WO1995012612A1 - Substituted di- and tripeptide inhibitors of protein:farnesyl transferase - Google Patents
Substituted di- and tripeptide inhibitors of protein:farnesyl transferase Download PDFInfo
- Publication number
- WO1995012612A1 WO1995012612A1 PCT/US1994/011553 US9411553W WO9512612A1 WO 1995012612 A1 WO1995012612 A1 WO 1995012612A1 US 9411553 W US9411553 W US 9411553W WO 9512612 A1 WO9512612 A1 WO 9512612A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- obn
- tyr
- cbz
- ser
- conh
- 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
- C07K5/06—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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Definitions
- the compounds of Formula I may be prepared by solid phase peptide synthesis on a peptide synthesizer, for example, an Applied Biosystems 431A peptide synthesizer using activated esters or anhydrides of Boc or Fmoc protected amino acids, acid chlorides, isocyanates, isothiocyanates, etc., on PAM, MBHA, or NH 2 -Rink resins with solution phase modifications to the carboxyl terminus as appropriate.
- Methodology for the solid phase synthesis of peptides is widely known to those skilled in the art thereof (see, for example: J.M. Stewart and J.D. Young in Solid Phase Peptide Synthesis: Pierce Chemical Co.; Rockford, IL (1984); Fields G.B. and Noble R.L.
- the compounds of Formula I may be prepared by simultaneous multiple solid phase syntheses using an apparatus described by S. H. DeWitt, et al. , Proc. Natl. Acad. Sci. USA. 9 . 0:6909 (1993), and referred to by the trademark, DiversomerTM, both trademark and apparatus being owned in whole by the Warner-Lambert Company.
- the multiple solid phase synthesis apparatus is currently the subject of now abandoned US Serial 07/958,383 filed October 8, 1992 and pending continuation-in-part US Serial 08/012,557 filed February 2, 1993.
- the pharmaceutical preparation is preferably in unit dosage form.
- the preparation is subdivided into unit doses containing appropriate quantities of the active component.
- the unit dosage form can be a packaged preparation, the package containing discrete quantities of preparation, such as packeted tablets, capsules, and powders in vials or ampoules.
- the unit dosage form can be a capsules, tablet, cachet, or lozenge itself, or it can be the appropriate number of any of these in packaged form.
- Step 3 BnNHCO-His (Tr) -Tyr(OBn) -Ser(OBn) -CQ 2 Me
- Example 20 by substituting Boc- ( ⁇ !-Me)Tyr(OBn) for Boc-Tyr(OBn) , the title compound was obtained, mp 66-78°C; ES-MS 690 (m+1) .
- EXAMPLE 23 N- (2-Phenylethyl) -N a - fN- f (phenylmethoxy) carbonyl! - L-histidyl! -0- (phenylmethyl) -L-tyrosinamide ⁇ Cbz-His-Tyr(OBn) -C0NHCH CH 2 Ph) According to Example 19, Step 3, by substituting
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Claims
Priority Applications (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP94930725A EP0730605A1 (en) | 1993-11-05 | 1994-10-12 | Substituted di- and tripeptide inhibitors of protein:farnesyl transferase |
NZ275691A NZ275691A (en) | 1993-11-05 | 1994-10-12 | Di and tripeptides and compositions thereof which inhibit farnesyl transferase |
JP51322495A JP3597863B2 (en) | 1993-11-05 | 1994-10-12 | Protein: substituted di- and tripeptide inhibitors of farnesyltransferase |
AU79760/94A AU681454B2 (en) | 1993-11-05 | 1994-10-12 | Substituted DI- and tripeptide inhibitors of protein:farnesyl transferase |
FI961819A FI961819A0 (en) | 1993-11-05 | 1996-04-29 | Substituted di- and tripeptide inhibitors of protein: farnesyl transferase |
NO961814A NO961814L (en) | 1993-11-05 | 1996-05-03 | Substituted di- and tripetide inhibitors for protein: farnesyl transferase |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14873593A | 1993-11-05 | 1993-11-05 | |
US30330194A | 1994-09-13 | 1994-09-13 | |
US08/148,735 | 1994-09-13 | ||
US08/303,301 | 1994-09-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1995012612A1 true WO1995012612A1 (en) | 1995-05-11 |
Family
ID=26846110
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1994/011553 WO1995012612A1 (en) | 1993-11-05 | 1994-10-12 | Substituted di- and tripeptide inhibitors of protein:farnesyl transferase |
Country Status (10)
Country | Link |
---|---|
EP (1) | EP0730605A1 (en) |
JP (1) | JP3597863B2 (en) |
KR (1) | KR100362338B1 (en) |
AU (1) | AU681454B2 (en) |
CA (1) | CA2170766A1 (en) |
FI (1) | FI961819A0 (en) |
HU (1) | HUT75308A (en) |
NO (1) | NO961814L (en) |
NZ (1) | NZ275691A (en) |
WO (1) | WO1995012612A1 (en) |
Cited By (75)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0675112A1 (en) * | 1994-03-31 | 1995-10-04 | Bristol-Myers Squibb Company | Imidazole-containing inhibitors of farnesyl protein transferase |
WO1996010034A2 (en) * | 1994-09-29 | 1996-04-04 | Merck & Co., Inc. | Thiol-free inhibitors of farnesyl-protein transferase |
FR2736641A1 (en) * | 1995-07-10 | 1997-01-17 | Rhone Poulenc Rorer Sa | NOVEL FARNESYL TRANSFERASE INHIBITORS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
EP0783318A1 (en) * | 1994-09-29 | 1997-07-16 | Merck & Co. Inc. | Inhibitors of farnesyl-protein transferase |
US5652257A (en) * | 1994-09-29 | 1997-07-29 | Merck & Co., Inc. | Heterocycle-containing inhibitors of farnesyl-protein transferase |
EP0787123A1 (en) * | 1994-09-29 | 1997-08-06 | Merck & Co. Inc. | Inhibitors of farnesyl-protein transferase |
WO1997044350A1 (en) * | 1996-05-22 | 1997-11-27 | Warner-Lambert Company | Inhibitors of protein farnesyl transferase |
US5756528A (en) * | 1995-06-06 | 1998-05-26 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
WO1998027109A1 (en) * | 1996-12-17 | 1998-06-25 | Warner-Lambert Company | Cycloalkyl inhibitors of protein farnesyltransferase |
FR2757855A1 (en) * | 1996-12-30 | 1998-07-03 | Rhone Poulenc Rorer Sa | NOVEL FARNESYL TRANSFERASE INHIBITORS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
EP0892797A1 (en) * | 1996-02-26 | 1999-01-27 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
US5968965A (en) * | 1996-01-30 | 1999-10-19 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
US5972984A (en) * | 1995-06-06 | 1999-10-26 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
WO1999055725A1 (en) * | 1998-04-27 | 1999-11-04 | Warner-Lambert Company | Functionalized alkyl and alkenyl side chain derivatives of glycinamides as farnesyl transferase inhibitors |
US5981562A (en) * | 1996-01-30 | 1999-11-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
US6013662A (en) * | 1996-12-30 | 2000-01-11 | Rhone-Poulenc Rorer S.A. | Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments |
WO2000034313A1 (en) * | 1998-12-10 | 2000-06-15 | F. Hoffmann-La Roche Ag | Procollagen c-proteinase inhibitors |
US6124465A (en) * | 1997-11-25 | 2000-09-26 | Rhone-Poulenc S.A. | Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments |
US6166052A (en) * | 1998-03-11 | 2000-12-26 | Warner-Lambert Company | Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers |
US6251919B1 (en) | 1998-02-27 | 2001-06-26 | Warner-Lambert | Heterocyclic substituted aniline calcium channel blockers |
US6291679B1 (en) | 1999-07-22 | 2001-09-18 | Rhone-Poulenc Rorer S.A. | Process for preparing benzoperhydroisoindole compounds |
US6300501B1 (en) | 1996-05-22 | 2001-10-09 | Warner-Lambert Company | Histidine-(N-benzyl glycinamide) inhibitors of protein farnesyl transferase |
US6423689B1 (en) | 1997-12-22 | 2002-07-23 | Warner-Lambert Company | Peptidyl calcium channel blockers |
US6441007B1 (en) | 1998-04-02 | 2002-08-27 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
US6627648B1 (en) | 1999-05-24 | 2003-09-30 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
WO2006123182A2 (en) | 2005-05-17 | 2006-11-23 | Merck Sharp & Dohme Limited | Cyclohexyl sulphones for treatment of cancer |
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---|---|---|---|---|
JPWO2005044780A1 (en) * | 2003-11-10 | 2007-05-17 | 杏林製薬株式会社 | Aminocarboxylic acid derivatives and their addition salts and S1P receptor modulators |
US8476305B2 (en) | 2008-02-07 | 2013-07-02 | Kyorin Pharmaceutical Co., Ltd. | Therapeutic agent or prophylactic agent for inflammatory bowel disease comprising amino alcohol derivative as active ingredient |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0523873A1 (en) * | 1991-06-28 | 1993-01-20 | Merck & Co. Inc. | Non-substrate peptide inhibitors of farnesyl protein transferase |
-
1994
- 1994-10-12 KR KR1019960702309A patent/KR100362338B1/en not_active IP Right Cessation
- 1994-10-12 AU AU79760/94A patent/AU681454B2/en not_active Ceased
- 1994-10-12 EP EP94930725A patent/EP0730605A1/en not_active Withdrawn
- 1994-10-12 WO PCT/US1994/011553 patent/WO1995012612A1/en not_active Application Discontinuation
- 1994-10-12 JP JP51322495A patent/JP3597863B2/en not_active Expired - Fee Related
- 1994-10-12 NZ NZ275691A patent/NZ275691A/en unknown
- 1994-10-12 HU HU9601193A patent/HUT75308A/en unknown
- 1994-10-12 CA CA002170766A patent/CA2170766A1/en not_active Abandoned
-
1996
- 1996-04-29 FI FI961819A patent/FI961819A0/en unknown
- 1996-05-03 NO NO961814A patent/NO961814L/en not_active Application Discontinuation
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0523873A1 (en) * | 1991-06-28 | 1993-01-20 | Merck & Co. Inc. | Non-substrate peptide inhibitors of farnesyl protein transferase |
Non-Patent Citations (2)
Title |
---|
K.MEDZIHRADSZKY ET AL: "Effect of secondary enzyme-substrate interactions on the cleavage of synthetic peptides by pepsin", BIOCHEMISTRY., vol. 9, no. 5, 3 March 1970 (1970-03-03), EASTON, PA US, pages 1154 - 1162 * |
T.R.HOLLANDS ET AL: "Action of pepsin on cationic synthetic substrates", BIOCHEMISTRY., vol. 8, no. 2, February 1969 (1969-02-01), EASTON, PA US, pages 575 - 585 * |
Cited By (118)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0675112A1 (en) * | 1994-03-31 | 1995-10-04 | Bristol-Myers Squibb Company | Imidazole-containing inhibitors of farnesyl protein transferase |
EP0787123A4 (en) * | 1994-09-29 | 1999-10-13 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase |
WO1996010034A2 (en) * | 1994-09-29 | 1996-04-04 | Merck & Co., Inc. | Thiol-free inhibitors of farnesyl-protein transferase |
EP0783318A4 (en) * | 1994-09-29 | 1999-10-20 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase |
WO1996010034A3 (en) * | 1994-09-29 | 1996-05-09 | Merck & Co Inc | Thiol-free inhibitors of farnesyl-protein transferase |
EP0783318A1 (en) * | 1994-09-29 | 1997-07-16 | Merck & Co. Inc. | Inhibitors of farnesyl-protein transferase |
US5652257A (en) * | 1994-09-29 | 1997-07-29 | Merck & Co., Inc. | Heterocycle-containing inhibitors of farnesyl-protein transferase |
EP0787123A1 (en) * | 1994-09-29 | 1997-08-06 | Merck & Co. Inc. | Inhibitors of farnesyl-protein transferase |
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 |
CN1096448C (en) * | 1995-07-10 | 2002-12-18 | 罗纳-布朗克·罗莱尔股份有限公司 | Farnesyl transferase inhibitors, its preparation and medicine composition thereof |
FR2736641A1 (en) * | 1995-07-10 | 1997-01-17 | Rhone Poulenc Rorer Sa | NOVEL FARNESYL TRANSFERASE INHIBITORS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
WO1997003050A1 (en) * | 1995-07-10 | 1997-01-30 | Rhone-Poulenc Rorer S.A. | 4,9-ethano-benzo(f)isoindole derivatives as farnesyl transferase inhibitors |
EA000797B1 (en) * | 1995-07-10 | 2000-04-24 | Рон-Пуленк Роре С.А. | Novel farnesyl transferase inhibitors, preparation thereof and pharmaceutical composition |
US5936097A (en) * | 1995-07-10 | 1999-08-10 | Rhone-Poulenc Rorer, S.A. | 4,9-ethano-benzo(F)isoindole derivatives as farnesyl transferase inhibitors |
US5981562A (en) * | 1996-01-30 | 1999-11-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
US5968965A (en) * | 1996-01-30 | 1999-10-19 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
EP1481975A1 (en) * | 1996-02-26 | 2004-12-01 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
EP0892797A1 (en) * | 1996-02-26 | 1999-01-27 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
EP0892797A4 (en) * | 1996-02-26 | 2004-10-20 | Bristol Myers Squibb Co | Inhibitors of farnesyl protein transferase |
WO1997044350A1 (en) * | 1996-05-22 | 1997-11-27 | Warner-Lambert Company | Inhibitors of protein farnesyl transferase |
US6300501B1 (en) | 1996-05-22 | 2001-10-09 | Warner-Lambert Company | Histidine-(N-benzyl glycinamide) inhibitors of protein farnesyl transferase |
US6281194B1 (en) | 1996-12-17 | 2001-08-28 | Warner-Lambert Company | Cycloalkyl inhibitors of protein farnesyltransferase |
WO1998027109A1 (en) * | 1996-12-17 | 1998-06-25 | Warner-Lambert Company | Cycloalkyl inhibitors of protein farnesyltransferase |
WO1998029390A1 (en) * | 1996-12-30 | 1998-07-09 | Rhone-Poulenc Rorer S.A. | Farnesyl transferase inhibitors |
US6013662A (en) * | 1996-12-30 | 2000-01-11 | Rhone-Poulenc Rorer S.A. | Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments |
US6218406B1 (en) | 1996-12-30 | 2001-04-17 | Aventis Pharma S.A. | Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments |
FR2757855A1 (en) * | 1996-12-30 | 1998-07-03 | Rhone Poulenc Rorer Sa | NOVEL FARNESYL TRANSFERASE INHIBITORS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
US6124465A (en) * | 1997-11-25 | 2000-09-26 | Rhone-Poulenc S.A. | Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments |
US6423689B1 (en) | 1997-12-22 | 2002-07-23 | Warner-Lambert Company | Peptidyl calcium channel blockers |
US6251919B1 (en) | 1998-02-27 | 2001-06-26 | Warner-Lambert | Heterocyclic substituted aniline calcium channel blockers |
US6166052A (en) * | 1998-03-11 | 2000-12-26 | Warner-Lambert Company | Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers |
US6989448B2 (en) | 1998-03-11 | 2006-01-24 | Lain-Yen Hu | Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers |
US6469038B1 (en) | 1998-03-11 | 2002-10-22 | Warner-Lambert Company | Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers |
US6441006B2 (en) | 1998-04-02 | 2002-08-27 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
US6441007B1 (en) | 1998-04-02 | 2002-08-27 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
WO1999055725A1 (en) * | 1998-04-27 | 1999-11-04 | Warner-Lambert Company | Functionalized alkyl and alkenyl side chain derivatives of glycinamides as farnesyl transferase inhibitors |
US6369034B1 (en) | 1998-04-27 | 2002-04-09 | Warner-Lambert Company | Functionalized alkyl and alenyl side chain derivatives of glycinamides as farnesyl transferase inhibitors |
US6951918B2 (en) | 1998-12-10 | 2005-10-04 | Syntex (U.S.A.) Llc | Peptidic procollagen C-proteinase inhibitors |
US6426402B1 (en) | 1998-12-10 | 2002-07-30 | Syntex (U.S.A.) Llc | Peptidic procollagen C-proteinase inhibitors |
WO2000034313A1 (en) * | 1998-12-10 | 2000-06-15 | F. Hoffmann-La Roche Ag | Procollagen c-proteinase inhibitors |
US6627648B1 (en) | 1999-05-24 | 2003-09-30 | Targacept, Inc. | Pharmaceutical compositions and methods for use |
US6291679B1 (en) | 1999-07-22 | 2001-09-18 | Rhone-Poulenc Rorer S.A. | Process for preparing benzoperhydroisoindole compounds |
WO2006123182A2 (en) | 2005-05-17 | 2006-11-23 | Merck Sharp & Dohme Limited | Cyclohexyl sulphones for treatment of cancer |
WO2007093827A1 (en) | 2006-02-15 | 2007-08-23 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Thiophene and thiazole substituted trifluoroethanone derivatives as histone deacetylase (hdac) inhibitors |
US8710048B2 (en) | 2006-04-19 | 2014-04-29 | Novartis Ag | 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling |
US7553854B2 (en) | 2006-04-19 | 2009-06-30 | Novartis Vaccines And Diagnostics, Inc. | 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling |
US8173689B2 (en) | 2006-04-19 | 2012-05-08 | Novartis Ag | 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling |
EP2946778A1 (en) | 2006-09-22 | 2015-11-25 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
EP2698157A1 (en) | 2006-09-22 | 2014-02-19 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
US11096950B2 (en) | 2006-11-01 | 2021-08-24 | Barbara Brooke Jennings | Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development |
EP2336120A1 (en) | 2007-01-10 | 2011-06-22 | Istituto di ricerche di Biologia Molecolare P. Angeletti S.R.L. | Combinations containing amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors |
EP2805945A1 (en) | 2007-01-10 | 2014-11-26 | MSD Italia S.r.l. | Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors |
WO2008106692A1 (en) | 2007-03-01 | 2008-09-04 | Novartis Vaccines And Diagnostics, Inc. | 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 |
WO2009002495A1 (en) | 2007-06-27 | 2008-12-31 | Merck & Co., Inc. | 4-carboxybenzylamino derivatives as histone deacetylase inhibitors |
EP3103791A1 (en) | 2007-06-27 | 2016-12-14 | Merck Sharp & Dohme Corp. | 4-carboxybenzylamino derivatives as histone deacetylase inhibitors |
WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
US9505784B2 (en) | 2009-06-12 | 2016-11-29 | Dana-Farber Cancer Institute, Inc. | Fused 2-aminothiazole compounds |
US8765747B2 (en) | 2009-06-12 | 2014-07-01 | Dana-Farber Cancer Institute, Inc. | Fused 2-aminothiazole compounds |
WO2011046771A1 (en) | 2009-10-14 | 2011-04-21 | Schering Corporation | SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF |
US11826365B2 (en) | 2009-12-29 | 2023-11-28 | Dana-Farber Cancer Institute, Inc. | Type II raf kinase inhibitors |
US8987275B2 (en) | 2010-03-16 | 2015-03-24 | Dana-Farber Cancer Institute, Inc. | Indazole compounds and their uses |
WO2011115725A2 (en) | 2010-03-16 | 2011-09-22 | Dana-Farber Cancer Institute, Inc. | Indazole compounds and their uses |
WO2011163330A1 (en) | 2010-06-24 | 2011-12-29 | 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) |
WO2012018754A2 (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) |
EP4079856A1 (en) | 2010-08-17 | 2022-10-26 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of hepatitis b virus (hbv) 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) |
WO2012027236A1 (en) | 2010-08-23 | 2012-03-01 | Schering Corporation | NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS |
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 |
EP3327125A1 (en) | 2010-10-29 | 2018-05-30 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina) |
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) |
EP3766975A1 (en) | 2010-10-29 | 2021-01-20 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina) |
WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
WO2012145471A1 (en) | 2011-04-21 | 2012-10-26 | Merck Sharp & Dohme Corp. | Insulin-like growth factor-1 receptor inhibitors |
US10172832B2 (en) | 2011-10-26 | 2019-01-08 | Allergan, Inc. | Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators |
US9974772B2 (en) | 2011-10-26 | 2018-05-22 | Allergan, Inc. | Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators |
US9351948B2 (en) | 2011-10-26 | 2016-05-31 | Allergan, Inc. | Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators |
US20140094614A1 (en) * | 2011-10-26 | 2014-04-03 | Allergan, Inc. | Amide derivatives of n-urea substituted amino acids as formyl peptide receptor like-1 (fprl-1) receptor modulators |
US10993931B2 (en) | 2011-10-26 | 2021-05-04 | Allergan, Inc. | Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators |
US9579307B2 (en) | 2011-10-26 | 2017-02-28 | Allergan, Inc. | Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators |
US8993780B2 (en) * | 2011-10-26 | 2015-03-31 | Allergan, Inc. | Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators |
WO2013063214A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
US10144730B2 (en) | 2011-11-17 | 2018-12-04 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
US10981903B2 (en) | 2011-11-17 | 2021-04-20 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
EP3919620A1 (en) | 2012-05-02 | 2021-12-08 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
WO2013165816A2 (en) | 2012-05-02 | 2013-11-07 | Merck Sharp & Dohme Corp. | SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS |
WO2014052563A2 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
US10787436B2 (en) | 2012-10-18 | 2020-09-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
US10000483B2 (en) | 2012-10-19 | 2018-06-19 | 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 |
WO2014085216A1 (en) | 2012-11-28 | 2014-06-05 | Merck Sharp & Dohme Corp. | Compositions and methods for treating cancer |
WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | 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 |
US11040957B2 (en) | 2013-10-18 | 2021-06-22 | Dana-Farber Cancer Institute, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
US10906889B2 (en) | 2013-10-18 | 2021-02-02 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
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 |
WO2016020864A1 (en) | 2014-08-06 | 2016-02-11 | Novartis Ag | Protein kinase c inhibitors and methods of their use |
EP3514151A1 (en) | 2014-08-06 | 2019-07-24 | 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) |
US10550121B2 (en) | 2015-03-27 | 2020-02-04 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
US11325910B2 (en) | 2015-03-27 | 2022-05-10 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
US11142507B2 (en) | 2015-09-09 | 2021-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
WO2018058022A1 (en) | 2016-09-26 | 2018-03-29 | Merck Sharp & Dohme Corp. | Anti-cd27 antibodies |
WO2018190719A2 (en) | 2017-04-13 | 2018-10-18 | Aduro Biotech Holdings, Europe B.V. | Anti-sirp alpha antibodies |
WO2019094311A1 (en) | 2017-11-08 | 2019-05-16 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
WO2019152642A1 (en) | 2018-02-01 | 2019-08-08 | Merck Sharp & Dohme Corp. | Anti-pd-1/lag3 bispecific antibodies |
WO2020033282A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
WO2020033284A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
US11981701B2 (en) | 2018-08-07 | 2024-05-14 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
US11993602B2 (en) | 2018-08-07 | 2024-05-28 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
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NO961814D0 (en) | 1996-05-03 |
NZ275691A (en) | 1998-03-25 |
EP0730605A1 (en) | 1996-09-11 |
FI961819A (en) | 1996-04-29 |
HU9601193D0 (en) | 1996-07-29 |
JP3597863B2 (en) | 2004-12-08 |
NO961814L (en) | 1996-05-06 |
CA2170766A1 (en) | 1995-05-11 |
AU7976094A (en) | 1995-05-23 |
JPH09504547A (en) | 1997-05-06 |
FI961819A0 (en) | 1996-04-29 |
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AU681454B2 (en) | 1997-08-28 |
HUT75308A (en) | 1997-05-28 |
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