AU2021236648A1 - Crystalline forms of a farnesoid X receptor agonist - Google Patents

Crystalline forms of a farnesoid X receptor agonist Download PDF

Info

Publication number
AU2021236648A1
AU2021236648A1 AU2021236648A AU2021236648A AU2021236648A1 AU 2021236648 A1 AU2021236648 A1 AU 2021236648A1 AU 2021236648 A AU2021236648 A AU 2021236648A AU 2021236648 A AU2021236648 A AU 2021236648A AU 2021236648 A1 AU2021236648 A1 AU 2021236648A1
Authority
AU
Australia
Prior art keywords
theta
crystalline form
disease
xrpd
crystalline
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.)
Pending
Application number
AU2021236648A
Other languages
English (en)
Inventor
Robert Mansfield
Nicholas D. Smith
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of AU2021236648A1 publication Critical patent/AU2021236648A1/en
Assigned to ORGANOVO, INC. reassignment ORGANOVO, INC. Request for Assignment Assignors: METACRINE, INC.
Assigned to ELI LILLY AND COMPANY reassignment ELI LILLY AND COMPANY Request for Assignment Assignors: ORGANOVO, INC.
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2021236648A 2020-03-18 2021-03-17 Crystalline forms of a farnesoid X receptor agonist Pending AU2021236648A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062991213P 2020-03-18 2020-03-18
US62/991,213 2020-03-18
PCT/US2021/022790 WO2021188692A1 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid x receptor agonist

Publications (1)

Publication Number Publication Date
AU2021236648A1 true AU2021236648A1 (en) 2022-10-13

Family

ID=77771306

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021236648A Pending AU2021236648A1 (en) 2020-03-18 2021-03-17 Crystalline forms of a farnesoid X receptor agonist

Country Status (13)

Country Link
US (1) US12545660B2 (https=)
EP (1) EP4121010A4 (https=)
JP (2) JP7664278B2 (https=)
KR (1) KR20220155356A (https=)
CN (1) CN115666521A (https=)
AR (1) AR121596A1 (https=)
AU (1) AU2021236648A1 (https=)
BR (1) BR112022018596A2 (https=)
CA (1) CA3171987A1 (https=)
IL (1) IL296532A (https=)
MX (2) MX2022011582A (https=)
TW (1) TW202144332A (https=)
WO (1) WO2021188692A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019344903B2 (en) 2018-09-18 2025-02-27 Eli Lilly And Company Farnesoid X receptor agonists and uses thereof
WO2021188695A1 (en) 2020-03-18 2021-09-23 Metacrine, Inc. Formulations of a farnesoid x receptor agonist
KR20220155356A (ko) 2020-03-18 2022-11-22 메타크린, 인크. 파르네소이드 x 수용체 효능제의 결정형

Family Cites Families (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000069810A1 (en) 1999-05-17 2000-11-23 Novo Nordisk A/S Glucagon antagonists/inverse agonists
US6645980B1 (en) 2000-05-25 2003-11-11 Sepracor Inc. Heterocyclic analgesic compounds and methods of use thereof
JP2003500392A (ja) 1999-05-25 2003-01-07 セプラコール， インク． 複素環式鎮痛性化合物およびその使用方法
US6511980B2 (en) 2000-05-05 2003-01-28 Ortho Mcneil Pharmaceutical, Inc. Substituted diamine derivatives useful as motilin antagonists
IL154363A0 (en) 2000-09-25 2003-09-17 Actelion Pharmaceuticals Ltd Substituted amino-aza-cycloalkanes useful against malaria
FR2815032B1 (fr) 2000-10-10 2003-08-08 Pf Medicament Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations
FR2825706B1 (fr) 2001-06-06 2003-12-12 Pf Medicament Nouveaux derives de benzothienyle ou d'indole, leur preparation et leur utilisation comme inhibiteurs de proteines prenyl transferase
FR2839974B1 (fr) 2002-05-24 2004-07-16 Pf Medicament Derives de phenyl-furane ou de phenyl-thiophene,leur preparation et leur application a titre de medicament
AU2003249983A1 (en) 2002-07-18 2004-02-09 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
BR0314126A (pt) 2002-09-20 2005-06-28 Pfizer Prod Inc Ligandos de amida acìclica e sulfonamida para o receptor de estrogênio
WO2004046162A2 (en) 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
US7647217B2 (en) 2002-11-15 2010-01-12 The Salk Institute For Biological Studies Structure of the farnesoid X receptor ligand binding domain and methods of use therefor
US20050143449A1 (en) 2002-11-15 2005-06-30 The Salk Institute For Biological Studies Non-steroidal farnesoid X receptor modulators and methods for the use thereof
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
US7759348B2 (en) 2003-07-30 2010-07-20 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
EP1648874B1 (en) 2003-07-30 2011-10-05 Xenon Pharmaceuticals Inc. Piperazine derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
WO2005058822A1 (en) 2003-12-17 2005-06-30 Actelion Pharmaceuticals Ltd Substituted amino-cycloalkanes
CN1914205A (zh) 2003-12-19 2007-02-14 葛兰素集团有限公司 吡唑并[3,4－b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途
PL1734970T3 (pl) 2004-03-12 2015-05-29 Intercept Pharmaceuticals Inc Leczenie zwłóknienia z zastosowaniem ligandów FXR
WO2005097760A1 (en) 2004-03-26 2005-10-20 Rigel Pharmaceuticals, Inc. Heterocyclic anti-viral compounds comprising metabolizable moieties and their uses
WO2005113522A1 (en) 2004-05-07 2005-12-01 Janssen Pharmaceutica, N.V. Azole carboxamide inhibitors of bacterial type iii protein secretion systems
JP2006199656A (ja) 2005-01-24 2006-08-03 Kowa Co アミド基を有する環状アミン化合物
MY144229A (en) 2006-01-26 2011-08-15 Xenon Pharmaceuticals Inc Pyridazine derivatives and their use as therapeutic agents
CN101395170A (zh) 2006-02-14 2009-03-25 英特塞普特药品公司 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物
EP2001851A2 (en) 2006-03-28 2008-12-17 Novartis AG Amide derivatives and their application for the treament of g protein related diseases
US20080081824A1 (en) 2006-09-29 2008-04-03 Bristol-Myers Squibb Company Substituted piperidines as modulators of chemokine receptor activity
WO2008065500A2 (en) 2006-11-30 2008-06-05 Pfizer Products Inc. Heteroaryl amides as type i glycine transport inhibitors
EP2234977A4 (en) 2007-12-19 2011-04-13 Boehringer Ingelheim Int VIRAL POLYMERASE INHIBITORS
US20090270418A1 (en) 2008-01-09 2009-10-29 Marianne Sloss Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith
US20100029657A1 (en) 2008-02-29 2010-02-04 Wyeth Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof
WO2010001869A1 (ja) 2008-06-30 2010-01-07 武田薬品工業株式会社 ４置換ベンゼン化合物およびその用途
JP2010077109A (ja) 2008-08-28 2010-04-08 Takeda Chem Ind Ltd 複素環化合物およびその用途
JP2012516885A (ja) 2009-02-04 2012-07-26 ファイザー・インク ４−アミノ−７，８−ジヒドロピリド［４，３−ｄ］ピリミジン−５（６Ｈ）−オン誘導体
CA2767089A1 (en) 2009-07-15 2011-01-20 Abbott Laboratories Pyrrolopyridine inhibitors of kinases
EP2454243A2 (en) 2009-07-15 2012-05-23 Merck Serono SA Tetrazole derivatives
FR2963005B1 (fr) 2010-07-23 2012-08-17 Sanofi Aventis Derives d'oxadiazoles et de pyridazines, leur preparation et leur application en therapeutique
WO2012087521A1 (en) 2010-12-20 2012-06-28 Irm Llc Compositions and methods for modulating farnesoid x receptors
KR101834362B1 (ko) 2011-03-18 2018-03-05 바이엘 인텔렉쳐 프로퍼티 게엠베하 N-(3-카바모일페닐)-1h-피라졸-5-카복사미드 유도체 및 동물 해충을 구제하기 위한 그의 용도
ME02754B (me) 2011-03-23 2018-01-20 Trevena Inc Ligandi opioidnih receptora i postupci njihove upotrebe i pripreme
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
EP2732871A4 (en) 2011-07-13 2015-03-04 M Tech Co Ltd PROCESS FOR PRODUCING MICROPARTICLES WITH CONTROLLED CRYSTALLITE DIAMETER
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
RU2543485C2 (ru) 2013-02-26 2015-03-10 Андрей Александрович Иващенко Гетероциклические агонисты рецепторов желчных кислот tgr5, фармацевтическая композиция, способы их получения и применения
DK3043865T3 (da) 2013-09-11 2021-02-01 Univ Claude Bernard Lyon Fremgangsmåder og farmaceutiske sammensætningr til behandlingen af hepatitis b-virusinfektion
GB201316824D0 (en) 2013-09-23 2013-11-06 R & D Vernalis Ltd New Chemical Entities
US20150258052A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Methods of using fexaramine and agents that increase sympathetic nervous system activity to promote browning of white adipose tissue
KR20160132111A (ko) 2014-03-13 2016-11-16 더 솔크 인스티튜트 포 바이올로지칼 스터디즈 Fxr 작용제와 제조방법 및 용도
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
EP3116851B1 (en) 2014-03-13 2023-07-26 Salk Institute for Biological Studies Analogs of fexaramine and methods of making and using
US20180116993A1 (en) 2015-01-22 2018-05-03 Xiamen University Modulators of farnesoid x receptor and methods for the use thereof
AU2016233579A1 (en) 2015-03-13 2017-10-12 Salk Institute For Biological Studies Treating latent autoimmune diabetes of adults with farnesoid X receptor agonists to activate intestinal receptors
WO2017018751A1 (ko) 2015-07-24 2017-02-02 동국대학교 산학협력단 Blt 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 염증성 질환 예방 또는 치료용 조성물
US10703712B2 (en) 2015-09-16 2020-07-07 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
US10626081B2 (en) 2015-09-16 2020-04-21 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
EP3350164A4 (en) 2015-09-16 2019-03-27 Metacrine, Inc. FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF
WO2017049177A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
MX389514B (es) 2015-10-01 2025-03-20 Firmenich Incorporated Compuestos útiles como moduladores de canal receptor 8 de potencial transitorio de melastatina (trpm8).
CN105477636B (zh) 2015-10-16 2019-09-17 厦门大学 使用阿维菌素及其衍生物治疗代谢疾病的方法
WO2017078928A1 (en) 2015-11-06 2017-05-11 Salk Institute For Biological Studies Fxr agonists and methods for making and using
CN107126419B (zh) 2016-02-26 2020-06-19 石药集团中诺药业（石家庄）有限公司 一种奥贝胆酸片剂及其制备方法
WO2017170182A1 (ja) 2016-03-31 2017-10-05 株式会社Adeka 感光性組成物及び新規化合物
WO2018170165A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
JP7258763B2 (ja) * 2017-03-15 2023-04-17 メタクリン，インク． ファルネソイドｘ受容体アゴニストおよびその使用
US20200131129A1 (en) 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CA3055990A1 (en) * 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2018170167A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CZ2017298A3 (cs) 2017-05-26 2018-12-05 Zentiva, K.S. Amorfní formy obeticholové kyseliny
WO2020060007A1 (ko) 2018-09-17 2020-03-26 엘지전자 주식회사 5g 이동통신에서 pdu 세션을 핸들링하는 방법 및 무선 기기
JP2022500393A (ja) * 2018-09-18 2022-01-04 メタクリン，インク． ファルネソイドｘ受容体アゴニストおよびその使用
WO2020061118A1 (en) 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EP3852749A4 (en) 2018-09-18 2022-08-24 Metacrine, Inc. CRYSTALLINE FORMS OF A FARNESOID X RECEPTOR AGONIST
WO2020061116A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
EA202190661A1 (ru) 2018-09-18 2021-08-13 Метакрайн, Инк. Агонисты фарнезоидного х-рецептора для лечения заболевания
CN113056264A (zh) 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂及其用途
AU2019344903B2 (en) 2018-09-18 2025-02-27 Eli Lilly And Company Farnesoid X receptor agonists and uses thereof
CN120732855A (zh) 2020-03-18 2025-10-03 伊莱利利公司 用于治疗疾病的法尼醇x受体激动剂
KR20220155356A (ko) 2020-03-18 2022-11-22 메타크린, 인크. 파르네소이드 x 수용체 효능제의 결정형
WO2021188695A1 (en) 2020-03-18 2021-09-23 Metacrine, Inc. Formulations of a farnesoid x receptor agonist

Also Published As

Publication number Publication date
TW202144332A (zh) 2021-12-01
CA3171987A1 (en) 2021-09-23
US12545660B2 (en) 2026-02-10
CN115666521A (zh) 2023-01-31
MX2022011582A (es) 2022-12-13
WO2021188692A1 (en) 2021-09-23
KR20220155356A (ko) 2022-11-22
MX2025009319A (es) 2025-09-02
EP4121010A1 (en) 2023-01-25
IL296532A (en) 2022-11-01
US20230147756A1 (en) 2023-05-11
JP7664278B2 (ja) 2025-04-17
EP4121010A4 (en) 2024-04-10
JP2025121901A (ja) 2025-08-20
AR121596A1 (es) 2022-06-22
JP2023518399A (ja) 2023-05-01
BR112022018596A2 (pt) 2023-03-07

Similar Documents

Publication Publication Date Title
CN110637015B (zh) 法尼醇x受体激动剂及其用途
CN110637011B (zh) 法尼醇x受体激动剂及其用途
CN108349893B (zh) 类法尼醇x受体激动剂及其用途
JP7554739B2 (ja) ファルネソイドｘ受容体アゴニストおよびその使用
US12545660B2 (en) Crystalline forms of a farnesoid X receptor agonist
JP2018532772A (ja) ファルネソイドｘ受容体アゴニストおよびそれらの使用
JP2022500391A (ja) ファルネソイドｘ受容体アゴニストおよびその使用
JP7813730B2 (ja) 甲状腺様作用剤
US20210347736A1 (en) Crystalline forms of a farnesoid x receptor agonist
CN113056265A (zh) 法尼醇x受体激动剂及其用途
TW202413326A (zh) Ｓｔａｔ３抑制劑的前藥
CN112209896B (zh) 噻唑烷二酮衍生物以及包含其的药物组合物
HK40019860A (en) Farnesoid x receptor agonists and uses thereof
WO2022029640A1 (en) Quinoline compounds as selective and/or dual modulators of bile acid receptors and leukotriene cysteinyl receptors
HK40019851A (en) Farnesoid x receptor agonists and uses thereof
JP2020186182A (ja) 標的蛋白質分解誘導化合物

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: ORGANOVO, INC.

Free format text: FORMER APPLICANT(S): METACRINE, INC.

PC1 Assignment before grant (sect. 113)

Owner name: ELI LILLY AND COMPANY

Free format text: FORMER APPLICANT(S): ORGANOVO, INC.