WO2010026110A3 - Benzoxazines à substitution en 6 - Google Patents

Benzoxazines à substitution en 6 Download PDF

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Publication number
WO2010026110A3
WO2010026110A3 PCT/EP2009/061152 EP2009061152W WO2010026110A3 WO 2010026110 A3 WO2010026110 A3 WO 2010026110A3 EP 2009061152 W EP2009061152 W EP 2009061152W WO 2010026110 A3 WO2010026110 A3 WO 2010026110A3
Authority
WO
WIPO (PCT)
Prior art keywords
disorders
receptor antagonists
present
substituted benzoxazines
substituted
Prior art date
Application number
PCT/EP2009/061152
Other languages
English (en)
Other versions
WO2010026110A2 (fr
Inventor
Sabine Kolczewski
Olivier Roche
Lucinda Steward
Juergen Wichmann
Thomas Woltering
Original Assignee
F. Hoffmann-La Roche Ag
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 F. Hoffmann-La Roche Ag filed Critical F. Hoffmann-La Roche Ag
Priority to MX2011001926A priority Critical patent/MX2011001926A/es
Priority to EP09782348A priority patent/EP2328880B1/fr
Priority to BRPI0918068A priority patent/BRPI0918068A2/pt
Priority to CA2735775A priority patent/CA2735775A1/fr
Priority to ES09782348T priority patent/ES2394766T3/es
Priority to JP2011525514A priority patent/JP5368566B2/ja
Priority to CN2009801350989A priority patent/CN102149697A/zh
Priority to AU2009289305A priority patent/AU2009289305B2/en
Publication of WO2010026110A2 publication Critical patent/WO2010026110A2/fr
Publication of WO2010026110A3 publication Critical patent/WO2010026110A3/fr
Priority to IL210927A priority patent/IL210927A0/en

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    • 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
    • C07D265/18—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 position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • C07D498/08—Bridged systems

Abstract

La présente invention concerne des dérivés de benzoxazine à substitution en 6 représentés par la formule (I) dans laquelle X, Y, R1 et R2 sont tels que décrits par les présentes, ainsi que leur fabrication, des compositions pharmaceutiques les contenant et leur utilisation en tant que médicaments. Les composés actifs de la présente invention sont des antagonistes du récepteur 5-HT5A, utiles dans la prévention et/ou le traitement de la dépression, de troubles de l'anxiété, de la schizophrénie, de troubles de panique, de l'agoraphobie, de la phobie sociale, de troubles obsessionnels compulsifs, de troubles liés au stress post-traumatique, de la douleur, de troubles de la mémoire, de la démence, de troubles du comportement alimentaire, de dysfonctionnements sexuels, de troubles du sommeil, de la toxicomanie, de troubles moteurs, de la maladie de Parkinson, de troubles psychiatriques ou de troubles gastro-intestinaux.
PCT/EP2009/061152 2008-09-08 2009-08-28 Benzoxazines à substitution en 6 WO2010026110A2 (fr)

Priority Applications (9)

Application Number Priority Date Filing Date Title
MX2011001926A MX2011001926A (es) 2008-09-08 2009-08-28 Benzoxazinas 6-sustituidas.
EP09782348A EP2328880B1 (fr) 2008-09-08 2009-08-28 Benzoxazines 6-substitues en tant qu'antagonistes des recepteurs 5-ht-5a
BRPI0918068A BRPI0918068A2 (pt) 2008-09-08 2009-08-28 benzoxazinas 6-substituídas
CA2735775A CA2735775A1 (fr) 2008-09-08 2009-08-28 Benzoxazines a substitution en 6
ES09782348T ES2394766T3 (es) 2008-09-08 2009-08-28 Benzoxazinas 6-sustituidas como antagonistas del receptor 5-ht-5a
JP2011525514A JP5368566B2 (ja) 2008-09-08 2009-08-28 ５−ｔｈ−５ａ受容体アンタゴニストとしての６−置換ベンゾオキサジン
CN2009801350989A CN102149697A (zh) 2008-09-08 2009-08-28 作为5-ht-5a受体拮抗剂的6-取代的苯并*嗪
AU2009289305A AU2009289305B2 (en) 2008-09-08 2009-08-28 6-substituted benzoxazines as 5-HT-5A receptor antagonists
IL210927A IL210927A0 (en) 2008-09-08 2011-01-27 6-substituted benzoxazines as 5-ht-5a receptor antagonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08163833.0 2008-09-08
EP08163833 2008-09-08

Publications (2)

Publication Number Publication Date
WO2010026110A2 WO2010026110A2 (fr) 2010-03-11
WO2010026110A3 true WO2010026110A3 (fr) 2010-05-27

Family

ID=41381608

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2009/061152 WO2010026110A2 (fr) 2008-09-08 2009-08-28 Benzoxazines à substitution en 6

Country Status (12)

Country Link
US (1) US8163740B2 (fr)
EP (1) EP2328880B1 (fr)
JP (1) JP5368566B2 (fr)
KR (1) KR20110038179A (fr)
CN (1) CN102149697A (fr)
AU (1) AU2009289305B2 (fr)
BR (1) BRPI0918068A2 (fr)
CA (1) CA2735775A1 (fr)
ES (1) ES2394766T3 (fr)
IL (1) IL210927A0 (fr)
MX (1) MX2011001926A (fr)
WO (1) WO2010026110A2 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0920520A2 (pt) * 2008-09-08 2015-12-22 Hoffmann La Roche benzoxazinas 5-subistituídas
WO2014066713A1 (fr) * 2012-10-26 2014-05-01 The Procter & Gamble Company Procédé de préparation de 2-méthoxyméthyl-1,4-benzènediamine et sels associés
MX362371B (es) * 2012-10-26 2019-01-14 Noxell Corp Proceso para preparar 2-metoximetil-1,4-bencenodiamina y sales de esta.
CN110872281B (zh) * 2019-11-29 2024-02-27 淮北绿洲新材料有限责任公司 一种叔酚-糠胺型苯并噁嗪单体、固化树脂及其共聚树脂的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003045313A2 (fr) * 2001-11-27 2003-06-05 Merck & Co. Inc. Composés de 2-aminoquinoline
WO2007022946A1 (fr) * 2005-08-21 2007-03-01 Abbott Gmbh & Co. Kg Composes heterocycliques et leur utilisation en tant que partenaires de liaison des recepteurs 5-ht5

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0309781D0 (en) 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
MX2007011156A (es) * 2005-03-15 2007-10-23 Hoffmann La Roche Uso de 2-anilino-3,4-dihidro-quinazolinas como antagonistas del receptor 5ht5a.
CN101155787B (zh) * 2005-04-11 2010-11-24 弗·哈夫曼-拉罗切有限公司 (3,4-二氢-喹唑啉-2-基)-茚满-1-基-胺
EP1888538B1 (fr) * 2005-05-04 2009-11-18 F. Hoffmann-Roche AG (3,4-dihydro-quinazolin-2-yl)-(2-aryloxy-ethyl)-amines exerçant une activite sur le recepteur 5-ht
FR2888748B1 (fr) * 2005-07-19 2007-10-12 Biocodex Composes neuroprotecteurs et compositions pharmaceutiques les comprenant

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003045313A2 (fr) * 2001-11-27 2003-06-05 Merck & Co. Inc. Composés de 2-aminoquinoline
WO2007022946A1 (fr) * 2005-08-21 2007-03-01 Abbott Gmbh & Co. Kg Composes heterocycliques et leur utilisation en tant que partenaires de liaison des recepteurs 5-ht5

Also Published As

Publication number Publication date
AU2009289305A1 (en) 2010-03-11
KR20110038179A (ko) 2011-04-13
MX2011001926A (es) 2011-04-05
WO2010026110A2 (fr) 2010-03-11
AU2009289305B2 (en) 2012-08-02
EP2328880A2 (fr) 2011-06-08
EP2328880B1 (fr) 2012-10-31
ES2394766T3 (es) 2013-02-05
US20100063037A1 (en) 2010-03-11
CA2735775A1 (fr) 2010-03-11
CN102149697A (zh) 2011-08-10
BRPI0918068A2 (pt) 2015-12-01
JP5368566B2 (ja) 2013-12-18
US8163740B2 (en) 2012-04-24
IL210927A0 (en) 2011-04-28
JP2012501993A (ja) 2012-01-26

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