[go: up one dir, main page]

WO2009038064A1 - Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体 - Google Patents

Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体 Download PDF

Info

Publication number
WO2009038064A1
WO2009038064A1 PCT/JP2008/066708 JP2008066708W WO2009038064A1 WO 2009038064 A1 WO2009038064 A1 WO 2009038064A1 JP 2008066708 W JP2008066708 W JP 2008066708W WO 2009038064 A1 WO2009038064 A1 WO 2009038064A1
Authority
WO
WIPO (PCT)
Prior art keywords
independently represent
bond
hydrogen
type
hydroxysteroid dehydrogenase
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.)
Ceased
Application number
PCT/JP2008/066708
Other languages
English (en)
French (fr)
Inventor
Akiko Itai
Susumu Muto
Ryuko Tokuyama
Hiroshi Fukasawa
Takeshi Yanase
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.)
Institute of Medicinal Molecular Design Inc IMMD
Shionogi and Co Ltd
Original Assignee
Institute of Medicinal Molecular Design Inc IMMD
Shionogi and 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 Institute of Medicinal Molecular Design Inc IMMD, Shionogi and Co Ltd filed Critical Institute of Medicinal Molecular Design Inc IMMD
Priority to JP2009533144A priority Critical patent/JPWO2009038064A1/ja
Priority to US12/679,159 priority patent/US20100234363A1/en
Priority to EP08831464A priority patent/EP2208728A4/en
Publication of WO2009038064A1 publication Critical patent/WO2009038064A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/24—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Steroid Compounds (AREA)

Abstract

Ｉ型１１βヒドロキシステロイド脱水素酵素阻害剤として有用な化合物を提供する。 式：　（式中、ＸはＯまたＳであり、破線および波線は結合の存在または不存在を示し、 (i) 破線が結合の存在を示す場合は、波線は結合の不存在を示し、Ｒ２およびＲ３は各々独立して水素、ハロゲン等であり、 (ii) 破線が結合の不存在を示す場合は、波線は結合の存在を示し、Ｒ１およびＲ４は各々独立して水素、ハロゲン等であり、Ｒ２およびＲ３は各々独立して水素、ハロゲン等であり、Ｒ５およびＲ６は各々独立して水素、置換されていてもよいアルキル等である。）で示される化合物、その製薬上許容される塩またはそれらの溶媒和物。
PCT/JP2008/066708 2007-09-19 2008-09-17 Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体 Ceased WO2009038064A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2009533144A JPWO2009038064A1 (ja) 2007-09-19 2008-09-17 Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体
US12/679,159 US20100234363A1 (en) 2007-09-19 2008-09-17 Heterocyclic derivative having inhibitory activity on type-i 11 data-hydroxysteroid dehydrogenase
EP08831464A EP2208728A4 (en) 2007-09-19 2008-09-17 HETEROCYCLIC DERIVATIVE DERIVATIVE DERIVATIVE TO 11 -? - HYDROXYSTEROIDDEHYDROGENASE TYPE I

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007241976 2007-09-19
JP2007-241976 2007-09-19

Publications (1)

Publication Number Publication Date
WO2009038064A1 true WO2009038064A1 (ja) 2009-03-26

Family

ID=40467876

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/066708 Ceased WO2009038064A1 (ja) 2007-09-19 2008-09-17 Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体

Country Status (4)

Country Link
US (1) US20100234363A1 (ja)
EP (1) EP2208728A4 (ja)
JP (1) JPWO2009038064A1 (ja)
WO (1) WO2009038064A1 (ja)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2011161030A1 (de) 2010-06-21 2011-12-29 Sanofi Heterocyclisch substituierte methoxyphenylderivate mit oxogruppe, verfahren zu ihrer herstellung und ihre verwendung als gpr40 rezeptor modulatoren
WO2012004269A1 (de) 2010-07-05 2012-01-12 Sanofi ( 2 -aryloxy -acetylamino) - phenyl - propionsäurederivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2012004270A1 (de) 2010-07-05 2012-01-12 Sanofi Spirocyclisch substituierte 1,3-propandioxidderivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2012010413A1 (de) 2010-07-05 2012-01-26 Sanofi Aryloxy-alkylen-substituierte hydroxy-phenyl-hexinsäuren, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US20130150414A1 (en) * 2010-08-31 2013-06-13 Meiji Seika Pharma Co., Ltd. Pest control agent
US20210147366A1 (en) * 2018-04-06 2021-05-20 H. Lundbeck A/S Process for preparation of 2,2-dimethylpiperazine

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103508980B (zh) * 2012-06-14 2016-07-06 四川大学 苯并噻嗪-4-酮衍生物及其制备方法和用途
CA2877826C (en) 2012-07-09 2016-08-16 Lupin Limited Tetrahydroquinazolinone derivatives as parp inhibitors
CN102850246B (zh) * 2012-07-10 2015-04-22 江西理工大学 一种苯胺类衍生物引入巯基的方法
US20140220331A1 (en) 2013-02-02 2014-08-07 Cosilion LLC Antimicrobial compositions
CN104693083B (zh) * 2013-12-06 2017-03-29 沈阳有色金属研究院 一种改进的烯丙基硫代氨基甲酸酯的制备方法
JP2023503926A (ja) * 2019-11-22 2023-02-01 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Ｔａｓｐａｓｅ１阻害剤およびその使用
CN116554063B (zh) * 2023-05-23 2025-03-07 江苏省农用激素工程技术研究中心有限公司 氟胺磺隆中间体的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS58210088A (ja) * 1982-05-17 1983-12-07 ジ・アツプジヨン・カンパニ− 抗アテロ−ム性動脈硬化症アザフロクロモン
DD273571A1 (de) * 1988-07-04 1989-11-22 Fahlberg List Veb Insektizide mittel
DD286171A5 (de) * 1989-07-13 1991-01-17 Veb Fahlberg-List,Chemische Und Pharmazeutische Fabriken,De Verfahren zur herstellung von 2-dialkylamino-5,6-dialkylsubstituierten-1,3-oxazin-4-onen
JPH05509302A (ja) * 1990-06-20 1993-12-22 ジ・アップジョン・カンパニー 抗アテローム性動脈硬化性および抗血栓性１―ベンゾピラン―４―オン類および２―アミノ―１，３―ベンゾオキサジン―４―オン類

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2585064A (en) * 1952-02-12 Meta-thiazines
US3470168A (en) * 1967-03-31 1969-09-30 American Home Prod 2-substituted-4h-1,3-benzothiazin-4-one derivatives
US3522247A (en) * 1967-11-07 1970-07-28 Pfizer & Co C 2-amino-6,7-disubstituted-4h-1,3-benzothiazine-4-ones as bronchodilators
GB8611618D0 (en) * 1986-05-13 1986-06-18 Shell Int Research Fungicides
WO1990002129A1 (en) * 1988-08-16 1990-03-08 The Upjohn Company Bivalent ligands effective for blocking acat enzyme
WO1990006921A1 (en) * 1988-12-21 1990-06-28 The Upjohn Company Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
MY148480A (en) * 2004-05-24 2013-04-30 Amgen Inc Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS58210088A (ja) * 1982-05-17 1983-12-07 ジ・アツプジヨン・カンパニ− 抗アテロ−ム性動脈硬化症アザフロクロモン
DD273571A1 (de) * 1988-07-04 1989-11-22 Fahlberg List Veb Insektizide mittel
DD286171A5 (de) * 1989-07-13 1991-01-17 Veb Fahlberg-List,Chemische Und Pharmazeutische Fabriken,De Verfahren zur herstellung von 2-dialkylamino-5,6-dialkylsubstituierten-1,3-oxazin-4-onen
JPH05509302A (ja) * 1990-06-20 1993-12-22 ジ・アップジョン・カンパニー 抗アテローム性動脈硬化性および抗血栓性１―ベンゾピラン―４―オン類および２―アミノ―１，３―ベンゾオキサジン―４―オン類

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
AKERBLOM, E. B.: "Synthesis and structure- activity relationships of a series of antibacterially active 5-(5-nitro-2- furfurylidene)thiazolones, 5-(5-nitro-2- furylpropenylidene)thiazolones, and 6-(5-nitro- 2-furyl)-4H-1,3-thiazinones", JOURNAL OF MEDICINAL CHEMISTRY, vol. 17, no. 6, 1974, pages 609 - 615, XP002272538 *
CAPUANO, L. ET AL.: "Syntheses with 2-diazo-1, 3-diketones, I. 1,3-Oxazines", CHEMISCHE BERICHTE, vol. 109, no. 7, 1976, pages 2456 - 2461, XP008132625 *
HERMANOWSKI-VOSATKA, A. ET AL.: "llbeta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice", THE JOURNAL OF EXPERIMENTAL MEDICINE, vol. 202, no. 4, 2005, pages 517 - 527, XP008132620 *
LARSEN, J. S. ET AL.: "Synthesis of annelated analogues of 6-benzyl-1-(ethoxymethyl)-5- isopropyluracil (MKC-442) using 1,3-oxazine-2, 4-(3H)-diones as key intermediates", JOURNAL OF THE CHEMICAL SOCIETY. PERKIN TRANSACTIONS, vol. 1, no. 18, 2000, pages 3035 - 3038, XP008132624 *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2011161030A1 (de) 2010-06-21 2011-12-29 Sanofi Heterocyclisch substituierte methoxyphenylderivate mit oxogruppe, verfahren zu ihrer herstellung und ihre verwendung als gpr40 rezeptor modulatoren
WO2012004269A1 (de) 2010-07-05 2012-01-12 Sanofi ( 2 -aryloxy -acetylamino) - phenyl - propionsäurederivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2012004270A1 (de) 2010-07-05 2012-01-12 Sanofi Spirocyclisch substituierte 1,3-propandioxidderivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2012010413A1 (de) 2010-07-05 2012-01-26 Sanofi Aryloxy-alkylen-substituierte hydroxy-phenyl-hexinsäuren, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
US20130150414A1 (en) * 2010-08-31 2013-06-13 Meiji Seika Pharma Co., Ltd. Pest control agent
US9073866B2 (en) * 2010-08-31 2015-07-07 Meiji Seika Pharma Co., Ltd. Pest control agent
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US20210147366A1 (en) * 2018-04-06 2021-05-20 H. Lundbeck A/S Process for preparation of 2,2-dimethylpiperazine

Also Published As

Publication number Publication date
JPWO2009038064A1 (ja) 2011-01-06
US20100234363A1 (en) 2010-09-16
EP2208728A4 (en) 2011-12-21
EP2208728A1 (en) 2010-07-21

Similar Documents

Publication Publication Date Title
WO2009038064A1 (ja) Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する複素環誘導体
WO2005110410A3 (en) Kinase inhibitors as therapeutic agents
WO2008142986A1 (ja) Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有する含窒素複素環誘導体
WO2005074603A3 (en) Aminobenzoxazoles as therapeutic agents
MY148703A (en) Polycyclic cinnamide derivatives
MX2009004920A (es) Nuevos derivados de aminopirimidina como inhibidores de plk1.
WO2008126889A1 (ja) ヒドラジド化合物及びそれを含有する有害節足動物防除剤
WO2008126901A1 (ja) 含窒素複素環化合物およびそれを含有する医薬組成物
MY150507A (en) Polycyclic compound
MX2011008305A (es) Compuestos de piridazinona.
WO2007081569A3 (en) Cetp inhibitors
WO2006049835A3 (en) Indole and benzimidazole derivatives
WO2008060476A3 (en) Nitrogen-containing heterocyclic compounds and methods of use thereof
WO2008120655A1 (ja) Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有するオキサゾリジノン誘導体
WO2009057784A1 (ja) 複素環化合物
WO2008096829A1 (ja) ３環系化合物
UA95972C2 (ru) Аминопиридиновые производные с селективной ингибирующей активностью в отношении авроры а
WO2007014054A3 (en) Benzenesulfonamide inhibitor of ccr2 chemokine receptor
WO2008114812A1 (ja) Jak阻害剤
WO2008126890A1 (ja) ヒドラジド化合物およびそれを含有する有害節足動物防除剤
WO2009054439A1 (ja) Pai-1産生抑制剤
WO2007056159A3 (en) Hydrazone derivatives and uses thereof
WO2008140066A3 (en) Pyridone derivatives as p38a mapk inhibitors
WO2005095395A3 (en) Tetrahydronaphthyridine derivatives as cholesteryl ester transfer protein inhibitors
WO2009020137A1 (ja) アミノピラゾールアミド誘導体

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08831464

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2009533144

Country of ref document: JP

Kind code of ref document: A

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2008831464

Country of ref document: EP