公开(公告)号：US12037324B2

公开(公告)日：2024-07-16

申请号：US17861809

申请日：2022-07-11

Applicant: Université de Montréal ,  Bristol-Myers Squibb Company

Inventor： Eldon Scott Priestley ,  Samuel Kaye Reznik ,  Edward H. Ruediger ,  James R. Gillard ,  Oz Scott Halpern ,  Wen Jiang ,  Jeremy Richter ,  Rejean Ruel ,  Sasmita Tripathy ,  Wu Yang ,  Xiaojun Zhang

IPC: C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

CPC classification number: C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

Abstract: The present invention provides compounds of Formula (I):




wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are biased agonists, or β-Arrestin agonists of the angiotensin II receptor, which may be used as medicaments.

公开(公告)号：US20240109889A1

公开(公告)日：2024-04-04

申请号：US18370186

申请日：2023-09-19

Applicant: C4 Therapeutics, Inc.

Inventor： Roger Norcross ,  Annick Goergler ,  Fabian Dey ,  Eric Andre Kusznir

IPC: C07D471/04 ,  C07D235/26 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/10 ,  C07D487/08

CPC classification number: C07D471/04 ,  C07D235/26 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/10 ,  C07D487/08

Abstract: The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

公开(公告)号：US20180105485A1

公开(公告)日：2018-04-19

申请号：US15842032

申请日：2017-12-14

Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

Inventor： Ming-Ming ZHOU ,  Michael OHLMEYER ,  Adam VINCEK ,  Nilesh ZAWARE

IPC: C07C225/20 ,  C07C237/40 ,  A61K31/5375 ,  A61K31/517 ,  A61K31/498 ,  A61K31/4965 ,  C07C229/68 ,  C07C229/48 ,  A61K31/4468 ,  A61K31/4409 ,  A61K31/4406 ,  A61K31/277 ,  C07C255/58 ,  A61K31/18 ,  C07C311/38 ,  A61K31/196 ,  C07C229/56 ,  C07C237/30 ,  A61K31/245 ,  C07C229/60 ,  C07D249/04 ,  C07D295/16 ,  C07D235/26 ,  C07D209/08 ,  C07D239/74 ,  C07D241/42 ,  C07D217/02 ,  C07D215/06 ,  C07D241/20 ,  C07D211/58 ,  C07D213/74 ,  C07D295/21 ,  C07D209/40 ,  C07D249/06 ,  C07D215/38 ,  C07D213/76 ,  C07D213/75 ,  A61K31/47 ,  A61K31/4402 ,  A61K31/44 ,  A61K31/4192 ,  A61K31/4184 ,  A61K31/404 ,  A61K31/195 ,  A61K31/166 ,  A61K31/136 ,  A61K45/06

CPC classification number: C07C225/20 ,  A61K31/136 ,  A61K31/166 ,  A61K31/18 ,  A61K31/195 ,  A61K31/196 ,  A61K31/245 ,  A61K31/277 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/517 ,  A61K31/5375 ,  A61K45/06 ,  C07C229/48 ,  C07C229/56 ,  C07C229/60 ,  C07C229/68 ,  C07C237/30 ,  C07C237/40 ,  C07C255/58 ,  C07C311/38 ,  C07D209/08 ,  C07D209/40 ,  C07D211/58 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D215/06 ,  C07D215/38 ,  C07D217/02 ,  C07D235/26 ,  C07D239/74 ,  C07D241/20 ,  C07D241/42 ,  C07D249/04 ,  C07D249/06 ,  C07D295/16 ,  C07D295/21 ,  A61K2300/00

Abstract: Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

公开(公告)号：US09944638B2

公开(公告)日：2018-04-17

申请号：US15136769

申请日：2016-04-22

Applicant: Janssen Sciences Ireland UC

Inventor： Ludwig Paul Cooymans ,  Samuël Dominique Demin ,  Lili Hu ,  Tim Hugo Maria Jonckers ,  Pierre Jean-Marie Bernard Raboisson ,  Abdellah Tahri ,  Sandrine Marie Helene Vendeville

IPC: C07D471/04 ,  C07D403/06 ,  C07D513/02 ,  C07D515/02 ,  A61K31/437 ,  A61P31/12 ,  C07D209/10 ,  C07D209/12 ,  C07D235/26

CPC classification number: C07D471/04 ,  C07D209/10 ,  C07D209/12 ,  C07D235/26 ,  C07D403/06

Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

公开(公告)号：US09822058B2

公开(公告)日：2017-11-21

申请号：US14390190

申请日：2013-03-13

Applicant: CHDI FOUNDATION, INC.

Inventor： Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Michael Prime ,  William Leonard Mitchell ,  Peter Johnson ,  Naomi Went

IPC: C07C62/38 ,  C07D307/94 ,  C07D309/10 ,  C07D215/18 ,  C07D311/58 ,  C07D317/46 ,  C07D317/60 ,  C07D319/18 ,  C07D233/64 ,  C07D235/26 ,  C07D403/10 ,  C07D405/08 ,  C07D405/10 ,  C07D405/12 ,  C07C317/44 ,  C07D413/08 ,  C07D413/10 ,  C07C323/62 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07D257/04 ,  C07D203/08 ,  C07D263/58 ,  C07C235/82 ,  C07D207/08 ,  C07D271/07 ,  C07D207/337 ,  C07D295/155 ,  C07D305/06 ,  C07D305/08 ,  C07D307/54 ,  C07D307/80 ,  C07C69/757 ,  C07D203/10 ,  C07D307/79 ,  C07D413/12 ,  C07H15/20

CPC classification number: C07C62/38 ,  C07C69/757 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07C235/82 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2602/50 ,  C07D203/08 ,  C07D203/10 ,  C07D207/08 ,  C07D207/337 ,  C07D215/18 ,  C07D233/64 ,  C07D235/26 ,  C07D257/04 ,  C07D263/58 ,  C07D271/07 ,  C07D295/155 ,  C07D305/06 ,  C07D305/08 ,  C07D307/54 ,  C07D307/79 ,  C07D307/80 ,  C07D307/94 ,  C07D309/10 ,  C07D311/58 ,  C07D317/46 ,  C07D317/60 ,  C07D319/18 ,  C07D403/10 ,  C07D405/08 ,  C07D405/10 ,  C07D405/12 ,  C07D413/08 ,  C07D413/10 ,  C07D413/12 ,  C07H15/20

Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

公开(公告)号：US20170327510A1

公开(公告)日：2017-11-16

申请号：US15520048

申请日：2016-07-07

Applicant: DIC Corporation

Inventor： Hitoshi KONDO ,  Yusuke OZAKI ,  Katsunori SHIMADA

IPC: C07D487/22 ,  C09B47/06 ,  C07D235/26 ,  G02B1/04 ,  G02B5/20

CPC classification number: C07D487/22 ,  C07D235/26 ,  C07D487/04 ,  C09B47/06 ,  C09B47/0676 ,  G02B1/04 ,  G02B5/20 ,  G02B5/223

Abstract: Provided is a phthalocyanine compound which has a green hue without having a halogen atom, and exhibits high luminance and an excellent coloring force at the time of being used for preparing a green pixel unit of a color filter. The phthalocyanine compound of the present invention has green hues without having a halogen atom, and exhibits high luminance and an excellent coloring force at the time of being used for preparing the green pixel unit of the color filter. In addition, the phthalocyanine compound can be used not only for the color filter, but also as a colorant for a wide range of applications as a general colorant such as printing ink, paint, colored plastic, toner, and ink for ink jet.

公开(公告)号：US20170291897A1

公开(公告)日：2017-10-12

申请号：US15508392

申请日：2015-09-03

Applicant: C4X Discovery Limited

Inventor： Emma Louise Blaney ,  Barrie Phillip Martin ,  Thorsten Nowak ,  Martin John Watson

IPC: C07D471/04 ,  C07D213/74 ,  C07D417/12 ,  C07D401/14 ,  C07C233/69 ,  C07D239/34 ,  C07D239/80 ,  C07D235/26 ,  C07D213/64 ,  C07D239/42 ,  C07D239/84 ,  C07D235/30 ,  C07D403/12 ,  C07D413/12 ,  C07C233/78 ,  C07C275/40 ,  C07D413/14 ,  C07D417/14 ,  C07D401/12

CPC classification number: C07D471/04 ,  C07C233/69 ,  C07C233/78 ,  C07C275/28 ,  C07C275/40 ,  C07D213/63 ,  C07D213/64 ,  C07D213/74 ,  C07D231/38 ,  C07D235/26 ,  C07D235/30 ,  C07D239/34 ,  C07D239/42 ,  C07D239/80 ,  C07D239/84 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to compounds that are inhibitors of the orexin-1 receptor. The compounds have the structural formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity.

公开(公告)号：US09732066B2

公开(公告)日：2017-08-15

申请号：US14923502

申请日：2015-10-27

Applicant: Hironori Otsu

Inventor： Hironori Otsu

IPC: C07D235/06 ,  C07D405/04 ,  C07D235/30 ,  C07D263/56 ,  C07D403/12 ,  A61K31/343 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D231/56 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D401/12 ,  C07D235/26 ,  C07D403/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D307/79

CPC classification number: C07D405/04 ,  A61K31/343 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/26 ,  C07D235/30 ,  C07D263/56 ,  C07D307/79 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.

公开(公告)号：US09724435B2

公开(公告)日：2017-08-08

申请号：US14196483

申请日：2014-03-04

Applicant: The University of Mississippi ,  The Board of Trustees of the Leland Stanford Junior University

Inventor： Christopher R. McCurdy ,  Christophe Mesangeau ,  Frederick T. Chin ,  Michelle L. James ,  Bin Shen ,  Sanjiv Gambhir ,  Sandip Biswal ,  Deepak Behera

IPC: A61K31/428 ,  C07D209/48 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D491/107 ,  C07D491/20 ,  A61K51/04 ,  C07D265/36 ,  C07D209/08 ,  C07D209/10 ,  C07D277/70 ,  C07D279/16 ,  C07D295/13 ,  C07D277/74

CPC classification number: A61K51/0468 ,  A61K31/428 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  C07D209/08 ,  C07D209/10 ,  C07D209/48 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D277/70 ,  C07D277/74 ,  C07D279/16 ,  C07D295/13 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D491/107 ,  C07D491/20

Abstract: A method for localizing and quantifying S1R role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an S1R selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased S1R density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SR1 selective compound or radioligand of the general formula III′, or IV′:

公开(公告)号：US09708267B2

公开(公告)日：2017-07-18

申请号：US14643107

申请日：2015-03-10

Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services

Inventor： Matthew B. Boxer ,  Min Shen ,  Douglas S. Auld ,  Craig J. Thomas ,  Martin J. Walsh

IPC: C07D215/227 ,  C07D209/30 ,  C07D215/36 ,  C07D223/16 ,  C07D265/36 ,  C07D209/12 ,  C07D209/34 ,  C07D235/26

CPC classification number: C07D215/227 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D215/36 ,  C07D223/16 ,  C07D235/26 ,  C07D265/36

Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2(I).