EA200100671A1 - 2,3,4,4a-TETRAHYDRO-1H-PIRAZINO [1,2a] CHINOXALIN-5 (6H) -OH DERIVATIVES, AHONIST 5HT2C AGONISTS - Google Patents

2,3,4,4a-TETRAHYDRO-1H-PIRAZINO [1,2a] CHINOXALIN-5 (6H) -OH DERIVATIVES, AHONIST 5HT2C AGONISTS

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Publication number
EA200100671A1
EA200100671A1 EA200100671A EA200100671A EA200100671A1 EA 200100671 A1 EA200100671 A1 EA 200100671A1 EA 200100671 A EA200100671 A EA 200100671A EA 200100671 A EA200100671 A EA 200100671A EA 200100671 A1 EA200100671 A1 EA 200100671A1
Authority
EA
Eurasian Patent Office
Prior art keywords
carbon atoms
alkyl
represents hydrogen
disorders
aroyl
Prior art date
Application number
EA200100671A
Other languages
Russian (ru)
Inventor
Аннмари Луиз Сабб
Грегори Скотт Велмейкер
Джеймс Альберт Нельсон
Original Assignee
Американ Хоум Продактс Корпорейшн
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 Американ Хоум Продактс Корпорейшн filed Critical Американ Хоум Продактс Корпорейшн
Publication of EA200100671A1 publication Critical patent/EA200100671A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

Настоящее изобретение предлагает соединения формулы (I)в которой R представляет водород или алкил с 1-6 атомами углерода; R' представляет водород, алкил с 1-6 атомами углерода, ацил с 2-7 атомами углерода или ароил; R, R, Rи R, каждый независимо, представляет водород, алкил с 1-6 атомами углерода, алкокси с 1-6 атомами углерода, галоген, трифторалкил, -CN, алкилсульфонамид с 1-6 атомами углерода, алкиламид с 1-6 атомами углерода, амино, алкиламино с 1-6 атомами углерода, диалкиламино с 1-6 атомами углерода в алкильном фрагменте, трифторалкокси с 1-6 атомами углерода, ацил с 2-7 атомами углерода или ароил; X представляет CRRили карбонильную группу; Rи R, каждый независимо, представляет водород или алкил с 1-6 атомами углерода; или их фармацевтически приемлемые соли, при условии, что, по меньшей мере, один из R, R, Rи Rне является водородом, и их энантиомеры, которые являются агонистами 5HT-рецептора, полезными для лечения расстройств, связанных с центральной нервной системой, таких как обсессивно-компульсивные нарушения; депрессия; тревога; состояние паники; шизофрения; мигрень; расстройства сна; расстройства аппетита; ожирение; диабет типа II и эпилепсия.Международная заявка была опубликована вместе с отчетом о международном поиске.The present invention provides compounds of formula (I) in which R represents hydrogen or alkyl with 1-6 carbon atoms; R 'represents hydrogen, alkyl with 1-6 carbon atoms, acyl with 2-7 carbon atoms or aroyl; R, R, R and R each independently represents hydrogen, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, halogen, trifluoroalkyl, -CN, alkylsulfonamide with 1-6 carbon atoms, alkylamide with 1-6 atoms carbon, amino, alkylamino with 1-6 carbon atoms, dialkylamino with 1-6 carbon atoms in the alkyl moiety, trifluoroalkoxy with 1-6 carbon atoms, acyl with 2-7 carbon atoms or aroyl; X represents a CRR or carbonyl group; R1 and R4 each independently represents hydrogen or alkyl with 1-6 carbon atoms; or their pharmaceutically acceptable salts, provided that at least one of R, R, R and R is not hydrogen, and their enantiomers, which are 5HT receptor agonists, are useful for treating central nervous system disorders, such as obsessive-compulsive disorders; depression; anxiety; state of panic; schizophrenia; migraine; sleep disorders; appetite disorders; obesity; Type II diabetes and epilepsy. The international application was published along with an international search report.

EA200100671A 1998-12-17 1999-12-16 2,3,4,4a-TETRAHYDRO-1H-PIRAZINO [1,2a] CHINOXALIN-5 (6H) -OH DERIVATIVES, AHONIST 5HT2C AGONISTS EA200100671A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21347198A 1998-12-17 1998-12-17
PCT/US1999/029894 WO2000035922A1 (en) 1998-12-17 1999-12-16 2,3,4,4a-tetrahydro-1h-pyrazino(1,2-a)quinoxalin-5(6h)one derivates being 5ht2c agonists

Publications (1)

Publication Number Publication Date
EA200100671A1 true EA200100671A1 (en) 2001-12-24

Family

ID=22795247

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100671A EA200100671A1 (en) 1998-12-17 1999-12-16 2,3,4,4a-TETRAHYDRO-1H-PIRAZINO [1,2a] CHINOXALIN-5 (6H) -OH DERIVATIVES, AHONIST 5HT2C AGONISTS

Country Status (18)

Country Link
EP (1) EP1140940A1 (en)
JP (1) JP2002532504A (en)
KR (1) KR20010108025A (en)
CN (1) CN1240701C (en)
AR (1) AR022687A1 (en)
AU (1) AU3123400A (en)
BR (1) BR9916326A (en)
CA (1) CA2351385A1 (en)
CZ (1) CZ20012193A3 (en)
EA (1) EA200100671A1 (en)
HU (1) HUP0104773A3 (en)
IL (1) IL143323A0 (en)
NO (1) NO20013001L (en)
NZ (1) NZ512765A (en)
PL (1) PL348815A1 (en)
SK (1) SK8192001A3 (en)
WO (1) WO2000035922A1 (en)
ZA (1) ZA200104598B (en)

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HUP0104773A3 (en) 2004-10-28
CN1240701C (en) 2006-02-08
PL348815A1 (en) 2002-06-17
AU3123400A (en) 2000-07-03
JP2002532504A (en) 2002-10-02
WO2000035922A1 (en) 2000-06-22
SK8192001A3 (en) 2001-12-03
NO20013001D0 (en) 2001-06-15
ZA200104598B (en) 2002-09-05
KR20010108025A (en) 2001-12-07
IL143323A0 (en) 2002-04-21
CZ20012193A3 (en) 2001-12-12
CA2351385A1 (en) 2000-06-22
NZ512765A (en) 2003-10-31
NO20013001L (en) 2001-06-15
EP1140940A1 (en) 2001-10-10
CN1330652A (en) 2002-01-09
AR022687A1 (en) 2002-09-04
HUP0104773A2 (en) 2002-04-29
BR9916326A (en) 2001-10-02

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