IL102337A - Aryl-pyrrolo (1,2-a) pyrazines their manufacture and pharmaceutical compositions containing them - Google Patents

Aryl-pyrrolo (1,2-a) pyrazines their manufacture and pharmaceutical compositions containing them

Info

Publication number
IL102337A
IL102337A IL10233792A IL10233792A IL102337A IL 102337 A IL102337 A IL 102337A IL 10233792 A IL10233792 A IL 10233792A IL 10233792 A IL10233792 A IL 10233792A IL 102337 A IL102337 A IL 102337A
Authority
IL
Israel
Prior art keywords
solution
formula
methylene chloride
treated
mixture
Prior art date
Application number
IL10233792A
Other languages
English (en)
Other versions
IL102337A0 (en
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of IL102337A0 publication Critical patent/IL102337A0/xx
Publication of IL102337A publication Critical patent/IL102337A/en

Links

Classifications

    • 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
    • C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to 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
    • C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/333—Radicals substituted by oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/60—Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/40—Radicals substituted by oxygen atoms
    • C07D307/46—Doubly bound oxygen atoms, or two oxygen atoms singly bound to the same carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
IL10233792A 1991-07-02 1992-06-26 Aryl-pyrrolo (1,2-a) pyrazines their manufacture and pharmaceutical compositions containing them IL102337A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH195091 1991-07-02
CH166792 1992-05-22

Publications (2)

Publication Number Publication Date
IL102337A0 IL102337A0 (en) 1993-01-14
IL102337A true IL102337A (en) 1996-01-31

Family

ID=25688329

Family Applications (1)

Application Number Title Priority Date Filing Date
IL10233792A IL102337A (en) 1991-07-02 1992-06-26 Aryl-pyrrolo (1,2-a) pyrazines their manufacture and pharmaceutical compositions containing them

Country Status (14)

Country Link
US (1) US5292732A (is")
EP (1) EP0521368A1 (is")
JP (1) JPH0774217B2 (is")
CN (1) CN1030986C (is")
AU (1) AU654362B2 (is")
CA (1) CA2072836A1 (is")
CS (1) CS202292A3 (is")
FI (1) FI100242B (is")
HU (1) HUT70163A (is")
IE (1) IE922152A1 (is")
IL (1) IL102337A (is")
NO (1) NO922604L (is")
NZ (1) NZ243310A (is")
TW (1) TW224974B (is")

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0572863A1 (de) * 1992-06-05 1993-12-08 F. Hoffmann-La Roche Ag ZNS Pyrazinoindole
US5378846A (en) * 1993-06-11 1995-01-03 Russian-American Institute For New Drug Development 1,2,3,4-tetrahydropyrrolo-[1,2-a]-pyrazine derivatives
US5352096A (en) * 1993-09-27 1994-10-04 Chi Wen Chen Air compressor for automobiles
TW334423B (en) * 1993-10-22 1998-06-21 Hoffmann La Roche Tricyclic 1-aminoethylpyrrole-derivatives
UA66370C2 (en) 1997-12-16 2004-05-17 Lilly Co Eli Arylpiperazines having activity to setotonin 1 receptors
IL143958A0 (en) 1998-12-25 2002-04-21 Shionogi & Co Heteroaromatic derivatives having an inhibitory activity against hiv integrase
JP2007501863A (ja) * 2003-06-12 2007-02-01 メルク　エンド　カムパニー　インコーポレーテッド 有糸分裂キネシン阻害剤
EP1741709A1 (en) 2005-06-28 2007-01-10 Sanofi-Aventis Deutschland GmbH Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals
DE102006049452A1 (de) * 2006-10-17 2008-05-08 Grünenthal GmbH Substituierte Tetrahydropyrolopiperazin-Verbindungen und deren Verwendung in Arzneimitteln
NZ603427A (en) 2010-06-09 2013-08-30 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
MY170715A (en) 2010-12-22 2019-08-27 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace)
PH12013501807A1 (en) 2011-03-01 2015-09-30 Janssen Pharmaceutica Nv 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace)
MY163346A (en) 2011-03-09 2017-09-15 Janssen Pharmaceutica Nv 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (base)
EA201591175A1 (ru) * 2012-12-19 2015-11-30 Новартис Аг Трициклические соединения в качестве ингибиторов cftr
ES2697684T3 (es) 2013-06-12 2019-01-25 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)
KR102243135B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진-3(2h)-온 유도체
AU2014280125B2 (en) 2013-06-12 2018-03-15 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE)
KR20170095881A (ko) 2014-12-18 2017-08-23 얀센 파마슈티카 엔.브이. 베타―세크레타제의 ２,３,４,５―테트라히드로피리딘―６―아민 및 ３,４―디히드로―２ｈ―피롤―５―아민 화합물 억제제
BR112019018051A2 (pt) 2017-04-12 2020-04-07 Hoffmann La Roche método para produzir um composto, composto e substância

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1185080A (en) * 1967-12-07 1970-03-18 Beecham Group Ltd Pyrrolidines
US3906010A (en) * 1974-06-17 1975-09-16 Morton Norwich Products Inc Series of 5-aryl-2-furamidines
US3931247A (en) * 1974-12-11 1976-01-06 Morton-Norwich Products, Inc. 5-(Substituted)phenylfurfuryl alcohols
JPS5811878B2 (ja) * 1974-12-19 1983-03-04 大正製薬株式会社 フロ （ ３ ２−ｂ ） インド−ルルイノ セイホウ
US4188389A (en) * 1978-11-03 1980-02-12 Ayerst Mckenna & Harrison, Inc. 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines
JPS5852995B2 (ja) * 1981-09-28 1983-11-26 武田薬品工業株式会社 フルフラ−ル誘導体の製造法
US4882354A (en) * 1987-12-16 1989-11-21 Norwich Eaton Pharmaceuticals, Inc. N-hydroxy-5-phenyl-2-furancarboximidamides useful as cardiotonic agents

Also Published As

Publication number Publication date
CS202292A3 (en) 1993-01-13
HU9202139D0 (en) 1992-10-28
FI923073A0 (fi) 1992-07-02
EP0521368A1 (de) 1993-01-07
NO922604L (no) 1993-01-04
NO922604D0 (no) 1992-07-01
TW224974B (is") 1994-06-11
HUT70163A (en) 1995-09-28
AU654362B2 (en) 1994-11-03
CN1068328A (zh) 1993-01-27
FI923073A7 (fi) 1993-01-03
IE922152A1 (en) 1993-01-13
NZ243310A (en) 1994-11-25
CA2072836A1 (en) 1993-01-03
US5292732A (en) 1994-03-08
CN1030986C (zh) 1996-02-14
JPH0774217B2 (ja) 1995-08-09
AU1930992A (en) 1993-01-07
FI100242B (fi) 1997-10-31
IL102337A0 (en) 1993-01-14
JPH06239865A (ja) 1994-08-30

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Legal Events

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FF Patent granted
RH Patent void