公开(公告)号：US20230027339A1

公开(公告)日：2023-01-26

申请号：US17731534

申请日：2022-04-28

申请人： CAMURUS AB

发明人： Krister THURESSON ,  Fredrik Tiberg ,  Markus Johansson ,  Ian Harwigsson ,  Fredrik Joabsson ,  Markus Johnsson

IPC分类号： A61K9/127 ,  A61K8/04 ,  A61K8/37 ,  A61K8/55 ,  A61K8/67 ,  A61K8/92 ,  A61K9/00 ,  A61K9/12 ,  A61K9/70 ,  A61Q11/00 ,  A61Q19/00 ,  A61K47/10 ,  A61K8/49 ,  A61K31/155 ,  A61K31/198 ,  A61K31/416 ,  A61K31/4468 ,  A61K31/519 ,  A61K31/522 ,  A61K31/5513 ,  A61K31/5685 ,  A61K38/23 ,  A61K38/27 ,  A61K38/31 ,  A61K47/14 ,  A61K47/22 ,  A61K47/24 ,  A61Q3/02 ,  A61Q17/04 ,  A61K8/02 ,  A61K8/68 ,  A61K31/485

摘要： The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

公开(公告)号：US20220184013A1

公开(公告)日：2022-06-16

申请号：US17685661

申请日：2022-03-03

申请人： Io Therapeutics, Inc. ,  The Johns Hopkins University

发明人： Gabriel Ghiaur ,  Richard J. Jones ,  Salvador Alonso ,  Roshantha A. Chandraratna

IPC分类号： A61K31/196 ,  A61K45/06 ,  A61K31/192 ,  A61K31/4166 ,  A61K31/454 ,  A61K31/4196 ,  A61K31/138 ,  A61K31/58 ,  A61K31/4545 ,  A61K31/5685 ,  A61K31/277 ,  A61P35/00 ,  A61K31/69

摘要： Disclosed herein are methods for treating a cancer comprising administering to a subject in need thereof an effective dose of a CYP26-resistant retinoic acid receptor (RAR) alpha (RARα) selective agonist, whereby as a result of the treatment the tumor burden is reduced in the subject and cancer stem cells resident in the bone marrow are substantially reduced.

公开(公告)号：US20220089780A1

公开(公告)日：2022-03-24

申请号：US17411753

申请日：2021-08-25

申请人： Genentech, Inc.

发明人： Luc Desnoyers

IPC分类号： C07K16/40 ,  G01N33/50 ,  A61K31/506 ,  A61K31/475 ,  A61K31/4196 ,  A61K31/138 ,  A61K31/565 ,  A61K31/4745 ,  A61K31/517 ,  A61K31/5685 ,  A61K38/17 ,  G01N33/74 ,  A61K39/395 ,  A61K45/06 ,  C07K14/71 ,  G01N33/574

摘要： The invention concerns uses of anti-KLβ agents, and detection of KLβ and/or FGF19 and/or FGFR4.

公开(公告)号：US20220079955A1

公开(公告)日：2022-03-17

申请号：US17405984

申请日：2021-08-18

申请人： Antares Pharma, Inc.

发明人： Shaowei Ong

IPC分类号： A61K31/5685 ,  A61K47/44 ,  A61K47/14 ,  A61K9/00 ,  A61K9/10 ,  A61K9/107

摘要： Testosterone ester triglyceride formulations, optionally further including adducts. Methods of in-situ control of the manufacture or formation of such adducts are also described.

公开(公告)号：US11131677B2

公开(公告)日：2021-09-28

申请号：US16380876

申请日：2019-04-10

申请人： University of Washington

发明人： Bhagwat Prasad ,  Abdul Basit ,  Haeyoung Zhang ,  John K. Amory

IPC分类号： G01N33/74 ,  A61K31/5685 ,  A61K31/192 ,  A61K31/196 ,  A61K31/506 ,  A61K31/167 ,  A61P5/26 ,  G01N33/573 ,  A61K31/4365 ,  A61K9/00

摘要： Treatment of testosterone deficiency in men by a precision medicine approach using a biomarker of activity of UGT2B17 that is involved in testosterone urinary elimination. By inhibiting UGT2B17, alone or in combination with administration of testosterone, testosterone deficiency in men can be treatable. Further, a method of dose selection for precise dosing of UGT2B17 substrate drugs is provided. Additionally, methods for safe dosing of pharmaceutical agents that undergo UGT2B17-mediated acyl glucuronidation are provided.

公开(公告)号：US11123352B2

公开(公告)日：2021-09-21

申请号：US16847067

申请日：2020-04-13

申请人： Antares Pharma, Inc.

发明人： Shaowei Ong

IPC分类号： A61K31/5685 ,  A61K47/44 ,  A61K47/14 ,  A61K9/00 ,  A61K9/10 ,  A61K9/107

摘要： Testosterone ester triglyceride formulations, optionally further including adducts. Methods of in-situ control of the manufacture or formation of such adducts are also described.

公开(公告)号：US20210137865A1

公开(公告)日：2021-05-13

申请号：US17135238

申请日：2020-12-28

申请人： Io Therapeutics, Inc. ,  The John Hopkins University

发明人： Gabriel Ghiaur ,  Richard J. Jones ,  Salvador Alonso ,  Roshantha A. Chandraratna

IPC分类号： A61K31/196 ,  A61K45/06 ,  A61K31/192 ,  A61K31/4166 ,  A61K31/454 ,  A61K31/4196 ,  A61K31/138 ,  A61K31/58 ,  A61K31/4545 ,  A61K31/5685 ,  A61K31/277 ,  A61P35/00 ,  A61K31/69

摘要： Disclosed herein are methods for treating a cancer comprising administering to a subject in need thereof an effective dose of a CYP26-resistant retinoic acid receptor (RAR) alpha (RARα) selective agonist, whereby as a result of the treatment the tumor burden is reduced in the subject and cancer stem cells resident in the bone marrow are substantially reduced.

公开(公告)号：US10975079B2

公开(公告)日：2021-04-13

申请号：US15555152

申请日：2016-02-24

申请人： SCANDION ONCOLOGY A/S

发明人： Steffen Rump ,  Henning Weigt

IPC分类号： A61K31/15 ,  A61K31/519 ,  A61K31/565 ,  A61K31/566 ,  A61K31/5685 ,  A61K45/06 ,  C07D487/04 ,  A61K31/015

摘要： The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula (I) or pharmaceutically acceptable salts or propharmacons thereof for use as BCRP inhibitors, wherein at least one hydrogen atom in at least one of the phenyl groups A and B is substituted by a substituent RH, which has a Hammett constant σp greater than 0.23. For corresponding compounds, surprisingly a particularly high inhibitory activity against BCRP has been discovered which can be exploited for suppressing the multidrug resistance modulator BCRP, thus providing an improvement in efficacy of BCRP affected drugs. This has useful implications for cancer and HIV treatment.

公开(公告)号：US20210069169A1

公开(公告)日：2021-03-11

申请号：US16951783

申请日：2020-11-18

申请人： ENDORECHERCHE, INC.

发明人： Fernand LABRIE

IPC分类号： A61K31/453 ,  A61K9/00 ,  A61K31/56 ,  A61K31/5685

摘要： Novel methods for treating or reducing the likelihood of acquiring symptoms or diseases due to the menopause, in postmenopausal women, particularly osteoporosis, vaginal atrophy and dryness, hypogonadism, diminished libido, skin atrophy, connective tissue disease, urinary incontinence, breast, endometrial, ovarian and uterine cancers, hot flashes, loss of muscle mass, insulin resistance, fatigue, loss of energy, aging, physical symptoms of menopause, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor are disclosed. Said method comprising novel ways of administering and dosing dehydroepiandrosterone (DHEA) in order to take advantage of positive androgenic effects in the vaginal layers lamina propia and/or the layer muscularis, without undesirably causing systemic estrogenic effects in order to avoid the risk of breast and uterine cancer. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are also disclosed.

公开(公告)号：US20200254066A1

公开(公告)日：2020-08-13

申请号：US16637502

申请日：2018-08-07

申请人： INTERVENE IMMUNE, INC.

发明人： Gregory M. Fahy ,  Robert T. Brooke

IPC分类号： A61K38/27 ,  A61K31/5685

摘要： A combination of medications and medication doses is disclosed whereby age-related changes in systemic inflammation, cancer risk, heart disease risk, CD38 expression, hair color, thymotrophic hormones, immune cell populations, the CD4/CD8 cell ratio, bone marrow density, thymus structure, kidney function, and epigenetic age can be reversed in humans. Surprisingly, agents that accelerate the growth of cells reduce cancer risk, agents that intensify immune responses attenuate age-related inflammation, agents with no prior connection to hair color reverse age-related hair whitening, and a combination of agents that induces IGF-1, a hormone previously thought to drive systemic aging, results in a reversal of systemic aging as documented by an epigenetic clock. Medication combinations useful in the present invention include human growth hormone (GH) or GH releasers, dehydroepiandrosterone (DHEA), and metformin.