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1. 发明申请

WO2023081800A1 ALPHA-2A ADRENERGIC RECEPTOR MODULATORS AND USES THEREOF 审中-公开
公开(公告)号：WO2023081800A1
公开(公告)日：2023-05-11
申请号：PCT/US2022/079276
申请日：2022-11-04
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , FRIEDRICH-ALEXANDER-UNIVERSITATERLANGEN-NURNBERG , CHINESE UNIVERSITY OF HONG KONG, SHENZHEN , GMEINER, Peter , HUBNER, Harald , SEEMANN, Philipp , PFEIFFER, Tara , DU, Yang , XU, Jun
发明人： SHOICHET, Brian, K. , FINK, Elissa, A. , BASBAUM, Allan, J. , BRAZ, Joao, M.
IPC分类号： A61K31/33 , A61K31/395 , A61K31/40
摘要： Described herein, inter alia, are 0.2 A adrenergic receptor agonists and uses thereof.

2. 发明申请

WO2023076586A1 DELIVERY OF THERAPEUTIC ALKALOID COMPOUNDS 审中-公开
公开(公告)号：WO2023076586A1
公开(公告)日：2023-05-04
申请号：PCT/US2022/048206
申请日：2022-10-28
申请人： SENSORIUM THERAPEUTICS, INC.
发明人： HOOKER, Jacob, M. , PLACZEK, Michael, S.
IPC分类号： A61K31/33 , A61K31/395 , A61K31/40
摘要： Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

3. 发明申请

WO2023044104A1 PHOSPHORAMIDATES FOR THE TREATMENT OF HEPATITIS B VIRUS 审中-公开
公开(公告)号：WO2023044104A1
公开(公告)日：2023-03-23
申请号：PCT/US2022/043978
申请日：2022-09-19
申请人： EMORY UNIVERSITY
发明人： BLUEMLING, Gregory , PAINTER, George
IPC分类号： A61K31/54 , A61K31/66 , C07F9/02 , A61K31/33 , A61K31/395 , C07F9/547 , A61K31/662
摘要： Disclosed are compounds and compositions to the treatment of infectious diseases and methods of treating such diseases. The compounds and compositions include derivatives of clevudine. The compounds and compositions include derivatives of clevudine in combination with another antiviral agent. The compounds and compositions include derivatives of clevudine in combination with a phosphoramidate of lamivudine, adefovir, tenofovir, telbivudine, entecavir, or combinations thereof.

4. 发明申请

WO2023039020A1 PROCESSES AND INTERMEDIATES FOR SYNTHESIS OF ADAGRASIB 审中-公开
公开(公告)号：WO2023039020A1
公开(公告)日：2023-03-16
申请号：PCT/US2022/042835
申请日：2022-09-08
申请人： MIRATI THERAPEUTICS, INC.
发明人： SCATTOLIN, Thomas , CHEN, Cheng , GHARBAOUI, Tawfik , GAN, Yonghong , ACHMATOWICZ, Michal , SNEAD, David
IPC分类号： A61K31/33 , A61K31/395 , C07D401/06 , C07D401/14 , C07D401/02
摘要： The present invention relates to improved synthetic routes of synthesizing adagrasib. The invention also provides intermediates used in the provided synthetic routes.

5. 发明申请

WO2023034965A2 CO-CRYSTALS 审中-公开
公开(公告)号：WO2023034965A2
公开(公告)日：2023-03-09
申请号：PCT/US2022/075902
申请日：2022-09-02
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： LI, Peng
IPC分类号： A61K31/33 , A61K31/395 , A61K31/495 , A61K31/519 , A61K31/18
摘要： The present invention relates to co-crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one with a co-crystal former, compositions comprising the same, as well as related methods of making and using such co-crystals.

6. 发明申请

WO2023019220A2 COMPOSITION AND METHODS FOR ALLEVIATING PAIN AND REDUCING AVERSIVENESS OF STIMULI 审中-公开
公开(公告)号：WO2023019220A2
公开(公告)日：2023-02-16
申请号：PCT/US2022/074863
申请日：2022-08-11
申请人： UNIVERSITY OF WASHINGTON
发明人： DHAKA, Ajay
IPC分类号： A61K31/44 , A61K31/33 , A61K31/4375 , A61K31/395
摘要： Use of 4-(Propan-2-yl)-N-(pyridin-4-yl)benzamide (C15H16N2O) and similar compounds to treat pain and reduce the aversiveness of negative stimuli is described. The treatments can alleviate pain, anxiety, and depression. Such treatment may reduce the perception of pain or experience of an aversive reaction to a stimulus. The treatments can activate particular portions of the brain region, such as a subpallium or a telencephalic region.

7. 发明申请

WO2023014979A1 CONJUGATES COMPRISING COVALENT BINDERS FOR TARGETING INTRACELLULAR KRAS G12C PROTEINS 审中-公开
公开(公告)号：WO2023014979A1
公开(公告)日：2023-02-09
申请号：PCT/US2022/039589
申请日：2022-08-05
申请人： RAYZEBIO, INC.
发明人： SMITH, Nicholas D. , HUDSON, Andrew
IPC分类号： A61K31/33 , A61K31/395 , C07D491/22 , A61K31/4738 , A61P35/00 , C07D403/04 , C07D471/04
摘要： Provided herein are radiopharmaceutical compositions, conjugates and uses thereof. In one aspect, provided herein are covalently modified KRAS proteins comprising a radiolabeled compound or conjugate. In some embodiments, the radiolabeled compound described herein comprises a covalently bound radioisotope. In some embodiments, the radiolabeled conjugate comprises a targeting ligand and a metal chelator configured to bind a radionuclide. The radiolabeled compound or conjugate described herein can form a covalent bond with a cysteine residue (such as G12C) in the mutated KRAS protein. Further provided herein are methods of treating and diagnosing cancer by administering the described radiolabeled compounds, conjugates, and compositions to a subject, thereby forming the covalently modified KRAS G12C protein.

8. 发明申请

WO2023007779A1 末梢神経損傷の治療のための医薬組成物审中-公开
公开(公告)号：WO2023007779A1
公开(公告)日：2023-02-02
申请号：PCT/JP2022/005504
申请日：2022-02-10
申请人：国立大学法人北海道大学
发明人：角家　健 , 山本　康弘
IPC分类号： A61K45/00 , A61K31/155 , A61K31/395 , A61K31/42 , A61K31/5377 , A61K39/395 , A61P25/02 , A61P43/00
摘要：本発明は、損傷末梢神経の実質外における好中球細胞外トラップ（Neurophil Extracellular Traps; NETs）の形成を抑制する物質、例えば損傷末梢神経への好中球の集積を阻害する物質、マクロファージ遊走阻止因子（Macrophage migration inhibitory factor; MIF）の発現を抑制する又は機能を阻害する物質等を含む、末梢神経損傷の治療のための医薬組成物を提供する。本発明はまた、損傷末梢神経の実質外におけるNETsの形成を抑制する活性、例えば損傷末梢神経への好中球の集積を阻害する活性、MIFの発現を抑制する活性又は機能を阻害する活性等を指標とした被験物質の末梢神経再生促進活性を評価する方法を提供する。

9. 发明申请

WO2023275649A1 COMPOSITIONS AND METHODS FOR INCREASING CANCER CELL SENSITIVITY TO ALTERNATING ELECTRIC FIELDS 审中-公开
公开(公告)号：WO2023275649A1
公开(公告)日：2023-01-05
申请号：PCT/IB2022/055589
申请日：2022-06-16
申请人： NOVOCURE GMBH
发明人： AVIGDOR, Lilach , VOLOSHIN-SELA, Tali
IPC分类号： A61N1/36 , A61K31/395 , A61K31/436 , A61K31/505 , A61K31/554 , A61P35/00 , A61P43/00 , A61N1/40 , A61N1/06 , A61N1/36002 , A61N1/403
摘要： Disclosed herein are methods of increasing sensitivity of a cancer cell to alternating electric fields comprising exposing the cancer cell to an alternating electric field for a period of time, the alternating electric field having a frequency and field strength, and exposing the cancer cell to an IGFR1 inhibitor, JNK inhibitor, RPS6 inhibitor or ERK inhibitor. Disclosed are methods of increasing treatment efficacy comprising applying an alternating electric field to a target site of the subject for a period of time, the alternating electric field having a frequency and field strength, wherein the target site comprises one or more cancer cells, and administering a therapeutically effective amount of one or more of an IGF1R inhibitor, JNK inhibitor, RPS6 inhibitor, and/or ERK inhibitor to the subject. Disclosed are methods of treating a subject having cancer comprising applying an alternating electric field to a target site of the subject for a period of time, the alternating electric field having a frequency and field strength, wherein the target site comprises one or more cancer cells, and administering a therapeutically effective amount of one or more of an IGF1R inhibitor, JNK inhibitor, RPS6 inhibitor, and/or ERK inhibitor to the subject. Disclosed are methods of reducing viability of cancer cells using an alternating electric field for a period of time, the alternating electric field having a frequency and field strength in combination with either an IGF1R inhibitor, JNK inhibitor, RPS6 inhibitor, and/or ERK inhibitor. Disclosed are methods of increasing apoptosis of a cancer cell comprising exposing the cancer cell to an alternating electric field for a period of time, the alternating electric field having a frequency and field strength; and exposing the cancer cell to an IGFR1 inhibitor, JNK inhibitor, RPS6 inhibitor or ERK inhibitor.

10. 发明申请

WO2022256690A1 CLEANING COMPOSITION AND METHOD FOR REMOVAL OF STAINS FROM ROOF SHINGLES 审中-公开
公开(公告)号：WO2022256690A1
公开(公告)日：2022-12-08
申请号：PCT/US2022/032217
申请日：2022-06-03
申请人： W.M. BARR & COMPANY, INC.
发明人： FARMER, Rachel, Ann , PETKUS, Matthew, Michael
IPC分类号： A61K31/395 , E04D13/002 , C09D5/1656 , C11D11/0052 , A61K8/44
摘要： A composition is provided containing a pH adjuster, a surfactant, and a solvent, wherein the composition has the ability to solubilize MAAs that creates dark streaks on roof shingles. The method of making the composition involves mixing a pH adjuster and a surfactant with water. A method of using is provided in which additional water is added to the composition. Once the composition is diluted and the desired alkalinity is reached, the composition is sprayed on a roof through a device having a spray/stream end. The output from the spray/stream end of the device transforms secreted MAA present on the roof shingles into an orange color upon contact. The resulting orange residue is then rinsed off from the shingles to provide a new looking roof.

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