DK168919B1 - Analogifremgangsmåde til fremstilling af ((bis(aryl)methylen)-1-piperidinyl)alkyl-pyrimidinoner og farmaceutisk acceptable syreadditionssalte deraf - Google Patents

Analogifremgangsmåde til fremstilling af ((bis(aryl)methylen)-1-piperidinyl)alkyl-pyrimidinoner og farmaceutisk acceptable syreadditionssalte deraf Download PDF

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Publication number
DK168919B1
DK168919B1 DK498483A DK498483A DK168919B1 DK 168919 B1 DK168919 B1 DK 168919B1 DK 498483 A DK498483 A DK 498483A DK 498483 A DK498483 A DK 498483A DK 168919 B1 DK168919 B1 DK 168919B1
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parts
formula
methyl
alk
fluorophenyl
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DK498483A
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Danish (da)
English (en)
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DK498483A (da
DK498483D0 (da
Inventor
Ludo Edmond Josephine Kennis
Jan Vandenberk
Josephus Carolus Mertens
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Janssen Pharmaceutica Nv
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46—Oxygen atoms
    • C07D213/50—Ketonic radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)
DK498483A 1982-11-01 1983-10-31 Analogifremgangsmåde til fremstilling af ((bis(aryl)methylen)-1-piperidinyl)alkyl-pyrimidinoner og farmaceutisk acceptable syreadditionssalte deraf DK168919B1 (da)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US43807982A 1982-11-01 1982-11-01
US43807982 1982-11-01
US51761283 1983-07-27
US06/517,612 US4485107A (en) 1982-11-01 1983-07-27 [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones

Publications (3)

Publication Number Publication Date
DK498483D0 DK498483D0 (da) 1983-10-31
DK498483A DK498483A (da) 1984-05-02
DK168919B1 true DK168919B1 (da) 1994-07-11

Family

ID=27031541

Family Applications (1)

Application Number Title Priority Date Filing Date
DK498483A DK168919B1 (da) 1982-11-01 1983-10-31 Analogifremgangsmåde til fremstilling af ((bis(aryl)methylen)-1-piperidinyl)alkyl-pyrimidinoner og farmaceutisk acceptable syreadditionssalte deraf

Country Status (26)

Country Link
US (1) US4485107A (pt)
EP (1) EP0110435B1 (pt)
KR (1) KR870000825B1 (pt)
AU (1) AU559176B2 (pt)
BG (2) BG51158A3 (pt)
CA (1) CA1211438A (pt)
CS (1) CS238396B2 (pt)
CY (1) CY1607A (pt)
DE (1) DE3378825D1 (pt)
DK (1) DK168919B1 (pt)
ES (1) ES8601965A1 (pt)
FI (1) FI77868C (pt)
GR (1) GR81277B (pt)
HK (1) HK52691A (pt)
IE (1) IE56180B1 (pt)
IL (1) IL70094A0 (pt)
IN (1) IN159576B (pt)
MA (1) MA19941A1 (pt)
NO (1) NO166133C (pt)
NZ (1) NZ205993A (pt)
PH (1) PH20483A (pt)
PT (1) PT77493B (pt)
RO (1) RO86698B (pt)
SG (1) SG46791G (pt)
SU (1) SU1313349A3 (pt)
ZW (1) ZW23283A1 (pt)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4529727A (en) * 1982-04-21 1985-07-16 Janssen Pharmaceutical, N.V. Pyrimido[2,1-b][1,3]-thiazines
US4533665A (en) * 1983-07-27 1985-08-06 Janssen Pharmaceutica [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones
US4581171A (en) * 1983-07-27 1986-04-08 Janssen Pharmaceutica, N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones useful for treating psychotropic disorders
US4695569A (en) * 1983-11-30 1987-09-22 Janssen Pharmaceutica N.V. Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines
US4888426A (en) * 1983-11-30 1989-12-19 Janssen Pharmaceutica N.V. 1-(5-methyl-furan-2-ylmethyl)-N-(4-piperidinyl)imidazo [4,5-6]pyridine-2-amine
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
US4874766A (en) * 1986-09-22 1989-10-17 Janssen Pharmaceutica N.V. Method of promoting wound-healing
US4921854A (en) * 1986-12-30 1990-05-01 Egis Gyogyszergyar Condensed thiazolopyrimidine, pyrimido-thiazine or thiazepine pyrimidine compounds
DE3738844A1 (de) * 1987-11-16 1989-05-24 Merck Patent Gmbh Analgetikum
IL90858A (en) * 1988-07-07 1994-08-26 Rhone Poulenc Sante History (Aza) Naftalensultam, their preparation and preparations containing them
IL90879A0 (en) * 1988-09-02 1990-02-09 Janssen Pharmaceutica Nv 3-piperidinyl-indazole derivatives,their preparation and antihypertensive compositions containing them
US5158952A (en) * 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
US5256659A (en) * 1989-01-09 1993-10-26 Janssen Pharmaceutica N.V. 2-aminopyrimidinone derivatives
US5140029A (en) * 1989-01-09 1992-08-18 Janssen Pharmaceutica N.V. 2-aminopyrimidinone derivatives
GB8900382D0 (en) * 1989-01-09 1989-03-08 Janssen Pharmaceutica Nv 2-aminopyrimidinone derivatives
FR2643373B1 (fr) * 1989-01-10 1993-12-31 Adir Cie Nouveaux derives des bisarylalcenes, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
GB9008850D0 (en) * 1990-04-19 1990-06-13 Janssen Pharmaceutica Nv Novel 2,9-disubstituted-4h-pyridol(1,2-a)pyrimidin-4-ones
ES2050069B1 (es) * 1992-07-10 1994-12-16 Vita Invest Sa Procedimiento para la obtencion de 3-(2-(4-(6-fluoro-1,2-benzisoxazol-3-il)piperidino)etil)-2-metil-6,7,8,9-tetrahidro-4h-pirido(1,2-a) pirimidin-4-ona.
NZ276088A (en) 1993-11-19 1999-07-29 Janssen Pharmaceutica Nv [(1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-6,7,8,9-tetrahydro-4h- pyrido[1,2-a]-pyrimidin-4-one derivatives (ie risperidone)
ZA979781B (en) * 1996-11-14 1998-06-08 Akzo Nobel Nv Piperidine derivatives.
UA72189C2 (uk) 1997-11-17 2005-02-15 Янссен Фармацевтика Н.В. Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот
UA75051C2 (en) 1999-09-03 2006-03-15 Syngenta Participations Ag Tetrahydropiridines as pesticides, a composition, a method for the preparation thereof and a method of controlling pests
AU2003206872A1 (en) * 2002-02-11 2003-09-04 Syngenta Participations Ag Derivatives of (1-benzyl-piperidine-4-yl)-diphenyl-methanol and their use as pesticide
KR20040034996A (ko) * 2002-10-18 2004-04-29 한미약품 주식회사 리스페리돈의 개선된 제조방법
MXPA05006427A (es) * 2002-12-18 2005-09-08 Fmc Corp Piperidinas y piridinas (arilmetilo sustituido)-n-4-(metilo disustituido).
WO2004094414A1 (en) * 2003-04-22 2004-11-04 Synthon B.V. Water soluble salts of risperidone
BRPI0810621A2 (pt) 2007-04-13 2017-06-06 Southern Res Inst métodos de inibição ou redução da angiogênese, do crescimento ou metástase de tumor dependente da mesma e de tratamento de doença ou desordem associada a angiogênese.
RS60352B1 (sr) * 2014-12-12 2020-07-31 Japan Tobacco Inc Dihidropirimidin-2-on jedinjenja i njihova medicinska upotreba
WO2019167981A1 (ja) 2018-02-28 2019-09-06 日本たばこ産業株式会社 ４－メチルジヒドロピリミジノン化合物及びその医薬用途
CN112724070B (zh) * 2021-01-08 2022-11-25 南京方生和医药科技有限公司 一种α，α-二苯基-4-哌啶甲醇的制备方法

Family Cites Families (5)

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Publication number Priority date Publication date Assignee Title
GB1252315A (pt) * 1969-06-05 1971-11-03
US3960863A (en) * 1974-06-25 1976-06-01 Sankyo Company Limited Pyrido[1,2-a]pyrimidinone derivatives
DE3000923A1 (de) * 1979-01-17 1980-07-31 Degussa Neue n-alkoxy-dithienylpiperidine
US4342870A (en) * 1980-03-28 1982-08-03 Janssen Pharmaceutica N.V. Novel 3-(1-piperidinylalkyl)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives
US4443451A (en) * 1981-07-15 1984-04-17 Janssen Pharmaceutica N.V. Bicyclic pyrimidin-5-one derivatives

Also Published As

Publication number Publication date
PH20483A (en) 1987-01-16
NO166133B (no) 1991-02-25
PT77493A (en) 1983-11-01
AU2083483A (en) 1984-05-10
KR850000462A (ko) 1985-02-27
FI833995A0 (fi) 1983-10-31
CY1607A (en) 1992-04-03
EP0110435B1 (en) 1989-01-04
DK498483A (da) 1984-05-02
CA1211438A (en) 1986-09-16
RO86698A (ro) 1985-04-17
NO166133C (no) 1991-06-05
SG46791G (en) 1991-07-26
ES526868A0 (es) 1985-11-01
HK52691A (en) 1991-07-19
FI77868C (fi) 1989-05-10
IE56180B1 (en) 1991-05-08
DE3378825D1 (de) 1989-02-09
IN159576B (pt) 1987-05-30
PT77493B (en) 1986-05-28
IL70094A0 (en) 1984-01-31
FI77868B (fi) 1989-01-31
EP0110435A1 (en) 1984-06-13
BG60538B2 (bg) 1995-07-28
NO833956L (no) 1984-05-02
ES8601965A1 (es) 1985-11-01
BG51158A3 (en) 1993-02-15
GR81277B (pt) 1984-12-11
IE832540L (en) 1984-05-01
RO86698B (ro) 1985-05-02
FI833995A (fi) 1984-05-02
NZ205993A (en) 1986-06-11
AU559176B2 (en) 1987-02-26
DK498483D0 (da) 1983-10-31
SU1313349A3 (ru) 1987-05-23
CS766383A2 (en) 1984-12-14
KR870000825B1 (ko) 1987-04-23
ZW23283A1 (en) 1985-05-22
US4485107A (en) 1984-11-27
MA19941A1 (fr) 1984-07-01
CS238396B2 (en) 1985-11-13

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B1 Patent granted (law 1993)
PUP Patent expired