PE20030592A1 - Antagonista de nk1 - Google Patents

Antagonista de nk1

Info

Publication number
PE20030592A1
PE20030592A1 PE2002001095A PE2002001095A PE20030592A1 PE 20030592 A1 PE20030592 A1 PE 20030592A1 PE 2002001095 A PE2002001095 A PE 2002001095A PE 2002001095 A PE2002001095 A PE 2002001095A PE 20030592 A1 PE20030592 A1 PE 20030592A1
Authority
PE
Peru
Prior art keywords
alkyl
ch2f
cycloalkyl
cor12
chf2
Prior art date
Application number
PE2002001095A
Other languages
English (en)
Inventor
Gregory A Reichard
Sunil Paliwal
Neng-Yang Shih
Hon-Chung Tsui
Cheng Wang
Michelle Laci Wrobleski
Sapna Majmundar Shah
Dong Xiao
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of PE20030592A1 publication Critical patent/PE20030592A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
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    • A61P11/06—Antiasthmatics
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    • A61P11/14—Antitussive agents
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/38—2-Pyrrolones
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
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  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I DONDE Ar1 Y Ar2 SON R17-HETEROARILO, ARIL SUSTITUIDO CON R8, R9, R10; X1 ES O, S, SO, SO2, NR18, N(COR12)N(SO2R15); X2 ES C, S, SO, CUANDO X2 ES C; Y ES O, S, NR11; X2 ES S, SO, Y ES O; X1 ES SO, SO2, N(COR12), N(SOR15); R1 Y R2 SON H, ALQUILO, HIDROXI-ALQUILO, CICLOALQUILO, CH2F; O JUNTOS FORMAN ALQUILENO; SI X1 ES O, S, NR18a; R3 ES H, ALQUILO, HIDROXI-ALQUILO, CICLOALQUILO, CH2F, CF3, ENTRE OTROS; R7 ES H, ALQUILO; R6 Y R7 FORMAN CO; n2 ES 1-4; R4 Y R5 SON (CR28R29)n1-G, COCR28R29)n4-G; n1 ES 0-5; n4 ES 1-5; G ES H, CF3, CHF2, CH2F, OH, O-ALQUILO, ENTRE OTROS; R4 Y R5 FORMAN CO, NR12, ANILLO DE 4-7 MIEMBROS; X3 ES NR20, N(CONR13R14), ENTRE OTROS; R8, R9, R10 SON H, ALQUILO, CICLOALQUILO, OR18, HALOGENO, CN, NO2, CF3, CHF2, ENTRE OTROS. UN COMPUESTO PREFERIDO DE FORMULA II. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS UN INHIBIDOR SELECTIVO DE REABSORCION DE SEROTONINA (FLUOXETINA, FLUVOXAMINA, PAROXETINA, SERTRALINA), ANTAGONISTA DEL RECEPTOR 5HT3 DE SEROTONINA (PALONSETRON, ONDANSETRON, GRANISETRON). LOS COMPUESTOS SON ANTAGONISTAS DE NK1 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE EMESIS, NAUSEAS, DEPRESION, ANSIEDAD, TOS
PE2002001095A 2001-11-13 2002-11-12 Antagonista de nk1 PE20030592A1 (es)

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US33765201P 2001-11-13 2001-11-13

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PE20030592A1 true PE20030592A1 (es) 2003-07-07

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Country Status (14)

Country Link
US (1) US7122677B2 (es)
EP (1) EP1451153B1 (es)
JP (2) JP4459621B2 (es)
CN (1) CN100509782C (es)
AR (1) AR038002A1 (es)
AT (1) ATE374183T1 (es)
CA (1) CA2466465A1 (es)
DE (1) DE60222693T2 (es)
ES (1) ES2291538T3 (es)
HK (1) HK1063791A1 (es)
MX (1) MXPA04004477A (es)
PE (1) PE20030592A1 (es)
TW (1) TW200300347A (es)
WO (1) WO2003042173A1 (es)

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PE20030762A1 (es) * 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
GB0308968D0 (en) * 2003-04-17 2003-05-28 Glaxo Group Ltd Medicaments
EP1750862B1 (en) 2004-06-04 2011-01-05 Teva Pharmaceutical Industries Ltd. Pharmaceutical composition containing irbesartan
SG187416A1 (en) * 2004-07-01 2013-02-28 Opko Health Inc Piperidine derivatives as nk1 antagonists
AU2012216435B8 (en) * 2004-07-01 2015-02-19 Opko Health, Inc. Piperidine derivatives as NK1 antagonists
CN101316816B (zh) * 2005-12-01 2011-07-27 弗·哈夫曼-拉罗切有限公司 5-羟色胺转运体(sert)抑制剂
SG10201500028RA (en) 2006-04-05 2015-02-27 Opko Health Inc Pharmaceutical formulations: salts of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
AR066191A1 (es) 2007-03-22 2009-08-05 Schering Corp Proceso e intermediarios para la sintesis de compuestos 8- [ ( 1- (3,5- bis- ( trifluorometil) fenil) - etoxi ) - metil]- 8 fenil - 1,7- diaza - espiro (4, 5) decan -2 ona
PL2346823T3 (pl) * 2008-09-05 2016-01-29 Opko Health Inc Związki pośrednie w syntezie związków 8-[{1-(3,5-bis-(trifluorometylo)fenylo)etoksy}metylo]-8-fenylo-1,7-diaza-spiro[4.5]dekan-2-onu
JP5860399B2 (ja) 2009-08-14 2016-02-16 オプコ ヘルス， インコーポレイテッド ニューロキニン−１アンタゴニストの静脈内用製剤
CA2834164A1 (en) 2011-05-10 2012-11-15 Gilead Sciences, Inc. Fused benzoxazinones as ion channel modulators
NO3175985T3 (es) 2011-07-01 2018-04-28
TWI478908B (zh) 2011-07-01 2015-04-01 Gilead Sciences Inc 作為離子通道調節劑之稠合雜環化合物
PL3104847T3 (pl) * 2014-02-07 2021-07-05 Támogatott Kutatócsoportok Irodája Nowe zastosowanie związków agonistycznych receptora sigma-1
CN105367510B (zh) * 2015-11-02 2017-07-21 叶海伟 一种(2R，4S)‑3‑Cbz‑2，4‑二苯基‑1，3‑恶唑烷‑5‑酮的制备方法
CN106967000B (zh) * 2017-04-19 2021-02-02 成都百特万合医药科技有限公司 用于防治肿瘤化疗的医药中间体的制备方法

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WO2003042173A8 (en) 2003-10-02
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CN100509782C (zh) 2009-07-08
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ATE374183T1 (de) 2007-10-15
ES2291538T3 (es) 2008-03-01
JP2010090163A (ja) 2010-04-22
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