CN114728954A - Tropifexor的新晶型及其制备方法 - Google Patents

Tropifexor的新晶型及其制备方法 Download PDF

Info

Publication number
CN114728954A
CN114728954A CN202080080614.9A CN202080080614A CN114728954A CN 114728954 A CN114728954 A CN 114728954A CN 202080080614 A CN202080080614 A CN 202080080614A CN 114728954 A CN114728954 A CN 114728954A
Authority
CN
China
Prior art keywords
tropifexor
crystal form
acid
ray powder
degrees
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CN202080080614.9A
Other languages
English (en)
Other versions
CN114728954B (zh
Inventor
张�杰
廖伟龙
邝润桥
徐巾超
陈勇
罗忠华
黄芳芳
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sunshine Lake Pharma Co Ltd
Original Assignee
Sunshine Lake Pharma Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sunshine Lake Pharma Co Ltd filed Critical Sunshine Lake Pharma Co Ltd
Publication of CN114728954A publication Critical patent/CN114728954A/zh
Application granted granted Critical
Publication of CN114728954B publication Critical patent/CN114728954B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明提供了Tropifexor的新晶型及其制备方法，属于药物化学领域。所述晶型为晶型II。所述晶型II的XRPD图含有如下2θ(误差±0.2度)值的特征峰：5.7,6.9,9.1,10.0,11.1,12.0,14.4,16.4,17.4,20.5,20.9,21.6,23.1,23.8,25.3和26.2度。所述晶型II均具有较好的溶解性和稳定性，有利于储存、转移、生产工艺中操作，适于制备成制剂。

Description

PCT国内申请，说明书已公开。

Claims (11)

  1. PCT国内申请，权利要求书已公开。
CN202080080614.9A 2019-11-29 2020-11-11 Tropifexor的新晶型及其制备方法 Active CN114728954B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201911203282 2019-11-29
CN2019112032824 2019-11-29
PCT/CN2020/128097 WO2021104022A1 (zh) 2019-11-29 2020-11-11 Tropifexor的新晶型及其制备方法

Publications (2)

Publication Number Publication Date
CN114728954A true CN114728954A (zh) 2022-07-08
CN114728954B CN114728954B (zh) 2023-10-17

Family

ID=76130247

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080080614.9A Active CN114728954B (zh) 2019-11-29 2020-11-11 Tropifexor的新晶型及其制备方法

Country Status (2)

Country Link
CN (1) CN114728954B (zh)
WO (1) WO2021104022A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021233461A1 (zh) * 2020-05-22 2021-11-25 苏州晶云药物科技股份有限公司 苯并噻唑类化合物的新晶型及其制备方法
CN114835682B (zh) * 2022-06-17 2024-04-26 华东理工常熟研究院有限公司 一种吡虫啉的盐及其制备方法与用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103443099A (zh) * 2010-12-20 2013-12-11 Irm责任有限公司 调节fxr的组合物和方法
CN107106555A (zh) * 2014-12-18 2017-08-29 诺华股份有限公司 氮杂双环辛烷衍生物作为fxr激动剂在治疗肝脏和胃肠疾病中的应用
WO2019053581A1 (en) * 2017-09-12 2019-03-21 Novartis Ag PHARMACEUTICAL COMPOSITION
CN113874019A (zh) * 2019-05-20 2021-12-31 辉瑞大药厂 用于治疗nash/nafld及相关疾病的包含作为glp-1r激动剂的苯并二氧杂环戊烯的组合

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103443099A (zh) * 2010-12-20 2013-12-11 Irm责任有限公司 调节fxr的组合物和方法
CN107106555A (zh) * 2014-12-18 2017-08-29 诺华股份有限公司 氮杂双环辛烷衍生物作为fxr激动剂在治疗肝脏和胃肠疾病中的应用
WO2019053581A1 (en) * 2017-09-12 2019-03-21 Novartis Ag PHARMACEUTICAL COMPOSITION
CN113874019A (zh) * 2019-05-20 2021-12-31 辉瑞大药厂 用于治疗nash/nafld及相关疾病的包含作为glp-1r激动剂的苯并二氧杂环戊烯的组合

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DAVID C. TULLY ET AL.: "Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)" *

Also Published As

Publication number Publication date
CN114728954B (zh) 2023-10-17
WO2021104022A1 (zh) 2021-06-03

Similar Documents

Publication Publication Date Title
IL228916A (en) Common Crystals of N- [2- (7-Methoxy-1-Naphthyl) Ethyl] Acetamide Adapted Pharmacist and Methods for Preparing
CN114728954A (zh) Tropifexor的新晶型及其制备方法
WO2019228485A1 (zh) 一种甲磺酸乐伐替尼新晶型及其制备方法
CN111377944A (zh) Baloxavir marboxil晶型及其制备方法
CN116829144A (zh) 一种化合物的固体形式及其制备方法和用途
CN114746412A (zh) Kd-025的新晶型及其制备方法
CN114728955A (zh) Tropifexor的新晶型及其制备方法
CN114790210A (zh) 一种核苷类化合物盐的晶型
CN109096306A (zh) 一种1/2水头孢唑林钠化合物
CN112638865B (zh) 药物共晶体及其制备方法
CN114075145A (zh) 一种法匹拉韦盐及其晶型和制备方法
US11214547B2 (en) Crystalline Eltrombopag monoethanolamine salt form D
CN110776450B (zh) 一种辛波莫德晶型及其制备方法
CN111278828B (zh) 巴瑞替尼磷酸盐的新晶型及其制备方法
WO2020178847A1 (en) Cocrystal of roxadustat and d-proline
CN116041395A (zh) 一种抗病毒药物与苯甲酸的共晶及其制备方法
WO2017028762A1 (zh) 一种萘环化合物的晶型
CN114773211B (zh) 一种葡甲胺盐的晶型、其制备方法及应用
CN114591211A (zh) 一种酰胺化合物的共晶及其制备方法
CN115124514A (zh) Kd-025的共晶及其制备方法
CN114341112A (zh) 乙酰化艾曲波帕的新晶型及其制备方法
CN114524845A (zh) 瑞德西韦与水杨酸的共晶及其制备方法
CN111201218A (zh) 一种哌马色林半酒石酸盐的新晶型及其制备方法
CN115996720A (zh) 一种低氧诱导因子脯氨酰羟化酶抑制剂的晶型及其制备方法
CN106397306A (zh) 一种盐酸多奈哌齐晶型化合物及其制备方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
CB02 Change of applicant information
CB02 Change of applicant information

Address after: 523808 No.1, Gongye North Road, Songshanhu Park, Dongguan City, Guangdong Province

Applicant after: Guangdong Dongyangguang Pharmaceutical Co.,Ltd.

Address before: 523000 Songshan Lake Science and Technology Industrial Park, Dongguan, Guangdong

Applicant before: SUNSHINE LAKE PHARMA Co.,Ltd.

GR01 Patent grant
GR01 Patent grant