JP2004532209A5 - - Google Patents

Download PDF

Info

Publication number
JP2004532209A5
JP2004532209A5 JP2002576959A JP2002576959A JP2004532209A5 JP 2004532209 A5 JP2004532209 A5 JP 2004532209A5 JP 2002576959 A JP2002576959 A JP 2002576959A JP 2002576959 A JP2002576959 A JP 2002576959A JP 2004532209 A5 JP2004532209 A5 JP 2004532209A5
Authority
JP
Japan
Prior art keywords
optionally substituted
group
compound
fluoro
alkyl
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
Application number
JP2002576959A
Other languages
English (en)
Other versions
JP2004532209A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2002/005115 external-priority patent/WO2002078693A2/en
Publication of JP2004532209A publication Critical patent/JP2004532209A/ja
Publication of JP2004532209A5 publication Critical patent/JP2004532209A5/ja
Pending legal-status Critical Current

Links

Claims (4)


  1. Figure 2004532209
    [式中、
    Xは、−O−、−NH−、−S−、−SO2−、−CH2−、−CH(F)−、−CH(OH)−、および−C(O)−からなる群から選択され;
    1は、場合により置換されたフェニル、場合により置換されたナフチル、イミダゾリル、および窒素、酸素、硫黄からなる群から選択される1個のヘテロ原子を有する、場合により置換された、5〜6員環の単環式芳香族複素環からなる群から選択され、該5〜6員環の単環式芳香族複素環は場合によりベンソ縮合しており;
    2は、水素およびC1−C3アルキルからなる群から選択され;
    3は、水素、フルオロ、およびメチルからなる群から選択され;
    4は、水素、アリル、C2−C4アルキル、フッ素化されたC2−C4アルキル、場合により置換されたフェニル、ナフチル、場合により置換されたフェニルスルホニル、場合により置換されたベンジル、および窒素、酸素、硫黄からなる群から選択される1または2個のヘテロ原子を有する、場合により置換された5〜6員環の単環式芳香族複素環からなる群から選択され、但し、Xが−SO2−、−CH2−、−CH(F)−、−CH(OH)−または−C(O)−であるとき、R4は場合により置換されたフェニルスルホニルでない]
    で示される化合物またはその製薬的に許容し得る塩。
  2. 化合物が、N−(2−(6−フルオロ−1H−インドール−3−イル)エチル)−3−(2,2,3,3−テトラフルオロプロポキシ)ベンジルアミンまたはその製薬的に許容し得る塩である、請求項1に記載の化合物。
  3. 化合物が、N−(2−(6−フルオロ−1H−インドール−3−イル)エチル)−3−(2,2,3,3−テトラフルオロプロポキシ)ベンジルアミン塩酸塩である、請求項2記載の化合物。
  4. 請求項1記載の化合物および製薬的に許容し得る希釈剤を含有する医薬組成物。
JP2002576959A 2001-03-29 2002-03-15 5−ht6受容体の拮抗薬としてのn−(2−アリールエチル)ベンジルアミン Pending JP2004532209A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US27992801P 2001-03-29 2001-03-29
US32944901P 2001-10-15 2001-10-15
PCT/US2002/005115 WO2002078693A2 (en) 2001-03-29 2002-03-15 N-(2-arylethyl)benzylamines as antagonists of the 5-ht6 receptor

Publications (2)

Publication Number Publication Date
JP2004532209A JP2004532209A (ja) 2004-10-21
JP2004532209A5 true JP2004532209A5 (ja) 2005-12-22

Family

ID=26959969

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2002576959A Pending JP2004532209A (ja) 2001-03-29 2002-03-15 5−ht6受容体の拮抗薬としてのn−(2−アリールエチル)ベンジルアミン

Country Status (29)

Country Link
US (3) US7157488B2 (ja)
EP (1) EP1379239B1 (ja)
JP (1) JP2004532209A (ja)
KR (1) KR100894189B1 (ja)
CN (1) CN1610547A (ja)
AT (1) ATE372768T1 (ja)
AU (1) AU2002303094B2 (ja)
BR (1) BR0208179A (ja)
CA (1) CA2442114C (ja)
CY (1) CY1110362T1 (ja)
CZ (1) CZ305838B6 (ja)
DE (1) DE60222396T2 (ja)
DK (2) DK1379239T3 (ja)
DZ (1) DZ3493A1 (ja)
EA (1) EA007493B1 (ja)
ES (2) ES2292758T3 (ja)
HK (1) HK1061649A1 (ja)
HR (1) HRP20030771B1 (ja)
HU (1) HU230322B1 (ja)
IL (3) IL157651A0 (ja)
MX (1) MXPA03008726A (ja)
NO (1) NO326160B1 (ja)
NZ (1) NZ527815A (ja)
PL (1) PL220721B1 (ja)
PT (2) PT1379239E (ja)
SI (1) SI1859798T1 (ja)
SK (1) SK287463B6 (ja)
WO (1) WO2002078693A2 (ja)
ZA (1) ZA200306795B (ja)

Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
AU2002303094B2 (en) * 2001-03-29 2006-11-23 Eli Lilly And Company N-(2-arylethyl)benzylamines as antagonists of the 5-HT6 receptor
EP1411925A1 (en) * 2001-08-03 2004-04-28 PHARMACIA & UPJOHN COMPANY 5-arylsulfonyl indoles having 5-ht6 receptor affinity
DK1523486T3 (da) 2002-06-21 2008-03-03 Suven Life Sciences Ltd Tetracykliske arylsulfonylindoler med serotoninreceptor-affinitet
NZ537635A (en) * 2002-07-17 2006-11-30 Lek Pharmaceuticals D Novel derivatives of pyridylethanol (phenylethyl) amines as inhibitors of cholesterol biosynthesis, processes for their preparation, and pharmaceutical compositions containing them
CA2499690C (en) 2002-09-19 2011-05-24 Eli Lilly And Company Diaryl ethers as opioid receptor antagonist
JP4897221B2 (ja) * 2002-12-20 2012-03-14 チバ ホールディング インコーポレーテッド アミン類の合成及びその合成のための中間体
BRPI0407616A (pt) 2003-03-07 2006-02-14 Lilly Co Eli composto, composição farmacêutica, método para bloquear uma combinação de receptor de mu, capa, delta (heterodìmero) deste em mamìferos, método para tratar ou prevenir obesidade e doenças relacionadas, uso de um composto, e método de suprimir o apetite em um paciente em necessidade deste"
JP2006519855A (ja) 2003-03-07 2006-08-31 イーライ リリー アンド カンパニー オピオイド受容体アンタゴニスト
DE10320782A1 (de) * 2003-05-09 2004-11-25 Bayer Cropscience Ag Substituierte Oxyarene
DE602004000260T2 (de) 2003-07-22 2006-08-24 Arena Pharmaceuticals, Inc., San Diego Diaryl- und arylheteroarylharnstoffderivate als modulatoren des 5-ht2a-serotoninrezeptors, die sich zur prophylaxe und behandlung von damit im zusammenhang stehenden erkrankungen eignen
CN1894240A (zh) 2003-12-22 2007-01-10 伊莱利利公司 阿片受体拮抗剂
US7381750B2 (en) 2004-03-12 2008-06-03 Eli Lilly And Company Amino-phenoxymethyl-benzamide opioid receptor antagonists
EP1735268B1 (en) 2004-03-15 2012-02-15 Eli Lilly And Company Opioid receptor antagonists
WO2005090303A1 (en) 2004-03-15 2005-09-29 Eli Lilly And Company 4- (5- (aminomethyl) -indole-1-ylmethyl) -benzamide derivatives and related compounds as opioid receptor antagonists for the treatment of obesity
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
ME02970B (me) 2004-06-24 2018-07-20 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
EP1632491A1 (en) * 2004-08-30 2006-03-08 Laboratorios Del Dr. Esteve, S.A. Substituted indole compounds and their use as 5-HT6 receptor modulators
JP5156378B2 (ja) * 2004-09-22 2013-03-06 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ MDM2とp53の間の相互作用の阻害剤
US7459469B2 (en) 2004-11-10 2008-12-02 Targacept, Inc. Hydroxybenzoate salts of metanicotine compounds
DE102004062542A1 (de) * 2004-12-24 2006-07-06 Bayer Cropscience Ag Substituierte Oxyarene
LT1993360T (lt) 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma
JP5170742B2 (ja) * 2005-12-28 2013-03-27 積水メディカル株式会社 凝集測定用試薬及び凝集測定方法
EP1973905A4 (en) * 2006-01-06 2010-12-08 Astrazeneca Ab COMPOUNDS
JP5162574B2 (ja) 2006-03-22 2013-03-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Mdm2及びp53間の相互作用のインヒビターとしての環式アルキルアミン誘導体
JP5385125B2 (ja) * 2006-03-22 2014-01-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ MDM2とp53の間の相互作用の阻害剤
TWI389889B (zh) 2006-05-09 2013-03-21 Targacept Inc (2s)-(4e)-n-甲基-5-〔3-(5-異丙氧基吡啶)基〕-4-戊烯-2-胺之新穎多晶型
CN101528698A (zh) 2006-05-09 2009-09-09 阿斯利康公司 (2s)-(4e)-n-甲基-5-[3-(5-异丙氧基吡啶)基]-4-戊烯-2-胺的盐形式
EP1953153A1 (en) * 2007-01-31 2008-08-06 Laboratorios del Dr. Esteve S.A. Heterocyclyl-substituted sulfonamides for the treatment of cognitive or food ingestion related disorders
US8853406B2 (en) 2007-08-06 2014-10-07 Janssen Pharmaceutica Nv Substituted phenylenediamines as inhibitors of the interaction between MDM2 and P53
JO2704B1 (en) * 2007-09-21 2013-03-03 جانسين فارماسوتيكا ان في Interference inhibition factors between MD2 and B53
EP2209380A4 (en) * 2007-10-09 2011-09-14 Mark T Hamann METHOD OF USE OF COMPOSITIONS WITH ANTIDEPRESSIVE EFFICACY, MOOD EFFICACY AND OTHER NEUROLOGICAL EFFECTIVENESS AND COMPOSITIONS THEREOF
WO2009073118A1 (en) * 2007-12-04 2009-06-11 Merck & Co., Inc. Tryptamine sulfonamides as 5-ht6 antagonists
EP2508177A1 (en) 2007-12-12 2012-10-10 Glaxo Group Limited Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline
US20090318527A1 (en) * 2008-02-11 2009-12-24 Howard Sard Indole compounds and methods of use thereof
US20110021538A1 (en) 2008-04-02 2011-01-27 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
WO2010062321A1 (en) 2008-10-28 2010-06-03 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and crystalline forms related thereto
US8541442B2 (en) 2009-02-04 2013-09-24 Janssen Pharmaceutica N.V. Indole derivatives as anticancer agents
EP2821400B1 (en) 2009-03-20 2017-09-27 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
JP5083256B2 (ja) * 2009-03-20 2012-11-28 株式会社デンソー 半導体装置およびその製造方法
WO2011019738A1 (en) 2009-08-10 2011-02-17 Galenea Corporation Compounds and methods of use thereof
EP2311823A1 (en) 2009-10-15 2011-04-20 AC Immune S.A. 2,6-Diaminopyridine compounds for treating diseases associated with amyloid proteins or for treating ocular diseases
TW201139370A (en) * 2009-12-23 2011-11-16 Lundbeck & Co As H Processes for the manufacture of a pharmaceutically active agent
FR2961097B1 (fr) * 2010-06-09 2012-07-13 Oreal Procede cosmetique de traitement des odeurs corporelles humaines utilisant un compose 6-alkoxy tryptamine
FR2961095B1 (fr) * 2010-06-09 2012-06-15 Oreal Composition cosmetique et/ou dermatologique comprenant au moins un compose 6-alcoxy tryptamine
US8293218B2 (en) * 2010-07-29 2012-10-23 Conopco, Inc. Skin care compositions comprising substituted monoamines
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
WO2013130669A1 (en) 2012-02-27 2013-09-06 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
UA112109C2 (uk) * 2012-03-20 2016-07-25 Адамед Сп. З О.О. Сульфонамідні похідні бензиламіну для лікування захворювань центральної нервової системи (цнс)
CN102746211B (zh) * 2012-06-27 2015-05-27 上海泰坦化学有限公司 一种取代吲哚-3-甲醛类化合物的制备方法
JO3459B1 (ar) * 2012-09-09 2020-07-05 H Lundbeck As تركيبات صيدلانية لعلاج مرض الزهايمر
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物
US20160038484A1 (en) * 2013-04-03 2016-02-11 The University Of Utah Research Foundation Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
CN104725249B (zh) * 2013-12-20 2019-02-12 广东东阳光药业有限公司 苄胺类衍生物及其在药物上的应用
JO3639B1 (ar) * 2014-07-04 2020-08-27 H Lundbeck As صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد
AU2015330923B2 (en) 2014-10-07 2020-03-12 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
ES2570452B1 (es) * 2014-10-15 2017-04-19 Fundación Para La Investigación Biomédida Del Hospital Universitario De La Princesa Compuestos derivados de acrilato de 3-Alquilamino-1H-Indolilo y su uso en el tratamiento de enfermedades neurodegenerativas
CN105175307A (zh) * 2014-11-18 2015-12-23 苏州晶云药物科技有限公司 Lu AE58054的盐酸盐晶型A及其制备方法和用途
CN104529865B (zh) * 2014-12-12 2017-02-01 广东东阳光药业有限公司 苄胺类衍生物及其在药物上的应用
TW201630881A (zh) 2014-12-12 2016-09-01 H 朗德貝克公司 用於生產艾達魯吡啶之方法
JP2018516992A (ja) 2015-06-12 2018-06-28 アクソファント サイエンシーズ ゲーエムベーハーAxovant Sciences Gmbh レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体
RU2018103338A (ru) 2015-07-15 2019-08-15 Аксовант Сайенсиз Гмбх Производные диарил- и арилгетероарилмочевины для профилактики и лечения галлюцинаций, ассоциированных с нейродегенеративным заболеванием
CN108271369A (zh) 2015-10-23 2018-07-10 法尔玛赞公司 用于制备色胺及其衍生物的新工艺
JP2019513742A (ja) 2016-04-08 2019-05-30 ハー・ルンドベック・アクチエゼルスカベット イミンの水素化によるイダロピルジンの製造方法
DK3448430T3 (da) * 2016-04-26 2023-07-03 H Lundbeck As Anvendelse af en acetylcholinesterase-inhibitor og idalopirdin til reduktion af fald hos patienter med parkinsons sygdom
US10864191B2 (en) 2016-05-11 2020-12-15 H. Lundbeck A/S 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease with apathy as comorbidity
WO2018013686A1 (en) * 2016-07-12 2018-01-18 Concert Pharmaceuticals, Inc. Deuterated idalopirdine
EP3333154A1 (en) 2016-12-07 2018-06-13 Sandoz Ag Crystalline form of a selective 5-ht6 receptor antagonist
CN106632303A (zh) * 2017-01-09 2017-05-10 湖南华腾制药有限公司 一种6‑噻唑基吲哚衍生物的制备方法
US11339144B2 (en) 2017-04-10 2022-05-24 Navitor Pharmaceuticals, Inc. Heteroaryl Rheb inhibitors and uses thereof
BR112019001145A2 (pt) 2017-05-24 2019-04-30 H. Lundbeck A/S combinação de um antagonista do receptor 5-ht6 e de um inibidor de acetilcolinesterase para uso no tratamento da doença de alzheimer em uma subpopulação de pacientes portadores de alelos de apoe4
CA3185336A1 (en) * 2017-11-06 2019-05-09 Acelot, Inc. Small molecule drugs and related methods for treatment of diseases related to a.beta.42 oligomer formation
US20220185815A1 (en) 2019-03-06 2022-06-16 Daiichi Sankyo Company, Limited Pyrrolopyrazole derivative
CN109942527A (zh) * 2019-04-26 2019-06-28 新乡市润宇新材料科技有限公司 一种3-溴二苯并呋喃的合成方法
US20230219889A1 (en) 2020-05-19 2023-07-13 Cybin Irl Limited Deuterated tryptamine derivatives and methods of use
KR20230061473A (ko) * 2020-09-02 2023-05-08 인베릭 바이오사이언시스 캐나다 인크. 니트로화된 실로시빈 유도체 및 5-ht2a 수용체를 조절하고 정신 장애를 치료하기 위한 이의 용도
CN117500788A (zh) * 2021-03-02 2024-02-02 明德赛特制药公司 作为血清素能药物的用于治疗与之相关的疾病的吲哚衍生物
WO2022261240A2 (en) 2021-06-08 2022-12-15 ATAI Life Sciences AG Dimethoxyphenylalkylamine activators of serotonin receptors
CA3221823A1 (en) 2021-06-09 2022-12-15 Glenn Short Novel prodrugs and conjugates of dimethyltryptamine
WO2023044577A1 (en) * 2021-09-24 2023-03-30 Psygen Inc. Recovery method for tryptamines
WO2023129909A1 (en) 2021-12-27 2023-07-06 ATAI Life Sciences AG Aminotetraline activators of serotonin receptors
US20230357185A1 (en) 2022-03-18 2023-11-09 Enveric Biosciences Canada Inc. C4-carboxylic acid-substituted tryptamine derivatives and methods of using

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3597149A (en) * 1969-04-29 1971-08-03 Showa Denko Kk Inhibition of gas-fume fading of dyed cellulose acetate material
FR2181559A1 (en) 1972-04-28 1973-12-07 Aec Chimie Organique Bio N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity
JPS5764632A (en) 1980-10-09 1982-04-19 Mitsui Toatsu Chem Inc Novel 2-arylethyl ether derivative and thioether derivative, their production and insecticide and acaricide
US5202336A (en) * 1986-09-24 1993-04-13 Bayer Aktiengesellschaft Antiflammatory quinolin methoxy phenylsulphonamides
DE3632329A1 (de) 1986-09-24 1988-03-31 Bayer Ag Substituierte phenylsulfonamide
SE9103745D0 (sv) 1991-12-18 1991-12-18 Wikstroem Haakan Aryl-triflates and related compounds
DE69411143T2 (de) 1993-09-01 1998-10-22 Allelix Biopharma Tryptamin analoge mit 5-ht1d selektivität
US5504101A (en) 1994-05-06 1996-04-02 Allelix Biopharmaceuticals, Inc. 5-HT-1D receptor ligands
DK1032559T3 (da) 1997-09-29 2007-02-26 Aventis Pharma Inc Aminoalkylphenolderivater til behandling af depression og hukommelsessvigt
GB9820113D0 (en) * 1998-09-15 1998-11-11 Merck Sharp & Dohme Therapeutic agents
WO2000034242A1 (en) * 1998-12-11 2000-06-15 Virginia Commonwealth University Selective 5-ht6 receptor ligands
BR9916905A (pt) * 1999-01-13 2002-01-29 Millennium Pharm Inc Composto, composição farmacêutica, métodos para modular a atividade de um receptor de quimiocina, para prevenir infecção por hiv, tratar infecção por hiv, retardar o ìnicio de aids, ou tratar aids e para tratar uma doença inflamatória, e, combinação
US6750348B1 (en) 1999-03-24 2004-06-15 Anormed, Inc. Chemokine receptor binding heterocyclic compounds
US6187895B1 (en) * 1999-08-09 2001-02-13 General Electric Company Method for preparing polymers by solid state polymerization
AU2002303094B2 (en) * 2001-03-29 2006-11-23 Eli Lilly And Company N-(2-arylethyl)benzylamines as antagonists of the 5-HT6 receptor

Similar Documents

Publication Publication Date Title
JP2004532209A5 (ja)
NO20014479L (no) Fremgangsmåte ved behandling av spiseforstyrrelser
JP2003531118A5 (ja)
JP2002543183A5 (ja)
JP2002501049A5 (ja)
JP2005053931A5 (ja)
JP2007502806A5 (ja)
CZ305838B6 (cs) N-(2-arylethyl)benzylaminy jako antagonisté receptoru 5-HT6
JP2005523922A5 (ja)
JP2001526218A5 (ja)
EE200300403A (et) N-asendatud mittearomaatne heterotsükliline ühend, seda sisaldav ravimkompositsioon ning ühendi kasutamine ravimina
RU94036774A (ru) Ингибирование пролиферации клеток гладкой мускулатуры и рестеноза
JP2004509857A5 (ja)
DE60302157D1 (de) Opioidrezeptorantagonisten
JP2007502817A5 (ja)
JP2005511602A5 (ja)
JP2005529164A5 (ja)
JP2005507880A5 (ja)
JP2004525184A5 (ja)
JP2005510457A5 (ja)
JP2004523545A5 (ja)
JP2002514623A5 (ja)
WO2000056315A8 (en) Treatment of pain
DE60127535D1 (de) Vorbeugende oder therapeutische mittel gegen gastrische oder ösophageale regurgitation
JP2005513103A5 (ja)