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1. 发明授权

US12037600B2 Transfection complexes and methods of using the same 有权
公开(公告)号：US12037600B2
公开(公告)日：2024-07-16
申请号：US17397815
申请日：2021-08-09
申请人： MOLECULAR TRANSFER, INC.
发明人： Gulilat Gebeyehu , Joel Jessee
IPC分类号： C07K14/00 , C07K5/00 , C07K5/068 , C07K5/072 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/097 , C07K5/11 , C07K7/04 , C07K7/06 , C07K7/08 , C12N15/87
CPC分类号： C12N15/87 , C07K5/00 , C07K5/06086 , C07K5/06095 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K5/0817 , C07K5/0821 , C07K5/1019 , C07K7/04 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/001 , C07K2319/09 , C07K2319/80
摘要： Disclosed herein are transfection complexes comprising at least one cell surface ligand; at least one helper lipid component; and a transfection enhancer. Also disclosed are pharmaceutical compositions comprising the disclosed transfection complexes, and a pharmaceutically acceptable carrier. Further, disclosed are methods of transfecting a cell, the method comprising the steps of: obtaining a transfection complex as disclosed; and contacting a cell with the transfection complex.

2. 发明公开

US20240228535A1 PROTEASE INHIBITORS FOR TREATING OR PREVENTING CORONAVIRUS INFECTION 审中-公开
公开(公告)号：US20240228535A1
公开(公告)日：2024-07-11
申请号：US18513791
申请日：2023-11-20
申请人： Merck Sharp & Dohme LLC
发明人： John J. Acton, III , Mayuri Gupta , Michael J. Kelly, III , Franca-Maria Klingler , Mark Eric Layton , John A. McCauley , Gregori J. Morriello , Christopher Charles Nawrat , Craig A. Parish , Anthony J. Roecker , Manuel de Lera Ruiz , Jing Su , Valerie W. Shurtleff , Quang T. Truong
IPC分类号： C07K5/097 , A61K45/06
CPC分类号： C07K5/0821 , A61K45/06 , A61K38/00
摘要： The present invention provides a compound of Formula I

wherein R1, R2, R3, R4, R5, R6, R7, and subscripts x and n are as described herein and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for the treatment, inhibition, or amelioration of one or more disease states that could benefit from inhibition of a coronavirus, including SARS-CoV, MERS-CoV and SARS-CoV-2. The compounds of this invention could further be used in combination with other therapeutically effective agents, including but not limited to, other drugs useful for the treatment of coronavirus infection. The invention furthermore relates to processes for preparing compounds of Formula I, and pharmaceutical compositions which comprise compounds of Formula I and pharmaceutically acceptable salts thereof.

3. 发明授权

US12012467B2 Small molecule DCN1 inhibitors and therapeutic methods using the same 有权
公开(公告)号：US12012467B2
公开(公告)日：2024-06-18
申请号：US16496974
申请日：2018-03-28
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： Shaomeng Wang , Haibin Zhou , Jianfeng Lu , Liu Liu , Yi Sun , Denzil Bernard
IPC分类号： A61K31/426 , A61K31/427 , A61K31/428 , A61K31/454 , A61K31/5377 , A61K38/05 , A61K38/06 , A61K38/07 , A61K45/06 , C07D277/30 , C07D277/64 , C07D417/12 , C07K5/02 , C07K5/062 , C07K5/078 , C07K5/097 , C07K5/113 , C07K5/117 , C07K7/02
CPC分类号： C07K5/1021 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/454 , A61K31/5377 , A61K38/05 , A61K38/06 , A61K38/07 , A61K45/06 , C07D277/30 , C07D277/64 , C07D417/12 , C07K5/02 , C07K5/021 , C07K5/06026 , C07K5/06139 , C07K5/0821 , C07K5/1024 , C07K7/02
摘要： Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

4. 发明公开

US20240132542A1 TREATMENTS FOR DISEASES AND DISORDERS THAT INVOLVE OXIDATIVE STRESS 审中-公开
公开(公告)号：US20240132542A1
公开(公告)日：2024-04-25
申请号：US18206415
申请日：2023-06-06
申请人： Allegro Pharmaceuticals, LLC
发明人： Hampar L. Karageozian , Vicken H. Karageozian , John Y. Park
IPC分类号： C07K5/062 , A61K9/00 , A61K31/185 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , A61K38/12 , A61K47/20 , C07K5/083 , C07K5/09 , C07K5/093 , C07K5/097 , C07K5/103 , C07K5/12 , C07K7/06 , C07K7/64
CPC分类号： C07K5/06026 , A61K9/0048 , A61K31/185 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08 , A61K38/12 , A61K47/20 , C07K5/0806 , C07K5/081 , C07K5/0815 , C07K5/0817 , C07K5/0819 , C07K5/0821 , C07K5/1008 , C07K5/12 , C07K7/06 , C07K7/64
摘要： Peptide compounds and their use in treating diseases and disorders that cause, are caused by, or are characterized by cellular oxidative stress.

5. 发明公开

US20230312644A1 COMPOUNDS HAVING TRIPLE ACTIVITIES OF THROMBOLYSIS, ANTITHROMBOTIC AND RADICAL SCAVENGING 审中-公开
公开(公告)号：US20230312644A1
公开(公告)日：2023-10-05
申请号：US18181494
申请日：2023-03-09
申请人： Shanghai Lumosa Therapeutics Co., Ltd.
发明人： Shi-Qi Peng , Ming Zhao , Jian-Hui Wu , Yu-Ji Wang , Qi-Qi Feng
IPC分类号： C07K5/097 , C07D217/00 , C07K5/02 , C07K5/11 , C07K5/078 , A61K47/54 , A61K47/55
CPC分类号： C07K5/0821 , C07D217/00 , C07K5/0215 , C07K5/1019 , C07K5/06165 , A61K47/545 , A61K47/55 , A61K38/00
摘要： The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below:

wherein the definitions of T, Q, R1 and R2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

6. 发明授权

US10836791B2 Compounds 有权
公开(公告)号：US10836791B2
公开(公告)日：2020-11-17
申请号：US16332506
申请日：2017-09-13
申请人： DSM IP ASSETS B.V.
发明人： Marc Heidl , Eileen Jackson
IPC分类号： C07K5/083 , C07K5/097 , C07K5/08 , A61K47/54 , A61K8/64 , A61Q19/02
CPC分类号： C07K5/0808 , A61K47/542 , C07K5/0804 , C07K5/0821 , C07K5/0827 , A61K8/64 , A61Q19/02
摘要： The present invention relates to novel compounds which effectively inhibit the melanin synthesis in human melanocytes and are thus suitable for the treatment of senile lentigines, for smoothening skin color irregularities and/or for lightening natural skin color.

7. 发明授权

US10640533B2 Epoxyketone compounds for enzyme inhibition 有权
公开(公告)号：US10640533B2
公开(公告)日：2020-05-05
申请号：US15325998
申请日：2015-07-14
申请人： CENTRAX INTERNATIONAL, INC.
发明人： Jinfu Yang , Jian James Cen , Xiaoqing Michelle Fan
IPC分类号： C07K5/06 , C07K5/065 , C07K5/02 , C07K5/097 , C07K5/083 , A61K38/00
CPC分类号： C07K5/06078 , C07K5/0202 , C07K5/0806 , C07K5/0821 , A61K38/00
摘要： The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.

8. 发明申请

US20190142723A1 PRO-PIGMENTING PEPTIDES 审中-公开
公开(公告)号：US20190142723A1
公开(公告)日：2019-05-16
申请号：US16259176
申请日：2019-01-28
申请人： Sederma
发明人： Olivier Peschard , Philippe Mondon
IPC分类号： A61K8/64 , A61Q19/08 , C07K5/062 , A61Q19/00 , A61Q19/04 , A61Q5/10 , C07K5/078 , C07K5/083 , C07K5/103 , C07K5/097 , C07K5/093 , C07K5/087
CPC分类号： A61K8/64 , A61K38/00 , A61K2800/74 , A61Q5/10 , A61Q19/007 , A61Q19/04 , A61Q19/08 , C07K5/06026 , C07K5/06165 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008
摘要： The invention is directed to the use of at least one peptide of formula: X-(Xaa1)n-Pro*-(Xaa2)m-Y (I) With: —n=0, 1 or 2; —m=0 or 1 and if m=0 then n≠0 —Xaa1 is: —An hydrophobic aminoacid selected from Alanine (Ala, A), Valine (Val, V), Methionine (Met, M), Leucine (Leu, L), Isoleucine (Ile, I), Phenylalanine (Phe, F), Proline (Pro, P) and analogues and derivatives thereof; —A polar aminoacid selected from Serine (Ser, S), Threonine (Thr, T), Tyrosine (Tyr, Y), Asparagine (Asn, N), Glutamine (Gln, Q) and analogues and derivatives thereof; —or Glycine (Gly, G); When n=2 the two aminoacids Xaa1 can be the same or different; —Xaa2 is: —An hydrophobic aminoacid selected from Alanine (Ala, A), Valine (Val, V), Methionine (Met, M), Leucine (Leu, L), Isoleucine (Ile, I), Phenylalanine (Phe, F), Proline (Pro, P) and analogues and derivatives thereof; —A basic aminoacid selected from Arginine (Arg, R), Lysine (Lys, K) and Histidine (His, H) and analogues and derivatives thereof; —Glycine (Gly, G) or Serine (Ser, S); —At the N terminal end of the peptide, X is selected from H, —CO—R1 and —SO2—R1; —At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 or NR1R2, R1 and R2 being independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulphured, with the possibility to have in said group skeleton a O, S and/or N heteroatom; —Pro* corresponding to a Proline, an analogue or derivative thereof; Excluding the peptides where X=H and Y=OH, for a non therapeutical cosmetic pro-pigmenting treatment of skin. The invention also encompasses new tripeptides of formula (I) suitable for a non therapeutical cosmetic treatment of skin.

9. 发明授权

US09982015B2 Cyclin based inhibitors of CDK2 and CDK4 有权
公开(公告)号：US09982015B2
公开(公告)日：2018-05-29
申请号：US15192247
申请日：2016-06-24
申请人： University of South Carolina
发明人： Campbell McInnes , Padmavathy Nandha Premnath , Joshua K. Bolger
IPC分类号： A61K38/06 , C07K7/06 , C07K5/117 , A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , A61K38/06 , A61K38/07 , C07K5/0202 , C07K5/06095 , C07K5/06139 , C07K5/0821 , C07K5/101 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K14/4738
摘要： Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

10. 发明授权

US09834580B2 Pharmaceutical compositions comprising selective peptide-based agonists of melanocortin 1 receptor 有权
公开(公告)号：US09834580B2
公开(公告)日：2017-12-05
申请号：US14646410
申请日：2013-11-20
申请人： University of Cincinnati
发明人： Zalfa A. Abdel-Malek , Leonid Koikov , James J. Knittel
IPC分类号： A61K38/06 , A61K38/07 , C07K5/08 , C07K5/10 , A61K9/00 , C07K5/117 , C07K5/097 , A61K8/64 , A61Q19/00 , A61Q19/04 , A61Q19/08 , A61K8/06 , A61Q17/04 , A61K38/00
CPC分类号： C07K5/1024 , A61K8/06 , A61K8/64 , A61K9/0014 , A61K38/00 , A61K38/06 , A61K38/07 , A61Q17/04 , A61Q19/004 , A61Q19/04 , A61Q19/08 , C07K5/0821
摘要： Short tri- and tetrapeptides according to the following Formula I Ar(CH2)mX1—X2—CO—X3—X4—X5-(Trp)n-NX6R are potent, selective agonists of melanocortin 1 receptor (MC1R). Provided herein are pharmaceutical compositions including Formula I peptide agonists of MC1R and methods of treating skin diseases and disorders that include administering to an individual in need thereof a therapeutic amount of a Formula I peptide. The peptides, pharmaceutical compositions, and methods described herein are useful in the treatment of diseases and disorders that benefit from agonism of MCIR, including melanoma, basal cell carcinoma, squamous cell carcinoma, porphyria, polymorphous light eruption, vitiligo, and solar urticaria.

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