MC1314A1 - BENZAZEPINE DERIVATIVES - Google Patents

BENZAZEPINE DERIVATIVES

Info

Publication number
MC1314A1
MC1314A1 MC801426A MC1426A MC1314A1 MC 1314 A1 MC1314 A1 MC 1314A1 MC 801426 A MC801426 A MC 801426A MC 1426 A MC1426 A MC 1426A MC 1314 A1 MC1314 A1 MC 1314A1
Authority
MC
Monaco
Prior art keywords
hydrogen
lower alkyl
hydroxy
group
halogen
Prior art date
Application number
MC801426A
Other languages
French (fr)
Inventor
E Trybulski
R Fryer
A Walser
N Gilman
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 MC1314A1 publication Critical patent/MC1314A1/en

Links

Classifications

    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C291/00—Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/00 - C07C281/00
    • C07C291/02—Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/00 - C07C281/00 containing nitrogen-oxide bonds
    • C07C291/04—Compounds containing carbon and nitrogen and having functional groups not covered by groups C07C201/00 - C07C281/00 containing nitrogen-oxide bonds containing amino-oxide bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66—Methanesulfonates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/63—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/32—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing keto groups
    • C07C65/34—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing keto groups polycyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/16—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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

Abstract

Pyrimido-2-benzazepines of the formula <IMAGE> wherein A is one of the groups <IMAGE> R<1> is hydrogen, chlorine, bromine, lower alkyl, the group NR<4>R<5>, the group -CH2-CO-R<7>, the group -NH(CH2)mNR<8>R<9>, hydroxy, lower alkoxy, mercapto or lower alkyl mercapto, R<2> is hydrogen, amino or di-lower alkyl amino, R<3> is hydrogen, lower acyloxy or hydroxy, X is hydrogen, halogen, trifluoromethyl, ethyl alpha -hydroxy ethyl or acetyl, Y is hydrogen or halogen, R<4> and R<5> each are hydrogen or lower alkyl or, together complete a five to seven membered heterocyclic ring, R<7> is hydroxy, lower alkoxy or NR<8>R<9>, R<8> and R<9> each are hydrogen or lower alkyl, n is 0 or 1 and m is 1 to 7, with certain provisos, and pharmaceutically acceptable acid addition salts thereof, exhibit pharmacological utility as anxiolytics and sedatives.
MC801426A 1979-02-07 1980-02-06 BENZAZEPINE DERIVATIVES MC1314A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1011879A 1979-02-07 1979-02-07
US1670979A 1979-03-01 1979-03-01
CH51080 1980-01-22

Publications (1)

Publication Number Publication Date
MC1314A1 true MC1314A1 (en) 1981-03-10

Family

ID=27172162

Family Applications (1)

Application Number Title Priority Date Filing Date
MC801426A MC1314A1 (en) 1979-02-07 1980-02-06 BENZAZEPINE DERIVATIVES

Country Status (26)

Country Link
EP (1) EP0014470B1 (en)
AT (1) ATE14225T1 (en)
AU (1) AU535233B2 (en)
CA (1) CA1138863A (en)
DD (1) DD149066A5 (en)
DE (2) DE3004381A1 (en)
ES (1) ES8101590A1 (en)
FI (1) FI68832C (en)
FR (1) FR2450833A1 (en)
GB (1) GB2043636B (en)
HU (1) HU182662B (en)
IE (1) IE49630B1 (en)
IL (1) IL59316A (en)
IN (1) IN151574B (en)
IT (1) IT1140535B (en)
LU (1) LU82143A1 (en)
MC (1) MC1314A1 (en)
MT (1) MTP864B (en)
NL (1) NL8000715A (en)
NO (1) NO153138C (en)
NZ (1) NZ192803A (en)
PT (1) PT70794B (en)
RO (1) RO79168A (en)
SE (1) SE8000964L (en)
SU (1) SU1181547A3 (en)
YU (1) YU32380A (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK347781A (en) * 1980-08-05 1982-02-06 Hoffmann La Roche PROCEDURE FOR PREPARING PYRIMIDO- (4,5-D) (2) -BENZEZEPINS OR PHARMACEUTICAL ACCEPTABLE SALTS THEREOF
EP0273697A3 (en) * 1986-12-30 1989-11-29 Merck & Co. Inc. 2-benzazepines with 5- and 6- membered heterocyclic rings
US5013333A (en) * 1990-04-13 1991-05-07 Tennant Company Unattended air cleaning system for surface maintenance machine
JP5097539B2 (en) * 2004-05-07 2012-12-12 アムジエン・インコーポレーテツド Protein kinase modulators and methods of use
MXPA06013042A (en) 2004-05-14 2007-02-12 Millennium Pharm Inc Compounds and methods for inhibiting mitotic progression.
WO2008021038A2 (en) 2006-08-09 2008-02-21 Millennium Pharmaceuticals, Inc. Pyridobenzazepine compounds and methods for inhibiting mitotic progression
CL2007003244A1 (en) 2006-11-16 2008-04-04 Millennium Pharm Inc COMPOUNDS DERIVED FROM PIRIMIDO [5,4-D] [2] BENZAZEPINA; PHARMACEUTICAL COMPOSITION THAT INCLUDES SUCH COMPOUND; AND USE OF THE COMPOUND FOR THE TREATMENT OF CANCER.
JP5738196B2 (en) 2008-12-22 2015-06-17 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Combination of Aurora kinase inhibitor and anti-CD20 antibody
JO3635B1 (en) 2009-05-18 2020-08-27 Millennium Pharm Inc Solid pharmaceutical compositions and processes for their production
CN102770024A (en) 2010-02-19 2012-11-07 米伦纽姆医药公司 Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6--methoxyphenyl)-5h -pyrimido[5,4-d][2]benzazepin-2yl]amino}-2-methoxybenzoate
US20130303519A1 (en) 2012-03-20 2013-11-14 Millennium Pharmaceuticals, Inc. Methods of treating cancer using aurora kinase inhibitors
WO2014153509A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3947585A (en) * 1974-06-03 1976-03-30 Ciba-Geigy Corporation Pyrazolobenzazepines

Also Published As

Publication number Publication date
HU182662B (en) 1984-02-28
DD149066A5 (en) 1981-06-24
NZ192803A (en) 1984-08-24
EP0014470A3 (en) 1982-02-10
CA1138863A (en) 1983-01-04
GB2043636A (en) 1980-10-08
IL59316A0 (en) 1980-05-30
IE49630B1 (en) 1985-11-13
FI800367A (en) 1980-08-08
IN151574B (en) 1983-05-28
IE800227L (en) 1980-08-07
DE3004381A1 (en) 1980-09-04
NO153138C (en) 1986-01-22
AU535233B2 (en) 1984-03-08
ATE14225T1 (en) 1985-07-15
ES488311A0 (en) 1980-12-16
NO800316L (en) 1980-08-08
FI68832B (en) 1985-07-31
FR2450833B1 (en) 1983-06-10
FR2450833A1 (en) 1980-10-03
PT70794B (en) 1981-06-11
PT70794A (en) 1980-03-01
SE8000964L (en) 1980-08-08
AU5529680A (en) 1980-08-14
ES8101590A1 (en) 1980-12-16
RO79168A (en) 1982-06-25
DE3070847D1 (en) 1985-08-14
IT8019740A0 (en) 1980-02-06
FI68832C (en) 1985-11-11
SU1181547A3 (en) 1985-09-23
IL59316A (en) 1983-07-31
MTP864B (en) 1981-04-29
NO153138B (en) 1985-10-14
IT1140535B (en) 1986-10-01
GB2043636B (en) 1983-05-11
NL8000715A (en) 1980-08-11
EP0014470A2 (en) 1980-08-20
EP0014470B1 (en) 1985-07-10
YU32380A (en) 1983-12-31
LU82143A1 (en) 1981-09-10

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