公开(公告)号：US11964025B2

公开(公告)日：2024-04-23

申请号：US17400387

申请日：2021-08-12

Applicant: Mersana Therapeutics, Inc.

Inventor： Aleksandr V. Yurkovetskiy ,  Natalya D. Bodyak ,  Bingfan Du ,  Dmitry R. Gumerov ,  Mariya Kozytska ,  Timothy B. Lowinger ,  Cheri A. Stevenson ,  Mao Yin

IPC: A61K47/65 ,  A61K38/07 ,  A61K47/68 ,  A61P35/00 ,  A61K47/54 ,  A61K47/60

CPC classification number: A61K47/6889 ,  A61K38/07 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6883 ,  A61K47/6885 ,  A61P35/00 ,  A61K47/549 ,  A61K47/60

Abstract: The present disclosure relates generally to antibody-drug conjugates comprising peptide-containing linkers and to methods of using these conjugates as therapeutics and/or diagnostics. Also disclosed herein are peptide-containing scaffolds useful to conjugate with a targeting moiety (e.g., an antibody), a drug, or both to produce the antibody-drug conjugates.

公开(公告)号：US20240058450A1

公开(公告)日：2024-02-22

申请号：US17804696

申请日：2022-05-31

Applicant: AbbVie Inc.

Inventor： Scott L. Ackler ,  Nathan B. Bennett ,  Erwin R. Boghaert ,  Steve C. Cullen ,  George Doherty ,  Robin R. Frey ,  Anthony R. Haight ,  Andrew S. Judd ,  Aaron R. Kunzer ,  Violeta L. Marin ,  Xiaoqiang Shen ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Xilu Wang ,  Dennie S. Welch ,  Michael D. Wendt

IPC: A61K45/06 ,  C07D417/14 ,  C07D513/04 ,  A61K47/68 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/538 ,  C07D487/04

CPC classification number: A61K45/06 ,  C07D417/14 ,  C07D513/04 ,  A61K47/6889 ,  A61K47/6803 ,  A61K47/6849 ,  C07D487/04 ,  A61K47/6883 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/538 ,  A61K47/6851

Abstract: The present disclosure concerns Bcl-xL inhibitors having low cell permeability, antibody drug conjugates (ADCs) comprising the inhibitors, synthons useful for synthesizing the ADCs, compositions comprising the inhibitors or ADCs, and various methods of using the inhibitors and ADCs.

公开(公告)号：US20240018208A1

公开(公告)日：2024-01-18

申请号：US18343689

申请日：2023-06-28

Applicant: Janssen Pharmaceutica NV

Inventor： Mark MACIELAG ,  Raymond J. PATCH ,  Rui ZHANG ,  Martin A. CASE ,  Mark J. WALL ,  Yue-Mei ZHANG

IPC: C07K14/575 ,  A61K47/68 ,  C07K16/24 ,  A61K9/00 ,  A61K38/17 ,  A61K38/26 ,  C07K1/06 ,  C07K1/107 ,  A61K47/64 ,  A61P3/10 ,  A61K49/00 ,  C07K1/12 ,  C07K1/18 ,  C07K5/02 ,  A61K47/60 ,  A61P3/08 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61K38/22 ,  A61K45/06 ,  C07K16/00

CPC classification number: C07K14/575 ,  A61K47/6845 ,  C07K16/24 ,  A61K47/68 ,  A61K47/6883 ,  A61K9/0019 ,  A61K38/1709 ,  A61K38/26 ,  C07K1/061 ,  C07K1/1072 ,  C07K14/57545 ,  A61K47/64 ,  A61P3/10 ,  A61K38/17 ,  A61K49/0032 ,  A61K49/0052 ,  A61K49/0056 ,  C07K1/12 ,  C07K1/18 ,  C07K5/0205 ,  A61K47/60 ,  A61P3/08 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61K38/22 ,  A61K45/06 ,  A61K47/6811 ,  C07K16/00 ,  C07K2317/14 ,  C07K2317/56 ,  C07K2317/71 ,  C07K2317/33 ,  A61K38/00

Abstract: The present invention comprises compounds of Formula I.






wherein:
Z4, Z7, Z9, Z11, Z22, Z23, Z26, Z30, Z34, Z35, p, m, n, q, and BRIDGE are defined in the specification. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel compounds are useful for preventing, treating or ameliorating diseases and disorders, such as obesity, type 2 diabetes, the metabolic syndrome, insulin resistance, and dyslipidemia, among others.

公开(公告)号：US20230405142A1

公开(公告)日：2023-12-21

申请号：US18208672

申请日：2023-06-12

Applicant: University of Massachusetts

Inventor： Sankaran Thayumanavan ,  Jiaming Zhuang

IPC: A61K47/68

CPC classification number: A61K47/6883

Abstract: The invention provides polymers and polymer-based nano-structures, in particular, polymers and polymer network to which biomolecules (e.g., proteins, antibodies, peptide aptamers) can be covalently conjugated and stably encapsulated therein and be controllably delivered and released upon degradation of the nano-structures in response to specific microenvironment, and compositions and methods of preparation and use thereof.

公开(公告)号：US20230365644A1

公开(公告)日：2023-11-16

申请号：US18154020

申请日：2023-01-12

Applicant: Janssen Pharmaceutica NV

Inventor： Mark MACIELAG ,  Raymond J. PATCH ,  Rui ZHANG ,  Martin A. CASE ,  Shamina M. RANGWALA ,  James N. LEONARD ,  Raul C. CAMACHO ,  Michael J. HUNTER ,  Katharine E. D'AQUINO ,  Wilson EDWARDS ,  Ronald V. SWANSON ,  Wenying JIAN ,  Yue-Mei ZHANG ,  Mark WALL ,  Ellen CHI

IPC: C07K14/575 ,  A61K47/68 ,  C07K16/24 ,  A61K9/00 ,  A61K38/17 ,  A61K38/26 ,  C07K1/06 ,  C07K1/107 ,  A61K47/64 ,  A61P3/10 ,  A61K49/00 ,  C07K1/12 ,  C07K1/18 ,  C07K5/02 ,  A61K47/60 ,  A61P3/08 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61K38/22 ,  A61K45/06 ,  C07K16/00

CPC classification number: C07K14/575 ,  A61K47/6845 ,  C07K16/24 ,  A61K47/68 ,  A61K47/6883 ,  A61K9/0019 ,  A61K38/1709 ,  A61K38/26 ,  C07K1/061 ,  C07K1/1072 ,  C07K14/57545 ,  A61K47/64 ,  A61P3/10 ,  A61K38/17 ,  A61K49/0032 ,  A61K49/0052 ,  A61K49/0056 ,  C07K1/12 ,  C07K1/18 ,  C07K5/0205 ,  A61K47/60 ,  A61P3/08 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61K38/22 ,  A61K45/06 ,  A61K47/6811 ,  C07K16/00 ,  C07K2317/14 ,  C07K2317/56 ,  C07K2317/71 ,  C07K2317/33 ,  A61K38/00

Abstract: The present invention comprises conjugates comprising a monoclonal antibody conjugated to a cyclic PYY peptide. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel conjugates are useful for preventing, treating or ameliorating diseases and disorders disclosed herein.

公开(公告)号：US11793880B2

公开(公告)日：2023-10-24

申请号：US17533002

申请日：2021-11-22

Applicant: Seagen Inc.

Inventor： Patrick J. Burke ,  Joel Courter

IPC: A61K47/55 ,  A61K47/68 ,  C07K5/02 ,  A61K47/65 ,  A61K47/64 ,  A61P35/02 ,  A61K9/00 ,  A61K9/08 ,  A61K31/454 ,  A61K38/05 ,  A61K38/06 ,  A61K38/00

CPC classification number: A61K47/551 ,  A61K9/0019 ,  A61K9/08 ,  A61K31/454 ,  A61K38/05 ,  A61K38/06 ,  A61K47/64 ,  A61K47/65 ,  A61K47/6811 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6883 ,  A61K47/6889 ,  A61P35/02 ,  C07K5/021 ,  A61K38/00

Abstract: Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.

公开(公告)号：US11767354B2

公开(公告)日：2023-09-26

申请号：US17168503

申请日：2021-02-05

Applicant: Janssen Pharmaceutica NV

Inventor： Mark Macielag ,  Raymond J. Patch ,  Rui Zhang ,  Martin A. Case ,  Shamina M. Rangwala ,  James N. Leonard ,  Raul C. Camacho ,  Michael J. Hunter ,  Katharine E. D'Aquino ,  Wilson Edwards ,  Ronald V. Swanson ,  Wenying Jian ,  Yue-Mei Zhang ,  Mark J. Wall ,  Ellen Chi

IPC: C07K14/575 ,  A61K47/68 ,  C07K16/24 ,  A61K9/00 ,  A61K38/17 ,  A61K38/26 ,  C07K1/06 ,  C07K1/107 ,  A61K47/64 ,  A61P3/10 ,  A61K49/00 ,  C07K1/12 ,  C07K1/18 ,  C07K5/02 ,  A61K47/60 ,  A61P3/08 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61K38/22 ,  A61K45/06 ,  C07K16/00 ,  A61K38/00 ,  A61K39/00

CPC classification number: C07K14/575 ,  A61K9/0019 ,  A61K38/17 ,  A61K38/1709 ,  A61K38/22 ,  A61K38/26 ,  A61K45/06 ,  A61K47/60 ,  A61K47/64 ,  A61K47/68 ,  A61K47/6811 ,  A61K47/6845 ,  A61K47/6883 ,  A61K49/0032 ,  A61K49/0052 ,  A61K49/0056 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07K1/061 ,  C07K1/1072 ,  C07K1/12 ,  C07K1/18 ,  C07K5/0205 ,  C07K14/57545 ,  C07K16/00 ,  C07K16/24 ,  A61K38/00 ,  A61K2039/505 ,  C07K2317/14 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/52 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/71 ,  C07K2317/92 ,  C07K2317/94 ,  C07K2319/30

Abstract: The present invention comprises conjugates comprising a monoclonal antibody conjugated to a cyclic PYY peptide. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel conjugates are useful for preventing, treating or ameliorating diseases and disorders disclosed herein.

公开(公告)号：US11759528B2

公开(公告)日：2023-09-19

申请号：US16213485

申请日：2018-12-07

Applicant: JenKem Technology Co., Ltd. (Beijing)

Inventor： Yanping Song ,  Wen Li ,  Jinliang Wang ,  Yan Liu ,  Kun Zheng ,  Meina Lin ,  Zhen Wei ,  Zewang Feng ,  Xuan Zhao

IPC: A61K47/68 ,  A61K31/4745 ,  C08G65/48 ,  A61P37/02 ,  A61P31/00 ,  A61P35/00 ,  C08G65/334 ,  C07C69/708 ,  A61K47/60 ,  C08G65/333 ,  A61K31/436 ,  A61K47/10 ,  A61K47/34 ,  C07C59/125 ,  C07C247/04 ,  C07C309/65 ,  C07D207/452 ,  C07D207/46 ,  C07K16/28 ,  C07K16/32

CPC classification number: A61K47/6855 ,  A61K31/436 ,  A61K31/4745 ,  A61K47/10 ,  A61K47/34 ,  A61K47/60 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6883 ,  A61P31/00 ,  A61P35/00 ,  A61P37/02 ,  C07C59/125 ,  C07C69/708 ,  C07C247/04 ,  C07C309/65 ,  C07D207/452 ,  C07D207/46 ,  C07K16/2809 ,  C07K16/32 ,  C08G65/334 ,  C08G65/3332 ,  C08G65/3344 ,  C08G65/33303 ,  C08G65/33317 ,  C08G65/48 ,  C07K2317/94

Abstract: A PEG linker as represented by formula (I), wherein n and m are respectively an integer from 1 to 7, providing the PEG linker with 1 to 49 linking sites. A ligand drug conjugate as represented by formula (II). The conjugate uses the PEG linker to increase a drug loading capacity and drug loading diversity, thereby improving pharmaceutical efficacy.

Y1-PEG1-{R1-PEG2-{Y4}n}m  (I)

TM-{R2-PEG1-{R1-PEG2-{R3-A′-drug}n}m}l  (II)

公开(公告)号：US20190241649A1

公开(公告)日：2019-08-08

申请号：US16382735

申请日：2019-04-12

Applicant: Asana BioSciences, LLC

Inventor： Roger A. Smith ,  Nitin K. Damle ,  Aleksandr V. Yurkovetskiy ,  Mao Yin ,  Timothy B. Lowinger ,  Joshua D. Thomas ,  Cheri A. Stevenson ,  Venu R. Gurijala

IPC: C07K16/18 ,  A61K47/68 ,  A61K47/59

CPC classification number: C07K16/18 ,  A61K47/59 ,  A61K47/6843 ,  A61K47/6883

Abstract: A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.

公开(公告)号：US20190216945A1

公开(公告)日：2019-07-18

申请号：US16334301

申请日：2017-10-13

Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION

Inventor： Jiyuan Yang ,  Jindrich Kopecek ,  Libin Zhang ,  Yixin Fang

IPC: A61K47/68 ,  A61K47/58 ,  C07K16/28 ,  A61P35/00

CPC classification number: A61K47/6883 ,  A61K31/337 ,  A61K31/351 ,  A61K38/07 ,  A61K39/395 ,  A61K47/58 ,  A61K2039/505 ,  A61P35/00 ,  C07K16/2803 ,  C07K16/2887 ,  C07K2317/92 ,  C07K2319/035

Abstract: Disclosed herein, are antibody-polymer-drug conjugates. The conjugate comprises a targeting moiety, one or more polymers, and one or more therapeutic agents. Also described herein, are compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.