CA1184175A - Imidazodiazepines - Google Patents

Imidazodiazepines

Info

Publication number
CA1184175A
CA1184175A CA000393811A CA393811A CA1184175A CA 1184175 A CA1184175 A CA 1184175A CA 000393811 A CA000393811 A CA 000393811A CA 393811 A CA393811 A CA 393811A CA 1184175 A CA1184175 A CA 1184175A
Authority
CA
Canada
Prior art keywords
signifies
methyl
formula
compound
general formula
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
CA000393811A
Other languages
English (en)
French (fr)
Inventor
Walter Hunkeler
Emilio Kyburz
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of CA1184175A publication Critical patent/CA1184175A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/24—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
    • C07D265/26—Two oxygen atoms, e.g. isatoic anhydride
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—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 three hetero rings
    • C07D495/14—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Toxicology (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA000393811A 1981-02-27 1982-01-08 Imidazodiazepines Expired CA1184175A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH1338/81 1981-02-27
CH133881 1981-02-27

Publications (1)

Publication Number Publication Date
CA1184175A true CA1184175A (en) 1985-03-19

Family

ID=4208140

Family Applications (1)

Application Number Title Priority Date Filing Date
CA000393811A Expired CA1184175A (en) 1981-02-27 1982-01-08 Imidazodiazepines

Country Status (8)

Country Link
US (3) US4352815A (https=)
EP (1) EP0059386B1 (https=)
JP (2) JPS57156487A (https=)
AU (1) AU551769B2 (https=)
CA (1) CA1184175A (https=)
DE (1) DE3266263D1 (https=)
DK (1) DK87782A (https=)
ZA (2) ZA821130B (https=)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1184175A (en) * 1981-02-27 1985-03-19 Walter Hunkeler Imidazodiazepines
MC1528A1 (fr) * 1982-07-21 1984-04-13 Hoffmann La Roche Imidazobenzodiazepines
DK151808C (da) * 1982-11-16 1988-06-20 Ferrosan As Analogifremgangsmaade til fremstilling af oxadiazolylimidazo-oe1,4aa-benzodiazepinderivater
US4723003A (en) * 1983-05-18 1988-02-02 Hoechst-Roussel Pharmaceuticals Inc. Benzopyrrolobenzodiazepines and quinobenzodiazepines
US4521534A (en) * 1983-12-19 1985-06-04 Ayerst, Mckenna & Harrison, Ltd. Imidazo[2,1-a]pyrrolo[2,1-c][1,4]benzodiazepine derivatives, methods of preparation and use
IL74070A (en) * 1984-01-19 1988-12-30 Hoffmann La Roche Imidazodiazepine derivatives,their manufacture and pharmaceutical compositions containing them
DK476885D0 (da) * 1985-10-17 1985-10-17 Ferrosan As Heterocycliske forbindelser og fremgangsmaader til fremstilling heraf
CA1327008C (en) * 1988-01-15 1994-02-15 Walter Merz Anti-psychotic imidazobenzodiazepine
CA1312825C (en) * 1988-01-27 1993-01-19 F. Hoffmann-La Roche Ag Prevention or interruption of panic states with an imidazobenzodiazepine
CA1318668C (en) * 1988-08-05 1993-06-01 Heinz Carmann Radioiodine benzodiazepine derivatives
CA2015336A1 (en) * 1989-05-19 1990-11-19 F. Hoffmann-La Roche Ag Imidazodiazepines for the treatment of neurological symptoms
GB8927928D0 (en) * 1989-12-11 1990-02-14 Roussel Lab Ltd Chemical compounds
CA2055308A1 (en) * 1990-11-29 1992-05-30 F. Hoffmann-La Roche Ag Imidazobenzodiazepine for the treatment of sleep disorders
JP2525125B2 (ja) * 1991-07-23 1996-08-14 シェリング・コーポレーション 血清コレステロ―ル低下薬として有用な置換β−ラクタム化合物およびそれらの製法
US5561227A (en) * 1991-07-23 1996-10-01 Schering Corporation Process for the stereospecific synthesis of azetidinones
US5250679A (en) * 1991-10-18 1993-10-05 Genentech, Inc. Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III.sub. receptor
US5674863A (en) * 1991-10-18 1997-10-07 Genentech, Inc. Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa receptor
US5438035A (en) * 1994-06-24 1995-08-01 American Cyanamid Company Methods for controlling undesirable plant species with benzodiazepine compounds
JO2259B1 (en) 1999-05-12 2004-10-07 اف. هوفمان- لاروش أيه جي‏ Method for the manufacture of diazapine derivatives
US7595395B2 (en) * 2005-05-16 2009-09-29 Wisys Technology Foundation Gabaergic agents to treat memory deficits
KR101589314B1 (ko) 2007-08-20 2016-01-28 에보텍 인터내셔널 게엠베하 수면 장애의 치료
US20090054412A1 (en) * 2007-08-20 2009-02-26 John Alan Kemp Treatment of Sleep Disorders
GB0917611D0 (en) * 2009-10-08 2009-11-25 Ge Healthcare Ltd Automated radiosynthesis
JP5875083B2 (ja) 2010-04-15 2016-03-02 メディミューン リミテッド 増殖性疾患治療用ピロロベンゾジアゼピン
CA2795349C (en) 2010-04-15 2016-11-29 Seattle Genetics, Inc. Targeted pyrrolobenzodiazepine conjugates
SG11201400770SA (en) 2011-09-20 2014-04-28 Spirogen Sarl Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates
EP2751111B1 (en) 2011-10-14 2017-04-26 MedImmune Limited Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases
CN103997893B (zh) 2011-10-14 2019-04-12 西雅图基因公司 吡咯并苯并二氮杂卓和靶向结合物
AU2012322932B2 (en) 2011-10-14 2016-11-10 Medimmune Limited Pyrrolobenzodiazepines
CA2850373C (en) 2011-10-14 2019-07-16 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
EP2906297B1 (en) 2012-10-12 2017-12-06 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
HRP20190366T1 (hr) 2012-10-12 2019-04-19 Medimmune Limited Pirolobenzodiazepini i njihovi konjugati
EP2906296B1 (en) 2012-10-12 2018-03-21 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
HRP20182129T1 (hr) 2012-10-12 2019-02-08 Adc Therapeutics Sa Konjugati protutijelo - pirolobenzodiazepin
MX338711B (es) 2012-10-12 2016-04-28 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de las mismas.
JP6392765B2 (ja) 2012-10-12 2018-09-19 エイディーシー・セラピューティクス・エス・アーＡｄｃ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｓａ ピロロベンゾジアゼピン−抗体結合体
EP2906249B1 (en) 2012-10-12 2018-06-27 MedImmune Limited Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation
RS57694B1 (sr) 2012-10-12 2018-11-30 Adc Therapeutics Sa Pirolobenzodiazepin - anti-psma konjugati antitela
ES2680153T3 (es) 2012-10-12 2018-09-04 Adc Therapeutics Sa Conjugados de anticuerpos anti-PSMA-pirrolobenzodiazepinas
GB201317981D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052534A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
EP3054983B1 (en) 2013-10-11 2019-03-20 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
WO2015052535A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
CN107148285B (zh) 2014-11-25 2022-01-04 Adc治疗股份有限公司 吡咯并苯并二氮杂䓬-抗体缀合物
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
GB201506411D0 (en) 2015-04-15 2015-05-27 Bergenbio As Humanized anti-axl antibodies
GB201601431D0 (en) 2016-01-26 2016-03-09 Medimmune Ltd Pyrrolobenzodiazepines
GB201602359D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201602356D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201607478D0 (en) 2016-04-29 2016-06-15 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201617466D0 (en) 2016-10-14 2016-11-30 Medimmune Ltd Pyrrolobenzodiazepine conjugates
GB201702031D0 (en) 2017-02-08 2017-03-22 Medlmmune Ltd Pyrrolobenzodiazepine-antibody conjugates
RS61795B1 (sr) 2017-02-08 2021-06-30 Adc Therapeutics Sa Konjugati pirolobenzodiazepin antitela
CN110582505B (zh) 2017-04-18 2021-04-02 免疫医疗有限公司 吡咯并苯并二氮杂*缀合物
WO2018193102A1 (en) 2017-04-20 2018-10-25 Adc Therapeutics Sa Combination therapy with an anti-axl antibody-drug conjugate
CA3064804A1 (en) 2017-06-14 2018-12-20 Adc Therapeutics Sa Dosage regimes for the administration of an anti-cd19 adc
CN107325101B (zh) * 2017-06-29 2019-03-26 上海合全药物研发有限公司 6-羟甲基-6,7-二氢-5h,9h-咪唑并二氮杂卓-8-羧酸叔丁酯的合成方法
KR102270107B1 (ko) 2017-08-18 2021-06-30 메디뮨 리미티드 피롤로벤조디아제핀 컨쥬게이트
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
GB201806022D0 (en) 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
CN113631560B (zh) 2019-03-15 2025-02-18 麦迪穆有限责任公司 氮杂环丁烷并苯并二氮杂䓬二聚体和用于治疗癌症的包含它们的缀合物
CN113087713B (zh) * 2021-03-29 2022-10-04 中国人民解放军军事科学院军事医学研究院 一类苯并二氮䓬衍生物及其制备方法和用途

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1008856A (en) * 1971-11-15 1977-04-19 Ciba-Geigy Ag Triazolo-benzodiazepines
DE2609486A1 (de) * 1975-08-07 1977-05-12 Hoffmann La Roche Imidazo eckige klammer auf 1,5-a eckige klammer zu eckige klammer auf 1,4 eckige klammer zu diazepin-verbindungen und verfahren zu ihrer herstellung
US4022767A (en) * 1975-09-22 1977-05-10 Mcneil Laboratories, Incorporated 2-Aminobenzodiazepine-5-ones
GB1600600A (en) * 1977-03-10 1981-10-21 Diamond Shamrock Chem Plasticiser compositions for use with synthetic resin polymers
US4118386A (en) * 1977-04-04 1978-10-03 Hoffmann-La Roche Inc. Synthesis of imidazo[1,5-a]diazepine-3-carboxylates
CA1143728A (en) * 1979-10-04 1983-03-29 Max Gerecke Imidazodiazepine derivatives
CA1184175A (en) * 1981-02-27 1985-03-19 Walter Hunkeler Imidazodiazepines

Also Published As

Publication number Publication date
JPH0354105B2 (https=) 1991-08-19
AU551769B2 (en) 1986-05-08
US4386028A (en) 1983-05-31
ZA821130B (en) 1983-01-26
JPS57156487A (en) 1982-09-27
ZA821128B (en) 1983-01-26
DK87782A (da) 1982-08-28
JPS57163380A (en) 1982-10-07
DE3266263D1 (en) 1985-10-24
EP0059386A2 (de) 1982-09-08
EP0059386B1 (de) 1985-09-18
EP0059386A3 (en) 1982-11-03
AU8066782A (en) 1982-09-02
US4352815A (en) 1982-10-05
US4405516A (en) 1983-09-20

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