FI90977B - Förfarande för framställning av piperidylidendihydrodibenso/a,d/cykloheptener och deras azaderivat - Google Patents

Förfarande för framställning av piperidylidendihydrodibenso/a,d/cykloheptener och deras azaderivat Download PDF

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Publication number
FI90977B
FI90977B FI861987A FI861987A FI90977B FI 90977 B FI90977 B FI 90977B FI 861987 A FI861987 A FI 861987A FI 861987 A FI861987 A FI 861987A FI 90977 B FI90977 B FI 90977B
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FI
Finland
Prior art keywords
compound
substituted
alkyl
solution
formula
Prior art date
Application number
FI861987A
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English (en)
Finnish (fi)
Other versions
FI90977C (sv
FI861987A0 (sv
FI861987A (sv
Inventor
Frank J Villani
Doris Pickel Schumacher
Jesse Kwok-Keung Wong
Bruce Lee Murphy
Jon Edward Clark
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.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27419175&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=FI90977(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US06/839,016 external-priority patent/US4731447A/en
Priority claimed from US06/838,974 external-priority patent/US4659716A/en
Application filed by Schering Corp filed Critical Schering Corp
Publication of FI861987A0 publication Critical patent/FI861987A0/sv
Publication of FI861987A publication Critical patent/FI861987A/sv
Application granted granted Critical
Publication of FI90977B publication Critical patent/FI90977B/sv
Publication of FI90977C publication Critical patent/FI90977C/sv

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Classifications

    • 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
    • C07D213/60—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 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (4)

1. Förfarande för framställning av föreningar med den all-männa formeIn I /-\ r1 "jf / V"2 ΊΤ·’ 1 ^ N ^ r5 där a, b, c och d är CH eller en av grupperna a, b, c och d är N och de övriga är CH; 12 3 4 R , R , R och R , vilka kan vara samma eller olika, är envar oberoende av varandra väte, 1-6 kolatomers alkyl, fluor, klor, brom, jod, nitro, 1-6 kolatomers alkoxi eller trifluormetyl; 32 ^ V/sv r2 rY «*4Ä f·0 T* 11 :* där a, b, c, d, R1, R2, R3 och R4 avser samma som ovan och R5' avser samma som R5 ovan eller är en N-skyddande grupp, kondenseras intramolukärt och därefter om nödvändigt eller vid behov utföres ett eller flera av följande steg: a) avlägsnas eventuell N-skyddande grupp R5> ; b) omvandlas en förening, där R5 är lägre alkyl eller -COOR7, tili en förening där R5 är väte; c) omvandlas en förening, där R5 är väte, tili en förening där R5 är -COOR7 eller lägre alkyl; d) omvandlas en förening, där R5 är lägre alkyl, till en förening där R5 är -COOR7; eller e) omvandlas en förening med formeln I, som erhällits enligt nägot av stegen ovan, tili ett farmaceutiskt godtagbart sait; kännetecknad därav, att intramolekulära konden-sationen utföres genom att behandla förening enligt formeln III med en syra, vars Hammet surhetsfunktion är minus 12 eller lägre. 90977 33
2. Förfarande enligt patentkrav 1, kännetecknad därav, att syrans Hammett syrafunktion är minus 13 eller minus 14.
3. Förfarande enligt patentkrav 1 eller 2, kännetecknad därav, att den använda syran valts frän gruppen HF/BF3, CF3S03H, CH3S03H/BF3 och FS03H.
4. Förfarande enligt nägon patentkrav 1-3, kännetecknad därav, att N-skyddsgruppen R är lägre alkyl, företrädesvis metyl.
FI861987A 1985-05-13 1986-05-13 Förfarande för framställning av piperidylidendihydrodibenso/a,d/cykloheptener och deras azaderivat FI90977C (sv)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US73342885A 1985-05-13 1985-05-13
US73342885 1985-05-13
US83901686 1986-03-12
US06/839,016 US4731447A (en) 1985-05-13 1986-03-12 Process for preparing piperidylidene dihydro-dibenzo(a,d)-cycloheptenes or aza-derivatives thereof
US83897486 1986-03-12
US06/838,974 US4659716A (en) 1984-02-15 1986-03-12 Antihistaminic 8-(halo)-substituted 6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridines

Publications (4)

Publication Number Publication Date
FI861987A0 FI861987A0 (sv) 1986-05-13
FI861987A FI861987A (sv) 1986-11-14
FI90977B true FI90977B (sv) 1994-01-14
FI90977C FI90977C (sv) 1994-04-25

Family

ID=27419175

Family Applications (2)

Application Number Title Priority Date Filing Date
FI861987A FI90977C (sv) 1985-05-13 1986-05-13 Förfarande för framställning av piperidylidendihydrodibenso/a,d/cykloheptener och deras azaderivat
FI902315A FI87648C (sv) 1985-05-13 1990-05-09 Förfarande för framställning av terapeutiskt aktiv 8-halogen-11-(4-pip eridyliden)-6,11-dihydro-5H-bentso/5,6/cyklohepta/1,2-b/-pyridin

Family Applications After (1)

Application Number Title Priority Date Filing Date
FI902315A FI87648C (sv) 1985-05-13 1990-05-09 Förfarande för framställning av terapeutiskt aktiv 8-halogen-11-(4-pip eridyliden)-6,11-dihydro-5H-bentso/5,6/cyklohepta/1,2-b/-pyridin

Country Status (15)

Country Link
EP (1) EP0208855B1 (sv)
JP (2) JP2511412B2 (sv)
AR (1) AR241463A1 (sv)
AU (2) AU600665B2 (sv)
CA (1) CA1272480A (sv)
DE (1) DE3677842D1 (sv)
DK (1) DK173765B1 (sv)
ES (1) ES8800679A1 (sv)
FI (2) FI90977C (sv)
HK (1) HK75993A (sv)
HU (1) HU199138B (sv)
IE (1) IE59110B1 (sv)
IL (1) IL78771A (sv)
PT (1) PT82570B (sv)
SG (1) SG69193G (sv)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4804666A (en) * 1985-08-14 1989-02-14 Schering Corporation Antiallergic 6,11-dihydro-11-(4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-B)pyridines
US4826853A (en) * 1986-10-31 1989-05-02 Schering Corporation 6,11-Dihydro-11-(N-substituted-4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-B)pyridines and compositions and methods of use
WO1989010369A1 (en) * 1988-04-28 1989-11-02 Schering Corporation Novel benzopyrido piperidine, piperidylidene and piperazine compounds, compositions, methods of manufacture and methods of use
US4863931A (en) * 1988-09-15 1989-09-05 Schering Corporation Antihistaminic fluoro substituted benzocycloheptapyridines
US5095022A (en) * 1989-07-04 1992-03-10 Hokuriku Pharmaceutical Co., Ltd. Piperidine derivatives and pharmaceutical compositions comprising the same
ES2080699B1 (es) * 1994-07-27 1996-10-16 Farmahispania S A Nuevos derivados de 2-(1-etoxicarbonil-4-piperidiliden)metil)piridina y un procedimiento para su obtencion.
ES2080700B1 (es) * 1994-07-27 1996-10-16 Farmihispania S A Nuevo procedimiento para la obtencion de loratadina.
CN1047774C (zh) * 1996-09-10 1999-12-29 上海华联制药有限公司 氮杂二苯并环庚烯酮类化合物的制备方法
WO1998048803A1 (fr) * 1997-04-25 1998-11-05 Schering-Plough Kabushiki Kaisha Collyres
UA62976C2 (en) * 1997-07-02 2004-01-15 Schering Corp Polymorphs of 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5h-benzo[5,6]cyclohepta[1,2-b]pyridine
DE69919720D1 (de) * 1998-07-24 2004-09-30 Russinsky Ltd Verfahren zur herstellung von benzocycloheptapyridin-11-one
US6372909B1 (en) 1998-11-20 2002-04-16 Schering Corporation Synthesis of intermediates useful in preparing tricyclic compounds
EP1131296A2 (en) * 1998-11-20 2001-09-12 Schering Corporation Synthesis of intermediates useful in preparing tricyclic compounds
DE69911252T2 (de) * 1998-12-18 2004-07-01 Schering Corp. Verfahren zur herstellung von tricyclischen verbindungen mit antihistaminischer wirkung
HU226998B1 (en) * 2000-11-23 2010-04-28 Richter Gedeon Nyrt Desloratadine hemisulphate, process for the preparation thereof and pharmaceutical compositions containing the same
PL2034970T3 (pl) 2006-06-01 2012-12-31 Msd Consumer Care Inc Preparat farmaceutyczny o przedłużonym uwalnianiu zawierający fenylefrynę
TR200806298A2 (tr) 2008-08-22 2010-03-22 Bi̇lgi̇ç Mahmut Farmasötik formülasyon

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL132137C (sv) * 1963-04-24
US3717647A (en) * 1971-04-09 1973-02-20 Schering Corp Alpha-nicotinoyl phenylacetonitriles
GB1489332A (en) * 1973-10-11 1977-10-19 Beecham Group Ltd Reduced bicyclic pyridone derivatives
US4282233B1 (en) * 1980-06-19 2000-09-05 Schering Corp Antihistaminic 11-(4-piperidylidene)-5h-benzoÄ5,6Ü-cyclohepta-Ä1,2Ü-pyridines
HU194864B (en) * 1984-02-15 1988-03-28 Schering Corp Process for production of 8-chlor-6,11-dihydro-11-(4-piperidilidene)-5h-benzo (5,6)-cyclo-hepta (1,2-b) pyridine and its salts

Also Published As

Publication number Publication date
DK220986D0 (da) 1986-05-13
IL78771A0 (en) 1986-08-31
JP2511412B2 (ja) 1996-06-26
AU600665B2 (en) 1990-08-23
PT82570B (pt) 1988-11-30
EP0208855A1 (en) 1987-01-21
JPH0859657A (ja) 1996-03-05
FI90977C (sv) 1994-04-25
CA1272480A (en) 1990-08-07
DK220986A (da) 1986-11-14
SG69193G (en) 1993-08-06
ES8800679A1 (es) 1987-11-16
FI87648C (sv) 1993-02-10
HUT41731A (en) 1987-05-28
AU5702690A (en) 1990-10-04
HK75993A (en) 1993-08-06
AU638019B2 (en) 1993-06-17
PT82570A (en) 1986-06-01
IE861259L (en) 1986-11-13
DE3677842D1 (de) 1991-04-11
AU5737486A (en) 1986-12-18
AR241463A1 (es) 1992-07-31
EP0208855B1 (en) 1991-03-06
DK173765B1 (da) 2001-09-17
FI861987A0 (sv) 1986-05-13
FI87648B (fi) 1992-10-30
ES554898A0 (es) 1987-11-16
FI902315A0 (fi) 1990-05-09
JPS61289087A (ja) 1986-12-19
HU199138B (en) 1990-01-29
IE59110B1 (en) 1994-01-12
FI861987A (sv) 1986-11-14
JP2519880B2 (ja) 1996-07-31
IL78771A (en) 1990-11-29

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BB Publication of examined application
FG Patent granted

Owner name: SCHERING CORPORATION

MA Patent expired