CN105164134B - 作为pde10抑制剂的咪唑并‑三嗪衍生物 - Google Patents
作为pde10抑制剂的咪唑并‑三嗪衍生物 Download PDFInfo
- Publication number
- CN105164134B CN105164134B CN201480024798.1A CN201480024798A CN105164134B CN 105164134 B CN105164134 B CN 105164134B CN 201480024798 A CN201480024798 A CN 201480024798A CN 105164134 B CN105164134 B CN 105164134B
- Authority
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- China
- Prior art keywords
- methyl
- bases
- pharmaceutically acceptable
- acceptable salt
- mmol
- 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.)
- Expired - Fee Related
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- 0 C*1*CCC1 Chemical compound C*1*CCC1 0.000 description 3
- VJZRCEYUXOUVNY-QOCNPQIPSA-N B/C(/C(/CC)=C(/C)\NC)=C\C(OC)=O Chemical compound B/C(/C(/CC)=C(/C)\NC)=C\C(OC)=O VJZRCEYUXOUVNY-QOCNPQIPSA-N 0.000 description 1
- ZDGDGQPIOQEJCQ-UHFFFAOYSA-N C(C1)C1c1nc(CCNC2)c2cn1 Chemical compound C(C1)C1c1nc(CCNC2)c2cn1 ZDGDGQPIOQEJCQ-UHFFFAOYSA-N 0.000 description 1
- JGFZNNIVVJXRND-UHFFFAOYSA-N CCN(C(C)C)C(C)C Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 1
- QZJCVZCHEHLGQZ-UHFFFAOYSA-N Cc1nc(-c(c(Cl)c2)ccc2F)c2[n]1ncnc2N1Cc2cnc(C3CC3)nc2CC1 Chemical compound Cc1nc(-c(c(Cl)c2)ccc2F)c2[n]1ncnc2N1Cc2cnc(C3CC3)nc2CC1 QZJCVZCHEHLGQZ-UHFFFAOYSA-N 0.000 description 1
- NCJAULVUNGNDFA-DOSYZTLSSA-O Cc1nc(Br)c(/C(/[n]2ncnc2)=N\C=[NH2+])[nH]1 Chemical compound Cc1nc(Br)c(/C(/[n]2ncnc2)=N\C=[NH2+])[nH]1 NCJAULVUNGNDFA-DOSYZTLSSA-O 0.000 description 1
- JFJMZCWUAQSDBT-UHFFFAOYSA-N Cc1nc(Br)c2[n]1ncnc2N(CC1)Cc2c1nc(C1CC1)nc2 Chemical compound Cc1nc(Br)c2[n]1ncnc2N(CC1)Cc2c1nc(C1CC1)nc2 JFJMZCWUAQSDBT-UHFFFAOYSA-N 0.000 description 1
- WPPRAPIAKXDXIP-UHFFFAOYSA-N Cc1ncc(C(OC)=O)[nH]1 Chemical compound Cc1ncc(C(OC)=O)[nH]1 WPPRAPIAKXDXIP-UHFFFAOYSA-N 0.000 description 1
- AFFCPJJXCDJEMG-UHFFFAOYSA-N NOP(c1ccccc1)(c1ccccc1)=N Chemical compound NOP(c1ccccc1)(c1ccccc1)=N AFFCPJJXCDJEMG-UHFFFAOYSA-N 0.000 description 1
- HBVNBRKDFAEQLE-UHFFFAOYSA-N OBc(c(Cl)c1)ccc1F Chemical compound OBc(c(Cl)c1)ccc1F HBVNBRKDFAEQLE-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- 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
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Addiction (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361818650P | 2013-05-02 | 2013-05-02 | |
| US61/818,650 | 2013-05-02 | ||
| PCT/IB2014/060945 WO2014177977A1 (en) | 2013-05-02 | 2014-04-23 | Imidazo-triazine derivatives as pde10 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105164134A CN105164134A (zh) | 2015-12-16 |
| CN105164134B true CN105164134B (zh) | 2017-09-22 |
Family
ID=50841902
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480024798.1A Expired - Fee Related CN105164134B (zh) | 2013-05-02 | 2014-04-23 | 作为pde10抑制剂的咪唑并‑三嗪衍生物 |
Country Status (33)
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ712949A (en) * | 2013-05-02 | 2017-04-28 | Pfizer | Imidazo-triazine derivatives as pde10 inhibitors |
| WO2018047081A1 (en) | 2016-09-09 | 2018-03-15 | Novartis Ag | Compounds and compositions as inhibitors of endosomal toll-like receptors |
| US12448374B2 (en) | 2018-06-07 | 2025-10-21 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| EP3897670A4 (en) | 2018-12-19 | 2022-09-07 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS |
| MX2022004741A (es) * | 2019-10-21 | 2022-05-16 | Sk Biopharmaceuticals Co Ltd | Uso de compuestos de imidazopirimidina o imidazotriazina para prevencion, alivio, o tratamiento de trastornos cognitivos, o para mejorar la funcion cognitiva. |
| CN117486878A (zh) * | 2023-10-27 | 2024-02-02 | 扬州市普林斯医药科技有限公司 | 一种恩那司他的制备方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102596961A (zh) * | 2009-10-30 | 2012-07-18 | 詹森药业有限公司 | 咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途 |
| WO2012114222A1 (en) * | 2011-02-23 | 2012-08-30 | Pfizer Inc. | IMIDAZO[5,1-f][1,2,4]TRIAZINES FOR THE TREATMENT OF NEUROLOGICAL DISORDERS |
| CN102791713A (zh) * | 2010-03-09 | 2012-11-21 | 詹森药业有限公司 | 咪唑并[1,2-a]吡嗪衍生物及其预防或治疗神经病、精神病和代谢性障碍和疾病的用途 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20010007867A1 (en) | 1999-12-13 | 2001-07-12 | Yuhpyng L. Chen | Substituted 6,5-hetero-bicyclic derivatives |
| DE10130167A1 (de) | 2001-06-22 | 2003-01-02 | Bayer Ag | Imidazotriazine |
| US7220862B2 (en) | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| DE10230604A1 (de) | 2002-07-08 | 2004-01-29 | Bayer Ag | Heterocyclisch substituierte Imidazotriazine |
| JP2007508241A (ja) | 2003-07-31 | 2007-04-05 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | Ｐｄｅ１０ａ阻害剤を用いる糖尿病および関連障害の処置方法 |
| JP4559749B2 (ja) * | 2004-02-16 | 2010-10-13 | あすか製薬株式会社 | ピペラジニルピリジン誘導体 |
| EP1595881A1 (en) | 2004-05-12 | 2005-11-16 | Pfizer Limited | Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands |
| US20070167426A1 (en) | 2004-06-02 | 2007-07-19 | Schering Corporation | Compounds for the treatment of inflammatory disorders and microbial diseases |
| TW200716102A (en) | 2005-06-01 | 2007-05-01 | Wyeth Corp | Bicyclic 6-alkylidene-penems as class-D β -lactamases inhibitors |
| US20080051419A1 (en) | 2006-07-26 | 2008-02-28 | Pfizer Inc. | Amine derivatives useful as anticancer agents |
| WO2008041571A1 (en) | 2006-09-26 | 2008-04-10 | Kaneka Corporation | Process for producing optically active beta-hydroxy-alpha-aminocarboxylic acid ester |
| WO2008057402A2 (en) | 2006-11-02 | 2008-05-15 | Cytovia, Inc. | N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof |
| EP2203171A2 (en) | 2007-08-21 | 2010-07-07 | Merck Sharp & Dohme Corp. | Cb2 receptor ligands for the treatment of pain |
| DE102007059723A1 (de) | 2007-12-12 | 2009-06-18 | Siemens Medical Instruments Pte. Ltd. | Hörvorrichtung mit Batterieklappenmodul |
| TWI431010B (zh) | 2007-12-19 | 2014-03-21 | Lilly Co Eli | 礦皮質素受體拮抗劑及使用方法 |
| MX2010010151A (es) | 2008-03-20 | 2010-10-25 | Amgen Inc | Moduladores de cinasa aurora y metodo de uso. |
| EP2526102B1 (en) | 2010-01-22 | 2017-03-08 | Fundación Centro Nacional de Investigaciones Oncológicas Carlos III | Inhibitors of PI3 kinase |
| TW201200518A (en) | 2010-03-10 | 2012-01-01 | Kalypsys Inc | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
| US20130131057A1 (en) | 2010-05-13 | 2013-05-23 | Centro Nacional De Investigaciones Oncologicas (Cnio | New bicyclic compounds as pi3-k and mtor inhibitors |
| BR112012029994A2 (pt) | 2010-05-28 | 2019-09-24 | Biocryst Pharm Inc | composto heterocíclicos como inibidores de janus quinase |
| US20130085161A1 (en) | 2010-06-17 | 2013-04-04 | Novartis Ag | Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives |
| NZ712949A (en) * | 2013-05-02 | 2017-04-28 | Pfizer | Imidazo-triazine derivatives as pde10 inhibitors |
-
2014
- 2014-04-23 NZ NZ712949A patent/NZ712949A/en not_active IP Right Cessation
- 2014-04-23 EP EP14727054.0A patent/EP2991989B1/en active Active
- 2014-04-23 ES ES14727054.0T patent/ES2637816T3/es active Active
- 2014-04-23 SG SG11201508201VA patent/SG11201508201VA/en unknown
- 2014-04-23 MD MDA20150103A patent/MD20150103A2/ro not_active Application Discontinuation
- 2014-04-23 AU AU2014261070A patent/AU2014261070A1/en not_active Abandoned
- 2014-04-23 PE PE2015002303A patent/PE20151940A1/es not_active Application Discontinuation
- 2014-04-23 BR BR112015027760A patent/BR112015027760A8/pt not_active Application Discontinuation
- 2014-04-23 JP JP2016511150A patent/JP6263606B2/ja not_active Expired - Fee Related
- 2014-04-23 TN TN2015000490A patent/TN2015000490A1/fr unknown
- 2014-04-23 GE GEAP201413979A patent/GEP201706675B/en unknown
- 2014-04-23 CN CN201480024798.1A patent/CN105164134B/zh not_active Expired - Fee Related
- 2014-04-23 MX MX2015015163A patent/MX2015015163A/es unknown
- 2014-04-23 CA CA2910759A patent/CA2910759C/en not_active Expired - Fee Related
- 2014-04-23 EA EA201591819A patent/EA027936B1/ru not_active IP Right Cessation
- 2014-04-23 MA MA38559A patent/MA38559B1/fr unknown
- 2014-04-23 UA UAA201510060A patent/UA111696C2/uk unknown
- 2014-04-23 WO PCT/IB2014/060945 patent/WO2014177977A1/en not_active Ceased
- 2014-04-23 DK DK14727054.0T patent/DK2991989T3/en active
- 2014-04-23 AP AP2015008843A patent/AP2015008843A0/xx unknown
- 2014-04-23 KR KR1020157034216A patent/KR101770905B1/ko not_active Expired - Fee Related
- 2014-04-29 TW TW103115365A patent/TWI508966B/zh not_active IP Right Cessation
- 2014-04-30 US US14/265,458 patent/US8933224B2/en not_active Expired - Fee Related
- 2014-04-30 UY UY0001035547A patent/UY35547A/es not_active Application Discontinuation
- 2014-04-30 AR ARP140101792A patent/AR096161A1/es unknown
- 2014-11-21 US US14/549,871 patent/US9145427B2/en not_active Expired - Fee Related
-
2015
- 2015-08-19 US US14/829,842 patent/US9296761B2/en not_active Expired - Fee Related
- 2015-10-13 CL CL2015003037A patent/CL2015003037A1/es unknown
- 2015-10-19 CU CUP2015000144A patent/CU20150144A7/es unknown
- 2015-10-23 PH PH12015502462A patent/PH12015502462A1/en unknown
- 2015-10-27 CR CR20150591A patent/CR20150591A/es unknown
- 2015-10-30 NI NI201500157A patent/NI201500157A/es unknown
- 2015-11-02 DO DO2015000271A patent/DOP2015000271A/es unknown
- 2015-11-30 EC ECIEPI201550110A patent/ECSP15050110A/es unknown
- 2015-12-01 ZA ZA2015/08968A patent/ZA201508968B/en unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102596961A (zh) * | 2009-10-30 | 2012-07-18 | 詹森药业有限公司 | 咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途 |
| CN102791713A (zh) * | 2010-03-09 | 2012-11-21 | 詹森药业有限公司 | 咪唑并[1,2-a]吡嗪衍生物及其预防或治疗神经病、精神病和代谢性障碍和疾病的用途 |
| WO2012114222A1 (en) * | 2011-02-23 | 2012-08-30 | Pfizer Inc. | IMIDAZO[5,1-f][1,2,4]TRIAZINES FOR THE TREATMENT OF NEUROLOGICAL DISORDERS |
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