds of formula (IV).

公开(公告)号：US20180230091A1

公开(公告)日：2018-08-16

申请号：US15751547

申请日：2016-08-10

Applicant: ALZHEON, INC.

Inventor： Petr KOCIS ,  Martin TOLAR ,  John HEY

IPC: C07C309/26 ,  C07C309/19 ,  A61P25/28

CPC classification number: C07C309/26 ,  A61P25/28 ,  C07B2200/07 ,  C07C309/19 ,  C07C309/27 ,  C07C317/50 ,  C07C323/59 ,  C07C323/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/14 ,  C07D207/16 ,  C07D209/20 ,  C07D211/58 ,  C07D233/26 ,  C07D295/185 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07K5/00 ,  C07K5/06165

Abstract: Compounds, pharmaceutical compositions, methods and kits are described for treating or preventing neurodegenerative diseases such as Alzheimer's disease.

公开(公告)号：US20180228772A1

公开(公告)日：2018-08-16

申请号：US15949335

申请日：2018-04-10

Applicant: Allergan, Inc.

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

IPC: A61K31/417 ,  C07D233/64 ,  C07C317/50 ,  C07C275/30 ,  C07C323/44 ,  C07C317/42 ,  A61K31/198 ,  A61K31/17 ,  C07K5/072 ,  C07K5/062 ,  C07K5/078 ,  A61K31/216 ,  A61K31/197 ,  A61K31/4045 ,  C07C323/60 ,  C07D209/20

CPC classification number: A61K31/417 ,  A61K31/17 ,  A61K31/197 ,  A61K31/198 ,  A61K31/216 ,  A61K31/4045 ,  C07C275/30 ,  C07C317/42 ,  C07C317/50 ,  C07C323/44 ,  C07C323/60 ,  C07D209/20 ,  C07D233/64 ,  C07K5/06017 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/06156 ,  Y02A50/401

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

公开(公告)号：US20180170877A1

公开(公告)日：2018-06-21

申请号：US15579111

申请日：2016-06-03

Applicant: LEAD PHARMA HOLDING B.V. ,  SANOFI

Inventor： Joseph Maria Gerardus Barbara CALS ,  Vera DE KIMPE ,  Sander Bernardus NABUURS

IPC: C07D213/75 ,  C07D213/82 ,  C07C317/50

CPC classification number: C07D213/75 ,  C07C311/20 ,  C07C317/44 ,  C07C317/50 ,  C07C2601/02 ,  C07C2601/04 ,  C07D207/06 ,  C07D209/08 ,  C07D211/16 ,  C07D211/26 ,  C07D211/60 ,  C07D213/82 ,  C07D215/08 ,  C07D217/02 ,  C07D223/16 ,  C07D231/40 ,  C07D241/04 ,  C07D261/08 ,  C07D277/46 ,  C07D285/135 ,  C07D295/13 ,  C07D295/192 ,  C07D307/52 ,  C07D333/36 ,  C07D417/04 ,  C07D495/04

Abstract: Compounds according to Formula I: or a pharmaceutically acceptable salt wherein: A1 is NR1 or CR1, with R1 herein; the cyclopropyl moiety with one or more methyl and one or more F; A2-A5 are N or CR2-CR5, with no more than two of the four positions A in A2-A5 can be simultaneously N; R2-R5 are described; R6 and R7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R6 and R7 together is carbonyl, all alkyl groups, if substituted with one or more F; R8 is H or C(1-6)alkyl; A9-A12 are N or CR9-CR12, with no more than two of the four positions A in A9-A12 can be simultaneously N; R9-R12 herein; R13 and R14 herein; or R13 and R14 fused forming a ring having 5 to 7 atoms by joining R13 being C(1-6)alkyl or C(2-6)alkenyl. The RORγ compounds can treat RORγ mediated diseases.

公开(公告)号：US20170369426A1

公开(公告)日：2017-12-28

申请号：US15615276

申请日：2017-06-06

Applicant: Achaogen, Inc.

Inventor： Brian D. Patterson ,  Qing Lu ,  James Bradley Aggen ,  Paola Dozzo ,  Ramesh Annasaheb Kasar ,  Martin Sheringham Linsell ,  Timothy Robert Kane ,  Micah James Gliedt ,  Darin James Hildebrandt ,  Glenn A. McEnroe ,  Frederick Cohen

IPC: C07C259/06 ,  C07D333/70 ,  C07C313/04 ,  C07C313/12 ,  C07D213/81 ,  C07D213/79 ,  C07D213/64 ,  C07C323/60 ,  C07C323/42 ,  C07C317/50 ,  C07C317/46 ,  C07C317/28 ,  C07D471/04 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08

CPC classification number: C07C259/06 ,  C07C313/04 ,  C07C313/12 ,  C07C317/28 ,  C07C317/46 ,  C07C317/50 ,  C07C323/42 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/64 ,  C07D213/79 ,  C07D213/81 ,  C07D333/70 ,  C07D471/04

Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.

公开(公告)号：US09795140B2

公开(公告)日：2017-10-24

申请号：US15092646

申请日：2016-04-07

Applicant: Dow AgroSciences LLC

Inventor： Timothy P. Martin ,  Joseph D. Eckelbarger ,  Ronald Ross, Jr. ,  Kyle DeKorver ,  Ronald J. Heemstra ,  Daniel I. Knueppel ,  Peter Vednor ,  Ricky Hunter ,  David A. Demeter ,  Tony K. Trullinger ,  Erich Baum ,  Zoltan 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 ,  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 ,  C07D215/38

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：US20170210723A1

公开(公告)日：2017-07-27

申请号：US15408503

申请日：2017-01-18

Applicant: Dow AgroSciences LLC

Inventor： Paul R. LePlae, JR. ,  Thomas Barton ,  Xin Gao ,  Jim Hunter ,  William C. Lo ,  Joshodeep Boruwa ,  Raghuram Tangirala ,  Gerald B. Watson ,  John Herbert

IPC: C07D317/62 ,  A01N37/20 ,  C07C317/28 ,  A01N37/34 ,  C07D305/08 ,  A01N43/20 ,  A01N43/30 ,  C07C323/42 ,  A01N41/10

CPC classification number: C07D317/62 ,  A01N37/20 ,  A01N37/34 ,  A01N41/10 ,  A01N43/20 ,  A01N43/30 ,  C07C255/57 ,  C07C317/28 ,  C07C317/50 ,  C07C323/42 ,  C07C323/60 ,  C07C2601/02 ,  C07D305/08

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, compositions containing such molecules, and processes of using such molecules and compositions against such pests. These molecules and compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).