公开(公告)号：US11992531B2

公开(公告)日：2024-05-28

申请号：US17107781

申请日：2020-11-30

申请人： C4 Therapeutics, Inc.

发明人： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Minsheng He ,  Kiel Lazarski ,  Gesine Kerstin Veits ,  Harit U. Vora

IPC分类号： C07D401/14 ,  A61K31/45 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K47/54 ,  C07D211/86 ,  C07D211/88 ,  C07D211/90 ,  C07D221/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14 ,  C07D519/00 ,  C07K14/47 ,  C07K14/72

CPC分类号： A61K47/545 ,  A61K31/45 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/86 ,  C07D211/88 ,  C07D211/90 ,  C07D221/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D495/04 ,  C07D495/14 ,  C07D519/00 ,  C07K14/47 ,  C07K14/72

摘要： This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.

公开(公告)号：US20240150290A1

公开(公告)日：2024-05-09

申请号：US18272435

申请日：2022-01-05

申请人： Kenneth A. Jacobson ,  Young-Hwan Jung ,  Zhiwei Wen

发明人： Kenneth A. Jacobson ,  Young-Hwan Jung ,  Zhiwei Wen

IPC分类号： C07D211/34 ,  A61P25/02 ,  C07D205/04 ,  C07D205/12 ,  C07D207/08 ,  C07D209/52 ,  C07D211/62 ,  C07D221/04 ,  C07D221/22 ,  C07D223/04 ,  C07D225/02 ,  C07D249/06 ,  C07D261/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D451/06 ,  C07F9/6518

CPC分类号： C07D211/34 ,  A61P25/02 ,  C07D205/04 ,  C07D205/12 ,  C07D207/08 ,  C07D209/52 ,  C07D211/62 ,  C07D221/04 ,  C07D221/22 ,  C07D223/04 ,  C07D225/02 ,  C07D249/06 ,  C07D261/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D451/06 ,  C07F9/6518

摘要： Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R1-R8, X, Y, Z, X′, Y′, Z′, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

公开(公告)号：US20210371460A1

公开(公告)日：2021-12-02

申请号：US17149565

申请日：2021-01-14

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  Marie-Celine Frantz

IPC分类号： C07K5/08 ,  A61K31/454 ,  C07D211/58 ,  C07D401/12 ,  A61K47/64 ,  C07D417/12 ,  C07C237/16 ,  C07D209/46 ,  C07D211/94 ,  C07D221/22 ,  C07D209/44 ,  C07D279/06 ,  C07D471/08

摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

公开(公告)号：US11008337B2

公开(公告)日：2021-05-18

申请号：US16425407

申请日：2019-05-29

申请人： Turning Point Therapeutics, Inc.

发明人： Jingrong J. Cui ,  Yishan Li ,  Evan W. Rogers ,  Dayong Zhai ,  Wei Deng ,  Jane Ung

IPC分类号： A61K31/407 ,  A61K31/4353 ,  C07D209/56 ,  C07D221/22 ,  C07D498/22 ,  C07D498/14

摘要： The present disclosure relates to certain chiral diaryl macrocyclic derivatives, of the formula I: pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.

公开(公告)号：US10913726B2

公开(公告)日：2021-02-09

申请号：US16029267

申请日：2018-07-06

申请人： The Regents of the University of California ,  The Scripps Research Institute

发明人： Palmer Taylor ,  Zoran Radic ,  Karl Barry Sharpless ,  Valery Fokin ,  Rakesh Sit

IPC分类号： C07D295/13 ,  C07D221/22 ,  C07D223/04 ,  C07D451/02 ,  C07D471/08 ,  C07D209/56 ,  A61K31/55 ,  C07D223/06 ,  C07D451/14 ,  C07D487/08

摘要： In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps. In alternative embodiments, the invention provides pumps, devices, subcutaneous infusion devices, continuous subcutaneous infusion devices, infusion pens, needles, reservoirs, ampoules, a vial, a syringe, a cartridge, a disposable pen or jet injector, a prefilled pen or a syringe or a cartridge, a cartridge or a disposable pen or jet injector, a two chambered or multi-chambered pump, a syringe, a cartridge or a pen or a jet injector, comprising a compound of the invention.

公开(公告)号：US20210000818A1

公开(公告)日：2021-01-07

申请号：US16913404

申请日：2020-06-26

申请人： Alkermes Pharma Ireland Limited

发明人： Laura Cook Blumberg ,  Daniel R. Deaver ,  David J. Eyerman ,  Thomas Andrew Wynn

IPC分类号： A61K31/485 ,  C07D211/62 ,  C07D217/04 ,  C07D221/22 ,  C07D221/28 ,  C07D223/04 ,  C07D401/12 ,  C07D405/12 ,  C07D489/00 ,  C07D489/09

摘要： The present application relates methods for treating a depressive symptom comprising administering an effective amount of a μ opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.

公开(公告)号：US20200345718A1

公开(公告)日：2020-11-05

申请号：US16784574

申请日：2020-02-07

申请人： Alkermes Pharma Ireland Limited

发明人： Bernard Silverman ,  Fen-Ni Fu ,  Chengyun Guo

IPC分类号： A61K31/4748 ,  C07D221/28 ,  C07D221/22 ,  A61K31/485 ,  A61P25/30 ,  A61P25/36

摘要： The instant application relates to morphinan derivatives of Formula I with sustained effectiveness in treating drug toxicity and overdose:

公开(公告)号：US20200339514A1

公开(公告)日：2020-10-29

申请号：US16963026

申请日：2019-01-23

申请人： Gooddoctor Pharmaceutical Group Co., Ltd.

发明人： Yuefei Geng ,  Funeng Geng ,  Xiuying Ma ,  Ruobing Chao

IPC分类号： C07D221/22

摘要： The present invention relates to crystalline forms of mesaconine. Specifically, the present invention relates to crystalline form A, crystalline form B and crystalline form C of mesaconine and preparation methods thereof. In the method, the mesaconine is crystallized in solvent, and then the crude crystal is dried to obtain target crystalline form. The crystalline forms of mesaconine according to the present invention have good solubility, good stability, low hygroscopicity, long-term storage capability and good reproducibility, and have a good prospect to be developed as pharmaceuticals.

公开(公告)号：US10603313B2

公开(公告)日：2020-03-31

申请号：US16048051

申请日：2018-07-27

申请人： Chiromics, LLC

发明人： Joel Francis Austin ,  Michael David VanHeyst ,  James S. Harvey ,  Elizabeth Gerig Rowley ,  Christophe Lamarque-Lacoste

IPC分类号： A61K31/451 ,  A61K31/4545 ,  A61K38/07 ,  A61P25/04 ,  C07D401/06 ,  C07D401/04 ,  A61K31/439 ,  C07D401/12 ,  C07D211/96 ,  C07D401/14 ,  C07D221/22 ,  A61K31/506 ,  A61K38/17 ,  C07D209/52 ,  C07D207/48

摘要： Disclosed herein are compounds, of the class of amine-bearing heterocycles, which act as positive allosteric modulators and silent allosteric modulators of the mu opioid receptor. These compounds are useful for the treatment of pain, drug addiction, and other CNS derived maladies that are controlled directly or indirectly by activation of the mu opioid receptor. Methods for making and using the allosteric modulators disclosed herein are also provided.

公开(公告)号：US10457643B2

公开(公告)日：2019-10-29

申请号：US15848350

申请日：2017-12-20

申请人： Yale University

发明人： Seth Herzon ,  Maung Kyaw Moe Tun

IPC分类号： C07D221/22 ,  A61K31/439 ,  C07F7/10

摘要： The invention provides (1) processes for making substantially-pure (−) huperzine A and substantially-pure (−) huperzine A derivatives; (2) compositions useful in making substantially-pure (−) huperzine A and substantially-pure (−) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (−) huperzine A and substantially-pure (−) huperzine A derivatives.