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 (136)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995000497A1 (en) * 1993-06-18 1995-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0723539B1 (en) 1993-10-15 2001-12-12 Schering Corporation 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
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
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
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
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
WO1997002817A1 (en) * 1995-07-13 1997-01-30 University Of Cincinnati Compounds useful in the treatment of neurofibromatosis
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
CZ292791B6 (cs) * 1995-12-22 2003-12-17 Schering Corporation Tricyklické amidy, které se používají pro inhibici G-proteinové funkce a k léčení proliferativních onemocnění
US6028201A (en) * 1996-01-30 2000-02-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997031641A1 (en) * 1996-02-29 1997-09-04 Duke University Method of treating hepatitis delta virus infection
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
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
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
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
US5985879A (en) * 1996-09-13 1999-11-16 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
ES2234036T3 (es) * 1996-09-13 2005-06-16 Schering Corporation Compuestos utiles para inhibir la farnesil-protein-transferasa.
BR9712831A (pt) * 1996-09-13 1999-11-16 Schering Corp Inibidores tricìclicos de farnesil proteìna transferase
JP2002515052A (ja) * 1996-09-13 2002-05-21 シェーリング コーポレイション ファルネシルタンパク質トランスフェラーゼの阻害に有用な化合物
US6071907A (en) * 1996-09-13 2000-06-06 Schering Corporation Tricyclic compounds useful as FPT inhibitors
WO1998011098A1 (en) * 1996-09-13 1998-03-19 Schering Corporation Novel tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein transferase
US5965570A (en) * 1996-09-13 1999-10-12 Schering Corporation Tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein transferase
US5861395A (en) * 1996-09-13 1999-01-19 Schering Corporation Compounds useful for inhibition of farnesyl proteins transferase
ES2242232T3 (es) * 1996-09-13 2005-11-01 Schering Corporation Benzocicloheptapiridinas sustituidas utiles como inhibidores de la farnesil-proteina-transferasa.
EP0929544B1 (en) * 1996-09-13 2004-11-10 Schering Corporation Tricyclic antitumor compounds being farnesyl protein transferase inhibitors
US5945429A (en) * 1996-09-13 1999-08-31 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
ES2169420T3 (es) * 1996-09-13 2002-07-01 Schering Corp Compuestos triciclicos utiles para inhibir la funcion de la proteina g y para tratar enfermedades proliferativas.
US6040305A (en) * 1996-09-13 2000-03-21 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US5994364A (en) * 1996-09-13 1999-11-30 Schering Corporation Tricyclic antitumor farnesyl protein transferase inhibitors
ES2192671T3 (es) * 1996-10-09 2003-10-16 Schering Corp Compuestos triciclicos que tienen actividad como inhibidores de ras-fpt.
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
WO1998057950A1 (en) * 1997-06-17 1998-12-23 Schering Corporation Novel phenyl-substituted tricyclic inhibitors of farnesyl-protein transferase
US6211193B1 (en) 1997-06-17 2001-04-03 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6689789B2 (en) 1997-06-17 2004-02-10 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6228865B1 (en) 1997-06-17 2001-05-08 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
US6159984A (en) 1997-06-17 2000-12-12 Schering Corporation Farnesyl protein transferase inhibitors
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
KR20010013882A (ko) * 1997-06-17 2001-02-26 둘락 노먼 씨. 파르네실 단백질 트랜스퍼라제의 억제에 유용한벤조(5,6)사이클로헵타(1,2b)피리딘 유도체
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
KR100640672B1 (ko) * 1997-06-17 2006-11-02 파마코페이아 드럭 디스커버리, 인크. 파르네실 단백질 트랜스퍼라제의 억제에 유용한 벤즈피리도 사이클로헵탄 화합물 및 이를 포함하는 약제학적 조성물
US5925639A (en) * 1997-06-17 1999-07-20 Schering Corporation Keto amide derivatives useful as farnesyl protein transferase inhibitors
ZA985214B (en) * 1997-06-17 1999-01-07 Schering Corp Compounds 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
US6239140B1 (en) 1997-06-17 2001-05-29 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
WO1998057955A1 (en) * 1997-06-17 1998-12-23 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
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
JP2001519428A (ja) * 1997-10-10 2001-10-23 シェーリング コーポレイション エチル4−(8−クロロ−5,6−ジヒドロ−11H−ベンゾ[5,6]シクロヘプタ[1,2−b]ピリジン−11−イリデン)−1−ピペリデンカルボキシレート多形物
DE19756212A1 (de) * 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue, mit einem cyclischen Imid substituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
DE19756235A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperidinylsubstituierte Pyridylalkan- alken- und -alkincarbonsäureamide
DE19756261A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue arylsubstituierte Pyridylalkan-, alken- und alkincarbonsäureamide
US6632455B2 (en) 1997-12-22 2003-10-14 Schering Corporation Molecular dispersion composition with enhanced bioavailability
WO2000001382A1 (en) 1998-07-02 2000-01-13 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2000001701A1 (en) 1998-07-02 2000-01-13 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
US6686502B1 (en) 1999-03-26 2004-02-03 Ucb S.A. Compounds and methods for treatment of asthma, allergy and inflammatory disorders
PE20001566A1 (es) 1999-03-26 2001-02-05 Ucb Sa Piperazinas 1,4-sustituidas, piperidinas 1,4-sustituidas y 4-alquilidenilpiperidinas 1-sustituidas
US6316462B1 (en) 1999-04-09 2001-11-13 Schering Corporation Methods of inducing cancer cell death and tumor regression
CA2384151A1 (en) * 1999-09-09 2001-03-15 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US7074921B2 (en) 2001-11-13 2006-07-11 Bristol Myers Squibb Company Process for the preparation of 3,7-disubstituted-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine compounds
US20040242619A1 (en) * 2003-03-12 2004-12-02 Toth Zoltan G. Processes for preparation of polymorphic forms of desloratadine
US7417026B2 (en) 2003-08-13 2008-08-26 Children's Hospital Medical Center Mobilization of hematopoietic cells
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
TW200804345A (en) 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
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
DK2010528T3 (en) 2006-04-19 2018-01-15 Novartis Ag 6-O-Substituted Benzoxazole and Benzothiazole Compounds and Methods for Inhibiting CSF-1R Signaling
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
EA016079B1 (ru) 2007-01-10 2012-01-30 Институто Ди Ричерке Ди Биолоджиа Молеколаре П. Анджелетти Спа Амидзамещенные индазолы в качестве ингибиторов поли(adp-рибоза)полимеразы (parp)
ES2431163T3 (es) 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
BRPI0812159A2 (pt) 2007-05-21 2017-05-02 Novartis Ag inibidores de csf-1r, composições e métodos de uso
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
JP5099731B1 (ja) 2009-10-14 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション p53活性を増大する置換ピペリジン及びその使用
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
BR112012023021A2 (pt) 2010-03-16 2016-05-31 Dana Farber Cancer Inst Inc compostos de indazol e seus usos
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
AU2011285909B2 (en) 2010-08-02 2016-11-10 Sirna Therapeutics, Inc. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP2606134B1 (en) 2010-08-17 2019-04-10 Sirna Therapeutics, Inc. 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
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
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
EP2699567A1 (en) 2011-04-21 2014-02-26 Merck Sharp & Dohme Corp. Insulin-like growth factor-1 receptor inhibitors
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel 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)
EP3358013B1 (en) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
KR20150060724A (ko) 2012-09-28 2015-06-03 머크 샤프 앤드 돔 코포레이션 Erk 억제제인 신규 화합물
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
DK2925888T3 (en) 2012-11-28 2017-12-18 Merck Sharp & Dohme COMPOSITIONS AND METHODS OF CANCER TREATMENT
EP2935263B1 (en) 2012-12-20 2018-12-05 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
WO2015034925A1 (en) 2013-09-03 2015-03-12 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
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
AU2015371251B2 (en) 2014-12-23 2020-06-11 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
JP7028766B2 (ja) 2015-09-09 2022-03-02 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 サイクリン依存性キナーゼの阻害剤
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
WO2018190719A2 (en) 2017-04-13 2018-10-18 Aduro Biotech Holdings, Europe B.V. Anti-sirp alpha antibodies
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
JP7590185B2 (ja) 2018-06-25 2024-11-26 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 Taireファミリーキナーゼインヒビターおよびそれらの使用
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2020033285A1 (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
BR112021002267A8 (pt) 2018-08-07 2023-02-07 Merck Sharp & Dohme Inibidores de prmt5
WO2020140098A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
BR112022012015A2 (pt) 2019-12-17 2022-08-30 Merck Sharp & Dohme Llc Inibidores de prmt5
EP4076460B1 (en) 2019-12-17 2026-01-21 Merck Sharp & Dohme LLC 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer
JP2026509792A (ja) 2023-03-02 2026-03-25 カルツィムン ビオテック ゲゼルシャフト ミット ベシュレンクテル ハフツング がん及び/又は急性炎症性疾患を診断するための手段及び方法
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
WO2026027944A1 (en) 2024-07-30 2026-02-05 Sairopa B.V. Anti-sirp alpha antibody formulations and uses thereof

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
DE69120430D1 (de) * 1990-12-18 1996-07-25 Wellcome Found Mittel zur verstaerkung der wirkung von antitumoralen mittel und zur widerstandsbekaempfung von vielfachdrogen

Also Published As

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

Similar Documents

Publication Publication Date Title
AU699043B2 (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
CA2266015C (en) Tricyclic antitumor compounds being farnesyl protein transferase inhibitors

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed