JP7212693B2 - ファルネソイドx受容体モジュレーターとしての架橋二環化合物 - Google Patents

ファルネソイドx受容体モジュレーターとしての架橋二環化合物 Download PDF

Info

Publication number
JP7212693B2
JP7212693B2 JP2020544333A JP2020544333A JP7212693B2 JP 7212693 B2 JP7212693 B2 JP 7212693B2 JP 2020544333 A JP2020544333 A JP 2020544333A JP 2020544333 A JP2020544333 A JP 2020544333A JP 7212693 B2 JP7212693 B2 JP 7212693B2
Authority
JP
Japan
Prior art keywords
methoxy
cyclopropyl
isoxazol
bicyclo
octan
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.)
Active
Application number
JP2020544333A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021501220A (ja
JP2021501220A5 (enExample
Inventor
デイビッド・エス・ユン
ルシト・クマール・アヌムラ
スリニバス・チェルク
ヤンティン・ホアン
エリザベス・アン・ユリカ
ウェイ・メン
スシール・ジェタナンド・ナラ
リシケシュ・ナラヤン
ラメシュ・クマール・シストラ
シーマオ・ウー
グオホア・ジャオ
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb 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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of JP2021501220A publication Critical patent/JP2021501220A/ja
Publication of JP2021501220A5 publication Critical patent/JP2021501220A5/ja
Application granted granted Critical
Publication of JP7212693B2 publication Critical patent/JP7212693B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2020544333A 2017-11-01 2018-10-31 ファルネソイドx受容体モジュレーターとしての架橋二環化合物 Active JP7212693B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762580075P 2017-11-01 2017-11-01
US62/580,075 2017-11-01
PCT/US2018/058315 WO2019089667A1 (en) 2017-11-01 2018-10-31 Bridged bicyclic compounds as farnesoid x receptor modulators

Publications (3)

Publication Number Publication Date
JP2021501220A JP2021501220A (ja) 2021-01-14
JP2021501220A5 JP2021501220A5 (enExample) 2021-11-11
JP7212693B2 true JP7212693B2 (ja) 2023-01-25

Family

ID=64332182

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020544333A Active JP7212693B2 (ja) 2017-11-01 2018-10-31 ファルネソイドx受容体モジュレーターとしての架橋二環化合物

Country Status (19)

Country Link
US (1) US10730863B2 (enExample)
EP (1) EP3704113B1 (enExample)
JP (1) JP7212693B2 (enExample)
KR (1) KR102732835B1 (enExample)
CN (1) CN111295382B (enExample)
AR (1) AR113820A1 (enExample)
AU (1) AU2018360577A1 (enExample)
BR (1) BR112020008457A2 (enExample)
CA (1) CA3079833A1 (enExample)
CL (1) CL2020001138A1 (enExample)
CO (1) CO2020005459A2 (enExample)
EA (1) EA202091063A1 (enExample)
ES (1) ES2964964T3 (enExample)
IL (1) IL274321A (enExample)
MX (1) MX2020004405A (enExample)
PE (1) PE20201170A1 (enExample)
SG (1) SG11202003827YA (enExample)
TW (1) TW201922722A (enExample)
WO (1) WO2019089667A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110128432B (zh) 2018-02-02 2021-03-02 广东东阳光药业有限公司 含氮三环化合物及其在药物中的应用
MA53827A (fr) 2018-10-05 2021-09-15 Vertex Pharma Modulateurs de l'alpha -1 antitrypsine
US12227496B2 (en) 2019-02-15 2025-02-18 Bristol-Myers Squibb Company Substituted bicyclic compounds as farnesoid X receptor modulators
MX2021009564A (es) 2019-02-15 2021-09-08 Bristol Myers Squibb Co Compuestos de amida sustituida utiles como moduladores del receptor de farnesoide x.
EA202192275A1 (ru) 2019-02-15 2021-11-03 Бристол-Маерс Сквибб Компани Замещенные амидные соединения, полезные в качестве модуляторов фарнезоидного x-рецептора
US11884672B2 (en) 2019-05-14 2024-01-30 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
MX2021014443A (es) 2019-05-31 2022-01-06 Ikena Oncology Inc Inhibidores del dominio asociado mejorador de la transcripcion (tead) y usos de los mismos.
US11458149B1 (en) 2019-05-31 2022-10-04 Ikena Oncology, Inc. TEAD inhibitors and uses thereof
CN110922368B (zh) * 2019-11-29 2022-08-16 扬州工业职业技术学院 一种氯代苯异噁唑氨基苯甲酸衍生物及其制备方法与应用
CN110804025B (zh) * 2019-11-29 2022-02-08 扬州工业职业技术学院 一种卤代苯异噁唑衍生物及其制备方法与应用
CA3159163A1 (en) 2020-01-15 2021-07-22 Raphael Darteil Use of fxr agonists for treating an infection by hepatitis d virus
CA3179189A1 (en) * 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
CN115768772A (zh) 2020-04-03 2023-03-07 弗特克斯药品有限公司 作为用于治疗α-1抗胰蛋白酶缺乏症(AATD)的α-1抗胰蛋白酶调节剂的吡喃并[4,3-b]L吲哚衍生物
WO2022120353A1 (en) * 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
CN115504972B (zh) * 2021-06-22 2024-11-12 广东药科大学 异恶唑类衍生物、其制备方法及其作为药物的用途
EP4590660A1 (en) 2022-09-19 2025-07-30 Basf Se Azole pesticidal compounds
CN117105779A (zh) * 2023-07-18 2023-11-24 河南师范大学 一种5-溴-2-甲酰基苯甲酸甲酯的制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010533722A (ja) 2007-07-16 2010-10-28 イーライ リリー アンド カンパニー Fxrを調節するための化合物および方法
JP2014500317A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー Fxr調節のための組成物および方法
WO2016096115A1 (en) 2014-12-17 2016-06-23 Gilead Sciences, Inc. Hydroxy containing fxr (nr1h4) modulating compounds
WO2017118294A1 (zh) 2016-01-06 2017-07-13 广州市恒诺康医药科技有限公司 Fxr受体调节剂及其制备方法和用途
JP2017537960A (ja) 2014-12-18 2017-12-21 ノバルティス アーゲー 肝疾患および胃腸疾患の治療に使用するためのfxrアゴニストとしてのアザビシクロオクタン誘導体

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993013101A1 (fr) 1991-12-27 1993-07-08 Yoshitomi Pharmaceutical Industries, Ltd. Compose de pyridonecarboxylate, son utilisation pharmaceutique et compose spiro
AU4999897A (en) 1996-10-25 1998-05-15 Merck & Co., Inc. Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists
CN1367775A (zh) 1998-04-17 2002-09-04 肯尼思·柯里 用作亲代谢型谷氨酸受体对抗剂的立方烷衍生物及其制备方法
BR0015545A (pt) 1999-11-12 2002-08-06 Biogen Inc Policicloalquilpurinas como antagonistas dos receptores para adenosina
WO2001079261A1 (en) 2000-04-14 2001-10-25 Corvas International, Inc. Tetrahydro-azepinone derivatives as thrombin inhibitors
ES2286089T3 (es) 2001-06-21 2007-12-01 Cesare Casagrande Compuesto para el tratamiento de estados patologicos ateroesclerotico-tromboticos.
CA2495179A1 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
JP2008505095A (ja) 2004-07-01 2008-02-21 ワイス エストロゲンリガンドとしての四環式化合物
WO2006006490A1 (ja) 2004-07-08 2006-01-19 Ono Pharmaceutical Co., Ltd. スピロ化合物
CA2603402C (en) 2005-04-08 2017-10-31 Ptc Therapeutics, Inc. Compositions of an orally active 1,2,4-oxadiazole for nonsense mutation suppression therapy
ES2374165T3 (es) 2005-12-19 2012-02-14 Glaxosmithkline Llc Agonistas del receptor x farnesoide.
SI2069336T1 (sl) 2006-09-07 2013-03-29 Actelion Pharmaceuticals Ltd. Derivati piridin-4-ila kot imunomodulirna sredstva
CL2007003035A1 (es) 2006-10-24 2008-05-16 Smithkline Beechman Corp Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos,
WO2008094556A2 (en) 2007-01-30 2008-08-07 Biogen Idec Ma Inc. Imidazolone compounds as tgf-beta family type i receptors, alk5 and/or alk4 antagonists
AU2008270784A1 (en) 2007-07-02 2009-01-08 Glaxosmithkline Llc Farnesoid X receptor agonists
WO2009009059A1 (en) 2007-07-09 2009-01-15 Biogen Idec Ma Inc. Spiro compounds as antagonists of tgf-beta
EP2217596B8 (en) 2007-10-22 2013-11-20 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and their use as modulators of the activity of gpr119
JP2012509309A (ja) 2008-11-21 2012-04-19 ファイザー・インク Faah阻害剤としての1−オキサ−8−アザスピロ[4.5]デカン−8−カルボキサミド化合物
CA2752804C (en) 2009-03-03 2017-04-04 Anna Quattropani Oxazole pyridine derivatives useful as s1p1 receptor agonists
CA2760746C (en) 2009-05-05 2017-07-11 F. Hoffmann-La Roche Ag Isoxazole-pyrazole derivatives
US8440710B2 (en) 2009-10-15 2013-05-14 Hoffmann-La Roche Inc. HSL inhibitors useful in the treatment of diabetes
TW201300380A (zh) 2010-10-19 2013-01-01 Comentis Inc 抑制β-分泌酶活性之噁二唑化合物及其使用方法
PH12013501001A1 (en) 2010-11-19 2019-09-02 Incyte Holdings Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
FI2699553T3 (fi) 2011-04-22 2024-01-24 Signal Pharm Llc Substituoituja diaminokarboksamidi- ja diaminokarbonitriilipyrimidiinejä, niiden koostumuksia ja niitä käyttäviä hoitomenetelmiä
EP2520566A1 (en) 2011-05-06 2012-11-07 Orion Corporation New Pharmaceutical Compounds
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
WO2014054053A1 (en) 2012-10-03 2014-04-10 Advinus Therapeutics Limited Spirocyclic compounds, compositions and medicinal applications thereof
US9567301B2 (en) 2012-11-02 2017-02-14 Dana-Farber Cancer Institute, Inc. Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors
EP2774919A1 (en) 2013-03-06 2014-09-10 Pharmeste S.R.L. In Liquidazione Novel sulfonamide TRPA1 receptor antagonists
AU2014244482B2 (en) 2013-03-14 2018-01-25 Bristol-Myers Squibb Company Bicyclo [2.2.2] acid GPR120 modulators
TW201605859A (zh) 2013-11-14 2016-02-16 必治妥美雅史谷比公司 作為酪蛋白激酶1δ/ε抑制劑之新穎經取代之吡唑并-哌
WO2015172747A1 (en) 2014-05-16 2015-11-19 Zhaoyin Wang Spirocyclic molecules as mth1 inhibitors
WO2016073545A1 (en) 2014-11-06 2016-05-12 Concert Pharmaceuticals, Inc. Phenyloxadiazole benzoic acids
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
CN106146483A (zh) 2015-04-23 2016-11-23 上海迪诺医药科技有限公司 杂环类法尼酯衍生物x受体调节剂
CN108602811B (zh) 2016-02-01 2021-11-16 轩竹生物科技有限公司 Fxr受体激动剂
CN107021958A (zh) 2016-02-01 2017-08-08 山东轩竹医药科技有限公司 Fxr受体激动剂
HUE053743T2 (hu) 2016-02-22 2021-07-28 Novartis Ag Eljárások FXR agonisták alkalmazására
KR20180115270A (ko) 2016-02-22 2018-10-22 노파르티스 아게 Fxr 효능제를 사용하는 방법
WO2017189652A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2017201155A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF
KR102269305B1 (ko) 2016-06-13 2021-06-25 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
AR108711A1 (es) 2016-06-13 2018-09-19 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4)
WO2018059314A1 (zh) 2016-09-28 2018-04-05 四川科伦博泰生物医药股份有限公司 氮杂双环衍生物及其制备方法和用途
CN106632294A (zh) 2016-12-15 2017-05-10 宁波百纳西药业有限公司 一种螺环化合物及其药物用途

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010533722A (ja) 2007-07-16 2010-10-28 イーライ リリー アンド カンパニー Fxrを調節するための化合物および方法
JP2014500317A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー Fxr調節のための組成物および方法
WO2016096115A1 (en) 2014-12-17 2016-06-23 Gilead Sciences, Inc. Hydroxy containing fxr (nr1h4) modulating compounds
JP2017537960A (ja) 2014-12-18 2017-12-21 ノバルティス アーゲー 肝疾患および胃腸疾患の治療に使用するためのfxrアゴニストとしてのアザビシクロオクタン誘導体
WO2017118294A1 (zh) 2016-01-06 2017-07-13 广州市恒诺康医药科技有限公司 Fxr受体调节剂及其制备方法和用途

Also Published As

Publication number Publication date
AR113820A1 (es) 2020-06-17
BR112020008457A2 (pt) 2020-10-20
KR102732835B1 (ko) 2024-11-22
SG11202003827YA (en) 2020-05-28
CL2020001138A1 (es) 2020-08-21
JP2021501220A (ja) 2021-01-14
WO2019089667A1 (en) 2019-05-09
MX2020004405A (es) 2020-08-06
EP3704113B1 (en) 2023-10-11
CO2020005459A2 (es) 2020-05-15
TW201922722A (zh) 2019-06-16
CA3079833A1 (en) 2019-05-09
PE20201170A1 (es) 2020-10-28
EP3704113A1 (en) 2020-09-09
EA202091063A1 (ru) 2020-09-18
US20190127358A1 (en) 2019-05-02
CN111295382A (zh) 2020-06-16
ES2964964T3 (es) 2024-04-10
KR20200081434A (ko) 2020-07-07
AU2018360577A1 (en) 2020-06-18
US10730863B2 (en) 2020-08-04
IL274321A (en) 2020-06-30
CN111295382B (zh) 2024-02-02

Similar Documents

Publication Publication Date Title
JP7212693B2 (ja) ファルネソイドx受容体モジュレーターとしての架橋二環化合物
JP7642098B2 (ja) カルボキシ-ベンズイミダゾールglp-1r調節化合物
AU2012312305B2 (en) Acyclic cyanoethylpyrazoles as janus kinase inhibitors
JP7264906B2 (ja) ファルネソイドx受容体モジュレーターとしてのアルケン化合物
JP7264905B2 (ja) ファルネソイドx受容体モジュレーターとしての多環化合物
AU2014234909B2 (en) Acyclic cyanoethylpyrazolo pyridones as Janus kinase inhibitors
JP2022519770A (ja) ファルネソイドx受容体モジュレータとしての置換二環式化合物
JP2024056742A (ja) キノリン誘導体から調製される新規な阻害剤
JP7223016B2 (ja) ファルネソイドx受容体モジュレーターとしてのアルケンスピロ環化合物
KR20200083528A (ko) 파르네소이드 x 수용체 조정제로서의 스피로시클릭 화합물
TW202409010A (zh) 人類呼吸道融合病毒及人類間質肺炎病毒之抑制劑
JP2022521895A (ja) ファルネソイドx受容体モジュレータとしての置換二環式化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211001

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20211001

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220915

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220920

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221031

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20230110

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230113

R150 Certificate of patent or registration of utility model

Ref document number: 7212693

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150