公开(公告)号：US20230026791A1

公开(公告)日：2023-01-26

申请号：US17778124

申请日：2019-11-22

申请人： CRITICAL OUTCOME TECHNOLOGIES INC.

发明人： Arthur BROWN ,  Todd HRYCIW ,  Tony DURST ,  Clinton THRELFALL

IPC分类号： A61K31/167 ,  A61K31/40 ,  A61K31/445 ,  A61P25/00

摘要： The present application provides SOX9 inhibitor compounds and compositions and methods of use thereof. In certain aspects, the SOX9 inhibitor is a peptide comprising a portion of the SOX9 dimerization motif. In other aspects, the SOX9 inhibitor is a compound of the general formula I where one A is H and the other is: and the remaining substituents are as defined in the application.

公开(公告)号：US11559521B2

公开(公告)日：2023-01-24

申请号：US16834863

申请日：2020-03-30

申请人： William Bradley Worthington

发明人： William Bradley Worthington

IPC分类号： A61K31/135 ,  A61P23/02 ,  A61K31/445 ,  A61M25/00 ,  A61K31/407 ,  A61P29/00

摘要： A multimodal anti-emetic anesthetic/analgesic formulation for pain control not limited to postoperative pain control is described herein. The opioid-free/sparing anesthetic/analgesic formulation comprises a local anesthetic, an N-methyl-D-aspartate (NMDA) receptor antagonist, and a cyclooxygenase (COX) inhibitor such as Bupivacaine Hydrochloride, Ketamine Hydrochloride, and Ketorolac Tromethamine, which is effective to significantly reduce postoperative nausea and vomiting and enhance postoperative pain relief as compared to existing prior art anesthetics/analgesics. The formulation is administered to a mammal in need of anesthesia/analgesia and can be used as a preemptive and preventative multimodal analgesic. The formulation may have a buffer to enhance its shelf life and improve pharmacokinetics. The formulation may further comprise an alpha agonist, a steroid, a Transient Receptor Potential Channel agonist or antagonist, a beta-lactam antibiotic, a protein kinase inhibitor, a competitive or non-competitive glycine or glutamate antagonist, a glutamate or glycine inhibitor, a cyclooxygenase 3 inhibitor, or combinations thereof.

公开(公告)号：US20230020927A1

公开(公告)日：2023-01-19

申请号：US17942015

申请日：2022-09-09

申请人： AVACA PHARMA PRIVATE LIMITED

发明人： Mahesh Kandula

IPC分类号： A61K31/445 ,  A61K9/00

摘要： The present disclosure provides a pharmaceutical composition comprising H1 antagonist or a salt or a hydrate or a solvate thereof: a diluent; a solvent; an emollient; a humectant; a preservative; an emulsifier; and a surfactant, said composition being formulated as a topical formulation. The composition may include one or more additional active agents. The composition is formulated into a topical lotion, solution, spray, emulsion, emulsion of water and oil (oil in water or water in oil emulsion), gel, or cream. The compositions of the present disclosure may find utility in treatment of allergic conditions/diseases of skin. It further relates to a method of treating an allergic condition using the compositions of the present disclosure.

公开(公告)号：US11554113B2

公开(公告)日：2023-01-17

申请号：US16997164

申请日：2020-08-19

申请人： The Trustees of the University of Pennsylvania

发明人： Daniel J. Rader

IPC分类号： A61K31/4468 ,  A61K31/21 ,  A61K31/405 ,  A61K31/445 ,  A61K9/00 ,  A61K31/52

摘要： The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.

公开(公告)号：US11541044B2

公开(公告)日：2023-01-03

申请号：US17082125

申请日：2020-10-28

申请人： The Regents of the University of California ,  Leidos Biomedical Research, Inc.

发明人： Frank McCormick ,  Adam R. Renslo ,  David Turner ,  Stephan Gysin ,  Anna E. Maciag ,  Oleg Chertov

IPC分类号： C07D209/30 ,  C07D211/60 ,  A61K31/445 ,  A61P35/00 ,  A61K47/54 ,  C07D207/16 ,  C07D211/28

摘要： Provided herein, inter alia, are methods and compounds for inhibiting K-Ras and for treating cancer.

公开(公告)号：US20220411413A1

公开(公告)日：2022-12-29

申请号：US17872680

申请日：2022-07-25

申请人： Takeda Pharmaceutical Company Limited

发明人： Masami YAMADA ,  Shinkichi SUZUKI ,  Takahiro SUGIMOTO ,  Minoru NAKAMURA ,  Hiroki SAKAMOTO ,  Makoto KAMATA

IPC分类号： C07D405/14 ,  C07D209/46 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D401/06 ,  C07D405/04 ,  A61K31/4035 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/13 ,  A61K31/325 ,  A61K31/445 ,  A61K31/55 ,  A61K31/045 ,  A61K31/4406

摘要： The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like.
The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.

公开(公告)号：US11530191B2

公开(公告)日：2022-12-20

申请号：US17026690

申请日：2020-09-21

申请人： Global Blood Therapeutics, Inc.

发明人： Brian W. Metcalf ,  Zhe Li ,  Qing Xu ,  Stephen L. Gwaltney, II ,  Jason R. Harris ,  Calvin W. Yee

IPC分类号： C07D401/04 ,  C07D213/30 ,  A61K31/445 ,  A61K31/5375 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D471/04 ,  C07D257/04 ,  C07D487/04 ,  C07D231/56 ,  C07D211/62 ,  C07D213/64 ,  C07C65/30 ,  C07F7/08 ,  A61K8/49 ,  C07D211/70 ,  C07D213/69 ,  C07D227/08 ,  C07D405/04

摘要： Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

公开(公告)号：US11529342B2

公开(公告)日：2022-12-20

申请号：US16197674

申请日：2018-11-21

申请人： Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center

发明人： Guochuan Emil Tsai

IPC分类号： A61K31/47 ,  A61K31/11 ,  A61K31/12 ,  A61K31/13 ,  A61K31/16 ,  A61K31/19 ,  A61K31/22 ,  A61K31/235 ,  A61K31/245 ,  A61K31/35 ,  A61K31/382 ,  A61K31/5513 ,  A61K33/00 ,  A61K36/16 ,  A61K45/06 ,  A61K31/196 ,  A61P25/00 ,  A61K31/192 ,  A61K31/167 ,  A61K31/27 ,  A61K31/438 ,  A61K31/445

摘要： Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.

公开(公告)号：US11517546B2

公开(公告)日：2022-12-06

申请号：US17004665

申请日：2020-08-27

申请人： Centrexion Therapeutics Corporation

发明人： James N. Campbell ,  Arthur F. Michaelis

IPC分类号： A61K31/167 ,  A61K9/06 ,  A61K47/10 ,  A61K47/38 ,  A61K31/245 ,  A61K31/445 ,  A61K31/47 ,  A61K9/00 ,  A61K47/22

摘要： A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.

公开(公告)号：US20220378768A1

公开(公告)日：2022-12-01

申请号：US17330182

申请日：2021-05-25

申请人： Louis HABASH

发明人： Louis HABASH

IPC分类号： A61K31/445 ,  A61P35/00 ,  A61P25/00 ,  A61P31/00 ,  A61P9/10

摘要： Some embodiments disclosed herein include a method for decreasing an expression level of a gene. The methods can include identifying a human subject having an increased expression level of APEX1; and administering to the human subject an effective amount of a nitroxide antioxidant, whereby expression level of the gene is decreased.