ZA200600693B - Combination of mGluR2 antagonist and AChE inhibitor for treatment of acute and/or chronic neurological disorders - Google Patents
Combination of mGluR2 antagonist and AChE inhibitor for treatment of acute and/or chronic neurological disorders Download PDFInfo
- Publication number
- ZA200600693B ZA200600693B ZA200600693A ZA200600693A ZA200600693B ZA 200600693 B ZA200600693 B ZA 200600693B ZA 200600693 A ZA200600693 A ZA 200600693A ZA 200600693 A ZA200600693 A ZA 200600693A ZA 200600693 B ZA200600693 B ZA 200600693B
- Authority
- ZA
- South Africa
- Prior art keywords
- benzo
- dihydro
- diazepin
- phenyl
- pyridin
- Prior art date
Links
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- 230000001154 acute effect Effects 0.000 title claims description 34
- 230000001684 chronic effect Effects 0.000 title claims description 33
- 208000012902 Nervous system disease Diseases 0.000 title claims description 32
- 239000005557 antagonist Substances 0.000 title claims description 24
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 title claims description 17
- 108010038421 metabotropic glutamate receptor 2 Proteins 0.000 title claims description 16
- 208000025966 Neurological disease Diseases 0.000 title description 7
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- 150000001875 compounds Chemical class 0.000 claims description 94
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 41
- 125000001424 substituent group Chemical group 0.000 claims description 33
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- PBHFNBQPZCRWQP-QUCCMNQESA-N [(3ar,8bs)-3,4,8b-trimethyl-2,3a-dihydro-1h-pyrrolo[2,3-b]indol-7-yl] n-phenylcarbamate Chemical compound CN([C@@H]1[C@@](C2=C3)(C)CCN1C)C2=CC=C3OC(=O)NC1=CC=CC=C1 PBHFNBQPZCRWQP-QUCCMNQESA-N 0.000 claims description 3
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- 229930195734 saturated hydrocarbon Natural products 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 208000020431 spinal cord injury Diseases 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 230000009529 traumatic brain injury Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Classifications
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- 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
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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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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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
- A61K31/66—Phosphorus compounds
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP03016968 | 2003-07-25 |
Publications (1)
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ZA200600693B true ZA200600693B (en) | 2007-05-30 |
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ZA200600693A ZA200600693B (en) | 2003-07-25 | 2006-01-24 | Combination of mGluR2 antagonist and AChE inhibitor for treatment of acute and/or chronic neurological disorders |
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US (1) | US7235547B2 (zh) |
EP (1) | EP1651234B1 (zh) |
JP (1) | JP5005343B2 (zh) |
KR (1) | KR100764330B1 (zh) |
CN (1) | CN1856312A (zh) |
AR (1) | AR045926A1 (zh) |
AT (1) | ATE374030T1 (zh) |
AU (1) | AU2004262897B9 (zh) |
BR (1) | BRPI0412919A (zh) |
CA (1) | CA2532347C (zh) |
CO (1) | CO5640124A2 (zh) |
DE (1) | DE602004009195T2 (zh) |
DK (1) | DK1651234T3 (zh) |
ES (1) | ES2293287T3 (zh) |
HR (1) | HRP20070552T3 (zh) |
IL (1) | IL173131A (zh) |
MX (1) | MXPA06000705A (zh) |
MY (1) | MY138394A (zh) |
NO (1) | NO20060328L (zh) |
NZ (1) | NZ544719A (zh) |
PL (1) | PL1651234T3 (zh) |
PT (1) | PT1651234E (zh) |
RU (1) | RU2357734C2 (zh) |
SI (1) | SI1651234T1 (zh) |
TW (1) | TW200524614A (zh) |
WO (1) | WO2005014002A1 (zh) |
ZA (1) | ZA200600693B (zh) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7612078B2 (en) * | 2003-03-31 | 2009-11-03 | Epix Delaware, Inc. | Piperidinylamino-thieno[2,3-D] pyrimidine compounds |
US20050222175A1 (en) * | 2004-03-31 | 2005-10-06 | Dhanoa Dale S | New piperidinylamino-thieno[2,3-D] pyrimidine compounds |
US7488736B2 (en) * | 2004-05-17 | 2009-02-10 | Epix Delaware, Inc. | Thienopyridinone compounds and methods of treatment |
US7407966B2 (en) * | 2004-10-07 | 2008-08-05 | Epix Delaware, Inc. | Thienopyridinone compounds and methods of treatment |
US7598265B2 (en) * | 2004-09-30 | 2009-10-06 | Epix Delaware, Inc. | Compositions and methods for treating CNS disorders |
US7576211B2 (en) * | 2004-09-30 | 2009-08-18 | Epix Delaware, Inc. | Synthesis of thienopyridinone compounds and related intermediates |
EP2275096A3 (en) | 2005-08-26 | 2011-07-13 | Braincells, Inc. | Neurogenesis via modulation of the muscarinic receptors |
EP2258357A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
WO2007047978A2 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
CA2625210A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
AU2007249435A1 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | 5 HT receptor mediated neurogenesis |
JP2009536669A (ja) | 2006-05-09 | 2009-10-15 | ブレインセルス,インコーポレイティド | アンジオテンシン調節による神経新生 |
KR20090064418A (ko) | 2006-09-08 | 2009-06-18 | 브레인셀즈 인코퍼레이션 | 4-아실아미노피리딘 유도체 포함 조합물 |
US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
DE102008022221A1 (de) * | 2008-05-06 | 2009-11-12 | Universität des Saarlandes | Inhibitoren der humanen Aldosteronsynthase CYP11B2 |
WO2010065743A2 (en) * | 2008-12-03 | 2010-06-10 | Nanotherapeutics, Inc. | Bicyclic compounds and methods of making and using same |
WO2010099217A1 (en) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
US8541404B2 (en) * | 2009-11-09 | 2013-09-24 | Elexopharm Gmbh | Inhibitors of the human aldosterone synthase CYP11B2 |
RU2472475C2 (ru) * | 2010-04-20 | 2013-01-20 | Учреждение образования "Белорусский государственный медицинский университет" (УО БГМУ) | Способ комбинированного лечения глаукомной оптической нейропатии |
SG11201503192XA (en) | 2012-10-23 | 2015-06-29 | Hoffmann La Roche | Mglu2/3 antagonists for the treatment of autistic disorders |
BR112016021727A2 (pt) | 2014-04-23 | 2017-08-15 | Hoffmann La Roche | Antagonistas de mglu2/3 para o tratamento de incapacidades intelectuais |
CN112462047B (zh) * | 2020-11-13 | 2023-02-07 | 北京元恩生物技术有限公司 | 一种尼卡巴嗪检测试剂盒及其用途 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
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US4663318A (en) * | 1986-01-15 | 1987-05-05 | Bonnie Davis | Method of treating Alzheimer's disease |
FI95572C (fi) * | 1987-06-22 | 1996-02-26 | Eisai Co Ltd | Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi |
AU4498799A (en) * | 1998-06-22 | 2000-01-10 | Neurosearch A/S | Method of preparing 5- or 8-bromoisoquinoline derivatives |
US6194403B1 (en) * | 1999-09-09 | 2001-02-27 | Unitech Pharmaceuticals, Inc. | Tacrine derivatives for treating Alzheimer's disease |
SI1224174T1 (en) * | 1999-10-15 | 2003-12-31 | F. Hoffmann-La Roche Ag | Benzodiazepine derivatives as metabotropic glutamate receptor antagonists |
CN1199954C (zh) * | 1999-10-15 | 2005-05-04 | 弗·哈夫曼-拉罗切有限公司 | 苯并二氮杂䓬衍生物 |
CA2310926C (en) * | 2000-04-03 | 2002-10-15 | Janssen Pharmaceutica N.V. | A use of galantamine for the treatment of neuropsychiatric behaviour associated with alzheimer's disease |
EP1203584A1 (en) | 2000-10-13 | 2002-05-08 | M.D.M. S.r.l. | Cholinergic precursor (in particular choline alfoscerate) associated with an acetylcholinesterase inhibitor (such as rivastigmine, donepezil) |
US6500972B2 (en) * | 2001-01-03 | 2002-12-31 | Chinese Petroleim Corp. | Synthesis of TMBQ with transition metal-containing molecular sieve as catalysts |
US6500955B1 (en) * | 2001-02-02 | 2002-12-31 | National Institute Of Pharmaceutical Education And Research | One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate |
CN100390235C (zh) * | 2001-04-09 | 2008-05-28 | 富士胶片株式会社 | 偶氮化合物及其生产方法、中间体化合物和利用该化合物生产偶氮化合物的方法 |
CZ20033002A3 (cs) * | 2001-04-12 | 2004-03-17 | F. Hoffmann-La Roche Ag | Deriváty dihydrobenzo [b] [1,4]diazepin-2-onu jako antagonisty mGluR2 |
DE60205100T2 (de) * | 2001-04-12 | 2006-06-01 | F. Hoffmann-La Roche Ag | DIHYDRO-BENZO (b) (1,4) DIAZEPIN-2-ON-DERIVATE ALS MGLUR2 ANTAGONISTEN |
US6949542B2 (en) * | 2002-02-06 | 2005-09-27 | Hoffman-La Roche Inc. | Dihydro-benzo[b][1,4]diazepin-2-one derivatives |
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2004
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- 2004-07-17 JP JP2006521458A patent/JP5005343B2/ja not_active Expired - Fee Related
- 2004-07-17 AU AU2004262897A patent/AU2004262897B9/en not_active Ceased
- 2004-07-17 CA CA2532347A patent/CA2532347C/en not_active Expired - Fee Related
- 2004-07-17 WO PCT/EP2004/008020 patent/WO2005014002A1/en active IP Right Grant
- 2004-07-17 SI SI200430524T patent/SI1651234T1/sl unknown
- 2004-07-17 ES ES04741126T patent/ES2293287T3/es active Active
- 2004-07-17 CN CNA2004800278083A patent/CN1856312A/zh active Pending
- 2004-07-17 BR BRPI0412919-9A patent/BRPI0412919A/pt not_active Application Discontinuation
- 2004-07-17 PT PT04741126T patent/PT1651234E/pt unknown
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- 2004-07-17 AT AT04741126T patent/ATE374030T1/de active
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- 2004-07-17 NZ NZ544719A patent/NZ544719A/xx unknown
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2007
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