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WO2009035020A1 - 新規ジヒドロナフタレン化合物及びその用途 - Google Patents

新規ジヒドロナフタレン化合物及びその用途 Download PDF

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Publication number
WO2009035020A1
WO2009035020A1 PCT/JP2008/066384 JP2008066384W WO2009035020A1 WO 2009035020 A1 WO2009035020 A1 WO 2009035020A1 JP 2008066384 W JP2008066384 W JP 2008066384W WO 2009035020 A1 WO2009035020 A1 WO 2009035020A1
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integer
atom
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formula
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PCT/JP2008/066384
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English (en)
French (fr)
Inventor
Isamu Shiina
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Tokyo University of Science
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Tokyo University of Science
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Application filed by Tokyo University of Science filed Critical Tokyo University of Science
Priority to JP2009532207A priority Critical patent/JP5565667B2/ja
Priority to US12/675,331 priority patent/US8183235B2/en
Priority to EP08830489A priority patent/EP2192108B1/en
Publication of WO2009035020A1 publication Critical patent/WO2009035020A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/24—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system containing rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

　ラソフォキシフェンあるいはナフォキシジンに比較し生産効率に優れた化学構造を有するジヒドロナフタレン化合物として以下の式（Ｉ）で表される化合物を提供する。この化合物は、プロテアソーム阻害剤及び／又は抗ガン剤として有効である。 （但し、式中、２つの－（ＣＨ２）ｌ－Ｎ（Ｒ１）（Ｒ２）基は同一の置換基を表し、Ｒ１及びＲ２は、水素原子、又はそれぞれ同一若しくは異なるアルキル基を表し、Ｒ１及びＲ２は、一緒になってそれらを有する窒素原子とともに、又はさらに酸素原子、硫黄原子、及び窒素原子のいずれか１種以上とともに、単環式複素環を形成してもよい。また、Ｒ３、Ｒ４、Ｒ５は、それぞれ水素原子、アルキル基、アシル基、脂環式基、芳香族基、ハロゲン原子、アシルオキシ基、シアノ基、及びニトロ基から選ばれた１種以上の置換基を表し、ｌは２～５の整数、ｎは１～４の整数、ｍは１～５の整数、ｑは１～３の整数をそれぞれ表す。）
PCT/JP2008/066384 2007-09-11 2008-09-11 新規ジヒドロナフタレン化合物及びその用途 Ceased WO2009035020A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2009532207A JP5565667B2 (ja) 2007-09-11 2008-09-11 新規ジヒドロナフタレン化合物及びその用途
US12/675,331 US8183235B2 (en) 2007-09-11 2008-09-11 Dihydronaphthalene compound and use thereof
EP08830489A EP2192108B1 (en) 2007-09-11 2008-09-11 Novel dihydronaphthalene compound and use thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007235933 2007-09-11
JP2007-235933 2007-09-11

Publications (1)

Publication Number Publication Date
WO2009035020A1 true WO2009035020A1 (ja) 2009-03-19

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PCT/JP2008/066384 Ceased WO2009035020A1 (ja) 2007-09-11 2008-09-11 新規ジヒドロナフタレン化合物及びその用途

Country Status (4)

Country Link
US (1) US8183235B2 (ja)
EP (1) EP2192108B1 (ja)
JP (2) JP5565667B2 (ja)
WO (1) WO2009035020A1 (ja)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2013165005A1 (ja) * 2012-05-01 2015-12-24 学校法人東京理科大学 新規化合物及びその製造方法並びに抗がん剤
WO2021075147A1 (ja) * 2019-10-15 2021-04-22 学校法人東京理科大学 Ｂｒａｐ２作用増強剤

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2748434T3 (es) 2014-01-10 2020-03-16 Univ Cornell Dipéptidos como inhibidores de inmunoproteasomas humanos
CN114796207A (zh) 2014-08-18 2022-07-29 康奈尔大学 作为人免疫蛋白酶体的抑制剂的二肽模拟物
CN108351169B (zh) * 2015-10-15 2022-01-28 康奈尔大学 蛋白酶体抑制剂及其用途
CN105541662B (zh) * 2015-12-28 2018-04-17 云南大学 二氢萘类化合物的固相合成方法
WO2019075252A1 (en) 2017-10-11 2019-04-18 Cornell University PEPTIDOMIMETIC INHIBITORS OF PROTEASOME

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3274213A (en) * 1961-09-05 1966-09-20 Upjohn Co Alkoxy-substituted 2-phenyl-1-(tertiary-aminoalkoxy)phenyl-3, 4-dihydronaphthalenes
JP2006117648A (ja) 2004-09-22 2006-05-11 Tokyo Univ Of Science タモキシフェン類縁体を有効成分として含有する抗ガン剤
JP2007224016A (ja) * 2006-01-26 2007-09-06 Tokyo Univ Of Science ラソフォキシフェン及びその類縁体の製造方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1336602A1 (en) * 2002-02-13 2003-08-20 Giovanni Scaramuzzino Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
JP4066238B2 (ja) * 2002-06-21 2008-03-26 学校法人東京理科大学 タモキシフェン類縁体及びその製造方法
JP4572407B2 (ja) * 2005-03-04 2010-11-04 学校法人東京理科大学 ドロロキシフェンの製造方法
JP2007246493A (ja) * 2006-03-20 2007-09-27 Tokyo Univ Of Science タモキシフェン類縁体を有効成分として含有する血管新生抑制剤
JP5207226B2 (ja) * 2006-09-13 2013-06-12 学校法人東京理科大学 タモキシフェン類縁体を有効成分として含有するプロテアソーム阻害剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3274213A (en) * 1961-09-05 1966-09-20 Upjohn Co Alkoxy-substituted 2-phenyl-1-(tertiary-aminoalkoxy)phenyl-3, 4-dihydronaphthalenes
JP2006117648A (ja) 2004-09-22 2006-05-11 Tokyo Univ Of Science タモキシフェン類縁体を有効成分として含有する抗ガン剤
JP2007224016A (ja) * 2006-01-26 2007-09-06 Tokyo Univ Of Science ラソフォキシフェン及びその類縁体の製造方法

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
F. L. STEINBAUM; R. L. DE JAGER; I. H. KRAKOFF: "Clinical Trial of Nafoxidine in Advanced Breast Cancer", MEDICAL AND PEDIATRIC ONCOLOGY, vol. 4, 1978, pages 123 - 126
HYDER M. SALMAN ET AL.: "Uterine Expression of Vascular Endothelial Growth Factor Is Increased by Estradiol and Tamoxifen1", CANCER RESEARCH, vol. 56, 1996, pages 3954 - 3960, XP008130181 *
See also references of EP2192108A4 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2013165005A1 (ja) * 2012-05-01 2015-12-24 学校法人東京理科大学 新規化合物及びその製造方法並びに抗がん剤
WO2021075147A1 (ja) * 2019-10-15 2021-04-22 学校法人東京理科大学 Ｂｒａｐ２作用増強剤

Also Published As

Publication number Publication date
EP2192108A1 (en) 2010-06-02
JP5565667B2 (ja) 2014-08-06
JP5747394B2 (ja) 2015-07-15
EP2192108A4 (en) 2010-12-01
US20100249400A1 (en) 2010-09-30
JPWO2009035020A1 (ja) 2010-12-24
JP2014167005A (ja) 2014-09-11
US8183235B2 (en) 2012-05-22
EP2192108B1 (en) 2013-03-27

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