DE69520499D1 - Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe - Google Patents

Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe

Info

Publication number
DE69520499D1
DE69520499D1 DE69520499T DE69520499T DE69520499D1 DE 69520499 D1 DE69520499 D1 DE 69520499D1 DE 69520499 T DE69520499 T DE 69520499T DE 69520499 T DE69520499 T DE 69520499T DE 69520499 D1 DE69520499 D1 DE 69520499D1
Authority
DE
Germany
Prior art keywords
homohistidine
histidine
derivatives
protein farnesyltransferase
farnesyltransferase inhibitors
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 - Fee Related
Application number
DE69520499T
Other languages
English (en)
Other versions
DE69520499T2 (de
Inventor
Louis Bolton
Cooke Hodges
William Wilson
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.)
Warner Lambert Co LLC
Original Assignee
Warner Lambert Co LLC
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 Warner Lambert Co LLC filed Critical Warner Lambert Co LLC
Application granted granted Critical
Publication of DE69520499D1 publication Critical patent/DE69520499D1/de
Publication of DE69520499T2 publication Critical patent/DE69520499T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147—Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
DE69520499T 1994-06-30 1995-05-30 Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe Expired - Fee Related DE69520499T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/268,364 US5571792A (en) 1994-06-30 1994-06-30 Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
PCT/US1995/006660 WO1996000736A1 (en) 1994-06-30 1995-05-30 Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase

Publications (2)

Publication Number Publication Date
DE69520499D1 true DE69520499D1 (de) 2001-05-03
DE69520499T2 DE69520499T2 (de) 2001-07-26

Family

ID=23022659

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69520499T Expired - Fee Related DE69520499T2 (de) 1994-06-30 1995-05-30 Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe

Country Status (17)

Country Link
US (1) US5571792A (de)
EP (1) EP0767800B1 (de)
JP (1) JPH10502078A (de)
AT (1) ATE200085T1 (de)
AU (1) AU699629B2 (de)
CA (1) CA2190977A1 (de)
DE (1) DE69520499T2 (de)
DK (1) DK0767800T3 (de)
ES (1) ES2158115T3 (de)
GR (1) GR3035936T3 (de)
HR (1) HRP950337B1 (de)
MX (1) MX9605945A (de)
NO (1) NO315427B1 (de)
NZ (1) NZ287696A (de)
PT (1) PT767800E (de)
WO (1) WO1996000736A1 (de)
ZA (1) ZA955411B (de)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5756528A (en) * 1995-06-06 1998-05-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5972984A (en) * 1995-06-06 1999-10-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JPH11509204A (ja) * 1995-07-13 1999-08-17 ユニバーシテイ・オブ・シンシナテイ 神経線維腫症の治療に有用な化合物
US6008372A (en) * 1996-01-16 1999-12-28 Warner-Lambert Company Substituted dinaphthylmethyl and diheteroarylmethylacetyl histidine inhibitors of protein farnesyltransferase
AU703203B2 (en) * 1996-01-30 1999-03-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000504017A (ja) * 1996-01-30 2000-04-04 メルク エンド カンパニー インコーポレーテッド ファルネシル―タンパク質転移酵素の阻害剤
US5968965A (en) * 1996-01-30 1999-10-19 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5981562A (en) * 1996-01-30 1999-11-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997027853A1 (en) * 1996-01-30 1997-08-07 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507586A (ja) * 1996-04-03 2000-06-20 メルク エンド カンパニー インコーポレーテッド ファルネシル―タンパク質転移酵素の阻害剤
US5922883A (en) * 1996-04-03 1999-07-13 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6300501B1 (en) * 1996-05-22 2001-10-09 Warner-Lambert Company Histidine-(N-benzyl glycinamide) inhibitors of protein farnesyl transferase
EA199801031A1 (ru) * 1996-05-22 1999-06-24 Варнер-Ламберт Компани Ингибиторы протеинфарнезилтрансферазы
US6093816A (en) 1996-06-27 2000-07-25 Isis Pharmaceuticals, Inc. Cationic lipids
IL121203A (en) * 1996-07-01 2001-04-30 Lilly Co Eli 1, 2, 3, 4-tetrahydroisoquinidines, process for their preparation and pharmaceutical compositions containing the same for treating hyperglycemia and hyperlipidemia
US6015817A (en) * 1996-12-05 2000-01-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5977134A (en) * 1996-12-05 1999-11-02 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5972966A (en) * 1996-12-05 1999-10-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5932590A (en) * 1996-12-05 1999-08-03 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
BR9713744A (pt) 1996-12-17 2000-03-21 Warner Lambert Co Inibidores de cicloalquia da proteìna farnesil transferase
US6737410B1 (en) 1997-04-11 2004-05-18 Warner-Lambert Company Inhibitors of protein farnesyl transferase
WO1998046625A1 (en) * 1997-04-11 1998-10-22 Warner-Lambert Company Dipeptide inhibitors of protein farnesyltransferase
US6060038A (en) * 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
US6792084B1 (en) * 1997-09-08 2004-09-14 Mci, Inc. Single telephone number access to multiple communications services
DE69914893T2 (de) * 1998-04-27 2004-07-22 Warner-Lambert Co. Llc Glycinamidederivate mit funktionalisierter alkyl- und alkenylseitenkette als inhibitoren der farnesyltransferase
CA2331295A1 (en) 1998-05-12 1999-11-18 Warner-Lambert Company Combinations of protein farnesyltransferase and hmg coa reductase inhibitors and their use to treat cancer
US6458935B1 (en) 1999-06-23 2002-10-01 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
US6624147B1 (en) 1999-09-28 2003-09-23 Rijksuniversiteit Leiden Inhibitors of prenylated pyrophosphate consuming enzymes
EP1090909A1 (de) * 1999-09-28 2001-04-11 Rijksuniversiteit Leiden Hemmer für Enzyme, die Prenylpyrophosphate umsetzen
EP1496982A4 (de) * 2002-04-16 2006-07-19 Merck & Co Inc Feste formen von salzen mit tyrosinkinase-wirkung
JP4866233B2 (ja) * 2003-04-29 2012-02-01 ウニヴェルジテート・チューリッヒ ｆａｃ配位により高効率で［Ｍ（ＯＨ２）３（ＣＯ）３］＋標識化するために生体分子にカップリングさせるための、Ｎεおよび／またはＮαで誘導体化され、金属および有機保護されたＬ−ヒスチジン
WO2005049589A2 (en) * 2003-10-14 2005-06-02 Cadila Healthcare Limited Heterocyclic compounds for the treatment of hyperlipidemia, diabetes, obesity and similar diseases
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
TW200804345A (en) 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
TW200806284A (en) * 2006-03-31 2008-02-01 Alcon Mfg Ltd Prenyltransferase inhibitors for ocular hypertension control and the treatment of glaucoma
LT2010528T (lt) 2006-04-19 2017-12-27 Novartis Ag 6-o-pakeistieji benzoksazolo junginiai bei csf-1r signalo perdavimo slopinimo būdai
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
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
BRPI0808523A2 (pt) 2007-03-01 2014-08-19 Novartis Vaccines & Diagnostic Inibidores de pim cinase e métodos de seu uso
CA2685967A1 (en) 2007-05-21 2008-11-21 Novartis Ag Csf-1r inhibitors, compositions, and methods of use
EP2170076B1 (de) 2007-06-27 2016-05-18 Merck Sharp & Dohme Corp. 4-carboxybenzylamino-derivate als histondeacetylase-hemmer
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
WO2011046771A1 (en) 2009-10-14 2011-04-21 Schering Corporation SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
CN103080093A (zh) 2010-03-16 2013-05-01 达纳－法伯癌症研究所公司 吲唑化合物及其应用
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel 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)
WO2012024170A2 (en) 2010-08-17 2012-02-23 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
EP2615916B1 (de) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Kondensierte pyrazolderivate als neue erk-hemmer
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
JP2014514321A (ja) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子１受容体阻害剤
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent 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
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
MX363243B (es) 2012-11-28 2019-03-14 Merck Sharp & Dohme Composiciones para tratar cáncer y usos de dichas composiciones.
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
JP6491202B2 (ja) 2013-10-18 2019-03-27 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 サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
WO2016105528A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
EP3307728A4 (de) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. Kombinationstherapie von transkriptionshemmern und kinasehemmern
EP4019515A1 (de) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Hemmer von cyclinabhängigen kinasen
CA3032046A1 (en) 2016-09-16 2018-03-22 Research Triangle Institute Tetrahydroisoquinoline kappa opioid antagonists
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
AU2018252546A1 (en) 2017-04-13 2019-10-10 Sairopa B.V. Anti-SIRPα antibodies
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
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668A4 (de) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. Prmt5-inhibitoren

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5141851A (en) * 1990-04-18 1992-08-25 Board Of Regents, The University Of Texas System Isolated farnesyl protein transferase enzyme
CA2044333A1 (en) * 1990-06-12 1991-12-13 Jackson B. Gibbs Chemotherapeutic agents
US5260276A (en) * 1991-06-14 1993-11-09 Warner-Lambert Company Linear and monocyclic endothelin antagonists
CA2072033A1 (en) * 1991-06-28 1992-12-29 Jackson B. Gibbs Non-substrate inhibitors of farnesyl protein transferase
CA2072048A1 (en) * 1991-06-28 1992-12-29 Jackson B. Gibbs Non-substrate inhibitors of farnesyl protein transferase
EP0528486A2 (de) * 1991-08-16 1993-02-24 Merck & Co. Inc. Nicht-Substrat Inhibitor des Farnesyl-Protein-Transferases
US5340828A (en) * 1991-09-30 1994-08-23 Merck & Co., Inc. Inhibitors of farnesyl protein transferase
US5352705A (en) * 1992-06-26 1994-10-04 Merck & Co., Inc. Inhibitors of farnesyl protein transferase
US5464820A (en) * 1993-06-22 1995-11-07 The University Hospital Specific inhibitors of tissue kallikrein
CA2172125A1 (en) * 1993-09-30 1995-04-06 S. Jane Desolms Inhibitors of farnesyl-protein transferase

Also Published As

Publication number Publication date
ZA955411B (en) 1996-02-05
GR3035936T3 (en) 2001-08-31
AU2650495A (en) 1996-01-25
ATE200085T1 (de) 2001-04-15
AU699629B2 (en) 1998-12-10
NO315427B1 (no) 2003-09-01
DE69520499T2 (de) 2001-07-26
ES2158115T3 (es) 2001-09-01
US5571792A (en) 1996-11-05
JPH10502078A (ja) 1998-02-24
DK0767800T3 (da) 2001-06-18
WO1996000736A1 (en) 1996-01-11
MX9605945A (es) 1997-12-31
NZ287696A (en) 1997-12-19
CA2190977A1 (en) 1996-01-11
PT767800E (pt) 2001-08-30
EP0767800B1 (de) 2001-03-28
HRP950337A2 (en) 1997-08-31
HRP950337B1 (en) 2001-12-31
NO965604D0 (no) 1996-12-27
EP0767800A1 (de) 1997-04-16
NO965604L (no) 1997-02-25

Similar Documents

Publication Publication Date Title
DE69520499T2 (de) Histidine und homohistidine derivate zur verwendung als protein farnesyltransferase hemmstoffe
ES2157994T3 (es) Inhibidores tetra y pentapeptidos sustituidos de la proteina farnesiltransferasa.
NO20061736L (no) Krystallform av epotilon B
BR0315688A (pt) Compostos, composições farmacêuticas e seus usos no tratamento ou prevenção de doenças ou condições de proliferação celular metabólicas
ATE311853T1 (de) Verwendung von krillenzymen zur behandlung von zahnbelag
DE60021381D1 (de) Chinonverbindungen zur behandlung von krankheiten
DE69728165D1 (de) Cycloalkyl inhibitoren der protein-farnesyltransferase
HK1074840A1 (en) Novel dithiolopyrrolones with therapeutic activity
AU2576901A (en) Agents and methods for the treatment of proliferative diseases
ECSP972339A (es) Inhibidores de cicloalquilo de la farnesil transferasa de las proteinas
DE50200757D1 (de) Verwendung von tryptophan-derivaten zur spezifischen zytostatischen behandlung von serotonin-produzierenden tumoren
AU2990300A (en) Deglycosylated kringle 1-5 region fragments of plasminogen and methods of use
MX9703208A (es) Tetra-y pentapeptidos substituidos inhibidores de proteina; farnesil transferasa.
ATE327240T1 (de) 2ß OXO-VORUSCHARIN UND DERIVATEN

Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee