IL59316A - Phenylpyrimidobenzazepine derivatives,their preparation and pharmaceutical compositions containing them - Google Patents
Phenylpyrimidobenzazepine derivatives,their preparation and pharmaceutical compositions containing themInfo
- Publication number
- IL59316A IL59316A IL59316A IL5931680A IL59316A IL 59316 A IL59316 A IL 59316A IL 59316 A IL59316 A IL 59316A IL 5931680 A IL5931680 A IL 5931680A IL 59316 A IL59316 A IL 59316A
- Authority
- IL
- Israel
- Prior art keywords
- hydrogen
- lower alkyl
- hydroxy
- group
- phenylpyrimidobenzazepine
- Prior art date
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
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Indole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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.
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 (2)
Publication Number | Publication Date |
---|---|
IL59316A0 IL59316A0 (en) | 1980-05-30 |
IL59316A true IL59316A (en) | 1983-07-31 |
Family
ID=27172162
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IL59316A IL59316A (en) | 1979-02-07 | 1980-02-05 | Phenylpyrimidobenzazepine derivatives,their preparation and pharmaceutical compositions containing them |
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 (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA815357B (en) * | 1980-08-05 | 1982-07-28 | Hoffmann La Roche | Benzazepine derivatives |
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 |
AU2005245386B2 (en) | 2004-05-07 | 2008-11-27 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
PT1905773E (en) | 2004-05-14 | 2012-10-25 | Millennium Pharm Inc | Compounds and methods for inhibiting mitotic progression by inhibition of aurora kinase |
JP2010500352A (en) | 2006-08-09 | 2010-01-07 | 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 | 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. |
MX2011006725A (en) | 2008-12-22 | 2011-09-15 | Millennium Pharm Inc | Combination of aurora kinase inhibitors and anti-cd20 antibodies. |
JO3635B1 (en) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | Solid pharmaceutical compositions and processes for their production |
US8653064B2 (en) | 2010-02-19 | 2014-02-18 | Millennium Pharmaceuticals, Inc. | Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-D][2]benzazepin-2-yl]amino}-2-methoxybenzoate |
US20130303519A1 (en) | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
CN105209042B (en) | 2013-03-22 | 2019-03-08 | 米伦纽姆医药公司 | The combination of 1/2 inhibitor of catalytic MTORC and selective aurora A kinase inhibitor |
JP2018524292A (en) | 2015-07-21 | 2018-08-30 | 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. | Administration of aurora kinase inhibitors and chemotherapeutic agents |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3947585A (en) * | 1974-06-03 | 1976-03-30 | Ciba-Geigy Corporation | Pyrazolobenzazepines |
-
1980
- 1980-02-05 FR FR8002469A patent/FR2450833A1/en active Granted
- 1980-02-05 CA CA000345062A patent/CA1138863A/en not_active Expired
- 1980-02-05 IL IL59316A patent/IL59316A/en unknown
- 1980-02-05 NL NL8000715A patent/NL8000715A/en not_active Application Discontinuation
- 1980-02-05 SU SU802879255A patent/SU1181547A3/en active
- 1980-02-05 NZ NZ192803A patent/NZ192803A/en unknown
- 1980-02-06 DE DE19803004381 patent/DE3004381A1/en not_active Withdrawn
- 1980-02-06 DD DD80218921A patent/DD149066A5/en unknown
- 1980-02-06 ES ES488311A patent/ES8101590A1/en not_active Expired
- 1980-02-06 IT IT19740/80A patent/IT1140535B/en active
- 1980-02-06 EP EP80100610A patent/EP0014470B1/en not_active Expired
- 1980-02-06 HU HU80271A patent/HU182662B/en unknown
- 1980-02-06 SE SE8000964A patent/SE8000964L/en not_active Application Discontinuation
- 1980-02-06 MT MT864A patent/MTP864B/en unknown
- 1980-02-06 DE DE8080100610T patent/DE3070847D1/en not_active Expired
- 1980-02-06 PT PT70794A patent/PT70794B/en unknown
- 1980-02-06 IN IN138/CAL/80A patent/IN151574B/en unknown
- 1980-02-06 AU AU55296/80A patent/AU535233B2/en not_active Ceased
- 1980-02-06 LU LU82143A patent/LU82143A1/en unknown
- 1980-02-06 IE IE227/80A patent/IE49630B1/en unknown
- 1980-02-06 NO NO800316A patent/NO153138C/en unknown
- 1980-02-06 FI FI800367A patent/FI68832C/en not_active IP Right Cessation
- 1980-02-06 AT AT80100610T patent/ATE14225T1/en not_active IP Right Cessation
- 1980-02-06 GB GB8003910A patent/GB2043636B/en not_active Expired
- 1980-02-06 MC MC801426A patent/MC1314A1/en unknown
- 1980-02-07 RO RO80100118A patent/RO79168A/en unknown
- 1980-02-07 YU YU00323/80A patent/YU32380A/en unknown
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