公开(公告)号：US20250115622A1

公开(公告)日：2025-04-10

申请号：US18730357

申请日：2023-02-03

Applicant: AMGEN INC.

Inventor： Ron C. Kelly ,  Mary Chaves ,  Jing Teng ,  Stephan Parent ,  Markian Stec ,  Van Luu ,  Robert P. Farrell ,  James E. Huckle ,  Michal Achmatowicz ,  Tian Wu ,  Darren Leonard Reid ,  Lingyun Xiao

IPC: C07D519/00 ,  A61K31/553

Abstract: Disclosed herein are crystalline forms of (4S,7aR,9aR,10R,11E,14S,15R)-6′-chloro-10-methoxy-14,15-dimethyl-10-{[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl}-3′,4′,7a,8,9,9a,10,13,14,15-decahydro-2′H,3H,5H-spiro[1,19-etheno-1616-cyclobuta[i] [1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-4,1′-naphthalene]-16,16,18(7H,17H)-trione (AMG 397): (AMG 397), hydrates, and solvates thereof. Also disclosed are methods of making the crystalline forms, and methods of treating diseases and disorders with the crystalline forms.

公开(公告)号：US20240140966A1

公开(公告)日：2024-05-02

申请号：US18296211

申请日：2023-04-05

Applicant: AMGEN INC.

Inventor： Yosup Rew ,  Van Luu ,  Manuel Zancanella ,  Mary Chaves

IPC: C07D513/10

CPC classification number: C07D513/10

Abstract: Disclosed herein are crystalline and amorphous forms of (1S,3′R,6′R,7′S,8′E,11′S,12′R)-6-chloro-7′-methoxy-11′,12′-dimethyl-3,4-dihydro-2H, 15′H-spiro[naphthalene-1,22′-[20]oxa[13]thia[1,14]diazatetracyclo[14.7.2.03,6,019,24]pentacosa[8,16,18,24]tetraen]-15′-one 13′,13′-dioxide (AMG 176):




and salts and hydrates thereof. Also disclosed are methods of making the crystalline and amorphous forms, and methods of treating diseases and disorders with the crystalline and amorphous forms.

公开(公告)号：US20250122224A1

公开(公告)日：2025-04-17

申请号：US18730353

申请日：2023-02-03

Applicant: AMGEN INC.

Inventor： Ron C. Kelly ,  Mary Chaves ,  Jing Teng ,  Stephan Parent ,  Van Luu ,  Robert P. Farrell ,  James E. Huckle ,  Michal Achmatowicz ,  Tian Wu ,  Darren Leonard Reid ,  Lingyun Xiao

IPC: C07D519/00 ,  A61K31/553

Abstract: Disclosed herein are salt and solvate forms of (4S,7aR,9aR,10R,11E,14S,15R)-6′-chloro-10-methoxy-14,15-dimethyl-10-{[(9aR)-octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]methyl}-3′,4′,7a,8,9,9a,10,13,14,15-decahydro-2′H,3H,5H-spiro[1,19-etheno-16,16-cyclobuta[i][1,4]oxazepino[3,4-f][1,2,7]thiadlazacyclohexadecine-4,1 naphthalene]-16,16,18 (7H,17H)-trione (AMG 397): (AMG 397), such as crystalline salt and solvate forms thereof. Also disclosed are methods of making the salt and solvate forms, and methods of treating diseases and disorders with the salt and solvate forms.

公开(公告)号：US20150299182A1

公开(公告)日：2015-10-22

申请号：US14441133

申请日：2013-11-08

Applicant: Array BioPharma Inc. ,  Amgen Inc.

Inventor： Sylvie Asselin ,  Lisa Brett ,  Ying Chen ,  Donald T. Corson ,  Andrew Cosbie ,  Robert Farrell ,  Indrani W. Gunawardana ,  Jinkun Huang ,  Jonathan W. Lane ,  Dennis Lei ,  Christopher M. Lindemann ,  Van Luu ,  Coralee G. Mannila ,  Robert Milburn ,  Henry Morrison ,  Helming Tan ,  Jason Tedrow ,  Daniel J. Watson

IPC: C07D417/14

CPC classification number: C07D417/14 ,  C07B2200/13

Abstract: The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments.

Abstract translation: 本发明涉及（1S）-1- [5 - （{3 - [（2-甲基吡啶-3-基）氧基] -5-（吡啶-2-基硫烷基）吡啶-2-基} 氨基）-1,2,4-噻二唑-3-基]乙烷-1,2-二醇，包括这种结晶多晶型物的药物组合物及其制备方法。 本发明还涉及治疗糖尿病相关病症的方法，包括将这种固态形式或其组合物施用于受试者，以及在制备药物中使用这种结晶多晶型物。