HUP0203131A2 - Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0203131A2
HUP0203131A2 HU0203131A HUP0203131A HUP0203131A2 HU P0203131 A2 HUP0203131 A2 HU P0203131A2 HU 0203131 A HU0203131 A HU 0203131A HU P0203131 A HUP0203131 A HU P0203131A HU P0203131 A2 HUP0203131 A2 HU P0203131A2
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Hungary
Prior art keywords
alkyl
cycloalkyl
group
carbon atoms
nr8r9
Prior art date
Application number
HU0203131A
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English (en)
Inventor
Charles Blum
Philip Albert Carpino
James W. Darrow
Stephane De Lombaert
Mark Giangiordano
David Andrew Griffith
Jennifer Tran
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Neurogen Corporation
Pfizer Inc.
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Publication date
Application filed by Neurogen Corporation, Pfizer Inc. filed Critical Neurogen Corporation
Publication of HUP0203131A2 publication Critical patent/HUP0203131A2/hu
Publication of HUP0203131A3 publication Critical patent/HUP0203131A3/hu

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • G01N2333/575—Hormones
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    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70571—Assays involving receptors, cell surface antigens or cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor

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  • Otolaryngology (AREA)
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  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A találmány (I) általános képletű vegyületekre vonatkozik, amelyekképletében R1, R2, R3, R4, R5, R6 és X jelentése az alábbiakbanmegadott. E vegyületek szelektív NPY1 receptormodulátorok. Ezek avegyületek számos CNS rendellenesség, anyagcserezavarok, perifériásrendellenességek, különösen táplálkozási zavarok és magas vérnyomáskezelésére alkalmasak. A találmány tárgyát képezik továbbá az ilyenrendellenességek kezelésére szolgáló kezelési eljárások, valamintezeket tartalmazó gyógyszerkészítmények. X jelentése N vagy CHR14; R1jelentése hidrogénatom, 1-6 szénatomszámú alkil-, 3-10 szénatomszámúcikloalkil-, (3-10 szénatomszámú cikloalkil)-(1-6 szén<- >atomszámúalkil)-, 2-6 szénatomszámú alkenil, 2-6 szén<- >atomszámú alkinil-,ciano-, halo-, 1-6 szénatomszámú halo-alkil-, -OR7, -(1-6szénatomszámú alkil)-OR7, 1-6 szénatomszámú ciano-alkil-, -NR8R9, és -(1-6 szénatomszámú alkil)-NR8R9 közül választott csoport; R2 jelentésehidrogénatom, 1-6 szénatomszámú alkilcsoport, amely adott esetben az Avagy a B csoporttal 3-6 szénatomszámú amino-karbociklust vagy 2-5szénatomszámú amino-heterociklust képez, amelyek mindegyike adottesetben R7 csoporttal helyettesített, 3-10 szénatomszámú cikloalkil-vagy (3-10 szénatomszámú cikloalkil)-(1-6 szénatomszámú alkil)-csoport; vagy R2 és R6 együttesen azzal a két nitrogénatommal,amelyhez kapcsolódnak 2-5 szénatomszámú amino- heterociklust képez,amely adott esetben R7 csoporttal helyettesített; A jelentése (CH2)mcsoport, amelyben m értéke 1, 2 vagy 3 és mindegyik szénatom adottesetben 1-6 szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10 szénatomszámú ciklo-alkil)-(1-6 szénatomszámú alkil)-, 2-6szénatomszámú alkenil, 2-6 szénatomszámú alkinil-, ciano-, halo-, 1-6szénatom-számú halo-alkil-, -OR7, -(1-6 szénatomszámú alkil)-OR7, 1-6szénatomszámú ciano-alkil-, -NR8R9, vagy -(1-6 szénatomszámú alkil)-NR8R9 csoporttal helyettesített, B jelentése (CH2)m csoport, amelybenm értéke 1, 2 vagy 3 és mindegyik szénatom adott esetben 1-6szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10szénatomszámú ciklo-alkil)-<- >(1-6 szénatomszámú alkil)-, 2-6szénatomszámú alkenil, 2-6 szénatomszámú alkinil-, ciano-, halo-, 1-6szénatomszámú haloalkil-, -OR7, -(1-6 szénatomszámú alkil)-OR7, 1-6szénatomszámú ciano-alkil-, -NR8R9, vagy -(1-6 szénatomszámú alkil)-NR8R9 csoporttal helyettesített, R3 jelentése hidrogénatom, 1-6szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10szénatomszámú cikloalkil)-(1-6 szén<- >atomszámú alkil)-, 2-6szénatomszámú alkenilcsoport; R4 jelentése aril- vagyheteroarilcsoport, amely adott esetben 1-6 szénatomszámú alkil-, 3-10szénatomszámú cikloalkil-, (3-10 szénatomszámú cikloalkil)-(1-6szénatomszámú alkil)-, 2-6 szénatomszámú alkenil, 2-6 szénatomszámúalkinil-, halo-, 1-6 szénatomszámú halo-alkil-, tri
HU0203131A 1999-09-30 2000-09-29 Amino substituted pyrazolo[1,5-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines, pharmaceutical compositions containing them and their use HUP0203131A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15686899P 1999-09-30 1999-09-30
PCT/US2000/026885 WO2001023388A2 (en) 1999-09-30 2000-09-29 AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES

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HUP0203131A2 true HUP0203131A2 (hu) 2003-01-28
HUP0203131A3 HUP0203131A3 (en) 2004-06-28

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HU0203131A HUP0203131A3 (en) 1999-09-30 2000-09-29 Amino substituted pyrazolo[1,5-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines, pharmaceutical compositions containing them and their use

Country Status (21)

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US (1) US6476038B1 (hu)
EP (1) EP1218381B1 (hu)
JP (2) JP2003510326A (hu)
KR (1) KR20020047201A (hu)
CN (1) CN1377355A (hu)
AT (1) ATE347553T1 (hu)
AU (1) AU7737900A (hu)
BG (1) BG106507A (hu)
CA (1) CA2379633C (hu)
CZ (1) CZ20021089A3 (hu)
DE (1) DE60032249T2 (hu)
EA (1) EA200200421A1 (hu)
ES (1) ES2277855T3 (hu)
HU (1) HUP0203131A3 (hu)
IL (1) IL148904A0 (hu)
NO (1) NO20021357L (hu)
OA (1) OA12049A (hu)
PL (1) PL354982A1 (hu)
WO (1) WO2001023388A2 (hu)
YU (1) YU23602A (hu)
ZA (1) ZA200202517B (hu)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6472528B1 (en) * 1999-08-10 2002-10-29 Neurocrine Biosciences, Inc. Synthesis of substituted pyrazolopyrimidines
IL148905A0 (en) * 1999-09-30 2002-09-12 Neurogen Corp Pfizer Inc Certain alkylene diamine-substituted pyrazolo{1,5,-a}-1,5-pyrimidines and pyrazolo{1,5,-a}-1,3,5-triazines
WO2003076441A1 (en) 2002-03-07 2003-09-18 Smithkline Beecham Corporation Pyrazolopyrimidine and pyrazolotriazine derivatives and pharmaceutical compositions containing them
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
FR2842809A1 (fr) * 2002-07-26 2004-01-30 Greenpharma Sas NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
NZ540612A (en) 2003-01-14 2008-02-29 Arena Pharm Inc 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7329658B2 (en) * 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
US7176210B2 (en) * 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
AU2004257267B2 (en) 2003-07-14 2009-12-03 Arena Pharmaceuticals,Inc Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
AU2004274309B2 (en) 2003-09-22 2010-04-08 Msd K.K. Novel piperidine derivative
US7208596B2 (en) 2003-11-25 2007-04-24 Bristol-Myers Squibb Pharma Company Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof
US7153961B2 (en) 2003-11-25 2006-12-26 Bristol-Myers Squibb Pharma Co. Salt and crystalline form thereof of a corticotropin releasing factor receptor antagonist
CA2550948A1 (en) 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc. Crf receptor antagonists and methods relating thereto
EP1697369A1 (en) * 2003-12-22 2006-09-06 SB Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto
EP1734963A4 (en) 2004-04-02 2008-06-18 Merck & Co Inc METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER
GB0519957D0 (en) * 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
DK1814590T4 (da) 2004-11-01 2014-02-24 Amylin Pharmaceuticals Llc Behandling af obesitet og beslægtede sygdomme.
EP1836205B1 (en) * 2004-12-21 2009-06-10 Schering Corporation PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS
WO2007022123A2 (en) 2005-08-11 2007-02-22 Amylin Pharmaceuticals, Inc. Hybrid polypeptides with selectable properties
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
EP1892241B1 (en) 2005-05-30 2016-03-30 Msd K.K. Novel piperidine derivative
CA2612900C (en) 2005-06-23 2016-08-09 Claus Aagaard Improved tuberculosis vaccines
CA2618112A1 (en) 2005-08-10 2007-02-15 Banyu Pharmaceutical Co., Ltd. Pyridone compound
BRPI0614649A2 (pt) 2005-08-11 2011-04-12 Amylin Pharmaceuticals Inc polipeptìdeos hìbridos com propriedades selecionáveis
CA2619770A1 (en) 2005-08-24 2007-03-01 Banyu Pharmaceutical Co., Ltd. Phenylpyridone derivative
AU2006288153A1 (en) 2005-09-07 2007-03-15 Msd K.K. Bicyclic aromatic substituted pyridone derivative
US8293900B2 (en) 2005-09-29 2012-10-23 Merck Sharp & Dohme Corp Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
AU2006304836A1 (en) 2005-10-21 2007-04-26 Novartis Ag Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent
CA2627139A1 (en) 2005-10-27 2007-05-03 Banyu Pharmaceutical Co., Ltd. Novel benzoxathiin derivative
JP4371164B2 (ja) 2005-11-10 2009-11-25 萬有製薬株式会社 アザ置換スピロ誘導体
AU2007297481B2 (en) 2006-09-20 2012-03-08 Eli Lilly And Company Thiophene pyrazolopyrimidine compounds
DK2094709T3 (da) 2006-09-20 2010-12-06 Lilly Co Eli Thiazol-pyrazolopyrimidiner som CRF1-receptorantagonister
AU2007300627B2 (en) 2006-09-22 2012-02-16 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
JPWO2008038692A1 (ja) 2006-09-28 2010-01-28 萬有製薬株式会社 ジアリールケチミン誘導体
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US20100120694A1 (en) 2008-06-04 2010-05-13 Synergy Pharmaceuticals, Inc. Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders
CA3089569C (en) 2007-06-04 2023-12-05 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US20120029204A1 (en) * 2007-06-07 2012-02-02 Schering Corporation Synthesis of substituted-3-aminopyrazoles
US20110015181A1 (en) 2008-03-06 2011-01-20 Makoto Ando Alkylaminopyridine derivative
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
JPWO2009154132A1 (ja) 2008-06-19 2011-12-01 Ｍｓｄ株式会社 スピロジアミン−ジアリールケトオキシム誘導体
US20100015171A1 (en) 2008-07-15 2010-01-21 Statens Serum Institute Vaccines comprising tb 10.4
EP2321341B1 (en) 2008-07-16 2017-02-22 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
US20110124674A1 (en) 2008-07-30 2011-05-26 Hiroyuki Kishino 5/5-or 5/6-membered condensed ring cycloalkylamine derivative
EP2348857B1 (en) 2008-10-22 2016-02-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP5635991B2 (ja) 2008-10-30 2014-12-03 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． イソニコチンアミドオレキシン受容体アンタゴニスト
CA2741672A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US20110245209A1 (en) 2008-12-16 2011-10-06 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
US20110243940A1 (en) 2008-12-16 2011-10-06 Schering Corporation Bicyclic pyranone derivatives and methods of use thereof
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP2619198A1 (en) 2010-09-22 2013-07-31 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
MX348131B (es) 2011-02-25 2017-05-26 Merck Sharp & Dohme Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos.
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
MX2015001500A (es) 2012-08-02 2015-04-08 Merck Sharp & Dohme Compuestos antidiabeticos triciclicos.
CA2889919C (en) 2012-11-16 2021-08-17 University Health Network Pyrazolopyrimidine compounds
AU2014219020A1 (en) 2013-02-22 2015-07-23 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
JP2016514670A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド 他の薬物と組み合わせたグアニル酸シクラーゼ受容体アゴニスト
RS65632B1 (sr) 2013-06-05 2024-07-31 Bausch Health Ireland Ltd Ultra-prečišćeni agonisti guanilat-ciklaze c, postupak njihove pripreme i upotrebe
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
CA2959208C (en) 2014-08-29 2023-09-19 Tes Pharma S.R.L. Pyrimidine derivatives and their use as inhibitors of alpha-amino-beta-carboxymuconate-epsilon-semialdehyde decarboxylase
EP4445956A2 (en) 2015-01-06 2024-10-16 Arena Pharmaceuticals, Inc. Compound for use in treating conditions related to the s1p1 receptor
WO2016209809A1 (en) 2015-06-22 2016-12-29 Arena Pharmaceuticals, Inc. Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(compound1) for use in sipi receptor-associated disorders
KR102411150B1 (ko) 2016-08-31 2022-06-21 아지오스 파마슈티컬스 아이엔씨. 세포 대사 과정의 억제제
TWI767945B (zh) 2016-10-14 2022-06-21 義大利商Ｔｅｓ製藥（股份）責任有限公司 α-胺基-β-羧基己二烯二酸半醛去羧酶之抑制劑
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. ANTIDIABETIC HETEROCYCLIC COMPOUNDS
US10968232B2 (en) 2016-12-20 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
EP3628005A4 (en) 2017-08-14 2021-01-20 Spruce Biosciences, Inc. CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS
BR112020019277B1 (pt) * 2018-04-10 2024-01-16 Bayer Aktiengesellschaft Processo para produção de ácidos 2,6-dialquilfenil acéticos, e seus intermediários
MA54092A (fr) 2018-10-30 2021-09-08 Kronos Bio Inc Composés, compositions et procédés de modulation de l'activité de cdk9
SG11202104550WA (en) 2018-11-20 2021-05-28 Tes Pharma S R L INHIBITORS OF a-AMINO-ß-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
TW202045476A (zh) 2019-02-13 2020-12-16 美商默沙東藥廠 5-烷基吡咯啶食慾素受體促效劑
US20230018413A1 (en) 2019-08-08 2023-01-19 Merck Sharp & Dohme Corp. Heteroaryl pyrrolidine and piperidine orexin receptor agonists
WO2022036123A1 (en) 2020-08-12 2022-02-17 Spruce Biosciences, Inc. Methods and compositions for treating polycystic ovary syndrome
CN116249697A (zh) 2020-08-18 2023-06-09 默沙东有限责任公司 二环庚烷吡咯烷食欲素受体激动剂
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof
CN115304607B (zh) * 2022-07-06 2023-06-27 华南农业大学 吡唑并嘧啶衍生物的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU747708B2 (en) 1996-07-24 2002-05-23 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
AU7927498A (en) * 1997-08-05 1999-03-01 Pfizer Products Inc. 4-aminopyrrole(3,2-d) pyrimidines as neuropeptide y receptor antagonists
US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases

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