IL149111A0 - Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors - Google Patents
Small molecule modulators of non-endogenous, constitutively activated human serotonin receptorsInfo
- Publication number
- IL149111A0 IL149111A0 IL14911100A IL14911100A IL149111A0 IL 149111 A0 IL149111 A0 IL 149111A0 IL 14911100 A IL14911100 A IL 14911100A IL 14911100 A IL14911100 A IL 14911100A IL 149111 A0 IL149111 A0 IL 149111A0
- Authority
- IL
- Israel
- Prior art keywords
- endogenous
- small molecule
- activated human
- constitutively activated
- serotonin receptors
- Prior art date
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)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Cell Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Zoology (AREA)
- Toxicology (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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 |
---|---|
IL149111A0 true IL149111A0 (en) | 2002-11-10 |
Family
ID=23659316
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IL14911100A IL149111A0 (en) | 1999-10-15 | 2000-10-13 | Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors |
Country Status (8)
Country | Link |
---|---|
US (1) | US6150393A (xx) |
EP (1) | EP1244632A1 (xx) |
CN (1) | CN1411448A (xx) |
AU (1) | AU1201001A (xx) |
CA (1) | CA2387031A1 (xx) |
IL (1) | IL149111A0 (xx) |
MX (1) | MXPA02003792A (xx) |
WO (1) | WO2001029008A1 (xx) |
Families Citing this family (55)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5891646A (en) * | 1997-06-05 | 1999-04-06 | Duke University | Methods of assaying receptor activity and constructs useful in such methods |
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 |
MXPA02008770A (es) * | 2000-03-06 | 2004-09-10 | Acadia Pharm Inc | Compuestos azaciclicos para uso en el tratamiento de enfermedades relacionadas con la serotonina. |
JP2003532057A (ja) * | 2000-04-07 | 2003-10-28 | 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 | 非内因性の、構成的に活性化される既知gタンパク質−共役受容体 |
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 |
US20050136431A1 (en) * | 2000-11-03 | 2005-06-23 | Oakley Robert H. | 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 |
MXPA04006280A (es) | 2001-12-28 | 2004-09-27 | Acadia Pharm Inc | Compuestos espiroazaciclicos como moduladores de receptor de monoamina. |
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 |
CA2490397A1 (en) * | 2002-06-24 | 2003-12-31 | 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 |
US7538222B2 (en) * | 2002-06-24 | 2009-05-26 | Acadia Pharmaceuticals, Inc. | 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 |
WO2004064738A2 (en) * | 2003-01-16 | 2004-08-05 | Acadia Pharmaceuticals Inc. | Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases |
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 |
DE10315571A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Pyrazolverbindungen |
DE10315573A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
PT1558582E (pt) * | 2003-07-22 | 2006-05-31 | Arena Pharm Inc | Derivados de diaril- e aril-heteroaril-ureia como moduladores do receptor de serotonina 5-ht2a uteis para a profilaxia e tratamento de desordens relacionadas com o mesmo |
EP1695966A1 (en) * | 2003-07-22 | 2006-08-30 | Arena Pharmaceuticals, Inc. | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto |
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 |
AU2004279438A1 (en) * | 2003-10-09 | 2005-04-21 | Inverseon, Inc. | Methods for treating diseases and conditions with inverse agonists |
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 |
ATE548353T1 (de) * | 2004-03-23 | 2012-03-15 | Arena Pharm Inc | Verfahren zur herstellung von substituierte n- aryl-n'-ä3-(1h-pyrazol-5-yl)phenylü-harnstoffe and intermediate davon. |
US20050261278A1 (en) | 2004-05-21 | 2005-11-24 | Weiner David M | Selective serotonin receptor inverse agonists as therapeutics for disease |
US7820695B2 (en) * | 2004-05-21 | 2010-10-26 | Acadia Pharmaceuticals, Inc. | Selective serotonin receptor inverse agonists as therapeutics for disease |
AU2005289635A1 (en) * | 2004-09-27 | 2006-04-06 | Acadia Pharmaceuticals Inc. | Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-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 |
WO2006078610A1 (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 |
CA2646081C (en) | 2006-05-18 | 2017-06-27 | Arena Pharmaceuticals, Inc. | Crystalline forms and processes for the preparation of phenyl-pyrazoles useful as modulators of the 5-ht2a serotonin receptor |
USRE45337E1 (en) | 2006-05-18 | 2015-01-13 | Arena Pharmaceuticals, Inc. | Ethers, secondary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto |
USRE45336E1 (en) | 2006-05-18 | 2015-01-13 | Arena Pharmaceuticals, Inc. | Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto |
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 |
US20090053329A1 (en) | 2007-03-19 | 2009-02-26 | Acadia Pharmaceuticals, Inc. | Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics |
ES2421237T7 (es) | 2007-08-15 | 2013-09-30 | Arena Pharmaceuticals, Inc. | Derivados de imidazo[1,2-a]piridin como moduladores del receptor serotoninérgico 5ht2a en el tratamiento de trastornos relacionados con el mismo |
DK2200610T3 (en) * | 2007-09-21 | 2018-04-23 | Acadia Pharm Inc | 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 |
US9126946B2 (en) | 2008-10-28 | 2015-09-08 | 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 |
PT2364142T (pt) | 2008-10-28 | 2018-04-23 | Arena Pharm Inc | Composições de um modulador do recetor da serotonina 5-ht2a para o tratamento de distúrbios com ele relacionados |
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 |
US9611292B2 (en) * | 2011-04-27 | 2017-04-04 | The Board Of Regents Of The University Of Texas System | Peptide inhibitors of serotonin 5-HT2c receptors:PTEN interaction |
RU2017145976A (ru) | 2015-06-12 | 2019-07-15 | Аксовант Сайенсиз Гмбх | Производные диарил- и арилгетероарилмочевины, применимые для профилактики и лечения нарушения поведения во время REM-фазы сна |
KR20180064373A (ko) | 2015-07-15 | 2018-06-14 | 엑소반트 사이언시즈 게엠베하 | 신경퇴행성 질환과 관련된 환각의 예방 및 치료에 유용한 5-ht2a 세로토닌 수용체의 조절자로서의 다이아릴 및 아릴헤테로아릴 우레아 유도체 |
PT3325444T (pt) | 2015-07-20 | 2021-09-22 | Acadia Pharm Inc | Métodos para preparar n-(4-fluorobenzil)-n-(1-metilpiperidina-4-il)-n'-(4-(2-metilpropiloxi)fenilmetil)carbamida e o seu sal de tartarato e forma polimórfica c |
WO2017165635A1 (en) | 2016-03-25 | 2017-09-28 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome p450 modulators |
US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
EP3558311A1 (en) | 2016-12-20 | 2019-10-30 | Acadia Pharmaceuticals Inc. | Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis |
EP3615028A1 (en) | 2017-04-28 | 2020-03-04 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating impulse control disorder |
US20210077479A1 (en) | 2017-08-30 | 2021-03-18 | Acadia Pharmaceuticals Inc. | Formulations of pimavanserin |
Family Cites Families (6)
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 |
ES2151652T3 (es) * | 1995-02-02 | 2001-01-01 | Smithkline Beecham Plc | Derivados de indol como antagonistas del receptor 5ht. |
CA2325559A1 (en) * | 1998-04-14 | 1999-10-21 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof |
-
1999
- 1999-10-15 US US09/418,721 patent/US6150393A/en not_active Expired - Lifetime
-
2000
- 2000-10-13 CA CA002387031A patent/CA2387031A1/en not_active Abandoned
- 2000-10-13 AU AU12010/01A patent/AU1201001A/en not_active Abandoned
- 2000-10-13 IL IL14911100A patent/IL149111A0/xx unknown
- 2000-10-13 WO PCT/US2000/028347 patent/WO2001029008A1/en not_active Application Discontinuation
- 2000-10-13 EP EP00973507A patent/EP1244632A1/en not_active Withdrawn
- 2000-10-13 CN CN00817253A patent/CN1411448A/zh active Pending
- 2000-10-13 MX MXPA02003792A patent/MXPA02003792A/es unknown
Also Published As
Publication number | Publication date |
---|---|
CA2387031A1 (en) | 2001-04-26 |
EP1244632A1 (en) | 2002-10-02 |
MXPA02003792A (es) | 2004-09-06 |
CN1411448A (zh) | 2003-04-16 |
US6150393A (en) | 2000-11-21 |
AU1201001A (en) | 2001-04-30 |
WO2001029008A1 (en) | 2001-04-26 |
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