PE20090814A1 - Cis-imidazolinas quirales - Google Patents

Cis-imidazolinas quirales

Info

Publication number
PE20090814A1
PE20090814A1 PE2008001740A PE2008001740A PE20090814A1 PE 20090814 A1 PE20090814 A1 PE 20090814A1 PE 2008001740 A PE2008001740 A PE 2008001740A PE 2008001740 A PE2008001740 A PE 2008001740A PE 20090814 A1 PE20090814 A1 PE 20090814A1
Authority
PE
Peru
Prior art keywords
phenyl
imidazolines
compounds
etoxy
piperazin
Prior art date
Application number
PE2008001740A
Other languages
English (en)
Inventor
David Bartkovitz
Jianping Cai
Xin-Jie Chu
Hongju Li
Allen John Lovey
Binh Vu
Chunlin Zhao
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40149549&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20090814(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20090814A1 publication Critical patent/PE20090814A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE IMIDAZOLINAS DE FORMULA (I) DONDE Y, X Y Z SON CADA UNO C O N; V1 Y V2 SON CADA UNO HALOGENO, CN, CF3, NITRO, ENTRE OTROS; R1 Y R2 SON CADA UNO H O CH3; R3 ES H O -C(=O)-R6, DONDE R6 ES ALQUILO INFERIOR, CICLOPROPILO, CICLOBUTILO, FENILO, ENTRE OTROS; R4 ES -OCH3, -OCH2CH3, -OCH2CH2F, ENTRE OTROS; R5 ES H, -CH3, -CF3, HALOGENO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-{4-[(4S,5R)-2-(2-TERT-BUTIL-4-ETOXI-PIRIMIDIN-5-IL)-4,5-BIS-(4-CLORO-FENIL)-4,5-DIMETIL-4,5-DIHIDRO-IMIDAZOL-1-CARBONIL]-PIPERAZIN-1-IL}-ACETAMIDA, [(4S,5R)-2-(2-TERT-BUTIL-4-ETOXI-PIRIMIDIN-5-IL)-4,5-BIS-(4-CLORO-FENIL)-4,5-DIMETIL-4,5-DIHIDRO-IMIDAZOL-1-IL]-[4-(1,1-DIOXO-HEXAHIDRO-TIOPIRAN-4-IL)-PIPERAZIN-1-IL]-METANONA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA INTERACCION ENTRE LA PROTEINA MDM2 Y UN PEPTIDO DE TIPO p-53 SIENDO UTILES EN EL TRATAMIENTO DE TUMORES DE MAMA, DE COLON, DE PULMON, DE PROSTATA
PE2008001740A 2007-10-09 2008-10-07 Cis-imidazolinas quirales PE20090814A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US97850607P 2007-10-09 2007-10-09
US9275908P 2008-08-29 2008-08-29

Publications (1)

Publication Number Publication Date
PE20090814A1 true PE20090814A1 (es) 2009-06-27

Family

ID=40149549

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001740A PE20090814A1 (es) 2007-10-09 2008-10-07 Cis-imidazolinas quirales

Country Status (20)

Country Link
US (1) US8513239B2 (es)
EP (2) EP2203437B1 (es)
JP (1) JP5324586B2 (es)
KR (1) KR101203020B1 (es)
CN (2) CN104710408A (es)
AR (1) AR068742A1 (es)
AU (1) AU2008309759A1 (es)
BR (1) BRPI0817850A2 (es)
CA (1) CA2701932C (es)
CL (1) CL2008002982A1 (es)
CO (1) CO6280486A2 (es)
CR (1) CR11333A (es)
ES (1) ES2395210T3 (es)
IL (1) IL204653A0 (es)
MA (1) MA31754B1 (es)
MX (1) MX2010003868A (es)
PE (1) PE20090814A1 (es)
RU (1) RU2487127C2 (es)
TW (1) TW200916446A (es)
WO (1) WO2009047161A1 (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2375899B1 (en) * 2009-01-12 2015-02-25 Array Biopharma Inc. Piperidine-containing compounds and use thereof in the treatment of diabetes
US8389731B2 (en) * 2009-05-15 2013-03-05 Northwestern University Chiral pyrrolidine core compounds en route to inhibitors of nitric oxide synthase
JP5658272B2 (ja) 2009-12-17 2015-01-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2の新規アンタゴニスト及びこれらの使用
PT3091012T (pt) 2009-12-17 2018-06-27 Centrexion Therapeutics Corp Antagonistas do receptor ccr2 e suas utilizações
JP2013526507A (ja) 2010-05-12 2013-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ccr2受容体アンタゴニスト、その製造方法及び薬物としてのその使用
JP5636094B2 (ja) 2010-05-25 2014-12-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2受容体アンタゴニスト
EP2576538B1 (en) 2010-06-01 2015-10-28 Boehringer Ingelheim International GmbH New CCR2 antagonists
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
CA2813256A1 (en) 2010-09-30 2012-04-05 St. Jude Children's Research Hospital Aryl-substituted imidazoles
WO2012080389A1 (en) 2010-12-16 2012-06-21 Roche Glycart Ag Combination therapy of an afucosylated cd20 antibody with a mdm2 inhibitor
CA2850166C (en) 2011-09-27 2019-12-03 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
WO2014082889A1 (en) * 2012-11-28 2014-06-05 F. Hoffmann-La Roche Ag Novel imidazolines as dual inhibitors of mdm2 and mdmx
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US11407721B2 (en) 2013-02-19 2022-08-09 Amgen Inc. CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
MX368703B (es) 2013-02-28 2019-10-11 Amgen Inc Un inhibidor de mdm2 derivado de acido benzoico para el tratamiento del cancer.
RU2737434C2 (ru) 2013-03-13 2020-11-30 Форма Терапьютикс, Инк. Новые соединения и композиции для ингибирования fasn
WO2014151863A1 (en) 2013-03-14 2014-09-25 Amgen Inc. Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
US10758525B2 (en) 2015-01-22 2020-09-01 MyoKardia, Inc. 4-methylsulfonyl-substituted piperidine urea compounds
PL3458101T3 (pl) 2016-05-20 2021-05-31 F. Hoffmann-La Roche Ag Koniugaty PROTAC-przeciwciało i sposoby ich stosowania
CN105906610B (zh) * 2016-05-24 2018-10-23 绍兴文理学院 一种3-(4-苯基-1h-咪唑-5-基)-1h-吲哚衍生物及其制备方法和应用
PL3415802T3 (pl) 2017-06-14 2020-03-31 Borealis Ag Dylatacja
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02101065A (ja) 1988-10-06 1990-04-12 Tanabe Seiyaku Co Ltd イミダゾリン誘導体及びその製法
GB2351082A (en) 1999-06-18 2000-12-20 Lilly Forschung Gmbh Synthesis of Cyclic Substituted Amidines
EP1463501B1 (en) * 2001-12-18 2008-06-11 F. Hoffmann-La Roche AG Cis-imidazolines as mdm2 inhibitors
JP4477351B2 (ja) 2001-12-18 2010-06-09 エフ.ホフマン−ラ ロシュ アーゲー シス−2,4,5−トリフェニル−イミダゾリン類及び腫瘍の処理へのそれらの使用
ATE414693T1 (de) 2004-05-18 2008-12-15 Hoffmann La Roche Neuartige cis-imidazoline
ES2377752T5 (es) 2005-07-08 2016-03-14 Vestas Wind Systems A/S Turbina eólica, buje para turbina eólica y uso del mismo
EP2130822A1 (en) * 2005-12-01 2009-12-09 F. Hoffmann-La Roche AG 2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between p53 and mdm2 proteins for use as anticancer agents
CN101370799B (zh) * 2006-01-18 2012-09-05 霍夫曼-拉罗奇有限公司 作为mdm2抑制剂的顺-4,5-二芳基-2-杂环-咪唑啉

Also Published As

Publication number Publication date
IL204653A0 (en) 2010-11-30
BRPI0817850A2 (pt) 2015-04-07
RU2487127C2 (ru) 2013-07-10
ES2395210T3 (es) 2013-02-11
TW200916446A (en) 2009-04-16
CN104710408A (zh) 2015-06-17
MX2010003868A (es) 2010-04-27
KR20100051742A (ko) 2010-05-17
CO6280486A2 (es) 2011-05-20
JP5324586B2 (ja) 2013-10-23
EP2203437B1 (en) 2012-11-07
EP2325180A1 (en) 2011-05-25
KR101203020B1 (ko) 2012-11-20
RU2010118018A (ru) 2011-11-20
CL2008002982A1 (es) 2009-10-16
CA2701932C (en) 2015-10-20
CN101821251A (zh) 2010-09-01
US8513239B2 (en) 2013-08-20
MA31754B1 (fr) 2010-10-01
CA2701932A1 (en) 2009-04-16
JP2010540675A (ja) 2010-12-24
US20090111789A1 (en) 2009-04-30
CR11333A (es) 2010-06-21
AU2008309759A1 (en) 2009-04-16
EP2203437A1 (en) 2010-07-07
AR068742A1 (es) 2009-12-02
WO2009047161A1 (en) 2009-04-16

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