公开(公告)号：US20230301974A1

公开(公告)日：2023-09-28

申请号：US18313428

申请日：2023-05-08

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Brian COCHRAN ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. MCGEE ,  Filisaty VOUNATSOS ,  Sean H. WIEDEMANN ,  Sarah WORTMAN

IPC: A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07C309/35 ,  C07D498/04 ,  C07D211/76

CPC classification number: A61K31/451 ,  C07D211/94 ,  C07D491/048 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07C309/35 ,  C07D498/04 ,  C07D211/76 ,  C07B2200/13

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US20210040120A1

公开(公告)日：2021-02-11

申请号：US17075864

申请日：2020-10-21

Applicant: AMGEN INC.

Inventor： Brian S. LUCAS ,  Nick A. PARAS

IPC: C07D513/10 ,  C07D513/08 ,  C07D498/00

Abstract: Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US20200062780A1

公开(公告)日：2020-02-27

申请号：US16569927

申请日：2019-09-13

Applicant: AMGEN INC.

Inventor： Sean P. BROWN ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Brian S. LUCAS ,  Nick A. PARAS ,  Joshua TAYGERLY ,  Marc VIMOLRATANA ,  Xianghong WANG ,  Ming YU ,  Manuel ZANCANELLA ,  Liusheng ZHU ,  Ana GONZALEZ BUENROSTRO ,  Zhihong LI

IPC: C07D513/10 ,  C07D498/00 ,  C07D513/08

Abstract: Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US20180092898A1

公开(公告)日：2018-04-05

申请号：US15820830

申请日：2017-11-22

Applicant: AMGEN INC.

Inventor： Matthew BIO ,  Sebastien CAILLE ,  Brian COCHRAN ,  Yuanqing FANG ,  Brian M. FOX ,  Brian S. LUCAS ,  Lawrence R. MCGEE ,  Filisaty VOUNATSOS ,  Sean H. WIEDEMANN ,  Sarah WORTMAN

IPC: A61K31/451 ,  C07C309/35 ,  C07C309/25 ,  C07C309/04 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

CPC classification number: A61K31/451 ,  C07B2200/13 ,  C07C309/04 ,  C07C309/25 ,  C07C309/35 ,  C07C313/02 ,  C07D211/76 ,  C07D211/94 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

公开(公告)号：US20170088560A1

公开(公告)日：2017-03-30

申请号：US15376456

申请日：2016-12-12

Applicant: AMGEN INC.

Inventor： Sean P. BROWN ,  Yunxiao LI ,  Mike Elias LIZARZABURU ,  Brian S. LUCAS ,  Nick A. PARAS ,  Joshua TAYGERLY ,  Marc VIMOLRATANA ,  Xianghong WANG ,  Ming YU ,  Manuel ZANCANELLA ,  Liusheng ZHU ,  Ana GONZALEZ BUENROSTRO ,  Zhihong LI

IPC: C07D513/10

CPC classification number: C07D513/10 ,  C07D513/08

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US20150045361A1

公开(公告)日：2015-02-12

申请号：US14520899

申请日：2014-10-22

Applicant: AMGEN INC.

Inventor： Yi CHEN ,  Timothy D. CUSHING ,  Jason A. DUQUETTE ,  Felix GONZALEZ LOPEZ DE TURISO ,  Xiaolin HAO ,  Xiao HE ,  Brian S. LUCAS ,  Lawrence R. MCGEE ,  Andreas REICHELT ,  Robert M. RZASA ,  Jennifer L. SEGANISH ,  Youngsook SHIN ,  Dawei ZHANG

IPC: C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D473/30 ,  C07D473/34

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Abstract translation: 取代的双环杂芳基和含有它们的组合物，用于治疗一般炎症，关节炎，风湿性疾病，骨关节炎，炎性肠病，炎症性眼病，炎症性或不稳定性膀胱病，牛皮癣，皮肤炎症成分的投诉，慢性炎性病症 不限于自身免疫疾病如系统性红斑狼疮（SLE），重症肌无力，类风湿性关节炎，急性播散性脑脊髓炎，特发性血小板减少性紫癜，多发性硬化症，Sjoegren综合征和自身免疫性溶血性贫血，包括所有形式的超敏反应的过敏症状 包括但不限于白血病，如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增生性疾病（MPD）慢性骨髓性白血病（MPD），介导，依赖或与p110δ活性相关的癌症的方法 （CML）T细胞急性淋巴细胞白血病（T-ALL）B细胞急性淋巴细胞白血病（B-ALL）非霍奇金淋巴瘤（NHL）B细胞淋巴瘤和实体瘤如乳腺癌。