JP6315991B2 - 認知機能および運動機能の増強剤としてのa2aアンタゴニスト - Google Patents
認知機能および運動機能の増強剤としてのa2aアンタゴニスト Download PDFInfo
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- JP6315991B2 JP6315991B2 JP2013537896A JP2013537896A JP6315991B2 JP 6315991 B2 JP6315991 B2 JP 6315991B2 JP 2013537896 A JP2013537896 A JP 2013537896A JP 2013537896 A JP2013537896 A JP 2013537896A JP 6315991 B2 JP6315991 B2 JP 6315991B2
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
- A61K31/198—Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/14—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
- A61P25/24—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Description
A2aアンタゴニストおよびそれらの薬学的に許容される塩は、任意でドーパミン前駆体またはドーパミン受容体アゴニストと共に、例えば、薬学的調製物の形態をとって、薬剤として用いることができる。薬学的調製物は、例えば、錠剤、被覆錠剤、糖衣錠、硬ゼラチンカプセルおよび軟ゼラチンカプセル、溶液、乳濁液、または懸濁液の形態をとって、経口で投与することができる。しかしながら、投与はまた、例えば座剤の形態をとって、直腸内に、例えば注射溶液の形態をとって、非経口でも実施することができる。
本開示の一態様において、対象を治療する方法が提供され、A2aアンタゴニストまたはその塩もしくは溶媒和物が、治療に必要な十分な期間、ドーパミン前駆体またはドーパミン受容体アゴニストと併用して投与される。
(実施例)
パーキンソン病(PD)患者は、A2aアンタゴニストのドーパミン前駆体との同時投与の認知機能および運動機能への効果を評価するための二重盲検のクロスオーバー研究に参加した。A2aアンタゴニストは、4−ヒドロキシ−4−メチル−ピペリジン−1−カルボン酸−(4−メトキシ−7−モルホリン−4−イル−ベンゾチアゾール−2−イル)−アミドであり、ドーパミン前駆体はレボドパであった。
Claims (5)
- 治療的有効量の4−ヒドロキシ−4−メチル−ピペリジン−1−カルボン酸−(4−メトキシ−7−モルホリン−4−イル−ベンゾチアゾール−2−イル)−アミドを含む神経変性疾患に関連した症状を治療するための医薬組成物であって、
前記組成物が、治療的有効量のドーパミン受容体アゴニストとの組み合わせで使用され、
前記症状が、認知機能障害または認知低下であり、
前記ドーパミン受容体アゴニストが、アポモルフィン、プラミペキソール、ブロモクリプチン、カベルゴリン、ロピニロール、ロチゴチン、およびそれらの組み合わせからなる群より選択され、
前記神経変性疾患がパーキンソン病であり、
前記組成物が、治療的有効量のドーパミン前駆体との組み合わせで使用され、
前記ドーパミン前駆体がレボドパまたはその塩である、前記医薬組成物。 - 哺乳動物を治療するための、請求項1に記載の医薬組成物。
- ヒトを治療するための、請求項2に記載の医薬組成物。
- 前記治療的有効量のドーパミン受容体アゴニストをさらに含む、請求項1に記載の医薬組成物。
- 前記治療的有効量のドーパミン受容体アゴニストからなる別の医薬組成物と組み合わせて使用される、請求項1に記載の医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
USPCT/US2010/055681 | 2010-11-05 | ||
PCT/US2010/055681 WO2012060844A1 (en) | 2010-11-05 | 2010-11-05 | A2a antagonists as cognition and motor function enhancers |
PCT/US2011/059466 WO2012061787A1 (en) | 2010-11-05 | 2011-11-04 | A2a antagonists as cognition and motor function enhancers |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016164379A Division JP6444951B2 (ja) | 2010-11-05 | 2016-08-25 | 認知機能および運動機能の増強剤としてのa2aアンタゴニスト |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2013541593A JP2013541593A (ja) | 2013-11-14 |
JP6315991B2 true JP6315991B2 (ja) | 2018-04-25 |
Family
ID=46024745
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013537896A Expired - Fee Related JP6315991B2 (ja) | 2010-11-05 | 2011-11-04 | 認知機能および運動機能の増強剤としてのa2aアンタゴニスト |
JP2016164379A Expired - Fee Related JP6444951B2 (ja) | 2010-11-05 | 2016-08-25 | 認知機能および運動機能の増強剤としてのa2aアンタゴニスト |
JP2018221977A Expired - Fee Related JP6611896B2 (ja) | 2010-11-05 | 2018-11-28 | 認知機能および運動機能の増強剤としてのa2aアンタゴニスト |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016164379A Expired - Fee Related JP6444951B2 (ja) | 2010-11-05 | 2016-08-25 | 認知機能および運動機能の増強剤としてのa2aアンタゴニスト |
JP2018221977A Expired - Fee Related JP6611896B2 (ja) | 2010-11-05 | 2018-11-28 | 認知機能および運動機能の増強剤としてのa2aアンタゴニスト |
Country Status (15)
Country | Link |
---|---|
US (2) | US20130317019A1 (ja) |
EP (1) | EP2635256B1 (ja) |
JP (3) | JP6315991B2 (ja) |
KR (2) | KR102166229B1 (ja) |
CN (3) | CN109223799A (ja) |
AU (3) | AU2011323152A1 (ja) |
BR (1) | BR112013011068A2 (ja) |
CA (1) | CA2816834A1 (ja) |
EA (2) | EA202091356A1 (ja) |
ES (1) | ES2842968T3 (ja) |
HK (1) | HK1245138A1 (ja) |
IL (2) | IL225868B (ja) |
MX (1) | MX2013005014A (ja) |
NZ (2) | NZ609803A (ja) |
WO (2) | WO2012060844A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10653699B2 (en) | 2015-06-19 | 2020-05-19 | Biotie Therapies, Inc. | Controlled-release tozadenant formulations |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6339758B2 (ja) * | 2012-07-02 | 2018-06-06 | 国立研究開発法人国立長寿医療研究センター | 軽度認知機能障害の有無の診断システム、認知機能検査用端末及び認知機能検査用プログラム |
JO3544B1 (ar) * | 2015-03-19 | 2020-07-05 | Kyowa Kirin Co Ltd | عامل علاجي للاختلال الوظيفي في الفص الجبهي |
WO2018013951A1 (en) * | 2016-07-15 | 2018-01-18 | Northwestern University | Targeting adenosine a2a receptors for the treatment of levodopa-induced dyskinesias |
WO2018059531A1 (zh) * | 2016-09-30 | 2018-04-05 | 苏州晶云药物科技有限公司 | 一种腺苷a2a受体拮抗剂药物的晶型及其制备方法和用途 |
EP4069239A4 (en) * | 2019-12-02 | 2023-11-29 | Sinopia Biosciences, Inc. | TREATMENT OF COGNITIVE DISORDERS USING TRAPIDIL |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2942082B1 (en) * | 2002-01-28 | 2019-03-06 | Kyowa Hakko Kogyo Co., Ltd | A2a receptor antogonists for use in the treatment of movement disorders |
PT1753760E (pt) * | 2004-05-24 | 2008-02-12 | Hoffmann La Roche | '' - metoxi - 7 - morfolin - 4 - il - benzotiazol - 2 - il) - amida do ácido 4 - hidroxi - 4 - metil - piperidina - 1 - carboxílico'' |
US7576073B2 (en) * | 2004-05-28 | 2009-08-18 | UNIVERSITé LAVAL | Combined therapy for the treatment of parkinson's disease |
US8168785B2 (en) * | 2009-06-17 | 2012-05-01 | Biotie Therapies, Inc. | Benzothiazole derivatives |
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2010
- 2010-11-05 WO PCT/US2010/055681 patent/WO2012060844A1/en active Application Filing
-
2011
- 2011-11-04 WO PCT/US2011/059466 patent/WO2012061787A1/en active Application Filing
- 2011-11-04 EA EA202091356A patent/EA202091356A1/ru unknown
- 2011-11-04 ES ES11838922T patent/ES2842968T3/es active Active
- 2011-11-04 KR KR1020197005483A patent/KR102166229B1/ko active IP Right Grant
- 2011-11-04 EP EP11838922.0A patent/EP2635256B1/en active Active
- 2011-11-04 MX MX2013005014A patent/MX2013005014A/es unknown
- 2011-11-04 US US13/882,132 patent/US20130317019A1/en not_active Abandoned
- 2011-11-04 JP JP2013537896A patent/JP6315991B2/ja not_active Expired - Fee Related
- 2011-11-04 CN CN201811049033.XA patent/CN109223799A/zh active Pending
- 2011-11-04 BR BR112013011068A patent/BR112013011068A2/pt not_active IP Right Cessation
- 2011-11-04 CA CA2816834A patent/CA2816834A1/en not_active Abandoned
- 2011-11-04 NZ NZ609803A patent/NZ609803A/en not_active IP Right Cessation
- 2011-11-04 AU AU2011323152A patent/AU2011323152A1/en not_active Abandoned
- 2011-11-04 NZ NZ746118A patent/NZ746118A/en not_active IP Right Cessation
- 2011-11-04 EA EA201390653A patent/EA035900B1/ru not_active IP Right Cessation
- 2011-11-04 CN CN2011800534450A patent/CN103429221A/zh active Pending
- 2011-11-04 CN CN201710583855.5A patent/CN107281491A/zh active Pending
- 2011-11-04 KR KR1020137014385A patent/KR101955045B1/ko active IP Right Grant
-
2013
- 2013-04-21 IL IL225868A patent/IL225868B/en active IP Right Grant
-
2016
- 2016-08-25 JP JP2016164379A patent/JP6444951B2/ja not_active Expired - Fee Related
-
2017
- 2017-03-02 AU AU2017201446A patent/AU2017201446A1/en not_active Abandoned
-
2018
- 2018-04-13 HK HK18104835.1A patent/HK1245138A1/zh unknown
- 2018-11-28 JP JP2018221977A patent/JP6611896B2/ja not_active Expired - Fee Related
- 2018-12-28 AU AU2018286608A patent/AU2018286608B2/en not_active Ceased
-
2019
- 2019-04-29 IL IL266321A patent/IL266321A/en unknown
-
2021
- 2021-06-07 US US17/341,106 patent/US20220125772A1/en not_active Abandoned
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10653699B2 (en) | 2015-06-19 | 2020-05-19 | Biotie Therapies, Inc. | Controlled-release tozadenant formulations |
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