JPH10512589A - 8−アザビシクロ[3.2.1]オクト−2−エン誘導体、それらの製造及び使用 - Google Patents
8−アザビシクロ[3.2.1]オクト−2−エン誘導体、それらの製造及び使用Info
- Publication number
- JPH10512589A JPH10512589A JP9514726A JP51472697A JPH10512589A JP H10512589 A JPH10512589 A JP H10512589A JP 9514726 A JP9514726 A JP 9514726A JP 51472697 A JP51472697 A JP 51472697A JP H10512589 A JPH10512589 A JP H10512589A
- Authority
- JP
- Japan
- Prior art keywords
- azabicyclo
- disorder
- alkyl
- oct
- ene
- 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.)
- Granted
Links
Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61P25/22—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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- C07D451/04—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 with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式: [式中、 Rは水素、アルキル、アルケニル、アルキニル、シクロアルキル、シクロアル キルアルキル又は2−ヒドロキシエチルであり; R4は、 ハロゲン、CF3、CN、アルコキシ、シクロアルコキシ、アルキル、シクロ アルキル、アルケニル、アルキニル、アミノ、ニトロ、ヘテロアリール及びアリ ールから成る群から選択される置換基によって1回以上置換されうるフェニル; 3,4−メチレンジオキシフェニル; ハロゲン、CF3、CN、アルコキシ、シクロアルコキシ、アルキル、シクロ アルキル、アルケニル、アルキニル、アミノ、ニトロ、ヘテロアリール及びアリ ールから成る群から選択される置換基によって1回以上置換されうるベンジル; ハロゲン、CF3、CN、アルコキシ、シクロアルコキシ、アルキル、シクロ アルキル、アルケニル、アルキニル、アミノ、ニトロ、ヘテロアリール及びアリ ールから成る群から選択される置換基によって1回以上置換されうるヘテロアリ ール; ハロゲン、CF3、CN、アルコキシ、シクロアルコキシ、アルキル、シクロ アルキル、アルケニル、アルキニル、アミノ、ニトロ、ヘテロアリール及びアリ ールから成る群から選択される置換基によって1回以上置換されうるナフチル である] で示される化合物又はそのエナンチオマーのいずれか又はそれらの任意の混合物 、又はそれらの製薬的に受容される塩。 2.下記化合物: (±)−3−(3,4−ジクロロフェニル)−8−メチル−8−アザビシクロ[ 3.2.1]オクト−2−エン、 (±)−3−(4−クロロフェニル)−8−メチル−8−アザビシクロ[3.2 .1]オクト−2−エン、又は (±)−3−(3,4−ジクロロフェニル)−8−アザビシクロ[3.2.1] オクト−2−エン、 又はこれらの製薬的に受容される付加塩 である、請求項1記載の化合物。 3.少なくとも1種の製薬的に受容されるキャリヤー又は希釈剤と共に、請求 項1記載の化合物の治療有効量を含む薬剤組成物。 4.中枢神経系におけるモノアミン神経伝達物質の再吸収の阻害に反応する、 ヒトを包含する生存動物体における障害又は疾患の治療用薬剤を製造するための 請求項1記載の化合物の使用。 5.中枢神経系におけるセロトニン再吸収の阻害に反応する、ヒトを包含する 生存動物体における障害又は疾患の治療用薬剤を製造するための請求項1記載の 化合物の使用。 6.うつ病と関連障害、例えば偽痴呆若しくはGanser症候群、強迫障害 、パニック障害、記憶欠損、注意力欠如機能亢進障害、肥満、不安及び摂食障害 の治療用薬剤を製造するための請求項1記載の化合物の使用。 7.用いる化合物が、 (±)−3−(3,4−ジクロロフェニル)−8−メチル−8−アザビシクロ[ 3.2.1]オクト−2−エン、 (±)−3−(4−クロロフェニル)−8−メチル−8−アザビシクロ[3.2 .1]オクト−2−エン、又は (±)−3−(3,4−ジクロロフェニル)−8−アザビシクロ[3.2.1] オクト−2−エン、 又はこれらの製薬的に受容される付加塩である、請求項4〜6のいずれか1項に 記載の使用。 8.モノアミン神経伝達物質の再吸収の阻害に反応する、ヒトを包含する生存 動物体の障害又は疾患の治療方法であって、治療を必要とする、このようなヒト を包含する生存動物体に請求項1記載の化合物の治療有効量を投与する工程を含 む方法。 9.セロトニンの再吸収の阻害に反応する、ヒトを包含する生存動物体の障害 又は疾患の治療方法であって、治療を必要とする、このようなヒトを包含する生 存動物体に請求項1記載の化合物の治療有効量を投与する工程を含む方法。 10.うつ病と関連障害、例えば偽痴呆若しくはGanser症候群、強迫障害 、パニック障害、記憶欠損、注意力欠如機能亢進障害、肥満、不安及び摂食障害 を治療する、請求項8又は9に記載の方法。 11.請求項1記載の化合物の製造方法であって、 式: [式中、RとR4は請求項1で定義した通りである] で示される化合物を脱水する工程と、その後に任意にその製薬的に受容される付 加塩を形成する工程を含む方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DK115695 | 1995-10-13 | ||
DK1156/95 | 1995-10-13 | ||
PCT/EP1996/004449 WO1997013770A1 (en) | 1995-10-13 | 1996-10-11 | 8-azabicyclo[3.2.1]oct-2-ene derivatives, their preparation and use |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH10512589A true JPH10512589A (ja) | 1998-12-02 |
JP3462505B2 JP3462505B2 (ja) | 2003-11-05 |
Family
ID=8101642
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP51472697A Expired - Fee Related JP3462505B2 (ja) | 1995-10-13 | 1996-10-11 | 8−アザビシクロ[3.2.1]オクト−2−エン誘導体、それらの製造及び使用 |
Country Status (24)
Country | Link |
---|---|
US (1) | US6100275A (ja) |
EP (1) | EP0859777B1 (ja) |
JP (1) | JP3462505B2 (ja) |
KR (1) | KR100274829B1 (ja) |
CN (1) | CN1083840C (ja) |
AT (1) | ATE362931T1 (ja) |
AU (1) | AU709327B2 (ja) |
BR (1) | BR9610960A (ja) |
CA (1) | CA2233541C (ja) |
CZ (1) | CZ285093B6 (ja) |
DE (1) | DE69637097T2 (ja) |
DK (1) | DK0859777T3 (ja) |
EE (1) | EE03446B1 (ja) |
HU (1) | HUP9802433A3 (ja) |
IL (1) | IL123583A (ja) |
IS (1) | IS4681A (ja) |
NO (1) | NO980919L (ja) |
NZ (1) | NZ320216A (ja) |
PL (1) | PL185357B1 (ja) |
RU (1) | RU2157372C2 (ja) |
SK (1) | SK283425B6 (ja) |
TR (1) | TR199800628T2 (ja) |
UA (1) | UA63894C2 (ja) |
WO (1) | WO1997013770A1 (ja) |
Families Citing this family (31)
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GB9510459D0 (en) | 1995-05-24 | 1995-07-19 | Zeneca Ltd | Bicyclic amines |
KR20000010972A (ko) * | 1996-05-13 | 2000-02-25 | 사라 엔 람베쓰 | 살충제용 이환식 아민 |
GB9623944D0 (en) * | 1996-11-15 | 1997-01-08 | Zeneca Ltd | Bicyclic amine derivatives |
GB9624114D0 (en) * | 1996-11-20 | 1997-01-08 | Zeneca Ltd | Pesticidal bicyclic amine derivatives |
GB9624611D0 (en) * | 1996-11-26 | 1997-01-15 | Zeneca Ltd | Bicyclic amine compounds |
CZ184199A3 (cs) | 1996-11-26 | 1999-08-11 | Zeneca Limited | Deriváty 8-azabicyklo[3,2,1]oktanu, 8-azabicyklo[3,2,1]okt-6-enu, 9-azabicyklo[3,3,1]nonanu, 9-aza-3-oxabicyklo[3,3,1]nonanu a 9-aza-3-thiabicyklo[3,3,1]nonanu, způsob jejich přípravy a insekticidní, akaricidní nebo nematocidní prostředky, které je obsahují |
GB9706222D0 (en) * | 1997-03-26 | 1997-05-14 | Zeneca Ltd | Bicyclic amine derivatives |
CZ298824B6 (cs) | 1997-05-30 | 2008-02-20 | Neurosearch A/S | Deriváty 8-azabicyklo[3.2.1]okt-2-enu, zpusob jejich prípravy a jejich použití |
GB9726033D0 (en) | 1997-12-09 | 1998-02-04 | Zeneca Ltd | Chemical process |
TWI221842B (en) * | 1997-12-11 | 2004-10-11 | Syngenta Ltd | Process for the preparation of 8-azabicyclo(3.2.1)octane derivatives |
WO1999038866A1 (en) * | 1998-01-28 | 1999-08-05 | Neurosearch A/S | 8-azabicyclo[3.2.1]oct-2-ene derivatives in labelled form and use of 8-azabicyclo[3.2.1]oct-2-ene derivatives in labelled and unlabelled form |
US6403605B1 (en) | 1998-05-29 | 2002-06-11 | Queen's University At Kingston | Methods for the normalization of sexual response and amelioration of long term genital tissue degradation |
CA2335336A1 (en) * | 1998-06-19 | 1999-12-23 | James Edmund Audia | Inhibition of serotonin reuptake |
ATE259804T1 (de) | 1998-11-27 | 2004-03-15 | Neurosearch As | 8-azabicyclo(3.2.1)okt-2-en- und -oktanderivate |
WO2000044746A1 (en) | 1999-01-28 | 2000-08-03 | Neurosearch A/S | Novel azabicyclo derivatives and their use |
JP2002538134A (ja) * | 1999-03-01 | 2002-11-12 | ファイザー・インク | 療法に有用な1,2,3,4−テトラヒドロ−1−ナフタレンアミン化合物 |
DE122009000036I2 (de) | 1999-09-03 | 2010-05-06 | Apbi Holdings Llc | Verwendung von Dapoxetin, ein selektiver Serotonin Aufnahme Inhibitor mit schnellem Wirkungseintritt, zur Behandlung von sexueller Dysfunktion |
AU2049501A (en) | 1999-12-20 | 2001-07-03 | Eli Lilly And Company | Benzofuran derivatives |
PT1289996E (pt) | 2000-05-25 | 2005-07-29 | Targacept Inc | Heteroarildiazabicicloalcanos como ligandos do receptor colinergico nicotinico |
US6667314B2 (en) | 2000-05-26 | 2003-12-23 | Pfizer, Inc. | Tropane derivatives useful in therapy |
US6579878B1 (en) | 2000-07-07 | 2003-06-17 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
US6624167B1 (en) | 2000-08-04 | 2003-09-23 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
JP4312456B2 (ja) * | 2000-10-13 | 2009-08-12 | ニューロサーチ、アクティーゼルスカブ | ニコチン性レセプターアゴニスト及びモノアミン作動性物質の組み合わせ作用による情動障害の治療法 |
EP1379269B1 (en) | 2001-04-09 | 2009-03-04 | Neurosearch A/S | Adenosine a2a receptor antagonists combined with neurotrophic activity compounds in the treatment of parkinson's disease |
AR035898A1 (es) | 2001-05-25 | 2004-07-21 | Wyeth Corp | Aril-8-azabiciclo[3.2.1]octanos, un proceso para su preparacion, una formulacion y el uso de dichos compuestos para la manufactura de un medicamento para el tratamiento de la depresion |
MXPA04010965A (es) | 2002-05-07 | 2005-01-25 | Neurosearch As | Derivados de etinilo azaciclico novedoso. |
EP2272847A1 (en) | 2005-04-08 | 2011-01-12 | NeuroSearch A/S | Enantiomers and their use as monoamine neurotransmitter re-uptake inhibitors |
TW200744590A (en) * | 2005-09-01 | 2007-12-16 | Neurosearch As | Novel compounds |
KR100812499B1 (ko) * | 2006-10-16 | 2008-03-11 | 이도훈 | 항경련제 |
TWI415850B (zh) * | 2007-07-20 | 2013-11-21 | Theravance Inc | 製備mu類鴉片受體拮抗劑之中間物的方法 |
WO2009109518A1 (en) * | 2008-03-05 | 2009-09-11 | Neurosearch A/S | Novel 4-benzhydryl-tetrahydro-pyridine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors |
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1996
- 1996-10-11 IL IL12358396A patent/IL123583A/xx not_active IP Right Cessation
- 1996-10-11 BR BR9610960A patent/BR9610960A/pt not_active Application Discontinuation
- 1996-10-11 AU AU72917/96A patent/AU709327B2/en not_active Ceased
- 1996-10-11 SK SK287-98A patent/SK283425B6/sk unknown
- 1996-10-11 DE DE69637097T patent/DE69637097T2/de not_active Expired - Lifetime
- 1996-10-11 US US09/043,294 patent/US6100275A/en not_active Expired - Fee Related
- 1996-10-11 CZ CZ98758A patent/CZ285093B6/cs not_active IP Right Cessation
- 1996-10-11 TR TR1998/00628T patent/TR199800628T2/xx unknown
- 1996-10-11 EE EE9800062A patent/EE03446B1/xx not_active IP Right Cessation
- 1996-10-11 JP JP51472697A patent/JP3462505B2/ja not_active Expired - Fee Related
- 1996-10-11 NZ NZ320216A patent/NZ320216A/xx not_active IP Right Cessation
- 1996-10-11 KR KR1019980702103A patent/KR100274829B1/ko not_active IP Right Cessation
- 1996-10-11 WO PCT/EP1996/004449 patent/WO1997013770A1/en active IP Right Grant
- 1996-10-11 CA CA002233541A patent/CA2233541C/en not_active Expired - Fee Related
- 1996-10-11 EP EP96934662A patent/EP0859777B1/en not_active Expired - Lifetime
- 1996-10-11 PL PL96326195A patent/PL185357B1/pl not_active IP Right Cessation
- 1996-10-11 CN CN96197566A patent/CN1083840C/zh not_active Expired - Fee Related
- 1996-10-11 DK DK96934662T patent/DK0859777T3/da active
- 1996-10-11 RU RU98105169/04A patent/RU2157372C2/ru not_active IP Right Cessation
- 1996-10-11 AT AT96934662T patent/ATE362931T1/de active
- 1996-10-11 HU HU9802433A patent/HUP9802433A3/hu unknown
- 1996-11-10 UA UA98031543A patent/UA63894C2/uk unknown
-
1998
- 1998-03-03 NO NO19980919A patent/NO980919L/no not_active Application Discontinuation
- 1998-03-04 IS IS4681A patent/IS4681A/is unknown
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