NO973607L - New farnesyl transferase inhibitors, their preparation and preparations containing the inhibitors - Google Patents
New farnesyl transferase inhibitors, their preparation and preparations containing the inhibitorsInfo
- Publication number
- NO973607L NO973607L NO973607A NO973607A NO973607L NO 973607 L NO973607 L NO 973607L NO 973607 A NO973607 A NO 973607A NO 973607 A NO973607 A NO 973607A NO 973607 L NO973607 L NO 973607L
- Authority
- NO
- Norway
- Prior art keywords
- residue
- alkyl
- optionally substituted
- radical
- hydrogen atom
- Prior art date
Links
Classifications
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
- C07K5/1013—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Abstract
Famesyltransferaselnhlbltorer med den generelle formel (I) der R]^ betyr Y-S-A^, (der Y er et hydrogenatom, en aralnosyrerest, en fettsyrerest, en alkyl- eller alkoksykarbonylrest eller R', en rest R4-S, der R4 er en C .-alkylrest, eventuelt substituert med en fenylrest, eller en rest med den generelle formel (II): (I) ¦S-A, ^1 I X. III) der Aj^. X^. Y^, R2' ^'2. ^2' ^2- ^' ^3- ^'3 og R er som angitt nedenfor. Idet A^ er en C. ,-alkylenrest, eventuelt ^ ' ^-" ' Q-substltuert 1 >C(Xj)(Yi )-gruppen med amino-, alkylamino-, alkanoylamino- eller alkoksykarbonylamlnorest); ^1 °S ^i hver er et hydrogenatoro eller, saninen med karbon- atomet, hvortil de er bundet, danner en >C-0-gruppe; R2 er en rett eller forgrenet C^_^-al kyl rest sen eventuelt er substituert med en cykloheksylrest; R'2 er hydrogen eller alkyl; X2 og Y2 hver er et hydrogenatam eller, sairmen med karbonatomet, hvortil de er bundet, danner en >C-0-gruppe; R3 er en C^_^-alkylrest som eventuelt er substituert med hydroksy, alkoksy, merkapto, alkyltio, alkylsulfinyl eller alkylsulfonyl, forutsatt at, når R3 er en alkylrest som er substituert med en hydroksyrest, kan R3 danne et lakton med a-karboksyresten; R'3 er hi'drogen eller alkyl; X er et oksygen- eller svovelatom; og R er et hydrogenatom eller en eventuelt substituert alkylrest eller en eventuelt substituert fenylrest. Disse produkter har Interessante antl-cancer-egenskaper ogdet beskrives videre preparater inneholdende forbindelsene.Famesyl transferase inhibitors of the general formula (I) wherein R 1 represents YSA 2, (where Y is a hydrogen atom, an aralnosuric residue, a fatty acid residue, an alkyl or alkoxycarbonyl residue or R ', a residue R 4 -S where R 4 is a C). -alkyl radical, optionally substituted with a phenyl radical, or a radical of the general formula (II): X ^. Y 2, R 2 '2' 2. ^ 2 '^ 2- ^' ^ 3- ^ '3 and R are as given below. As A ^ is a C ,alkyl alkylene residue, optionally '^ - "Q substituted 1> C (Xj) (Yi) group of amino, alkylamino, alkanoylamino or alkoxycarbonylamino residue); in each is a hydrogen atom or, the sanine with the carbon atom to which they are attached forms a> C-O group; R 2 is a straight or branched C 1-6 alkyl radical, optionally substituted with a cyclohexyl residue; "2 is hydrogen or alkyl; X 2 and Y 2 are each a hydrogen atom or, with the carbon atom to which they are attached, form a> C-O group; R 3 is a C 1-6 alkyl residue optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulfinyl or alkylsulfonyl, provided that when R3 is an alkyl residue substituted by a hydroxy residue, R3 may form a lactone with the α-carboxylic residue; R'3 is hydrogen or alkyl; X is an oxygen radical or R is a hydrogen atom or an optionally substituted alkyl residue or an optionally substituted phenyl residue.These products have interesting anti-cancer properties and further preparations containing the compounds are described.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9501490A FR2730492B1 (en) | 1995-02-09 | 1995-02-09 | NOVEL FARNESYL TRANSFERASE INHIBITORS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| PCT/FR1996/000199 WO1996024612A1 (en) | 1995-02-09 | 1996-02-07 | Novel farnesyl transferase inhibitors, preparation thereof, and pharmaceutical compositions containing same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO973607D0 NO973607D0 (en) | 1997-08-05 |
| NO973607L true NO973607L (en) | 1997-08-05 |
Family
ID=9475981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO973607A NO973607L (en) | 1995-02-09 | 1997-08-05 | New farnesyl transferase inhibitors, their preparation and preparations containing the inhibitors |
Country Status (16)
| Country | Link |
|---|---|
| EP (1) | EP0808329A1 (en) |
| JP (1) | JPH10513468A (en) |
| KR (1) | KR19980702049A (en) |
| CN (1) | CN1173873A (en) |
| AU (1) | AU4722896A (en) |
| BR (1) | BR9607318A (en) |
| CA (1) | CA2210953A1 (en) |
| CZ (1) | CZ249997A3 (en) |
| FI (1) | FI973279A (en) |
| FR (1) | FR2730492B1 (en) |
| NO (1) | NO973607L (en) |
| PL (1) | PL321710A1 (en) |
| SK (1) | SK108897A3 (en) |
| TR (1) | TR199700726T1 (en) |
| WO (1) | WO1996024612A1 (en) |
| ZA (1) | ZA961073B (en) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2730491B1 (en) * | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | NOVEL FARNESYL TRANSFERASE INHIBITORS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| US5932590A (en) * | 1996-12-05 | 1999-08-03 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US6015817A (en) * | 1996-12-05 | 2000-01-18 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5972966A (en) * | 1996-12-05 | 1999-10-26 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5977134A (en) * | 1996-12-05 | 1999-11-02 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| FR2796943A1 (en) * | 1999-07-30 | 2001-02-02 | Aventis Pharma Sa | BENZOXAZINN DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR USE IN THERAPEUTICS |
| FR2796946A1 (en) * | 1999-07-30 | 2001-02-02 | Aventis Pharma Sa | NOVEL 8-CARBONYL CHROMAN DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE |
| ATE550019T1 (en) | 2005-05-17 | 2012-04-15 | Merck Sharp & Dohme | CIS-4-Ä(4-CHLOROPHENYL)SULFONYLÜ-4-(2,5-DIFLUOROPHENYL)CYCLOHEXANEPROPANE ACID FOR THE TREATMENT OF CANCER |
| GB0603041D0 (en) | 2006-02-15 | 2006-03-29 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| 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 |
| DK2805945T3 (en) | 2007-01-10 | 2019-07-15 | Msd Italia Srl | AMID-SUBSTITUTED INDAZOLS AS POLY (ADP-RIBOSE) POLYMERASE (PARP) REQUESTS |
| MX2009009304A (en) | 2007-03-01 | 2009-11-18 | Novartis Ag | Pim kinase inhibitors and methods of their use. |
| WO2008144062A1 (en) | 2007-05-21 | 2008-11-27 | Novartis Ag | Csf-1r inhibitors, compositions, and methods of use |
| EP2170076B1 (en) | 2007-06-27 | 2016-05-18 | Merck Sharp & Dohme Corp. | 4-carboxybenzylamino derivatives as histone deacetylase inhibitors |
| US8691825B2 (en) | 2009-04-01 | 2014-04-08 | Merck Sharp & Dohme Corp. | Inhibitors of AKT activity |
| EP2440058A4 (en) | 2009-06-12 | 2012-11-21 | Dana Farber Cancer Inst Inc | Fused heterocyclic compounds and their uses |
| UA109417C2 (en) | 2009-10-14 | 2015-08-25 | Мерк Шарп Енд Доме Корп. | Substituted piperidines, which improve activity of p53, and use thereof |
| EA201290919A1 (en) | 2010-03-16 | 2013-03-29 | Дана-Фарбер Кэнсер Инститьют, Инк. | INDASOLIC COMPOUNDS AND THEIR APPLICATION |
| EP2584903B1 (en) | 2010-06-24 | 2018-10-24 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| EP3330377A1 (en) | 2010-08-02 | 2018-06-06 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina) |
| KR102072631B1 (en) | 2010-08-17 | 2020-02-03 | 시르나 쎄러퓨틱스 인코퍼레이티드 | RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) |
| EP2608669B1 (en) | 2010-08-23 | 2016-06-22 | Merck Sharp & Dohme Corp. | NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| US9242981B2 (en) | 2010-09-16 | 2016-01-26 | Merck Sharp & Dohme Corp. | 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) |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| CN103732592A (en) | 2011-04-21 | 2014-04-16 | 默沙东公司 | Insulin-like growth factor-1 receptor inhibitors |
| US9023865B2 (en) | 2011-10-27 | 2015-05-05 | Merck Sharp & Dohme Corp. | Compounds that are ERK inhibitors |
| EP2822935B1 (en) | 2011-11-17 | 2019-05-15 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| EP3358013B1 (en) | 2012-05-02 | 2020-06-24 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
| US9233979B2 (en) | 2012-09-28 | 2016-01-12 | Merck Sharp & Dohme Corp. | Compounds that are ERK inhibitors |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| CA2892361A1 (en) | 2012-11-28 | 2014-06-05 | Merck Sharp & Dohme Corp. | Use of a wee1 inhibitor for treating a cancer characterized by low pkmyt1 expression levels |
| WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| 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 |
| WO2015058126A1 (en) | 2013-10-18 | 2015-04-23 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| JP6491202B2 (en) | 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 | Polycyclic inhibitors of cyclin dependent kinase 7 (CDK 7) |
| 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 (en) | 2014-08-06 | 2020-07-05 | Novartis Ag | Protein kinase c inhibitors and methods of their use |
| US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| JP6861166B2 (en) | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | Inhibitor of cyclin-dependent kinase |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| EP3347018B1 (en) | 2015-09-09 | 2021-09-01 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| JOP20190055A1 (en) | 2016-09-26 | 2019-03-24 | Merck Sharp & Dohme | Anti-cd27 antibodies |
| KR20190140454A (en) | 2017-04-13 | 2019-12-19 | 아두로 바이오테크 홀딩스, 유럽 비.브이. | Anti-SIRP alpha antibody |
| EP3706742B1 (en) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2019148412A1 (en) | 2018-02-01 | 2019-08-08 | Merck Sharp & Dohme Corp. | Anti-pd-1/lag3 bispecific antibodies |
| EP3833668A4 (en) | 2018-08-07 | 2022-05-11 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US20210309688A1 (en) | 2018-08-07 | 2021-10-07 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
Family Cites Families (5)
| 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 |
| CA2072033A1 (en) * | 1991-06-28 | 1992-12-29 | Jackson B. Gibbs | Non-substrate inhibitors of farnesyl protein transferase |
| CA2118985A1 (en) * | 1993-04-02 | 1994-10-03 | Dinesh V. Patel | Heterocyclic inhibitors of farnesyl protein transferase |
| WO1994026723A2 (en) * | 1993-05-14 | 1994-11-24 | Genentech, Inc. | ras FARNESYL TRANSFERASE INHIBITORS |
| US5439918A (en) * | 1994-03-14 | 1995-08-08 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
-
1995
- 1995-02-09 FR FR9501490A patent/FR2730492B1/en not_active Expired - Fee Related
-
1996
- 1996-02-07 TR TR97/00726T patent/TR199700726T1/en unknown
- 1996-02-07 SK SK1088-97A patent/SK108897A3/en unknown
- 1996-02-07 CZ CZ972499A patent/CZ249997A3/en unknown
- 1996-02-07 WO PCT/FR1996/000199 patent/WO1996024612A1/en not_active Application Discontinuation
- 1996-02-07 JP JP8524038A patent/JPH10513468A/en active Pending
- 1996-02-07 KR KR1019970705444A patent/KR19980702049A/en not_active Application Discontinuation
- 1996-02-07 CA CA002210953A patent/CA2210953A1/en not_active Abandoned
- 1996-02-07 CN CN96191866A patent/CN1173873A/en active Pending
- 1996-02-07 EP EP96903062A patent/EP0808329A1/en not_active Withdrawn
- 1996-02-07 BR BR9607318A patent/BR9607318A/en not_active Application Discontinuation
- 1996-02-07 PL PL96321710A patent/PL321710A1/en unknown
- 1996-02-07 AU AU47228/96A patent/AU4722896A/en not_active Abandoned
- 1996-02-09 ZA ZA961073A patent/ZA961073B/en unknown
-
1997
- 1997-08-05 NO NO973607A patent/NO973607L/en unknown
- 1997-08-08 FI FI973279A patent/FI973279A/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| NO973607D0 (en) | 1997-08-05 |
| SK108897A3 (en) | 1997-12-10 |
| MX9705969A (en) | 1997-11-29 |
| WO1996024612A1 (en) | 1996-08-15 |
| ZA961073B (en) | 1996-08-20 |
| EP0808329A1 (en) | 1997-11-26 |
| JPH10513468A (en) | 1998-12-22 |
| FR2730492B1 (en) | 1997-03-14 |
| CN1173873A (en) | 1998-02-18 |
| AU4722896A (en) | 1996-08-27 |
| FI973279A0 (en) | 1997-08-08 |
| PL321710A1 (en) | 1997-12-22 |
| TR199700726T1 (en) | 1998-01-21 |
| KR19980702049A (en) | 1998-07-15 |
| FI973279A (en) | 1997-08-08 |
| BR9607318A (en) | 1997-12-30 |
| CA2210953A1 (en) | 1996-08-15 |
| FR2730492A1 (en) | 1996-08-14 |
| CZ249997A3 (en) | 1997-11-12 |
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