JP2013536859A - ５−ｈｔ２ｃアゴニストの非吸湿性塩 - Google Patents

５−ｈｔ２ｃアゴニストの非吸湿性塩 Download PDF

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JP2013536859A
JP2013536859A JP2013527264A JP2013527264A JP2013536859A JP 2013536859 A JP2013536859 A JP 2013536859A JP 2013527264 A JP2013527264 A JP 2013527264A JP 2013527264 A JP2013527264 A JP 2013527264A JP 2013536859 A JP2013536859 A JP 2013536859A
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salt
weight
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methyl
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JP2013536859A5 (enExample
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アンソニー シー． ブラックバーン，
ユン シャン，
アナ シフリナ，
スコット スティルン，
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アリーナ ファーマシューティカルズ， インコーポレイテッド
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Publication of JP2013536859A publication Critical patent/JP2013536859A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/05—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/06—Oxalic acid
    • C07C55/07—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/347—Saturated compounds containing more than one carboxyl group containing keto groups

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2013527264A 2010-09-01 2011-08-31 ５−ｈｔ２ｃアゴニストの非吸湿性塩 Pending JP2013536859A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40261110P 2010-09-01 2010-09-01
US61/402,611 2010-09-01
PCT/US2011/049960 WO2012030957A2 (en) 2010-09-01 2011-08-31 Non-hygroscopic salts of 5-ht2c agonists

Publications (2)

Publication Number Publication Date
JP2013536859A true JP2013536859A (ja) 2013-09-26
JP2013536859A5 JP2013536859A5 (enExample) 2014-10-16

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JP2013527264A Pending JP2013536859A (ja) 2010-09-01 2011-08-31 ５−ｈｔ２ｃアゴニストの非吸湿性塩

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US (2) US9365521B2 (enExample)
EP (1) EP2611433A2 (enExample)
JP (1) JP2013536859A (enExample)
KR (1) KR20130101524A (enExample)
CN (1) CN103189360A (enExample)
AU (1) AU2011296033A1 (enExample)
CA (1) CA2808904A1 (enExample)
MX (1) MX2013002421A (enExample)
SG (2) SG188361A1 (enExample)
WO (1) WO2012030957A2 (enExample)

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JP6272695B2 (ja) 2010-09-01 2018-01-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 体重管理のために有用な５−ｈｔ２ｃアゴニストの改変放出剤形
AU2011296033A1 (en) * 2010-09-01 2013-04-04 Arena Pharmaceuticals, Inc. Non-hygroscopic salts of 5-HT2C agonists
BR112015007779A2 (pt) 2012-10-09 2017-07-04 Arena Pharm Inc célula de fluxo de permeabilidade e sistema de condutância hidráulica
CN104936947B (zh) * 2013-12-27 2017-03-08 杭州普晒医药科技有限公司 氯卡色林盐及其晶体、其制备方法和用途
CN105228986B (zh) 2014-04-21 2017-11-07 杭州普晒医药科技有限公司 一种氯卡色林共晶及其制备方法、药物组合物和用途
TW201618787A (zh) 2014-10-30 2016-06-01 艾尼納製藥公司 組合物及方法
WO2020072675A1 (en) 2018-10-02 2020-04-09 Northwestern University Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c)

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH06508352A (ja) * 1991-06-21 1994-09-22 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 門脈圧亢進症および片頭痛の治療用のテトラヒドロベンズアゼピン誘導体の使用
JP2004532240A (ja) * 2001-05-08 2004-10-21 スミスクライン　ビーチャム　パブリック　リミテッド　カンパニー ５−ｈｔ６受容体アンタゴニストとしてのベンゾ［ｄ］アゼピン誘導体
JP2005502861A (ja) * 2001-08-10 2005-01-27 サイミックス テクノロジーズ， インコーポレイテッド 事前処方物を作製および試験するための装置および方法ならびにそのためのシステム
JP2007502272A (ja) * 2003-08-11 2007-02-08 イーライ リリー アンド カンパニー ５‐ＨＴ２Ｃ受容体アゴニストとしての６‐（２，２，２‐トリフルオロエチルアミノ）‐７‐クロロ‐２，３，４，５‐テトラヒドロ‐１Ｈ‐ベンゾ［ｄ］アゼピン
JP2007516941A (ja) * 2003-06-17 2007-06-28 アリーナ ファーマシューティカルズ， インコーポレイテッド ５ｈｔ２ｃレセプター関連疾患の処置に有用なベンズアゼピン誘導体
JP2007521269A (ja) * 2003-06-17 2007-08-02 アリーナ ファーマシューティカルズ， インコーポレイテッド ３−ベンズアゼピンを調製する方法
JP2007523951A (ja) * 2004-02-25 2007-08-23 イーライ リリー アンド カンパニー ５−ＨＴ２Ｃ受容体作用薬としての６−置換２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン
JP2008524262A (ja) * 2004-12-21 2008-07-10 アリーナ ファーマシューティカルズ， インコーポレイテッド （ｒ）−８−クロロ−１−メチル−２，３，４，５−テトラヒドロ−１ｈ−３−ベンザゼピン塩酸塩の結晶形
JP2008525480A (ja) * 2004-12-23 2008-07-17 アリーナ ファーマシューティカルズ， インコーポレイテッド ５ｈｔ２ｃレセプターモジュレーターの組成物およびその使用方法
JP2009507037A (ja) * 2005-09-01 2009-02-19 イーライ リリー アンド カンパニー ５−ＨＴ２Ｃ受容体アゴニストとしての６−置換された２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン
JP2009508818A (ja) * 2005-09-01 2009-03-05 イーライ リリー アンド カンパニー ５−ＨＴ２Ｃ受容体アゴニストとしての６−置換−２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン
JP2009532470A (ja) * 2006-04-03 2009-09-10 アリーナ ファーマシューティカルズ， インコーポレイテッド ８−クロロ−１−メチル−２，３，４，５−テトラヒドロ−１ｈ−３−ベンズアゼピンおよびこれに関連する中間体を調製するためのプロセス

Family Cites Families (141)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2900415A (en) 1954-12-14 1959-08-18 Lakeside Lab Inc Synthesized antispasmodic compounds
CH498122A (de) 1968-02-09 1970-10-31 Geigy Ag J R Verfahren zur Herstellung eines neuen Tetrahydroazepinderivates
CH481110A (de) 1967-02-17 1969-11-15 Geigy Ag J R Verfahren zur Herstellung von 1,2,4,5-Tetrahydro-3-azepinen
CH500194A (de) 1968-02-15 1970-12-15 Ciba Geigy Ag Verfahren zur Herstellung von Tetrahydroazepinderivaten
US4233217A (en) 1968-03-11 1980-11-11 Pennwalt Corporation Substituted 1,2,4,5-tetrahydro-3H, 3 benzazepines
GB1268243A (en) 1968-03-11 1972-03-22 Wallace & Tiernan Inc 0,2,4,5,-tetrahydro-3h,3-benzazepines
FR314F (enExample) 1968-03-22 1970-05-25
FR7736M (enExample) 1968-09-02 1970-03-09
US3716639A (en) 1970-03-11 1973-02-13 Ciba Geigy Corp Anorexigenic tetrahydrobenzazepines
US3795683A (en) 1970-08-19 1974-03-05 Hoffmann La Roche 2,3,4,5-tetrahydro-1h-3-benzazepines
LU65954A1 (enExample) 1972-08-25 1974-03-07
US4210749A (en) 1974-11-12 1980-07-01 Pennwalt Corporation Substituted 1,2,4,5-tetrahydro-3H,3 benzazepines
SE7510988L (sv) 1975-10-01 1977-04-02 Draco Ab Nya farmaceutiskt aktiva foreningar
US4111957A (en) 1977-02-02 1978-09-05 Smithkline Corporation Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds
US4108989A (en) 1977-04-01 1978-08-22 Smithkline Corporation 2,3,4,5-tetrahydro-1h-3-benzazepine-7,8-diones
DE2758001A1 (de) 1977-12-24 1979-07-12 Hoechst Ag Cephalosporinderivate und verfahren zu ihrer herstellung
CA1090797A (en) 1978-06-20 1980-12-02 Kenneth G. Holden Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1h- 3-benzazepine compounds
AU515236B2 (en) 1978-06-26 1981-03-26 Smithkline Corporation Substituted-1-thienyl and furyl-2,3,4,5-tetrahydro-14-3 benzazepine derivatives
ZA792785B (en) 1978-07-07 1980-08-27 Smithkline Corp Mercapto substituted-2,3,4,5-tetrahydro-1h-3-benzazepines
IE50355B1 (en) 1979-10-20 1986-04-02 Wyeth John & Brother Ltd Morpholine derivatives
US4477378A (en) 1980-02-05 1984-10-16 Schering Corp. Esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
ZA827887B (en) 1981-11-27 1983-11-30 Smithkline Beckman Corp Pharmaceutical compositions and method of producing alpha2 antagonism
EP0080779B1 (en) 1981-11-27 1986-07-16 Smithkline Beckman Corporation 3-benzazepines as alpha-2 antagonists
FR2518544A1 (fr) 1981-12-22 1983-06-24 Lipha Benzodiazepines-1,3 thione-2, procede de preparation et medicament les contenant
FR2525603A1 (fr) 1982-04-27 1983-10-28 Adir Benzoazacycloalkyl-spiro-imidazolinines, leur preparation et leur application en therapeutique
US4988690A (en) 1982-06-14 1991-01-29 Hoechst-Roussel Pharmaceuticals Inc. 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and anti-depressant use thereof
DE3418270A1 (de) 1984-05-17 1985-11-21 Dr. Karl Thomae Gmbh, 7950 Biberach Neue aminotetralinderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US4541954A (en) 1984-09-05 1985-09-17 Smithkline Beckman Corporation Method for preparing 6-chloro-N-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
EP0204349A3 (de) 1985-06-01 1990-01-03 Dr. Karl Thomae GmbH Neue heteroaromatische Aminderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
EG18188A (en) 1986-05-01 1992-09-30 Pfizer Ltd Process for preparation anti-arhythmia agents
GB8610668D0 (en) 1986-05-01 1986-06-04 Pfizer Ltd Anti-arrhythmia agents
US4762845A (en) 1986-05-21 1988-08-09 Abbott Laboratories 7-(3-Substituted imino-1-pyrrolidinyl)-quinolone-3-carboxylic acids
EP0285287A3 (en) 1987-03-23 1990-08-16 Smithkline Beecham Corporation 3-benzazepine compounds for use in treating gastrointestinal motility disorders
ZA882080B (en) 1987-03-27 1989-04-26 Schering Corp Substituted benzazepines,their preparation and pharmaceutical compositions containing them
US5247080A (en) 1987-03-27 1993-09-21 Schering Corporation Substituted benzazepines useful as intermediates for producing pharmaceutically active compounds
US5015639A (en) 1987-03-27 1991-05-14 Schering Corporation Substituted benzazepines, their preparation and pharmaceutical compositions containing them
WO1988007858A1 (en) 1987-04-09 1988-10-20 Smithkline Beckman Corporation Sulfinyl and sulfonyl substituted 3-benzazepines
US4957914A (en) 1987-05-15 1990-09-18 Syntex (U.S.A.) Inc. 1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines
DK107688D0 (da) 1988-03-01 1988-03-01 Novo Industri As Carbaminsyreestere af substituerede 7-hydroxy-2,3,4,5-tetrahydro-1h-3-benzazepiner
US5422355A (en) 1989-06-02 1995-06-06 John Wyeth & Brother, Limited Composition for treating depression with (N-heteroaryl)alkylamines
US5178786A (en) 1989-08-04 1993-01-12 The Lubrizol Corporation Corrosion-inhibiting compositions and functional fluids containing same
CA2037162A1 (en) 1990-03-12 1991-09-13 Steven Howard Shaber Heterocyclicacetonitriles and fungicidal use
AU8201591A (en) 1990-06-15 1992-01-07 Schering Corporation 8-lower alkyl-5-cycloalkyl or 5-cycloalkenyl substitued benzazepines and pharmaceutical compositions containing them
US5275915A (en) 1991-06-05 1994-01-04 Dainippon Ink And Chemicals, Inc. Developer for light-sensitive material
GB9116824D0 (en) 1991-08-05 1991-09-18 Smithkline Beecham Corp Chemical compounds
EP0558824A1 (en) 1992-02-04 1993-09-08 Duphar International Research B.V Method for the preparation of vicinal aminoalcohols and optically active O-protected derivatives thereof
US5241065A (en) 1992-02-25 1993-08-31 Schering Corporation 2,3,4,5-tetrahydro-1h-3-benzazepines having anti-psychotic activity
JPH05339263A (ja) 1992-06-08 1993-12-21 Wakunaga Pharmaceut Co Ltd ジヒドロピリジン誘導体
JPH06298746A (ja) 1993-04-19 1994-10-25 Showa Denko Kk 環状イミド酸エステルの製造法
EP0714292A4 (en) 1993-06-23 1996-10-09 Cambridge Neuroscience Inc SIGMA RECEPTOR LIGANDS AND THEIR USE
US5387685A (en) 1993-07-16 1995-02-07 American Cyanamid Co MDR reversal agents
GB9322976D0 (en) 1993-11-08 1994-01-05 Pfizer Ltd Therapeutic agents
DE4419246A1 (de) 1994-06-01 1995-12-07 Merckle Gmbh Heteroarylsubstituierte Pyrrolizinverbindungen und deren Anwendung in der Pharmazie
DE4419315A1 (de) 1994-06-01 1995-12-07 Merckle Gmbh Heteropyrrolizinverbindungen und deren Anwendung in der Pharmazie
DE4419247A1 (de) 1994-06-01 1995-12-07 Merckle Gmbh Sulfonylierte Pyrrolizincarbonsäureamide und deren Anwendung in der Pharmazie
DE4427838A1 (de) 1994-08-05 1996-02-08 Thomae Gmbh Dr K Kondensierte Azepinderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4429079A1 (de) 1994-08-17 1996-02-22 Thomae Gmbh Dr K Cyclische Harnstoffderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JPH08134048A (ja) 1994-11-08 1996-05-28 Sumitomo Chem Co Ltd オキサゾリン類の製造法
GB9508622D0 (en) 1995-04-28 1995-06-14 Pfizer Ltd Therapeutic agants
JPH0930960A (ja) 1995-07-18 1997-02-04 Takasago Internatl Corp 真菌感染症治療剤
JPH0987258A (ja) 1995-09-28 1997-03-31 Sumitomo Chem Co Ltd オキサゾリン類、その製造方法およびそれを用いる不斉シクロプロパンカルボン酸類の製造方法
CA2190708A1 (en) 1995-12-08 1997-06-09 Johannes Aebi Aminoalkyl substituted benzo-heterocyclic compounds
US5892116A (en) 1996-01-03 1999-04-06 Georgetown University Gelators
US5925651A (en) 1996-04-03 1999-07-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5691362A (en) 1996-06-05 1997-11-25 Schering-Plough Corporation Substituted benzene-fused hetero- and carbocyclics as nuerokinin antagonists
EP0920417A4 (en) 1996-08-15 1999-12-29 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
US5908830A (en) 1996-10-31 1999-06-01 Merck & Co., Inc. Combination therapy for the treatment of diabetes and obesity
EP0973778A1 (en) 1997-03-07 2000-01-26 Novo Nordisk A/S 4,5,6,7-TETRAHYDRO-THIENO 3,2-c]PYRIDINE DERIVATIVES, THEIR PREPARATION AND USE
US5795895A (en) 1997-06-13 1998-08-18 Anchors; J. Michael Combination anorexiant drug therapy for obesity using phentermine and an SSRI drug
AUPP020297A0 (en) 1997-11-05 1997-11-27 University Of Melbourne, The A novel receptor, and compounds which bind thereto
WO1999046232A1 (en) 1998-03-10 1999-09-16 Ono Pharmaceutical Co., Ltd. Carboxylic acid derivatives and drugs containing the same as the active ingredient
JP3603177B2 (ja) 1998-03-26 2004-12-22 参天製薬株式会社 新規ウレア誘導体
CN1305846C (zh) 1998-03-26 2007-03-21 参天制药株式会社 脲衍生物
GB9807354D0 (en) * 1998-04-07 1998-06-03 Glaxo Group Ltd Antiviral compound
EP0987235B1 (en) 1998-08-25 2003-03-12 MERCK PATENT GmbH Method for the conversion of arenes or alkenes with iodoalkenes, aryl iodides or arenediazonium salts
US7141593B1 (en) * 1999-06-04 2006-11-28 Abbott Laboratories Pharmaceutical formulations
US20080103179A1 (en) 2006-10-27 2008-05-01 Tam Peter Y Combination Therapy
ES2209728T3 (es) 1999-08-06 2004-07-01 F. Hoffmann-La Roche Ag Tetrahidro-benzo(d)azepinas y su uso como antagonistas de receptores de glutamato metabotropico.
EP1074549B1 (en) 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
JP2001076413A (ja) 1999-09-06 2001-03-23 Sony Corp フレキシブル磁気ディスク用ヘッドスライダー
US6403657B1 (en) 1999-10-04 2002-06-11 Martin C. Hinz Comprehensive pharmacologic therapy for treatment of obesity
DE10003708A1 (de) 2000-01-28 2001-08-02 Solvent Innovation Gmbh Neuartige chirale ionische Flüssigkeiten und Verfahren zu ihrer Darstellung in enantiomerenreiner oder enantiomerenangereicherter Form
CA2413134C (en) 2000-06-30 2010-05-11 Glaxo Group Limited Quinazoline ditosylate salt compounds
KR20030045187A (ko) 2000-11-14 2003-06-09 스미스클라인비이참피이엘시이 도파민 ｄ₃수용체 조절제 (정신병 치료제)로서 유용한테트라히드로벤즈아제핀 유도체
DE10057751A1 (de) 2000-11-22 2002-05-23 Bayer Ag Neue Carbamat-substituierte Pyrazolopyridinderivate
GB0030710D0 (en) 2000-12-15 2001-01-31 Hoffmann La Roche Piperazine derivatives
JPWO2002074746A1 (ja) 2001-03-16 2004-07-08 山之内製薬株式会社 ベンゾアゼピン誘導体
PT1390377E (pt) * 2001-05-22 2006-06-30 Pfizer Prod Inc Nova forma cristalina da azitromicina
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
BR0212787A (pt) 2001-09-24 2005-01-25 Elan Pharm Inc Composto ou sal farmaceuticamente aceitável do mesmo, métodos de tratamento ou prevenção de doenças e de preparação de um composto, uso de um composto ou sal, e, composição farmacêutica
EP1456178A1 (en) 2001-12-21 2004-09-15 Smithkline Beecham Plc 7-sulfonyl-3-benzazepine derivatives as modulators of the dopamine receptor and their use for the treatment of cns disorders
AU2002367323A1 (en) 2001-12-28 2003-07-24 Bayer Pharmaceuticals Corporation Benzothieno (3,2-
JP2005519915A (ja) 2002-01-18 2005-07-07 セレテック・リミテッド・ライアビリティ・カンパニー Ｅｄｇ受容体に関連する症状の処置方法
JP3813152B2 (ja) 2002-03-12 2006-08-23 メルク エンド カムパニー インコーポレーテッド 置換アミド類
EP1494533A2 (en) 2002-04-12 2005-01-12 The University of Chicago Farnesoid x-activated receptor agonists
US6953787B2 (en) 2002-04-12 2005-10-11 Arena Pharmaceuticals, Inc. 5HT2C receptor modulators
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
US6821502B2 (en) * 2002-06-12 2004-11-23 Chevron U.S.A. Inc. Method of making aluminum-containing zeolite with IFR structure
GB0224557D0 (en) 2002-10-22 2002-11-27 Glaxo Group Ltd Novel compounds
DE10261131A1 (de) 2002-12-20 2004-07-01 Grünenthal GmbH Substituierte 5-Aminomethyl-1H-pyrrol-2-carbonsäureamide
US7145012B2 (en) 2003-04-23 2006-12-05 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
US7232823B2 (en) 2003-06-09 2007-06-19 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
EP1644347A1 (en) 2003-06-20 2006-04-12 Arena Pharmaceuticals, Inc. N-PHENYL-PIPERAZINE DERIVATIVES AND METHODS OF PROPHYLAXIS OR TREATMENT OF 5HT sb 2C /sb RECEPTOR ASSOCIATED DISEASES
WO2005037424A1 (en) * 2003-10-06 2005-04-28 Solvias Ag Process for the parallel detection of crystalline forms of molecular solids
WO2005042490A1 (en) 2003-10-22 2005-05-12 Arena Pharmaceuticals, Inc. Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases
WO2005042491A1 (en) 2003-10-22 2005-05-12 Arena Pharmaceuticals, Inc. Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases
AR047541A1 (es) * 2004-02-13 2006-01-25 Sandoz Ag Fosfato de 5-[[4-[2-metil-2-piridinil-amino-etoxi]fenil]metil]-2,4 tiazolidinadiona (rosiglitazona) y sus formas polimorficas
SE0401871D0 (sv) 2004-07-15 2004-07-15 Glucogene Medical Hfm Ab New compositions
US7351833B2 (en) * 2004-07-23 2008-04-01 Abbott Laboratories (1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3.2.0]heptane benzenesulfonate
CN101087601A (zh) 2004-08-02 2007-12-12 根梅迪卡治疗公司 用于抑制含铜胺氧化酶的化合物及其应用
JPWO2006043710A1 (ja) 2004-10-19 2008-05-22 株式会社リバース・プロテオミクス研究所 創薬標的タンパク質及び標的遺伝子、並びにスクリーニング方法
US8436176B2 (en) * 2004-12-30 2013-05-07 Medicis Pharmaceutical Corporation Process for preparing 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
UA91546C2 (uk) * 2005-05-03 2010-08-10 Бьорінгер Інгельхайм Інтернаціональ Гмбх КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ
MY152185A (en) * 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
HRP20120073T1 (hr) * 2005-08-29 2012-07-31 Sanofi@Aventis@U@S@@LLC NOVI KRISTALNI OBLIK DERIVATA PIRIDAZINO[ b]INDOLA
EP2119723A1 (en) * 2005-09-13 2009-11-18 Sicor, Inc. Processes for the synthesis of rocuronium bromide
KR20090064400A (ko) * 2006-09-28 2009-06-18 머크 앤드 캄파니 인코포레이티드 Ｈｄａｃ 억제제 및 킬레이트화 가능한 금속 화합물 및 금속-ｈｄａｃ 억제제 킬레이트 착물의 약제학적 조성물
US7837978B2 (en) * 2006-10-13 2010-11-23 Chevron U.S.A. Inc. Process for preparing aluminum-containing molecular sieve SSZ-26
CN101547892B (zh) 2006-12-05 2014-08-20 艾尼纳制药公司 制备(r)-8-氯-1-甲基-2,3,4,5-四氢-1h-3-苯并氮杂卓的方法和其中间体
PE20081506A1 (es) * 2006-12-12 2008-12-09 Infinity Discovery Inc Formulaciones de ansamicina
SI2114933T1 (sl) 2007-01-04 2012-01-31 Prosidion Ltd Windrush Court Piperidinski gpcr-agonisti
CA2687647A1 (en) * 2007-05-22 2008-11-27 Ultimorphix Technologies B.V. Tenofovir disoproxil hemi-fumaric acid co-crystal
EP2164324B1 (en) 2007-06-15 2014-08-13 University Of Florida Research Foundation Therapeutic compounds
EP2237781A2 (en) 2007-12-20 2010-10-13 NeuroSearch A/S Pharmaceutical composition comprising tesofensine or its analogue and an anti-obesity
WO2009097416A1 (en) 2008-01-29 2009-08-06 Vanda Pharmaceuticals, Inc. Imidazolylalkyl- pyridines as dbh inhibitors
TW200944520A (en) * 2008-01-29 2009-11-01 Glaxo Group Ltd Spiro compounds as NPY Y5 receptor antagonists
US8822727B2 (en) 2008-03-04 2014-09-02 Arena Pharmaceuticals, Inc. Processes for the preparation of intermediates related to the 5-HT2C agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
US20090270404A1 (en) 2008-03-31 2009-10-29 Metabolex, Inc. Oxymethylene aryl compounds and uses thereof
US20110294836A1 (en) 2008-06-20 2011-12-01 Metabolex, Inc. Aryl gpr119 agonists and uses thereof
AU2009290911A1 (en) 2008-09-10 2010-03-18 Boehringer Ingelheim International Gmbh Combination therapy for the treatment of diabetes and related conditions
WO2010148207A2 (en) 2009-06-18 2010-12-23 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-ht2c receptor agonists
EP2445878A1 (en) 2009-06-24 2012-05-02 Boehringer Ingelheim International GmbH New compounds, pharmaceutical composition and methods relating thereto
BR112013004707A2 (pt) * 2010-09-01 2016-05-10 Arena Pharm Inc administração de um composto antiobesidade a indivíduos com comprometimento renal
SG10201506870PA (en) * 2010-09-01 2015-10-29 Arena Pharm Inc Salts of lorcaserin with optically active acids
JP6272695B2 (ja) 2010-09-01 2018-01-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 体重管理のために有用な５−ｈｔ２ｃアゴニストの改変放出剤形
WO2012030953A1 (en) 2010-09-01 2012-03-08 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists in the treatment of disorders ameliorated by reduction of norepinephrine level
KR20130138768A (ko) 2010-09-01 2013-12-19 아레나 파마슈티칼스, 인크. 5-ｈｔ2ｃ 아고니스트의 신속-용해성 투여 형태
AU2011296033A1 (en) * 2010-09-01 2013-04-04 Arena Pharmaceuticals, Inc. Non-hygroscopic salts of 5-HT2C agonists
CN102126988A (zh) 2010-12-17 2011-07-20 张家港瀚康化工有限公司 4-(4-氯苯基)-2-溴甲基-2-苯基丁腈的制备方法
BR112015007779A2 (pt) * 2012-10-09 2017-07-04 Arena Pharm Inc célula de fluxo de permeabilidade e sistema de condutância hidráulica

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH06508352A (ja) * 1991-06-21 1994-09-22 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 門脈圧亢進症および片頭痛の治療用のテトラヒドロベンズアゼピン誘導体の使用
JP2004532240A (ja) * 2001-05-08 2004-10-21 スミスクライン　ビーチャム　パブリック　リミテッド　カンパニー ５−ｈｔ６受容体アンタゴニストとしてのベンゾ［ｄ］アゼピン誘導体
JP2005502861A (ja) * 2001-08-10 2005-01-27 サイミックス テクノロジーズ， インコーポレイテッド 事前処方物を作製および試験するための装置および方法ならびにそのためのシステム
JP2007516941A (ja) * 2003-06-17 2007-06-28 アリーナ ファーマシューティカルズ， インコーポレイテッド ５ｈｔ２ｃレセプター関連疾患の処置に有用なベンズアゼピン誘導体
JP2007521269A (ja) * 2003-06-17 2007-08-02 アリーナ ファーマシューティカルズ， インコーポレイテッド ３−ベンズアゼピンを調製する方法
JP2007502272A (ja) * 2003-08-11 2007-02-08 イーライ リリー アンド カンパニー ５‐ＨＴ２Ｃ受容体アゴニストとしての６‐（２，２，２‐トリフルオロエチルアミノ）‐７‐クロロ‐２，３，４，５‐テトラヒドロ‐１Ｈ‐ベンゾ［ｄ］アゼピン
JP2007523951A (ja) * 2004-02-25 2007-08-23 イーライ リリー アンド カンパニー ５−ＨＴ２Ｃ受容体作用薬としての６−置換２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン
JP2008524262A (ja) * 2004-12-21 2008-07-10 アリーナ ファーマシューティカルズ， インコーポレイテッド （ｒ）−８−クロロ−１−メチル−２，３，４，５−テトラヒドロ−１ｈ−３−ベンザゼピン塩酸塩の結晶形
JP2008525480A (ja) * 2004-12-23 2008-07-17 アリーナ ファーマシューティカルズ， インコーポレイテッド ５ｈｔ２ｃレセプターモジュレーターの組成物およびその使用方法
JP2009507037A (ja) * 2005-09-01 2009-02-19 イーライ リリー アンド カンパニー ５−ＨＴ２Ｃ受容体アゴニストとしての６−置換された２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン
JP2009508818A (ja) * 2005-09-01 2009-03-05 イーライ リリー アンド カンパニー ５−ＨＴ２Ｃ受容体アゴニストとしての６−置換−２，３，４，５−テトラヒドロ−１Ｈ−ベンゾ［ｄ］アゼピン
JP2009532470A (ja) * 2006-04-03 2009-09-10 アリーナ ファーマシューティカルズ， インコーポレイテッド ８−クロロ−１−メチル−２，３，４，５−テトラヒドロ−１ｈ−３−ベンズアゼピンおよびこれに関連する中間体を調製するためのプロセス

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BERGE,S.M. ET AL: "Pharmaceutical salts", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 66, no. 1, JPN6015027493, 1977, pages 1 - 19, XP002009462, ISSN: 0003111779 *
真野高司: "創薬の探索段階における薬剤学的研究の意義と実践", 日本薬理学雑誌, vol. 第１３３巻，第３号, JPN6013044734, 1 March 2009 (2009-03-01), pages 149 - 153, ISSN: 0003111780 *

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