MXPA02003792A - Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados. - Google Patents

Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados.

Info

Publication number
MXPA02003792A
MXPA02003792A MXPA02003792A MXPA02003792A MXPA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A MX PA02003792 A MXPA02003792 A MX PA02003792A
Authority
MX
Mexico
Prior art keywords
receptors
pyrazole derivatives
serotonin receptors
candidate compounds
human serotonin
Prior art date
Application number
MXPA02003792A
Other languages
English (en)
Inventor
J Thomsen William
Original Assignee
Arena Pharm Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Arena Pharm Inc filed Critical Arena Pharm Inc
Publication of MXPA02003792A publication Critical patent/MXPA02003792A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70571—Receptors; Cell surface antigens; Cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

En la presente invencion se describen formas activadas constitutivamente no endogenas de los receptores 5HT2A humano y 5HT2c humano y usos de dichos receptores para seleccionar compuestos candidato. Ademas se describen los compuestos candidatos identificados por los metodos de seleccion que actuan en los receptores 5HT2A. Ademas se describe una nueva clase de compuestos (I) los cuales actuan en los receptores 5HT2A. Esta nueva clase comprende los compuestos candidato. En la formula (A) W es F, CI, Br, I, alquilo C1-8 de cadena recta o ramificada, cicloalquilo C3-8, alquilcicloalquilo C4-9 o alquenilo C2-8 ; X es O o S o NR2; Y es NR3R4, o (CH2)mR5 u O(CH 2)nR6; M es un entero entre 0 y 4, inclusive; N es un entero entre 0 y 4 inclusive; Z es H, alquilo C1-8 de cadena recta o ramificada, cicloalquilo C3-8 alquilcicloalquilo C4-9 o alquenilo C2-8; R1, R2, R3 y R10 son tal como se definen en la solicitud.
MXPA02003792A 1999-10-15 2000-10-13 Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados. MXPA02003792A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/418,721 US6150393A (en) 1998-12-18 1999-10-15 Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
PCT/US2000/028347 WO2001029008A1 (en) 1999-10-15 2000-10-13 Pyrazole derivatives which modulate human serotonin receptors

Publications (1)

Publication Number Publication Date
MXPA02003792A true MXPA02003792A (es) 2004-09-06

Family

ID=23659316

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA02003792A MXPA02003792A (es) 1999-10-15 2000-10-13 Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados.

Country Status (8)

Country Link
US (1) US6150393A (es)
EP (1) EP1244632A1 (es)
CN (1) CN1411448A (es)
AU (1) AU1201001A (es)
CA (1) CA2387031A1 (es)
IL (1) IL149111A0 (es)
MX (1) MXPA02003792A (es)
WO (1) WO2001029008A1 (es)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7541151B2 (en) 1997-06-05 2009-06-02 Duke University Single-cell biosensor for the measurement of GPCR ligands in a test sample
US6528271B1 (en) * 1997-06-05 2003-03-04 Duke University Inhibition of βarrestin mediated effects prolongs and potentiates opioid receptor-mediated analgesia
US5891646A (en) * 1997-06-05 1999-04-06 Duke University Methods of assaying receptor activity and constructs useful in such methods
AU780006B2 (en) * 2000-03-06 2005-02-24 Acadia Pharmaceuticals, Inc. Azacyclic compounds for use in the treatment of serotonin related diseases
IL152136A0 (en) * 2000-04-07 2003-05-29 Arena Pharm Inc Non-endogenous, constitutively activated known g protein-coupled receptors
US20050136431A1 (en) * 2000-11-03 2005-06-23 Oakley Robert H. Methods of screening compositions for G protein-coupled receptor desensitization inhibitory activity
US7018812B2 (en) 2000-11-03 2006-03-28 Duke University Modified G-protein coupled receptors
US7163800B2 (en) * 2000-11-03 2007-01-16 Molecular Devices Corporation Methods of screening compositions for G protein-coupled receptor desensitization inhibitory activity
US7279324B2 (en) * 2001-01-23 2007-10-09 Duke University Nucleic acid encoding G-protein coupled receptor with modified DRY motif
JP3929250B2 (ja) * 2001-03-08 2007-06-13 株式会社ルネサステクノロジ 半導体装置
KR100974901B1 (ko) * 2001-12-28 2010-08-10 아카디아 파마슈티칼스 인코포레이티드 모노아민 수용체 조정자로서의 스피로아자사이클릭 화합물
GB0210597D0 (en) * 2002-01-23 2002-06-19 Aventis Pharma Inc A nucleic acid encoding a G-protein-coupled receptor,and uses thereof
US20030182669A1 (en) * 2002-03-19 2003-09-25 Rockman Howard A. Phosphoinositide 3-kinase mediated inhibition of GPCRs
RU2320646C2 (ru) * 2002-06-24 2008-03-27 Акадиа Фармасьютикалз Инк. N-замещенные производные пиперидина в качестве агентов серотонинового рецептора
US7538222B2 (en) * 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
US7253186B2 (en) * 2002-06-24 2007-08-07 Carl-Magnus Andersson N-substituted piperidine derivatives as serotonin receptor agents
MY139563A (en) * 2002-09-04 2009-10-30 Bristol Myers Squibb Co Heterocyclic aromatic compounds useful as growth hormone secretagogues
CN1816524B (zh) 2003-01-16 2012-06-27 阿卡蒂亚药品公司 用于神经退行性疾病的治疗的选择性五羟色胺2a/2c受体反向激动剂
DE10315573A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
DE10315571A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
DE10315572A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
DE10315569A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
SI1558582T1 (sl) * 2003-07-22 2006-06-30 Arena Pharm Inc Diaril in arilheteroaril secninski derivati kot modulatorji 5-HT2A serotoninskega receptorja, koristnega za profilakso in zdravljenje motenj, ki so znjim povezane
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
EP1663972A1 (en) * 2003-09-03 2006-06-07 Galapagos N.V. The claimed invention relates to novel 4-piperidinecarboxamide and the use thereof for the preparation of medicaments against 5-ht2a receptor-related disorders
US20070276024A1 (en) * 2003-10-09 2007-11-29 Inverseon , Inc. Methods for Treating Diseases and Conditions with Inverse Agonists and for Screening for Agents Acting as Inverse Agonists
EP1684764A2 (en) * 2003-10-09 2006-08-02 Inverseon, Inc. Methods for treating diseases and conditions with inverse agonists and for screening for agents acting as inverse agonists
CA2559038C (en) * 2004-03-23 2013-09-10 Arena Pharmaceuticals, Inc. Processes for preparing substituted n-aryl-n'-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof
US7820695B2 (en) * 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
US20050261278A1 (en) * 2004-05-21 2005-11-24 Weiner David M Selective serotonin receptor inverse agonists as therapeutics for disease
US7868176B2 (en) * 2004-09-27 2011-01-11 Acadia Pharmaceuticals, Inc. Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-y1)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation
US7790899B2 (en) * 2004-09-27 2010-09-07 Acadia Pharmaceuticals, Inc. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
US7528175B2 (en) * 2004-10-08 2009-05-05 Inverseon, Inc. Method of treating airway diseases with beta-adrenergic inverse agonists
SA05260357B1 (ar) 2004-11-19 2008-09-08 ارينا فارماسيتو تيكالز ، أنك مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به
CA2594563A1 (en) * 2005-01-19 2006-07-27 Arena Pharmaceuticals, Inc. Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis or treatment of progressive multifocal leukoencephalopathy
JP5389642B2 (ja) 2006-05-18 2014-01-15 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 ５−ｈｔ２ａセロトニンレセプターに関連する障害の処置に有用な５−ｈｔ２ａセロトニンレセプターのモジュレーターとしての３−ピラゾリル−ベンズアミド−４−エーテル、二級アミンおよびその誘導体
SG171681A1 (en) 2006-05-18 2011-06-29 Arena Pharm Inc Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor
ES2536762T3 (es) 2006-05-18 2015-05-28 Arena Pharmaceuticals, Inc. Aminas primarias y sus derivados como moduladores del receptor de la serotonina 5-HT2A útiles para el tratamiento de trastornos relacionados con este
TWI415845B (zh) * 2006-10-03 2013-11-21 Arena Pharm Inc 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物
CA2681506C (en) 2007-03-19 2016-05-24 Perry Peters Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics
JP5393677B2 (ja) 2007-08-15 2014-01-22 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 ５−ＨＴ２Ａセロトニン受容体に関連した障害の治療のための５−ＨＴ２Ａセロトニン受容体のモジュレーターとしてのイミダゾ［１，２−ａ］ピリジン誘導体
EP2200610B1 (en) * 2007-09-21 2018-01-10 Acadia Pharmaceuticals Inc. Co-administration of pimavanserin with other agents
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
US9034911B2 (en) 2008-10-28 2015-05-19 Arena Pharmaceuticals, Inc. Composition of a 5-HT2A serotonin receptor modulator useful for the treatment of disorders related thereto
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
WO2011075596A1 (en) 2009-12-18 2011-06-23 Arena Pharmaceuticals, Inc. Crystalline forms of certain 3-phenyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
WO2012149481A1 (en) * 2011-04-27 2012-11-01 The Board Of Regents On The University Of Texas System Novel peptide inhibitors of serotonin 5-ht2c receptor:pten interaction
CA2989343A1 (en) 2015-06-12 2016-12-15 Yandong Wen Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of rem sleep behavior disorder
BR112018000728A2 (pt) 2015-07-15 2018-09-04 Axovant Sciences Gmbh resumo método para a profilaxia e/ou tratamento de alucinações visuais em um sujeito com necessidade do mesmo
US10597363B2 (en) 2015-07-20 2020-03-24 Acadia Pharmaceuticals Inc. Methods for preparing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form C
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
WO2018118626A1 (en) 2016-12-20 2018-06-28 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
WO2018200977A1 (en) 2017-04-28 2018-11-01 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. PIMAVANSERIN FORMULATIONS

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4985352A (en) * 1988-02-29 1991-01-15 The Trustees Of Columbia University In The City Of New York DNA encoding serotonin 1C (5HT1c) receptor, isolated 5HT1c receptor, mammalian cells expressing same and uses thereof
US5661024A (en) * 1989-10-31 1997-08-26 Synaptic Pharmaceutical Corporation DNA encoding a human serotonic (5-HT2) receptor and uses thereof
JPH04124178A (ja) * 1990-09-12 1992-04-24 Sds Biotech Kk 複素環式化合物および該化合物を含有する除草剤
CA2135253A1 (en) * 1994-11-07 1996-05-08 Michael Dennis Compound screening based on a window of chemical-messenger-independent activity
CA2212061A1 (en) * 1995-02-02 1996-08-08 Laramie Mary Gaster Indole derivatives as 5-ht receptor antagonist
JP2003514763A (ja) * 1998-04-14 2003-04-22 アリーナ・フアーマシユーチカルズ・インコーポレーテツド 非内在性の構成的に活性化されるヒトセロトニンレセプターおよびその小分子調節物質

Also Published As

Publication number Publication date
WO2001029008A1 (en) 2001-04-26
IL149111A0 (en) 2002-11-10
US6150393A (en) 2000-11-21
AU1201001A (en) 2001-04-30
CA2387031A1 (en) 2001-04-26
CN1411448A (zh) 2003-04-16
EP1244632A1 (en) 2002-10-02

Similar Documents

Publication Publication Date Title
MXPA02003792A (es) Moduladores de molecula pequena de receptores de serotonina endogenos constitutivamente activados.
MXPA05010652A (es) Pirazoles sustituidos.
MXPA00010060A (es) Receptores de serotonina humana constitutivamente activados, no endogenos y moduladores de molecula pequenos de los mismos.
HUP9802859A2 (hu) Acil-amino-szalicilsav-amid-származékok és alkalmazásuk peszticidként
IL135536A0 (en) Ortho-anthranilamide derivatives and pharmaceutical compositions containing the same
AR002986A1 (es) Nuevos derivados de piperazina sustituida particularmente utiles como antagonistas de receptores de taquiquinina, composiciones farmaceuticas, usosde dichos derivados y procedimiento de preparacion de los mismos.
MXPA02011370A (es) Iminoazinas substituidas.
EA200200510A1 (ru) 4-карбоксиамино-2-этил-1,2,3,4-тетрагидрохинолин в кристаллической форме как ингибитор сетр
DE69413393D1 (de) In 15-stellung substituierte 4-azasteroide
EA200200731A1 (ru) Производные фенилпиперазинила
HUP0100160A2 (hu) Módosított cellulóz-éterek, előállításuk, valamint e vegyületeket tartalmazó kompozíciók
HUP0003484A2 (hu) Pirrolidin-3-karbonsav-származékok és alkalmazásuk endotelin antagonistaként
MXPA06001094A (es) Compuestos quimicos.
BG105710A (en) 5ht1 antagonists for antidepressant therapy
EA200000910A1 (ru) Азабициклические лиганды рецепторов 5нт1
EA200300044A1 (ru) Новые замещенные фталиды, способ их получения и содержащие их фармацевтические композиции
EA200301317A1 (ru) Производные аминохинолина и его применение в качестве лигандов аденозина a3
MXPA05010651A (es) Compuestos de pirazol.
ATE244712T1 (de) Piperazino-derivative als neurokininantagonisten
FI962261A0 (fi) N-bis- tai N-tris-((1,2-dikarboksyyli-etoksi)-etyyN-bis- tai N-tris-((1,2-dikarboksyyli-etoksi)-etyyli)amiinijohdannaiset, niiden valmistus ja käyttö li)amiinijohdannaiset, niiden valmistus ja käyttö
MXPA04006113A (es) Derivados de triazoloquinolina utiles como ligandos receptores de adenosina.
MXPA05010650A (es) Pirazoles sustituidos.
EA200200727A1 (ru) Новые производные индола
MY132969A (en) New n-phenylamide and n-pyridylamide derivatives, method of preparing them and pharmaceutical compositions containing them
NO20002600D0 (no) Mellomprodukter og fremgangsmÕter for anvendelse ved semisyntesen av paclitaxel og analoger