AU2011256444B2 - Spiro isoxazoline compounds as SSTR5 antagonists - Google Patents

Spiro isoxazoline compounds as SSTR5 antagonists Download PDF

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Publication number
AU2011256444B2
AU2011256444B2 AU2011256444A AU2011256444A AU2011256444B2 AU 2011256444 B2 AU2011256444 B2 AU 2011256444B2 AU 2011256444 A AU2011256444 A AU 2011256444A AU 2011256444 A AU2011256444 A AU 2011256444A AU 2011256444 B2 AU2011256444 B2 AU 2011256444B2
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AU
Australia
Prior art keywords
halogen
mmol
heterocycle
pct
cioalkyl
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.)
Expired - Fee Related
Application number
AU2011256444A
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English (en)
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AU2011256444A1 (en
Inventor
Jianming Bao
Joseph L. Duffy
Paul E. Finke
Zahid Hussain
Revathi Katipally
Remond Moningka
Debra L. Ondeyka
Michael A. Plotkin
F. Anthony Romero
Patrick Shao
Sriram Tyagarajan
Feng Ye
Yi Zang
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.)
Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp & Dohme LLC
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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Publication of AU2011256444A1 publication Critical patent/AU2011256444A1/en
Application granted granted Critical
Publication of AU2011256444B2 publication Critical patent/AU2011256444B2/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2011256444A 2010-05-18 2011-05-13 Spiro isoxazoline compounds as SSTR5 antagonists Expired - Fee Related AU2011256444B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34568310P 2010-05-18 2010-05-18
US61/345,683 2010-05-18
PCT/US2011/036367 WO2011146324A1 (en) 2010-05-18 2011-05-13 Spiro isoxazoline compounds as sstr5 antagonists

Publications (2)

Publication Number Publication Date
AU2011256444A1 AU2011256444A1 (en) 2012-10-18
AU2011256444B2 true AU2011256444B2 (en) 2014-07-10

Family

ID=44991994

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011256444A Expired - Fee Related AU2011256444B2 (en) 2010-05-18 2011-05-13 Spiro isoxazoline compounds as SSTR5 antagonists

Country Status (8)

Country Link
US (1) US20130040978A1 (cg-RX-API-DMAC10.html)
EP (1) EP2571356A4 (cg-RX-API-DMAC10.html)
JP (1) JP2013529210A (cg-RX-API-DMAC10.html)
AR (1) AR081401A1 (cg-RX-API-DMAC10.html)
AU (1) AU2011256444B2 (cg-RX-API-DMAC10.html)
CA (1) CA2799414A1 (cg-RX-API-DMAC10.html)
TW (1) TW201200524A (cg-RX-API-DMAC10.html)
WO (1) WO2011146324A1 (cg-RX-API-DMAC10.html)

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US8742110B2 (en) 2010-08-18 2014-06-03 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
BR112014030412A2 (pt) 2012-06-14 2017-06-27 Basf Se método para combater ou controlar pragas, método para proteger culturas, compostos, processo para a preparação de compostos, uso de um composto, composição agrícola ou veterinária e semente.
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
CN110088089B (zh) 2016-10-25 2023-08-29 勃林格殷格翰国际有限公司 苄基氨基吡啶基环丙烷甲酸、药物组合物及其用途
US10919859B2 (en) 2017-01-26 2021-02-16 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
JP7049349B2 (ja) 2017-01-26 2022-04-06 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ベンジルアミノピラジニルシクロプロパンカルボン酸、その医薬組成物及び使用
NZ757081A (en) 2017-03-16 2023-03-31 Crinetics Pharmaceuticals Inc Somatostatin modulators and uses thereof
US11608335B2 (en) 2018-02-12 2023-03-21 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
TWI852944B (zh) * 2018-09-18 2024-08-21 美商克林提克斯醫藥股份有限公司 生長抑制素(somatostatin)調節劑及其用途
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
EP4073075A4 (en) * 2019-12-03 2023-12-27 Kallyope, Inc. Sstr5 antagonists
MX2022010548A (es) 2020-02-28 2022-09-23 Kallyope Inc Agonistas de gpr40.
MX2022014505A (es) 2020-05-19 2022-12-13 Kallyope Inc Activadores de la ampk.
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
US11773076B2 (en) 2021-02-17 2023-10-03 Crinetics Pharmaceuticals, Inc. Crystalline forms of a somatostatin modulator
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
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
AU2023396827A1 (en) 2022-12-13 2025-06-19 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
WO2024204277A1 (ja) 2023-03-27 2024-10-03 株式会社スコヒアファーマ 成長ホルモン分泌促進剤

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070179167A1 (en) * 2005-08-26 2007-08-02 Cottrell Kevin M Inhibitors of serine proteases
US20080269271A1 (en) * 2005-05-19 2008-10-30 Gruenenthal Gmbh Substituted Spiro Compounds and Their Use for Producing Pain-Relief Medicaments

Family Cites Families (4)

* 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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080269271A1 (en) * 2005-05-19 2008-10-30 Gruenenthal Gmbh Substituted Spiro Compounds and Their Use for Producing Pain-Relief Medicaments
US20070179167A1 (en) * 2005-08-26 2007-08-02 Cottrell Kevin M Inhibitors of serine proteases

Also Published As

Publication number Publication date
JP2013529210A (ja) 2013-07-18
EP2571356A1 (en) 2013-03-27
WO2011146324A1 (en) 2011-11-24
US20130040978A1 (en) 2013-02-14
CA2799414A1 (en) 2011-11-24
AR081401A1 (es) 2012-08-29
EP2571356A4 (en) 2013-11-20
TW201200524A (en) 2012-01-01
AU2011256444A1 (en) 2012-10-18

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Legal Events

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MK25 Application lapsed reg. 22.2i(2) - failure to pay acceptance fee