TW201200524A - Spiro isoxazoline compounds as SSTR5 antagonists - Google Patents

Spiro isoxazoline compounds as SSTR5 antagonists Download PDF

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Publication number
TW201200524A
TW201200524A TW100117097A TW100117097A TW201200524A TW 201200524 A TW201200524 A TW 201200524A TW 100117097 A TW100117097 A TW 100117097A TW 100117097 A TW100117097 A TW 100117097A TW 201200524 A TW201200524 A TW 201200524A
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TW
Taiwan
Prior art keywords
substituted
group
doc
mmol
halogen
Prior art date
Application number
TW100117097A
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English (en)
Chinese (zh)
Inventor
Joseph L Duffy
Jianming Bao
Debra L Ondeyka
Sriram Tyagarajan
Patrick Shao
Feng Ye
Revathi Katipally
Paul E Finke
Yi Zang
Michael A Plotkin
F Anthony Romero
Remond Moningka
Zahid Hussain
Original Assignee
Merck Sharp & Amp Dohme Corp
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.)
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Application filed by Merck Sharp & Amp Dohme Corp filed Critical Merck Sharp & Amp Dohme Corp
Publication of TW201200524A publication Critical patent/TW201200524A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW100117097A 2010-05-18 2011-05-16 Spiro isoxazoline compounds as SSTR5 antagonists TW201200524A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US34568310P 2010-05-18 2010-05-18

Publications (1)

Publication Number Publication Date
TW201200524A true TW201200524A (en) 2012-01-01

Family

ID=44991994

Family Applications (1)

Application Number Title Priority Date Filing Date
TW100117097A TW201200524A (en) 2010-05-18 2011-05-16 Spiro isoxazoline compounds as SSTR5 antagonists

Country Status (8)

Country Link
US (1) US20130040978A1 (enExample)
EP (1) EP2571356A4 (enExample)
JP (1) JP2013529210A (enExample)
AR (1) AR081401A1 (enExample)
AU (1) AU2011256444B2 (enExample)
CA (1) CA2799414A1 (enExample)
TW (1) TW201200524A (enExample)
WO (1) WO2011146324A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115215787A (zh) * 2021-04-19 2022-10-21 中国科学院上海药物研究所 生长抑素受体5拮抗剂及其用途
CN115380036A (zh) * 2019-12-03 2022-11-22 卡尔优普公司 Sstr5拮抗剂

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012024183A1 (en) 2010-08-18 2012-02-23 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
MX2014015265A (es) 2012-06-14 2015-08-12 Basf Se Metodos plaguicidas que utilizan compuestos de 3-piridiltiazol sustituido y derivados para combatir plagas de animales.
FR3000064A1 (fr) 2012-12-21 2014-06-27 Univ Lille Ii Droit & Sante Composes de type spiroisoxazoline ayant une activite potentialisatrice de l'activite d'un antibiotique-composition et produit pharmaceutiques comprenant de tels composes
US9605000B2 (en) 2013-03-14 2017-03-28 Takeda Pharmaceutical Company Limited Spiro azetidine isoxazole derivatives and their use as SSTR antagonists
US9663534B2 (en) 2013-12-17 2017-05-30 Merck Sharp & Dohme Corp. Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein
CN104945416B (zh) * 2014-03-24 2017-11-17 中国科学院上海药物研究所 一类螺异噁唑啉衍生物、其制备方法及医药用途
JPWO2015146561A1 (ja) * 2014-03-26 2017-04-13 住友精化株式会社 臭化芳香族エステル化合物の製造方法
EP3174537B1 (en) * 2014-07-29 2021-06-23 Merck Sharp & Dohme Corp. Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein
TW201712012A (zh) 2015-06-16 2017-04-01 美國禮來大藥廠 2-側氧基-1,3,8-三氮雜螺[4.5]癸-3-基羧酸衍生物
WO2018077699A1 (en) 2016-10-25 2018-05-03 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2018138028A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Benzylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
EP3573952B1 (en) 2017-01-26 2021-07-14 Boehringer Ingelheim International GmbH Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceuticalcompositions and uses thereof
JP7106564B2 (ja) 2017-03-16 2022-07-26 クリネティックス ファーマシューティカルズ,インク. ソマトスタチンモジュレータとその使用
JP7365347B2 (ja) 2018-02-12 2023-10-19 クリネティックス ファーマシューティカルズ,インク. ソマトスタチンモジュレーターおよびその使用
JP7431813B2 (ja) * 2018-09-18 2024-02-15 クリネティックス ファーマシューティカルズ,インク. ソマトスタチンモジュレーターとその使用
TWI841768B (zh) 2019-08-14 2024-05-11 美商克林提克斯醫藥股份有限公司 非肽生長抑制素(somatostatin)5型受體激動劑及其用途
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ,インク. Gpr119アゴニスト
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
AU2021275038A1 (en) 2020-05-19 2022-12-22 Kallyope, Inc. AMPK activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
JP2024506715A (ja) 2021-02-17 2024-02-14 クリネティックス ファーマシューティカルズ,インク. ソマトスタチンモジュレーターの結晶形態
CN116354961B (zh) * 2021-12-27 2025-07-25 中国科学院上海药物研究所 生长抑素受体5拮抗剂及其药物组合物及用途
CN114230552B (zh) * 2021-12-29 2023-11-03 江苏广域化学有限公司 三氟甲氧基二苯并噻吩、其制备方法及相关中间体的制备方法
WO2024129614A1 (en) 2022-12-13 2024-06-20 Crinetics Pharmaceuticals, Inc. Somatostatin subtype-2 receptor (sst2r) targeted therapeutics and uses thereof
CN115819186B (zh) * 2023-02-14 2023-05-16 广东银珠医药科技有限公司 一种3,5-二氯苯甲醇的新型制备方法
CN120752056A (zh) 2023-03-27 2025-10-03 思可海雅药品株式会社 生长激素分泌促进剂

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5939418A (en) * 1995-12-21 1999-08-17 The Dupont Merck Pharmaceutical Company Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors
WO1998043962A1 (en) * 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Heterocyclic integrin inhibitor prodrugs
DE102005044813A1 (de) * 2005-05-19 2007-10-04 Grünenthal GmbH Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
AR055395A1 (es) * 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
CN101253171B (zh) * 2005-09-02 2011-06-15 霍夫曼-拉罗奇有限公司 苯并噁唑、噁唑并吡啶、苯并噻唑和噻唑并吡啶衍生物
AU2006305620A1 (en) * 2005-10-19 2007-04-26 Ranbaxy Laboratories Limited Compositions of phosphodiesterase type IV inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115380036A (zh) * 2019-12-03 2022-11-22 卡尔优普公司 Sstr5拮抗剂
CN115215787A (zh) * 2021-04-19 2022-10-21 中国科学院上海药物研究所 生长抑素受体5拮抗剂及其用途

Also Published As

Publication number Publication date
WO2011146324A1 (en) 2011-11-24
CA2799414A1 (en) 2011-11-24
EP2571356A4 (en) 2013-11-20
AU2011256444B2 (en) 2014-07-10
EP2571356A1 (en) 2013-03-27
AR081401A1 (es) 2012-08-29
US20130040978A1 (en) 2013-02-14
AU2011256444A1 (en) 2012-10-18
JP2013529210A (ja) 2013-07-18

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