JP2011526596A5 - - Google Patents
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- Publication number
- JP2011526596A5 JP2011526596A5 JP2011515445A JP2011515445A JP2011526596A5 JP 2011526596 A5 JP2011526596 A5 JP 2011526596A5 JP 2011515445 A JP2011515445 A JP 2011515445A JP 2011515445 A JP2011515445 A JP 2011515445A JP 2011526596 A5 JP2011526596 A5 JP 2011526596A5
- Authority
- JP
- Japan
- Prior art keywords
- modulator
- alkyl
- hydrogen
- dopa
- parkinson
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 claims 9
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 claims 9
- 208000018737 Parkinson disease Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 7
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 229940099362 Catechol O methyltransferase inhibitor Drugs 0.000 claims 6
- 229940081615 DOPA decarboxylase inhibitor Drugs 0.000 claims 6
- 239000003543 catechol methyltransferase inhibitor Substances 0.000 claims 6
- 239000000534 dopa decarboxylase inhibitor Substances 0.000 claims 6
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 5
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 claims 4
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 229940052760 dopamine agonists Drugs 0.000 claims 3
- 239000012458 free base Substances 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 claims 1
- BKRGVLQUQGGVSM-KBXCAEBGSA-N Revanil Chemical compound C1=CC(C=2[C@H](N(C)C[C@H](C=2)NC(=O)N(CC)CC)C2)=C3C2=CNC3=C1 BKRGVLQUQGGVSM-KBXCAEBGSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 229960004046 apomorphine Drugs 0.000 claims 1
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 claims 1
- BNQDCRGUHNALGH-UHFFFAOYSA-N benserazide Chemical compound OCC(N)C(=O)NNCC1=CC=C(O)C(O)=C1O BNQDCRGUHNALGH-UHFFFAOYSA-N 0.000 claims 1
- 229960000911 benserazide Drugs 0.000 claims 1
- 229960002802 bromocriptine Drugs 0.000 claims 1
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical group C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims 1
- 229960004596 cabergoline Drugs 0.000 claims 1
- 229960004205 carbidopa Drugs 0.000 claims 1
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical group NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 229960003337 entacapone Drugs 0.000 claims 1
- JRURYQJSLYLRLN-BJMVGYQFSA-N entacapone Chemical compound CCN(CC)C(=O)C(\C#N)=C\C1=CC(O)=C(O)C([N+]([O-])=O)=C1 JRURYQJSLYLRLN-BJMVGYQFSA-N 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 229960004502 levodopa Drugs 0.000 claims 1
- 229960003587 lisuride Drugs 0.000 claims 1
- 229940124807 mGLUR antagonist Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 229960004851 pergolide Drugs 0.000 claims 1
- YEHCICAEULNIGD-MZMPZRCHSA-N pergolide Chemical compound C1=CC([C@H]2C[C@@H](CSC)CN([C@@H]2C2)CCC)=C3C2=CNC3=C1 YEHCICAEULNIGD-MZMPZRCHSA-N 0.000 claims 1
- 229960003089 pramipexole Drugs 0.000 claims 1
- FASDKYOPVNHBLU-ZETCQYMHSA-N pramipexole Chemical compound C1[C@@H](NCCC)CCC2=C1SC(N)=N2 FASDKYOPVNHBLU-ZETCQYMHSA-N 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 229960001879 ropinirole Drugs 0.000 claims 1
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 229960004603 tolcapone Drugs 0.000 claims 1
- MIQPIUSUKVNLNT-UHFFFAOYSA-N tolcapone Chemical group C1=CC(C)=CC=C1C(=O)C1=CC(O)=C(O)C([N+]([O-])=O)=C1 MIQPIUSUKVNLNT-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7677208P | 2008-06-30 | 2008-06-30 | |
| US61/076,772 | 2008-06-30 | ||
| PCT/EP2009/058230 WO2010000763A2 (en) | 2008-06-30 | 2009-06-30 | Combination products |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011526596A JP2011526596A (ja) | 2011-10-13 |
| JP2011526596A5 true JP2011526596A5 (https=) | 2012-08-16 |
Family
ID=41112516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011515445A Pending JP2011526596A (ja) | 2008-06-30 | 2009-06-30 | 組み合わせ製品 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US8703809B2 (https=) |
| EP (2) | EP2320892A2 (https=) |
| JP (1) | JP2011526596A (https=) |
| KR (1) | KR20110027817A (https=) |
| CN (2) | CN102131503A (https=) |
| AU (1) | AU2009265760B2 (https=) |
| BR (1) | BRPI0913642A2 (https=) |
| CA (1) | CA2729595C (https=) |
| MX (1) | MX2010014222A (https=) |
| RU (1) | RU2496494C2 (https=) |
| WO (1) | WO2010000763A2 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101572280B1 (ko) * | 2007-10-12 | 2015-11-26 | 노파르티스 아게 | 파킨슨병의 치료를 위한 대사성 글루타메이트 수용체 조절제 |
| RU2513856C2 (ru) * | 2008-08-12 | 2014-04-20 | Новартис Аг | Способы получения метилового эфира 4-оксооктагидроиндол-1-карбоновой кислоты и ее производные |
| WO2012084873A1 (en) * | 2010-12-20 | 2012-06-28 | Novartis Ag | 4- (hetero) aryl - ethynyl - octahydro - indole - 1 - carboxylic acid esters |
| GB201204962D0 (en) | 2012-03-21 | 2012-05-02 | Addex Pharmaceuticals Sa | Pharmaceutical combination products for parkinsons disease |
| PT2908805T (pt) | 2012-10-22 | 2021-09-10 | Civitas Therapeutics Inc | Formulações de levodopa para alívio rápido da doença de parkinson |
| JP5744112B2 (ja) * | 2013-06-11 | 2015-07-01 | デクセリアルズ株式会社 | パターン形成体の製造方法 |
| GB201312800D0 (en) | 2013-07-17 | 2013-08-28 | Heptares Therapeutics Ltd | mGlu5 modulators |
| WO2015163840A1 (en) * | 2014-04-21 | 2015-10-29 | Civitas Therapeutics, Inc. | Rapid relief of motor fluctuations in parkinson's disease |
| CA3066711A1 (en) * | 2017-07-31 | 2019-02-07 | Novartis Ag | Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use |
| CA3067688A1 (en) * | 2017-07-31 | 2019-02-07 | Novartis Ag | Use of mavoglurant in the reduction of alcohol use or in preventing relapse into alcohol use |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3769424A (en) * | 1970-10-01 | 1973-10-30 | Merck & Co Inc | Composition and method of treating dopamine deficiency in brain tissue |
| US5521297A (en) | 1993-06-04 | 1996-05-28 | Salk Institute Biotechnology/Industrial Associates | Nucleic acids encoding human metabotropic glutamate receptors |
| FR2777781B1 (fr) * | 1998-04-24 | 2004-04-09 | Rhone Poulenc Rorer Sa | Associations riluzole et l-dopa pour le traitement de la maladie de parkinson |
| GB0007193D0 (en) * | 2000-03-25 | 2000-05-17 | Univ Manchester | Treatment of movrmrnt disorders |
| GB0128996D0 (en) * | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
| SE0201943D0 (sv) | 2002-06-20 | 2002-06-20 | Astrazeneca Ab | New use |
| IL166510A0 (en) | 2002-08-09 | 2006-01-15 | Nps Pharma Inc | 1,2,4"oxadiazole as modulators of metabotropic glutamate receptor-5 |
| EP1539749A4 (en) * | 2002-09-13 | 2007-06-13 | Merck & Co Inc | BY CONDENSED HETEROBICYCLOGRUPPEN SUBSTITUTED PHENYL COMPOUNDS AS METOBOTROPE GLUTAMATE-5 MODULATORS |
| JP2006522137A (ja) * | 2003-04-04 | 2006-09-28 | メルク エンド カムパニー インコーポレーテッド | 代謝型グルタミン酸受容体−５のジ−アリール置換ピロールモジュレーター |
| MY142655A (en) | 2003-06-12 | 2010-12-15 | Euro Celtique Sa | Therapeutic agents useful for treating pain |
| WO2005030128A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Pyrazole modulators of metabotropic glutamate receptors |
| EP1677790A1 (en) | 2003-10-31 | 2006-07-12 | AstraZeneca AB | Alkynes ii |
| CA2549967A1 (en) | 2003-10-31 | 2005-05-19 | Astrazeneca Ab | Alkynes i |
| CA2549965A1 (en) | 2003-10-31 | 2005-05-19 | Astrazeneca Ab | Alkynes iii |
| EP1715867A4 (en) | 2004-02-12 | 2009-04-15 | Merck & Co Inc | BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5 |
| CA2562725C (en) | 2004-04-14 | 2015-02-03 | Digital River, Inc. | Geographic location based licensing system |
| GB0508319D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
| TW200801005A (en) | 2005-08-15 | 2008-01-01 | Astrazeneca Ab | Acetylenic piperazines as metabotropic glutamate receptor antagonists |
| AU2006329007A1 (en) | 2005-12-20 | 2007-06-28 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutamate receptors |
| EA015555B1 (ru) | 2006-05-30 | 2011-08-30 | Янссен Фармацевтика Н.В. | Замещенные пиридиламидные соединения в качестве модуляторов гистаминового h-рецептора |
| KR20090033871A (ko) * | 2006-06-16 | 2009-04-06 | 솔베이 파마슈티칼스 비. 브이 | 비페프루녹스 및 ｌ-ｄｏｐａ를 포함하는 병용 제제 |
| KR20090047450A (ko) * | 2006-08-04 | 2009-05-12 | 메르츠 파마 게엠베하 운트 코. 카가아 | 치환된 피라졸로피리미딘, 이의 제조 방법 및 의약품으로서의 이의 용도 |
| EP2272509A1 (en) | 2006-09-11 | 2011-01-12 | Novartis AG | New Uses of metabotropic glutamate receptors |
| KR101572280B1 (ko) * | 2007-10-12 | 2015-11-26 | 노파르티스 아게 | 파킨슨병의 치료를 위한 대사성 글루타메이트 수용체 조절제 |
-
2009
- 2009-06-30 EP EP09772463A patent/EP2320892A2/en not_active Withdrawn
- 2009-06-30 WO PCT/EP2009/058230 patent/WO2010000763A2/en not_active Ceased
- 2009-06-30 CN CN2009801331117A patent/CN102131503A/zh active Pending
- 2009-06-30 CN CN2013101485895A patent/CN103212078A/zh active Pending
- 2009-06-30 MX MX2010014222A patent/MX2010014222A/es not_active Application Discontinuation
- 2009-06-30 US US12/999,634 patent/US8703809B2/en not_active Expired - Fee Related
- 2009-06-30 AU AU2009265760A patent/AU2009265760B2/en not_active Ceased
- 2009-06-30 RU RU2011103083/15A patent/RU2496494C2/ru not_active IP Right Cessation
- 2009-06-30 JP JP2011515445A patent/JP2011526596A/ja active Pending
- 2009-06-30 BR BRPI0913642A patent/BRPI0913642A2/pt not_active IP Right Cessation
- 2009-06-30 CA CA2729595A patent/CA2729595C/en not_active Expired - Fee Related
- 2009-06-30 KR KR1020117002251A patent/KR20110027817A/ko not_active Ceased
- 2009-06-30 EP EP14167553.8A patent/EP2826478A1/en not_active Withdrawn
-
2014
- 2014-03-04 US US14/195,947 patent/US20140194423A1/en not_active Abandoned
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