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DK0873123T3 - Inhibitorer af protein-isoprenyltransferaser - Google Patents

Inhibitorer af protein-isoprenyltransferaser

Info

Publication number
DK0873123T3
DK0873123T3 DK96938647T DK96938647T DK0873123T3 DK 0873123 T3 DK0873123 T3 DK 0873123T3 DK 96938647 T DK96938647 T DK 96938647T DK 96938647 T DK96938647 T DK 96938647T DK 0873123 T3 DK0873123 T3 DK 0873123T3
Authority
DK
Denmark
Prior art keywords
heterocyclic
formula
inhibitors
protein isoprenyl
transferases
Prior art date
Application number
DK96938647T
Other languages
Danish (da)
English (en)
Inventor
Said M Sebti
Andrew D Hamilton
Saul H Rosenberg
David J Augeri
Kenneth J Barr
Bernard G Donner
Stephen A Fakhhoury
David A Janowick
Douglas M Kalvin
John J Larsen
Gang Liu
Stephen J O'connor
Wang Shen
Rolf E Swenson
Bryan K Sorenson
Gerard M Sullivan
Bruce Szczepankiewicz
Andrew S Tasker
James T Wasicak
Martin Winn
Original Assignee
Univ Pittsburgh
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 Univ Pittsburgh filed Critical Univ Pittsburgh
Application granted granted Critical
Publication of DK0873123T3 publication Critical patent/DK0873123T3/da

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    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • 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
    • C07D213/62—Oxygen or sulfur atoms
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    • 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
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    • 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
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    • 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
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    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

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DK96938647T 1995-11-06 1996-11-05 Inhibitorer af protein-isoprenyltransferaser DK0873123T3 (da)

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US724795P 1995-11-06 1995-11-06
PCT/US1996/017092 WO1997017070A1 (en) 1995-11-06 1996-11-05 Inhibitors of protein isoprenyl transferases

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EP (1) EP0873123B1 (de)
JP (1) JP4533466B2 (de)
AT (1) ATE236632T1 (de)
AU (1) AU7597596A (de)
CA (1) CA2235986C (de)
DE (1) DE69627377T2 (de)
DK (1) DK0873123T3 (de)
ES (1) ES2196186T3 (de)
MX (1) MX9803589A (de)
PT (1) PT873123E (de)
WO (1) WO1997017070A1 (de)
ZA (1) ZA969273B (de)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6693123B2 (en) * 1995-11-06 2004-02-17 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
US6117641A (en) 1996-04-11 2000-09-12 Mitotix, Inc. Assays and reagents for identifying anti-fungal agents and uses related thereto
US6727082B1 (en) 1996-04-11 2004-04-27 Gpc Biotech Inc. Assays and reagents for identifying anti-fungal agents, and uses related thereto
DE69713759T2 (de) 1996-04-11 2003-03-13 Mitotix, Inc. Assays und reaganzien zur identifizierung von fungiziden wirkstoffen und ihre verwendungen
ZA981080B (en) 1997-02-11 1998-08-12 Warner Lambert Co Bicyclic inhibitors of protein farnesyl transferase
WO1998050031A1 (en) 1997-05-07 1998-11-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
GB9801231D0 (en) 1997-06-05 1998-03-18 Merck & Co Inc A method of treating cancer
FR2766819B1 (fr) * 1997-07-31 1999-10-29 Pf Medicament Nouvelles sulfonamides derivees d'anilines substituees utiles comme medicaments
JP2001520222A (ja) * 1997-10-22 2001-10-30 ゼネカ・リミテッド イミダゾール誘導体およびファルネシルタンパク質トランスフェラーゼインヒビターとしてのそれらの使用
DK1025088T3 (da) 1997-10-22 2001-11-12 Astrazeneca Ab Imidazolderivater og deres anvendelse som farnesylproteintransferaseinhibitorer
GB9809889D0 (en) 1998-05-11 1998-07-08 Univ Strathclyde Prevention of restenosis
US6277871B1 (en) 1998-11-20 2001-08-21 Abbott Laboratories Inhibitors of protein isoprenyl transferases
AU2478500A (en) 1998-12-08 2000-06-26 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US6284755B1 (en) 1998-12-08 2001-09-04 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2000039716A2 (en) * 1998-12-23 2000-07-06 Astrazeneca Ab Arylpropenylimidazoles as farnesyl-protein transferase inhibitors
US6518292B1 (en) * 1999-03-12 2003-02-11 Bristol-Myers Squibb Co. Heterocyclic aromatic compounds usefuls as growth hormone secretagogues
AU2001230864A1 (en) 2000-01-12 2001-07-24 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
EP1261374A2 (de) * 2000-02-29 2002-12-04 Janssen Pharmaceutica N.V. Kombination von farnesyl proteintransferase mit weiteren therapeutisch wirksamen antikrebsmitteln
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
PE20070335A1 (es) 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
WO2007069020A2 (en) 2005-12-15 2007-06-21 Vicuron Pharmaceuticals Inc. N-hydroxyamide derivatives possessing antibacterial activity
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
US7994205B2 (en) 2006-03-31 2011-08-09 Takeda Pharmaceutical Company Limited Aryl-or heteroaryl-sulfonyl compounds as acid secretion inhibitors
ES2654847T3 (es) 2006-04-19 2018-02-15 Novartis Ag Compuestos de benzoxazol y benzotiazol sustituidos en 6-O y métodos para inhibir la señalización CSF-1R
EP2946778A1 (de) 2006-09-22 2015-11-25 Merck Sharp & Dohme Corp. Behandlungsverfahren mit verwendung von fettsäuresyntheseinhibitoren
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
BRPI0806245B1 (pt) 2007-01-10 2022-01-25 Msd Italia S.R.L. Compostos de fórmula i e seus usos
EA019951B1 (ru) 2007-03-01 2014-07-30 Новартис Аг Ингибиторы киназы pim и способы их применения
US8293769B2 (en) 2007-05-21 2012-10-23 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
KR101657323B1 (ko) * 2008-11-19 2016-09-13 포라 가세이 고교 가부시키가이샤 주름 개선제
CN101445468B (zh) * 2008-12-25 2012-02-01 西南大学 对氨基苯甲酸拟二肽酯及其制备方法和应用
US8895588B2 (en) 2009-03-26 2014-11-25 Takeda Pharmaceutical Company Limited Pyrazole compound
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JP6073677B2 (ja) 2009-06-12 2017-02-01 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 縮合複素環式化合物およびそれらの使用
NZ599343A (en) 2009-10-14 2014-05-30 Merck Sharp & Dohme Substituted piperidines that increase p53 activity and the uses thereof
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
JP2013522292A (ja) 2010-03-16 2013-06-13 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド インダゾール化合物およびそれらの使用
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
EP2608669B1 (de) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. Neue pyrazolo-[1,5-a-]pyrimidinderivate als mtor-hemmer
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
WO2012036997A1 (en) 2010-09-16 2012-03-22 Schering Corporation Fused pyrazole derivatives as novel erk inhibitors
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA)
EP2654748B1 (de) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
US20140046059A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Process for the preparation of morpholino sulfonyl indole derivatives
CN103012310A (zh) * 2011-09-23 2013-04-03 上海医药工业研究院 一种噻唑类化合物的制备方法
EP2760833A1 (de) * 2011-09-30 2014-08-06 Endo Pharmaceuticals Inc. Pyridinderivate
US8809372B2 (en) 2011-09-30 2014-08-19 Asana Biosciences, Llc Pyridine derivatives
EP2770987B1 (de) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Neue verbindungen als erk-hemmer
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
JP6280554B2 (ja) 2012-09-28 2018-02-14 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｅｒｋ阻害剤である新規化合物
EP2909194A1 (de) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Hemmer der cyclinabhängigen kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
AU2013352568B2 (en) 2012-11-28 2019-09-19 Merck Sharp & Dohme Llc Compositions and methods for treating cancer
JP6387013B2 (ja) 2012-12-20 2018-09-12 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｄｍ２阻害薬としての置換されたイミダゾピリジン類
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3057955B1 (de) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Zur behandlung von proliferativen erkrankungen geeignete heteroaromatische verbindungen
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3307728A4 (de) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. Kombinationstherapie von transkriptionshemmern und kinasehemmern
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CN105294415A (zh) * 2015-09-11 2016-02-03 烟台九目化学制品有限公司 一种3-卤代芴酮类化合物的制备方法
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
CN118267470A (zh) 2017-04-13 2024-07-02 赛罗帕私人有限公司 抗SIRPα抗体
EP3706747A4 (de) 2017-11-08 2021-08-04 Merck Sharp & Dohme Corp. Prmt5-inhibitoren
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
CA3099763A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833667B1 (de) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5-inhibitoren
KR20210046009A (ko) 2018-08-07 2021-04-27 머크 샤프 앤드 돔 코포레이션 Prmt5 억제제
US12281126B2 (en) 2018-12-28 2025-04-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
AU2024228641A1 (en) 2023-03-02 2025-07-24 Carcimun Biotech Gmbh Means and methods for diagnosing cancer and/or an acute inflammatory disease

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1615895A (en) * 1994-03-31 1995-10-12 Bristol-Myers Squibb Company Imidazole-containing inhibitors of farnesyl protein transferase

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DE69627377D1 (de) 2003-05-15
EP0873123A1 (de) 1998-10-28
EP0873123A4 (de) 1999-02-03
WO1997017070A1 (en) 1997-05-15
CA2235986A1 (en) 1997-05-15
CA2235986C (en) 2006-09-12
EP0873123B1 (de) 2003-04-09
ATE236632T1 (de) 2003-04-15
JP4533466B2 (ja) 2010-09-01
AU7597596A (en) 1997-05-29
JP2000500745A (ja) 2000-01-25
MX9803589A (es) 1998-11-30
ZA969273B (en) 1998-05-05
PT873123E (pt) 2003-08-29
DE69627377T2 (de) 2004-02-05
ES2196186T3 (es) 2003-12-16

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