公开(公告)号：US20240269304A1

公开(公告)日：2024-08-15

申请号：US18038435

申请日：2021-11-23

申请人： Novartis AG ,  Les Laboratoires Servier

发明人： Matthew T. Burger ,  Zhuoliang Chen ,  Joseph Anthony D'Alessio ,  Eric McNeill ,  Katsumasa Nakajima ,  Richard Vaughan Newcombe ,  Mark G. Palermo ,  Bing Yu ,  Qiang Zhang ,  Frédéric Colland ,  James Edward Paul Davidson ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  James Brooke Murray ,  Tibor Novak ,  Jérôme Benoit Starck

IPC分类号： A61K47/68 ,  A61P35/00

CPC分类号： A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61P35/00

摘要： Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure farther relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20240261372A1

公开(公告)日：2024-08-08

申请号：US18435440

申请日：2024-02-07

申请人： Novartis AG

发明人： BRIAN R. BOETTCHER ,  SHARI LYNN CAPLAN ,  DOUGLAS S. DANIELS ,  NORIO HAMAMATSU ,  STUART LICHT ,  STEPHEN CRAIG WELDON

IPC分类号： A61K38/18 ,  A61K38/00 ,  A61K45/06 ,  C07K14/50

CPC分类号： A61K38/1825 ,  A61K45/06 ,  C07K14/50 ,  A61K38/00 ,  C07K2319/30

摘要： The invention relates to the identification of fusion proteins comprising polypeptide and protein variants of fibroblast growth factor 21 (FGF21) with improved pharmaceutical properties. Also disclosed are methods for treating FGF21-associated disorders, including metabolic conditions.

公开(公告)号：US20240261284A1

公开(公告)日：2024-08-08

申请号：US18632528

申请日：2024-04-11

申请人： Novartis AG

发明人： Stephane FERRETTI ,  Sebastien JEAY

IPC分类号： A61K31/506 ,  A61K9/00 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K45/06

CPC分类号： A61K31/506 ,  A61K9/0019 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K45/06

摘要： The present disclosure relates to mdm2 inhibitors for use in specific dosing schedules. It was found that if sufficiently potent or, in alternative, sufficiently high dose of a Mdm2 inhibitor is used, it can cause antineoplastic effect by triggering much longer lasting antiproliferative mechanism in cells. The long lasting effect can sustain for several weeks after a single dose, which eliminates the need for daily treatment and allows administering the Mdm2i intermittently. A treatment with the intermittent dosing schedule of a Mdm2 inhibitor can be combined with a daily treatment of the Mdm2i or with another pharmaceutically acceptable ingredient.

公开(公告)号：US12054555B2

公开(公告)日：2024-08-06

申请号：US17127755

申请日：2020-12-18

申请人： NOVARTIS AG

发明人： Marta Cosenza ,  Christoph Heusser ,  Julia Neugebauer ,  Eveline Schaadt ,  Stefanie Urlinger ,  Maximilian Woisetschlaeger

IPC分类号： C07K16/28 ,  A61K9/00 ,  A61K9/08 ,  A61K9/19 ,  A61K9/20 ,  A61K39/395 ,  A61K47/10 ,  A61K47/18 ,  A61K47/26 ,  C07K14/705 ,  A61K39/00

CPC分类号： C07K16/2878 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/19 ,  A61K9/2018 ,  A61K39/39591 ,  A61K47/10 ,  A61K47/183 ,  A61K47/26 ,  C07K14/70578 ,  C07K16/2896 ,  A61K39/39533 ,  A61K39/3955 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73

摘要： Anti-BAFFR antibodies are formulated as lyophilisate or liquid formulation. The lyophilisates can be reconstituted to give a solution with a high concentration of the antibody active ingredient for delivery to a patient without high levels of antibody aggregation. The lyophilisate can be reconstituted with an aqueous reconstituent to provide an aqueous composition in which the antibody has a concentration of at least 50 mg/ml. The lyophilisate or aqueous pharmaceutical composition may include one or more of a sugar, a buffering agent, a surfactant, and/or a free amino acid.

公开(公告)号：US20240252668A1

公开(公告)日：2024-08-01

申请号：US18286664

申请日：2022-04-15

申请人： Anne-Sophie BLUEMMEL ,  Kathrin BUNTIN ,  Joseph Anthony D'ALESSIO ,  Liqiong FAN ,  Boris FESSLER ,  Doris GABRIEL ,  Dominik HAINZL ,  Keith HOFFMASTER ,  Shwetha IYER ,  Eshita KHERA ,  Eusebio Manchado ROBLES ,  Pierre MAUDENS ,  Dominik PISTORIUS ,  Roee RAMOT ,  Vincent ROMANET ,  Kuno WUERSCH ,  Padmaja YERRAMILLI-RAO ,  Novartis AG

发明人： Liqiong Fan ,  Dominik Hainzl ,  Roee Ramot ,  Shwetha Iyer ,  Joseph Anthony D'Alessio ,  Kuno Wuersch ,  Dominik Pistorius ,  Eusebio Manchado Robles ,  Kathrin Buntin ,  Doris Gabriel ,  Boris Fessler ,  Pierre Maudens ,  Vincent Romanet ,  Anne-Sophie Bluemmel ,  Keith Hoffmaster ,  Eshita Khera ,  Padmaja Yerramilli-Rao

IPC分类号： A61K47/68 ,  A61P35/00 ,  C07K11/02 ,  C07K14/47 ,  C07K16/28 ,  C12N9/00 ,  C12N9/02 ,  C12N9/04 ,  C12N9/18 ,  C12N15/52 ,  C12P21/02 ,  C12R1/01 ,  G01N33/574

CPC分类号： A61K47/6849 ,  A61K47/6811 ,  A61K47/6865 ,  A61P35/00 ,  C07K11/02 ,  C07K14/4722 ,  C07K16/28 ,  C12N9/0006 ,  C12N9/0073 ,  C12N9/18 ,  C12N9/93 ,  C12N15/52 ,  C12P21/02 ,  C12Y301/01001 ,  G01N33/57492 ,  C12R2001/01

摘要： This application discloses microorganisms and methods of producing GNAQ/GNA11 inhibitors and methods of making antibody drug conjugates of anti-PMEL17 antibodies or antigen binding fragments conjugated to a GNAQ/GNA11 inhibitor. The disclosure also relates to formulations comprising antibody drug conjugates of anti-PMEL 17 antibodies or antigen binding fragments conjugated to a GNAQ/GNA1 inhibitor and methods of treating or preventing cancer using the formulations.

公开(公告)号：US20240245670A1

公开(公告)日：2024-07-25

申请号：US17415923

申请日：2019-12-19

申请人： Novartis AG

发明人： Simone BONAZZI ,  Adam Crystal ,  John Scott Cameron ,  Eva Marie Genevieve D'Hennezel ,  Glenn Dranoff ,  Ry Roger Forseth ,  Dominik Johannes Hainzl ,  Jacqueline Kinyamu-Akunda ,  Guiqing Liang ,  Lilly Mary Petruzzelli

IPC分类号： A61K31/4545 ,  A61K9/00 ,  A61K31/55 ,  A61P35/00

CPC分类号： A61K31/4545 ,  A61K9/0053 ,  A61K31/55 ,  A61P35/00

摘要： The present disclosure relates to dosing regimens, formulations, and combinations comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione compounds or pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention IKAROS Family Zinc Finger 2 (IKZF2)-dependent diseases or disorders or where reduction of IKZF2 or IKZF4 protein levels can ameliorate a disease, for example, the treatment of cancers.

公开(公告)号：US20240245666A1

公开(公告)日：2024-07-25

申请号：US18559859

申请日：2022-05-10

申请人： Novartis AG

发明人： Stephanie Kay DODD ,  Florence HOURCADE-POTELLERET ,  Felix HUTH ,  Michelle QUINLAN ,  Julia ZACK

IPC分类号： A61K31/4439 ,  A61K31/506 ,  A61K45/06

CPC分类号： A61K31/4439 ,  A61K31/506 ,  A61K45/06

摘要： The present disclosure relates to dosing regimens and combinations comprising N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide or a pharmaceutically acceptable salt thereof, and their use for the treatment of breakpoint cluster region-abelson protein (BCR-ABL) mediated diseases or disorders.

公开(公告)号：US20240209097A1

公开(公告)日：2024-06-27

申请号：US18516831

申请日：2023-11-21

申请人： Novartis AG

发明人： Scott ROLLINS ,  Russell ROTHER ,  Jonathan STOCKER ,  Andreas BRUEDERLE

IPC分类号： C07K16/28 ,  A61P7/00

CPC分类号： C07K16/2854 ,  A61P7/00 ,  C07K2317/24 ,  C07K2317/76

摘要： The present invention relates to the treatment or prevention of P-selectin mediated disorders, and to anti-P-selectin antibodies or binding fragments thereof, for use in the treatment or prevention of such disorders. In particular, the invention relates to the treatment or prevention of pain crises associated with sickle cell disease, and to anti-P-selectin antibodies or binding fragments thereof, for use in the treatment or prevention of pain crises associated with sickle cell disease.

公开(公告)号：US20240199617A1

公开(公告)日：2024-06-20

申请号：US18221694

申请日：2023-07-13

申请人： Novartis AG

发明人： David R. Anderson ,  Robert A. Volkmann ,  Gregg F. Keaney ,  Steven C. Leiser ,  Sam Malekiani ,  Timothy Piser

IPC分类号： C07D487/04 ,  A61P25/28

CPC分类号： C07D487/04 ,  A61P25/28

摘要： Provided is 5-(3-chloro-4-fluorophenyl)-7-cyclopropyl-3-(2-(3-fluoro-3-methylazetidin-1-yl)-2-oxoethyl)-3,7-dihydro-4H-pyrrolo [2,3-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof, and their uses in the treatment of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system.

公开(公告)号：US12011449B2

公开(公告)日：2024-06-18

申请号：US17191205

申请日：2021-03-03

申请人： Novartis AG

发明人： Giordano Caponigro ,  Vesselina Cooke ,  Matthew John Meyer ,  Darrin Stuart

IPC分类号： A61K31/5377 ,  A61K31/4965 ,  A61P35/00

CPC分类号： A61K31/5377 ,  A61K31/4965 ,  A61P35/00

摘要： The present invention relates to a combination treatment which comprises (a) at least one ERK inhibitor preferably Compound B as described herein, and (b) a c-RAF inhibitor or a pharmaceutically acceptable salt thereof, preferably Compound A, which may be combined into a single pharmaceutical composition or prepared for separate or sequential administration. It includes a c-RAF inhibitor and an ERK inhibitor prepared for simultaneous, separate or sequential administration for the treatment of a proliferative disease, particularly an advanced solid tumor that harbors a Mitogen-activated protein kinase (MAPK) alteration, and includes methods of using these compounds in combination as well as a commercial package comprising such combination.