JP5616345B2 - 小胞モノアミン輸送体２のベンゾキノリン阻害剤 - Google Patents

小胞モノアミン輸送体２のベンゾキノリン阻害剤 Download PDF

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JP5616345B2
JP5616345B2 JP2011527995A JP2011527995A JP5616345B2 JP 5616345 B2 JP5616345 B2 JP 5616345B2 JP 2011527995 A JP2011527995 A JP 2011527995A JP 2011527995 A JP2011527995 A JP 2011527995A JP 5616345 B2 JP5616345 B2 JP 5616345B2
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compound
acid
pharmaceutical composition
deuterium
salt
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JP2012503010A (ja
JP2012503010A5 (Direct
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トーマス・ジー・ガント
マノーチャー・シャーバズ
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Auspex Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C07D455/06—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine 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
    • A61K31/435—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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2011527995A 2008-09-18 2009-09-18 小胞モノアミン輸送体２のベンゾキノリン阻害剤 Active JP5616345B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US9789608P 2008-09-18 2008-09-18
US61/097,896 2008-09-18
PCT/US2009/057480 WO2010044981A2 (en) 2008-09-18 2009-09-18 Benzoquinoline inhibitors of vesicular monoamine transporter 2

Related Child Applications (1)

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JP2014185634A Division JP5970037B2 (ja) 2008-09-18 2014-09-11 小胞モノアミン輸送体２のベンゾキノリン阻害剤

Publications (3)

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JP2012503010A JP2012503010A (ja) 2012-02-02
JP2012503010A5 JP2012503010A5 (Direct) 2012-11-01
JP5616345B2 true JP5616345B2 (ja) 2014-10-29

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JP2011527995A Active JP5616345B2 (ja) 2008-09-18 2009-09-18 小胞モノアミン輸送体２のベンゾキノリン阻害剤
JP2014185634A Active JP5970037B2 (ja) 2008-09-18 2014-09-11 小胞モノアミン輸送体２のベンゾキノリン阻害剤
JP2016136178A Active JP6138322B2 (ja) 2008-09-18 2016-07-08 小胞モノアミン輸送体２のベンゾキノリン阻害剤

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JP2016136178A Active JP6138322B2 (ja) 2008-09-18 2016-07-08 小胞モノアミン輸送体２のベンゾキノリン阻害剤

Country Status (20)

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US (16) US8524733B2 (Direct)
EP (4) EP2610254B1 (Direct)
JP (3) JP5616345B2 (Direct)
CN (2) CN102186848B (Direct)
AU (1) AU2009303758B8 (Direct)
BR (1) BRPI0913457B8 (Direct)
CA (2) CA2736409C (Direct)
CY (1) CY1120060T1 (Direct)
DK (2) DK3061760T3 (Direct)
ES (4) ES2896678T3 (Direct)
HR (1) HRP20180239T1 (Direct)
HU (1) HUE038158T2 (Direct)
LT (1) LT3061760T (Direct)
NO (1) NO3061760T3 (Direct)
NZ (1) NZ591615A (Direct)
PL (1) PL3061760T3 (Direct)
PT (1) PT3061760T (Direct)
SI (1) SI3061760T1 (Direct)
SM (1) SMT201800067T1 (Direct)
WO (1) WO2010044981A2 (Direct)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015007124A (ja) * 2008-09-18 2015-01-15 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 小胞モノアミン輸送体２のベンゾキノリン阻害剤

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011058474A1 (en) * 2009-11-10 2011-05-19 Pfizer Inc. N1-pyrazolospiroketone acetyl-coa carboxylase inhibitors
WO2011153157A2 (en) * 2010-06-01 2011-12-08 Auspex Pharmaceutical, Inc. Benzoquinolone inhibitors of vmat2
US9572880B2 (en) 2010-08-27 2017-02-21 Sienna Biopharmaceuticals, Inc. Ultrasound delivery of nanoparticles
WO2012027728A2 (en) 2010-08-27 2012-03-01 Sienna Labs, Inc. Compositions and methods for targeted thermomodulation
WO2012081031A1 (en) * 2010-12-15 2012-06-21 Enaltec Labs Pvt. Ltd. Process for preparing tetrabenazine
CA2883641C (en) * 2012-09-18 2021-09-14 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
RU2646809C2 (ru) 2012-10-11 2018-03-07 Нанокомпозикс, Инк. Композиции серебряных нанопластин и способы
HK1219095A1 (zh) * 2013-01-31 2017-03-24 Auspex Pharmaceuticals, Inc. Vmat2的benzoquinolone抑制剂
US20160207917A1 (en) * 2013-09-27 2016-07-21 Auspex Pharmaceuticals, Inc. Benzoquinolone inhibitors of vmat2
WO2015077521A1 (en) * 2013-11-22 2015-05-28 Auspex Pharmaceuticals, Inc. Benzoquinoline inhibitors of vesicular monoamine transporter 2
HK1224294A1 (zh) * 2013-11-22 2017-08-18 Auspex Pharmaceuticals, Inc. 治疗异常肌肉活动的方法
BR112016012747B1 (pt) 2013-12-03 2022-07-12 Auspex Pharmaceuticals, Inc Processo de preparação de uma mistura racêmica de (rr,ss)-d6-tetrabenazina
MX2016009817A (es) * 2014-01-27 2017-02-28 Auspex Pharmaceuticals Inc Inhibidores de benzoquinolina del transportador vesicular de monoaminas 2.
US10166183B2 (en) * 2014-02-07 2019-01-01 Auspex Pharmaceuticals, Inc. Pharmaceutical formulations
CN106061506A (zh) 2014-02-07 2016-10-26 纽罗克里生物科学有限公司 包含抗精神病药物和vmat2抑制剂的药物组合物及其用途
FI3936130T3 (fi) 2014-05-06 2024-04-23 Neurocrine Biosciences Inc Valbenatsiinin annostusohjelma hyperkineettisten liikehäiriöiden hoitoon
MA41557A (fr) * 2015-02-18 2017-12-26 Auspex Pharmaceuticals Inc Inhibiteurs diméthoxyphényles du transporteur vésiculaire des monoamines 2
CN114767672A (zh) * 2015-03-06 2022-07-22 奥斯拜客斯制药有限公司 氘代丁苯那嗪或包含氘代丁苯那嗪的组合物
WO2016154017A1 (en) * 2015-03-20 2016-09-29 Sienna Biopharmaceuticals, Inc. Enhanced efficacy and targeted topical delivery of drugs to skin with nanoparticles
MY193767A (en) 2015-10-30 2022-10-27 Neurocrine Biosciences Inc Valbenazine salts and polymorphs thereof
US10160757B2 (en) 2015-12-23 2018-12-25 Neuroscrine Biosciences, Inc. Synthetic methods for preparation of (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate)
US10479787B2 (en) 2016-04-22 2019-11-19 Lupin Limited Process for preparation of tetrabenazine and deutetrabenazine
WO2017221169A1 (en) 2016-06-24 2017-12-28 Lupin Limited Premixes of deutetrabenazine
CN107936008B (zh) * 2016-10-13 2022-06-14 泰州华元医药科技有限公司 氘代化合物及其医药用途
EP4400171A3 (en) 2016-12-02 2024-09-11 Neurocrine Biosciences, Inc. Use of valbenazine for treating schizophrenia or schizoaffective disorder
US10703750B2 (en) 2017-01-10 2020-07-07 Sandoz Ag Crystalline valbenazine free base
MX394415B (es) 2017-01-27 2025-03-24 Neurocrine Biosciences Inc Metodos para la administracion de ciertos inhibidores de proteina transportadora transportador de monoamina vesicular-2 (vmat2).
CA3054238A1 (en) 2017-02-27 2018-08-30 Sandoz Ag Crystalline forms of valbenazine salts
WO2018164996A1 (en) 2017-03-06 2018-09-13 Neurocrine Biosciences, Inc. Dosing regimen for valbenazine
WO2018170214A1 (en) * 2017-03-15 2018-09-20 Zhang Chengzi Analogs of deutetrabenazine, their preparation and use
JOP20190239A1 (ar) 2017-04-19 2019-10-09 Neurocrine Biosciences Inc مركبات مثبطة لـ vmat2 وتركيبات منها
WO2018200605A1 (en) 2017-04-26 2018-11-01 Neurocrine Biosciences, Inc. Use of valbenazine for treating levodopa-induced dyskinesia
IL309802A (en) 2017-09-21 2024-02-01 Neurocrine Biosciences Inc High dose valbenazine formulation and related preparations, methods and kits
US10786495B2 (en) * 2017-10-10 2020-09-29 The Regents Of The University Of California Vesicular monoamine transporter 2 inhibitors for treating stuttering
US20200230127A1 (en) 2017-10-10 2020-07-23 Neurocrine Biosciences, Inc. Methods for the Administration of Certain VMAT2 Inhibitors
KR20250070134A (ko) 2017-10-10 2025-05-20 뉴로크린 바이오사이언시즈 인코퍼레이티드 특정 vmat2 억제제의 투여 방법
WO2019130252A2 (en) * 2017-12-29 2019-07-04 Mylan Laboratories Ltd Methods and intermediates for preparing deutetrabenazine
CN111655243A (zh) 2018-01-29 2020-09-11 乔纳森·萨克纳-伯恩斯坦 在人类神经系统疾病中调节多巴胺的方法
US11505549B2 (en) * 2018-02-01 2022-11-22 Lakshmi Prasad ALAPARTHI Process for preparation of Deutetrabenazine
WO2019166962A1 (en) 2018-03-01 2019-09-06 Mylan Laboratories Ltd Deutetrabenazine polymorphs and methods for their preparation
IL278185B2 (en) 2018-04-25 2024-11-01 Shinkei Therapeutics Inc Tetrabenazine transdermal delivery device
CA3043075A1 (en) 2018-05-14 2019-11-14 Apotex Inc Novel crystalline forms of benzoquinoline inhibitors of vesicular monoamine transporter 2
KR20210021006A (ko) 2018-06-14 2021-02-24 뉴로크린 바이오사이언시즈 인코퍼레이티드 Vmat2 억제제 화합물, 조성물 및 그와 관련된 방법
CN108794337A (zh) * 2018-07-10 2018-11-13 上海华堇生物技术有限责任公司 一种3,4-二羟基-β-硝基苯乙烯的新制备方法
KR20210044817A (ko) 2018-08-15 2021-04-23 뉴로크린 바이오사이언시즈 인코퍼레이티드 특정 vmat2 억제제의 투여 방법
US12152087B2 (en) 2018-10-18 2024-11-26 Oncopeptides Innovation Ab Deuterated melflufen compounds
CA3123393A1 (en) * 2018-12-13 2020-06-18 Auspex Pharmaceuticals, Inc. Deutetrabenazine for the treatment of dyskinesia in cerebral palsy
US10940141B1 (en) 2019-08-23 2021-03-09 Neurocrine Biosciences, Inc. Methods for the administration of certain VMAT2 inhibitors
WO2021252741A1 (en) 2020-06-10 2021-12-16 Auspex Pharmaceuticals, Inc. Osmotic dosage forms comprising deutetrabenazine and methods of use thereof
JP2023542676A (ja) 2020-09-17 2023-10-11 オースペックス ファーマシューティカルズ インコーポレイテッド デューテトラベナジンを含む多粒子投薬形態
CN116456970A (zh) 2020-10-12 2023-07-18 奥斯佩克斯医药公司 包括氘代丁苯那嗪的胃滞留剂型
AR125188A1 (es) 2021-03-22 2023-06-21 Neurocrine Biosciences Inc Inhibidores del vmat2 y métodos de uso
IL309172A (en) 2021-06-30 2024-02-01 Neurocrine Biosciences Inc Vulbanazine for use in the additional treatment of schizophrenia
US20240374528A1 (en) 2021-09-17 2024-11-14 Auspex Pharmaceuticals, Inc. Multiparticulate dosage forms comprising deutetrabenazine
CA3242612A1 (en) 2022-01-05 2023-07-13 Terrence Joseph Connolly Deuterium-enriched piperidinyl-methyl-purine amines and related compounds and their use in treating diseases and conditions
EP4489754A1 (en) 2022-03-07 2025-01-15 Neurocrine Biosciences, Inc. Valbenazine, a vmat2 inhibitor, as a free base a tosylate or ditosylate salt, for use in the treatment of chorea associated with huntington's disease
KR20250019144A (ko) 2022-06-08 2025-02-07 오스펙스 파마슈티칼스, 인코포레이티드 듀테트라베나진을 포함하는 삼투성 제형 및 이의 사용 방법
WO2025038959A1 (en) 2023-08-17 2025-02-20 Neurocrine Biosciences, Inc. Methods for the administration of certain vmat2 inhibitors
TW202521119A (zh) 2023-08-17 2025-06-01 美商紐羅克里生物科學有限公司 用於投與特定vmat2抑制劑之方法
WO2025096823A1 (en) 2023-11-01 2025-05-08 Neurocrine Biosciences, Inc. Improvement, maintenance or reduction of decline of motor function associated with huntington disease using valbenazine
WO2025259267A1 (en) 2024-06-11 2025-12-18 Vector Vitale Ip Llc Pharmaceutical compositions for modulating inflammation and oxidative stress comprising chemically enriched elements

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2830993A (en) * 1958-04-15 Quinolizine derivatives
US3045021A (en) 1959-09-24 1962-07-17 Hoffmann La Roche Preparation of substituted 2-oxobenzoquinolizines
DE1253271B (de) * 1961-03-28 1967-11-02 Mta Verfahren zur Herstellung von 2-Oxo-1, 2, 3, 4, 6, 7-hexahydro-11bH-benzo[a]chinolizinen
US4316897A (en) * 1980-09-10 1982-02-23 Hoffmann-La Roche Inc. Method of lowering serum prolactin
US6221335B1 (en) * 1994-03-25 2001-04-24 Isotechnika, Inc. Method of using deuterated calcium channel blockers
ES2293638T3 (es) * 1994-03-25 2008-03-16 Isotechnika, Inc. Mejora de la eficacia de farmacos por deuteracion.
US6440710B1 (en) * 1998-12-10 2002-08-27 The Scripps Research Institute Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds
ATE234299T1 (de) * 1999-12-03 2003-03-15 Pfizer Prod Inc Sulfamoylheteroarylpyrazolverbindungen zur verwendung als analgetisches/entzündungshemmendes mittel
EP1134290A3 (en) * 2000-03-14 2004-01-02 Pfizer Products Inc. Pharmacophore models for the identification of the CYP2D6 inhibitory potency of selective serotonin reuptake inhibitors
TW200413273A (en) * 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
US20050153953A1 (en) * 2003-11-21 2005-07-14 Crista Trippodi-Murphy Compositions and methods of treatment using L-type calcium channel blockers and cholinesterase inhibitors
GB2410947B (en) * 2004-02-11 2008-09-17 Cambridge Lab Ltd Pharmaceutical compounds
WO2006053067A2 (en) 2004-11-09 2006-05-18 Prestwick Pharmaceuticals, Inc. Combination of amantadine and a tetrabenazine compound for treating hyperkinetic disorders
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US20080033011A1 (en) * 2005-07-29 2008-02-07 Concert Pharmaceuticals Inc. Novel benzo[d][1,3]-dioxol derivatives
US7750168B2 (en) * 2006-02-10 2010-07-06 Sigma-Aldrich Co. Stabilized deuteroborane-tetrahydrofuran complex
BRPI0711481A8 (pt) 2006-05-02 2017-11-28 Univ Michigan Regents derivados radiomarcados de dihidrotetrabenzeno e seu uso como agente de imagens
PT2081929E (pt) 2006-11-08 2013-04-15 Neurocrine Biosciences Inc Compostos de 3-isobutil-9,10-dimetoxi- 1,3,4,6,7,11b-hexahidro-2h-pirido[2,1-a]isoquinolin- 2-ol substituídos e métodos com estes relacionados
CA2673137C (en) 2006-11-21 2015-02-10 Rigel Pharmaceuticals, Inc. Prodrug salts of 2,4-pyrimidinediamine compounds and their uses
US20100204258A1 (en) * 2007-03-12 2010-08-12 The Trustees Of Columbia University In The City Of New York Methods and compositions for modulating insulin secretion and glucose metabolism
US8008500B2 (en) * 2007-06-08 2011-08-30 General Electric Company Intermediates useful for making tetrabenazine compounds
US9827210B2 (en) * 2007-06-29 2017-11-28 Phovitreal Pty Ltd Treatment or prophylaxis of a neurological or neuropsychiatric disorders via ocular administration
WO2009124357A1 (en) 2008-04-10 2009-10-15 Malvin Leonard Eutick Fast dissolving oral formulations for critical drugs
GB2462611A (en) 2008-08-12 2010-02-17 Cambridge Lab Pharmaceutical composition comprising tetrabenazine
NO3061760T3 (Direct) * 2008-09-18 2018-04-07
US20100113496A1 (en) * 2008-09-25 2010-05-06 Auspex Pharmaceuticals, Inc. Piperidine modulators of vmat2
JP2013501810A (ja) 2009-08-12 2013-01-17 ヴァリーント インターナショナル（バルバドス）エスアールエル 医薬組成物
BR112012020585A2 (pt) 2010-02-24 2018-04-17 Auspex Pharmaceuticals Inc composto, composição farmacêutica e método de tratamento de um distúrbio mediado por tirosina quinase
WO2011153157A2 (en) * 2010-06-01 2011-12-08 Auspex Pharmaceutical, Inc. Benzoquinolone inhibitors of vmat2

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015007124A (ja) * 2008-09-18 2015-01-15 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 小胞モノアミン輸送体２のベンゾキノリン阻害剤

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