CA2174105C - Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases - Google Patents

Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases Download PDF

Info

Publication number
CA2174105C
CA2174105C CA002174105A CA2174105A CA2174105C CA 2174105 C CA2174105 C CA 2174105C CA 002174105 A CA002174105 A CA 002174105A CA 2174105 A CA2174105 A CA 2174105A CA 2174105 C CA2174105 C CA 2174105C
Authority
CA
Canada
Prior art keywords
compound
pyridyl
formula
piperidyl
alkyl
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
CA002174105A
Other languages
English (en)
French (fr)
Other versions
CA2174105A1 (en
Inventor
W. Robert Bishop
Ronald J. Doll
Alan K. Mallams
F. George Njoroge
Joanne M. Petrin
John J. Piwinski
Stacy W. Remiszewski
Arthur G. Taveras
Ronald L. Wolin
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.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of CA2174105A1 publication Critical patent/CA2174105A1/en
Application granted granted Critical
Publication of CA2174105C publication Critical patent/CA2174105C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • C07D221/06Ring systems of three rings
    • C07D221/16Ring systems of three rings containing carbocyclic rings other than six-membered
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
CA002174105A 1993-10-15 1994-10-12 Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases Expired - Fee Related CA2174105C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13743593A 1993-10-15 1993-10-15
US08/137,435 1993-10-15
PCT/US1994/011391 WO1995010515A1 (en) 1993-10-15 1994-10-12 Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases

Publications (2)

Publication Number Publication Date
CA2174105A1 CA2174105A1 (en) 1995-04-20
CA2174105C true CA2174105C (en) 2002-02-12

Family

ID=22477422

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002174105A Expired - Fee Related CA2174105C (en) 1993-10-15 1994-10-12 Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases

Country Status (18)

Country Link
EP (1) EP0723538B1 (enExample)
JP (1) JP2875393B2 (enExample)
AT (1) ATE210652T1 (enExample)
AU (1) AU699043B2 (enExample)
CA (1) CA2174105C (enExample)
DE (1) DE69429438T2 (enExample)
DK (1) DK0723538T3 (enExample)
ES (1) ES2164716T3 (enExample)
HU (1) HUT76066A (enExample)
IL (1) IL111258A0 (enExample)
MA (1) MA23353A1 (enExample)
NZ (1) NZ274749A (enExample)
PT (1) PT723538E (enExample)
SG (1) SG48750A1 (enExample)
TN (1) TNSN94104A1 (enExample)
TW (1) TW308594B (enExample)
WO (1) WO1995010515A1 (enExample)
ZA (1) ZA947970B (enExample)

Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0703905A1 (en) * 1993-06-18 1996-04-03 Merck & Co. Inc. Inhibitors of farnesyl-protein transferase
MY134819A (en) 1993-10-15 2007-12-31 Schering Corp Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5721236A (en) * 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US6524832B1 (en) 1994-02-04 2003-02-25 Arch Development Corporation DNA damaging agents in combination with tyrosine kinase inhibitors
US5700806A (en) * 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5856326A (en) * 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
IL117797A0 (en) * 1995-04-07 1996-08-04 Pharmacopeia Inc Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL117798A (en) * 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5712280A (en) * 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5801175A (en) * 1995-04-07 1998-09-01 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
EP0840605A4 (en) * 1995-07-13 2000-05-10 Univ Cincinnati COMPOUNDS FOR USE IN THE TREATMENT OF NEUROFIBROMATOSE
US5874442A (en) * 1995-12-22 1999-02-23 Schering-Plough Corporation Tricyclic amides useful for inhibition of G-protein function and for treatment of proliferative disease
KR100295224B1 (ko) * 1995-12-22 2001-09-17 둘락 노먼 씨. G-단백질기능의억제및증식성질환의치료에유용한트리사이클릭아미드
US6028201A (en) * 1996-01-30 2000-02-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU6605196A (en) * 1996-02-29 1997-09-16 Duke University Method of treating hepatitis delta virus infection
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
US6451816B1 (en) 1997-06-20 2002-09-17 Klinge Pharma Gmbh Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression
US5925757A (en) * 1996-07-26 1999-07-20 Schering Corporation Method for preparing carboxamides
PE92098A1 (es) * 1996-07-31 1998-12-31 Schering Corp N-cianoiminas triciclicas utiles como inhibidores de transferasa de proteina farnesilo
US6030982A (en) 1996-09-13 2000-02-29 Schering Corporationm Compounds useful for inhibition of farnesyl protein transferase
US5985879A (en) * 1996-09-13 1999-11-16 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6040305A (en) * 1996-09-13 2000-03-21 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US5945429A (en) * 1996-09-13 1999-08-31 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
DE69731544T2 (de) * 1996-09-13 2005-10-27 Schering Corp. Trizyklische antitumor verbindungen mit farnesyl protein transferase inhibierender wirkung
SK33199A3 (en) * 1996-09-13 1999-12-10 Schering Corp Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US6071907A (en) * 1996-09-13 2000-06-06 Schering Corporation Tricyclic compounds useful as FPT inhibitors
KR20000036104A (ko) * 1996-09-13 2000-06-26 둘락 노먼 씨. 파르네실-단백질 트랜스퍼라제의 억제제로서 유용한 신규한트리사이클릭 피페리디닐 화합물
US5861395A (en) * 1996-09-13 1999-01-19 Schering Corporation Compounds useful for inhibition of farnesyl proteins transferase
US5958890A (en) * 1996-09-13 1999-09-28 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
HUP0000073A3 (en) * 1996-09-13 2002-02-28 Schering Corp Substituted benzocycloheptapyridine useful as inhibitors of farnesyl-protein transferase
US5994364A (en) 1996-09-13 1999-11-30 Schering Corporation Tricyclic antitumor farnesyl protein transferase inhibitors
EP0934303B1 (en) * 1996-09-13 2004-12-29 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
SK33299A3 (en) * 1996-09-13 2000-06-12 Schering Corp Tricyclic compounds useful for inhibition of farnesyl protein transferase
DE69732120T2 (de) * 1996-09-13 2005-12-08 Schering Corp. Trizyklische inhibitoren der farnesyl protein transferase
US5965570A (en) * 1996-09-13 1999-10-12 Schering Corporation Tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein transferase
JP2001505189A (ja) * 1996-10-09 2001-04-17 シェーリング コーポレイション Ras―FPTインヒビターとしての活性を有する三環式化合物
US6130229A (en) * 1996-10-09 2000-10-10 Schering Corporation Tricyclic compounds having activity as RAS-FPT inhibitors
US5760232A (en) * 1997-06-16 1998-06-02 Schering Corporation Synthesis of intermediates useful in preparing bromo-substituted tricyclic compounds
US5925639A (en) * 1997-06-17 1999-07-20 Schering Corporation Keto amide derivatives useful as farnesyl protein transferase inhibitors
AU754066B2 (en) * 1997-06-17 2002-11-07 Schering Corporation Benzo(5,6)cyclohepta(1,2B)pyridine derivatives useful for inhibition of farnesyl protein transferase
US6051582A (en) * 1997-06-17 2000-04-18 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
DE69825589T2 (de) * 1997-06-17 2005-09-08 Schering Corp. Benzpyrido cycloheptan derivate mit farnesyl protein transferase inhibierender wirkung
US6228865B1 (en) 1997-06-17 2001-05-08 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
AU8253498A (en) * 1997-06-17 1999-01-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
WO1998057961A1 (en) * 1997-06-17 1998-12-23 Schering Corporation Bispyrido-cycloheptane compounds useful for inhibition of farnesyl protein transferase
US5877177A (en) * 1997-06-17 1999-03-02 Schering Corporation Carboxy piperidylacetamide tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US6239140B1 (en) 1997-06-17 2001-05-29 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6159984A (en) 1997-06-17 2000-12-12 Schering Corporation Farnesyl protein transferase inhibitors
US6211193B1 (en) 1997-06-17 2001-04-03 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6576639B1 (en) 1997-06-17 2003-06-10 Schering Corporation Compounds for the inhibition of farnesyl protein transferase
US6689789B2 (en) 1997-06-17 2004-02-10 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6218401B1 (en) 1997-06-17 2001-04-17 Schering Corporation Phenyl-substituted tricyclic inhibitors of farnesyl-protein transferase
AU8253798A (en) * 1997-06-17 1999-01-04 Schering Corporation Novel phenyl-substituted tricyclic inhibitors of farnesyl-protein transferase
KR20010013953A (ko) * 1997-06-17 2001-02-26 둘락 노먼 씨. 파네실 단백질 트랜스퍼라제의 억제에 유용한 화합물
US6225322B1 (en) 1997-06-17 2001-05-01 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US5925648A (en) * 1997-07-29 1999-07-20 Schering Corporation Tricyclic N-cyanoimines useful as inhibitors of a farnesyl-protein transferase
US5958940A (en) * 1997-09-11 1999-09-28 Schering Corporation Tricyclic compounds useful as inhibitors of farnesyl-protein transferase
EP1021436A1 (en) * 1997-10-10 2000-07-26 Schering Corporation ETHYL 4-(8-CHLORO-5, 6-DIHYDRO-11H- BENZO 5,6]CYCLOHEPTA 1,2-b]PYRIDIN -11-YLIDENE)-1- PIPERIDENE CARBOXYLATE POLYMORPH
DE19756261A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue arylsubstituierte Pyridylalkan-, alken- und alkincarbonsäureamide
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
DE19756212A1 (de) * 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue, mit einem cyclischen Imid substituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
DE19756235A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperidinylsubstituierte Pyridylalkan- alken- und -alkincarbonsäureamide
US6632455B2 (en) 1997-12-22 2003-10-14 Schering Corporation Molecular dispersion composition with enhanced bioavailability
EP1090011A4 (en) 1998-07-02 2005-04-06 Merck & Co Inc INHIBITORS OF PRENYL-PROTEIN TRANSFERASE
US6358985B1 (en) 1998-07-02 2002-03-19 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US6372747B1 (en) 1998-12-18 2002-04-16 Schering Corporation Farnesyl protein transferase inhibitors
EP1031564A1 (en) 1999-02-26 2000-08-30 Klinge Pharma GmbH Inhibitors of cellular nicotinamide mononucleotide formation and their use in cancer therapy
PE20001566A1 (es) 1999-03-26 2001-02-05 Ucb Sa Piperazinas 1,4-sustituidas, piperidinas 1,4-sustituidas y 4-alquilidenilpiperidinas 1-sustituidas
US6686502B1 (en) 1999-03-26 2004-02-03 Ucb S.A. Compounds and methods for treatment of asthma, allergy and inflammatory disorders
US6316462B1 (en) 1999-04-09 2001-11-13 Schering Corporation Methods of inducing cancer cell death and tumor regression
WO2001018006A1 (en) * 1999-09-09 2001-03-15 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2003041658A2 (en) 2001-11-13 2003-05-22 Bristol-Myers Squibb Company Process for the preparation of 3,7-disubstituted-2,3,4,5- tetrahydro-1h-1,4-benzodiazepine compounds
WO2004080461A2 (en) * 2003-03-12 2004-09-23 TEVA Gyógyszergyár Részvénytársaság Stable pharmaceutical compositions of desloratadine
WO2005017160A2 (en) 2003-08-13 2005-02-24 Children's Hospital Medical Center Mobilization of hematopoietic cells
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
PE20070335A1 (es) 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
JP2009513580A (ja) * 2005-10-21 2009-04-02 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害剤
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
LT2010528T (lt) 2006-04-19 2017-12-27 Novartis Ag 6-o-pakeistieji benzoksazolo junginiai bei csf-1r signalo perdavimo slopinimo būdai
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
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
AU2008204380B2 (en) 2007-01-10 2013-08-15 Msd Italia S.R.L. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
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
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
AU2010307198B9 (en) 2009-10-14 2014-02-13 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
AU2011227643A1 (en) 2010-03-16 2012-09-20 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CN107090456B (zh) 2010-08-02 2022-01-18 瑟纳治疗公司 使用短干扰核酸的RNA干扰介导的联蛋白(钙粘蛋白关联蛋白质),β1基因表达的抑制
SI2606134T1 (sl) 2010-08-17 2019-08-30 Sirna Therapeutics, Inc. RNA-INTERFERENČNO POSREDOVANO ZAVIRANJE IZRAŽANJA GENA VIRUSA HEPATITISA B (HBV) Z UPORABO KRATKE INTERFERENČNE NUKLEINSKE KISLINE (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines 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
EP3327125B1 (en) 2010-10-29 2020-08-05 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US20140045832A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Insulin-Like Growth Factor-1 Receptor Inhibitors
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
AU2012340200B2 (en) 2011-11-17 2017-10-12 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
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
PL2925888T3 (pl) 2012-11-28 2018-03-30 Merck Sharp & Dohme Corp. Kompozycje i sposoby do stosowania w leczeniu nowotworów
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
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
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 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
HK1245260A1 (zh) 2014-12-23 2018-08-24 Dana-Farber Cancer Institute, Inc. 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂
EP3273966B1 (en) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2016201370A1 (en) 2015-06-12 2016-12-15 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 (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
AU2018252546B2 (en) 2017-04-13 2025-03-13 Sairopa B.V. Anti-SIRPα antibodies
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
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
AU2019295632B2 (en) 2018-06-25 2025-03-06 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020033288A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
US12441730B2 (en) 2019-12-17 2025-10-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
KR20250152667A (ko) 2023-03-02 2025-10-23 카르치문 바이오테크 게엠베하 암 및/또는 급성 염증성 질환을 진단하는 수단 및 방법
CN116496259B (zh) * 2023-04-24 2025-08-29 黑龙江珍宝岛药业股份有限公司 一种富马酸卢帕他定的制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4282233B1 (en) * 1980-06-19 2000-09-05 Schering Corp Antihistaminic 11-(4-piperidylidene)-5h-benzoÄ5,6Ü-cyclohepta-Ä1,2Ü-pyridines
US4826853A (en) * 1986-10-31 1989-05-02 Schering Corporation 6,11-Dihydro-11-(N-substituted-4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-B)pyridines and compositions and methods of use
US4863931A (en) * 1988-09-15 1989-09-05 Schering Corporation Antihistaminic fluoro substituted benzocycloheptapyridines
US5416091A (en) * 1990-12-18 1995-05-16 Burroughs Wellcome Co. Agents for potentiating the effects of antitumor agents and combating multiple drug resistance

Also Published As

Publication number Publication date
WO1995010515A1 (en) 1995-04-20
MA23353A1 (fr) 1995-07-01
JP2875393B2 (ja) 1999-03-31
NZ274749A (en) 1998-05-27
EP0723538A1 (en) 1996-07-31
ES2164716T3 (es) 2002-03-01
ATE210652T1 (de) 2001-12-15
CA2174105A1 (en) 1995-04-20
TNSN94104A1 (fr) 1995-09-21
AU699043B2 (en) 1998-11-19
HUT76066A (en) 1997-06-30
DE69429438T2 (de) 2002-08-08
AU7930994A (en) 1995-05-04
JPH08510759A (ja) 1996-11-12
IL111258A0 (en) 1994-12-29
TW308594B (enExample) 1997-06-21
PT723538E (pt) 2002-05-31
ZA947970B (en) 1996-07-12
EP0723538B1 (en) 2001-12-12
SG48750A1 (en) 1998-05-18
DE69429438D1 (de) 2002-01-24
HU9600963D0 (en) 1996-06-28
DK0723538T3 (da) 2002-03-18

Similar Documents

Publication Publication Date Title
CA2174105C (en) Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US6300338B1 (en) Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
AU700246B2 (en) Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
AU698960B2 (en) Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US6492381B1 (en) Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5661152A (en) Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5712280A (en) Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US6365588B1 (en) Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
NZ305137A (en) Tricyclic amide and urea derivatives, preparation and use in pharmaceutical compositions

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed