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

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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
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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
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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
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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

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic 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
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/16—Ring systems of three rings containing carbocyclic rings other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based 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 (cg-RX-API-DMAC10.html)
JP (1) JP2875393B2 (cg-RX-API-DMAC10.html)
AT (1) ATE210652T1 (cg-RX-API-DMAC10.html)
AU (1) AU699043B2 (cg-RX-API-DMAC10.html)
CA (1) CA2174105C (cg-RX-API-DMAC10.html)
DE (1) DE69429438T2 (cg-RX-API-DMAC10.html)
DK (1) DK0723538T3 (cg-RX-API-DMAC10.html)
ES (1) ES2164716T3 (cg-RX-API-DMAC10.html)
HU (1) HUT76066A (cg-RX-API-DMAC10.html)
IL (1) IL111258A0 (cg-RX-API-DMAC10.html)
MA (1) MA23353A1 (cg-RX-API-DMAC10.html)
NZ (1) NZ274749A (cg-RX-API-DMAC10.html)
PT (1) PT723538E (cg-RX-API-DMAC10.html)
SG (1) SG48750A1 (cg-RX-API-DMAC10.html)
TN (1) TNSN94104A1 (cg-RX-API-DMAC10.html)
TW (1) TW308594B (cg-RX-API-DMAC10.html)
WO (1) WO1995010515A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA947970B (cg-RX-API-DMAC10.html)

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
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
ES2164717T3 (es) 1993-10-15 2002-03-01 Schering Corp Compuestos triciclicos de sulfonamida utiles para inhibir la funcion de la proteina-g y para el tratamiento de enfermedades proliferativas.
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
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
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
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
JPH11509204A (ja) * 1995-07-13 1999-08-17 ユニバーシテイ・オブ・シンシナテイ 神経線維腫症の治療に有用な化合物
ES2248826T3 (es) * 1995-12-22 2006-03-16 Schering Corporation Amidas triciclicas utiles para la inhibicion de la funcion de la proteina g y para el tratamiento de enfermedades proliferativas.
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
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
US5965570A (en) * 1996-09-13 1999-10-12 Schering Corporation Tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein transferase
US6071907A (en) * 1996-09-13 2000-06-06 Schering Corporation Tricyclic compounds useful as FPT inhibitors
HUP0000191A2 (hu) * 1996-09-13 2001-04-28 Schering Corp. Farnezil-protein-transzferáz inhibitorként alkalmazható új triciklusos piperidinil-vegyületek
US5861395A (en) * 1996-09-13 1999-01-19 Schering Corporation Compounds useful for inhibition of farnesyl proteins transferase
US5985879A (en) * 1996-09-13 1999-11-16 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
ES2232888T3 (es) * 1996-09-13 2005-06-01 Schering Corporation Compuestos utiles para inhibir la farnesil protein transferasa.
US5945429A (en) * 1996-09-13 1999-08-31 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
KR20000036120A (ko) * 1996-09-13 2000-06-26 둘락 노먼 씨. 파르네실 단백질 트랜스퍼라제에 대한 트리사이클릭 저해제
AU5196698A (en) * 1996-09-13 1998-04-02 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
US6030982A (en) 1996-09-13 2000-02-29 Schering Corporationm 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
HUP9904067A2 (hu) * 1996-09-13 2000-05-28 Schering Corporation A G-protein-funkció gátlására és daganatos betegségek kezelésére alkalmazható triciklusos vegyületek
WO1998011092A1 (en) * 1996-09-13 1998-03-19 Schering Corporation Tricyclic antitumor compounds being farnesyl protein transferase inhibitors
NZ334341A (en) * 1996-09-13 2001-01-26 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
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
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
US6211193B1 (en) 1997-06-17 2001-04-03 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
ZA985203B (en) * 1997-06-17 1999-01-05 Schering Corp Compounds useful for inhibition of farnesyl protein transferase
CN1267293A (zh) * 1997-06-17 2000-09-20 先灵公司 用于抑制法呢基蛋白转移酶的苯并(5,6)芳庚并(1,2b)吡啶衍生物
US5925639A (en) * 1997-06-17 1999-07-20 Schering Corporation Keto amide derivatives useful as farnesyl protein transferase inhibitors
US6159984A (en) * 1997-06-17 2000-12-12 Schering Corporation Farnesyl protein transferase inhibitors
US6228865B1 (en) 1997-06-17 2001-05-08 Schering Corporation 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
US6051582A (en) * 1997-06-17 2000-04-18 Schering Corporation Compounds useful for inhibition of farnesyl protein transferase
NZ501613A (en) * 1997-06-17 2001-11-30 Schering Corp Benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl) piperazine derivatives useful as inhibitors of farnesyl-protein transferase
HUP0002186A3 (en) * 1997-06-17 2002-04-29 Schering Corp 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
US6225322B1 (en) 1997-06-17 2001-05-01 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
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
WO1998057961A1 (en) * 1997-06-17 1998-12-23 Schering Corporation Bispyrido-cycloheptane 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
CA2305801A1 (en) * 1997-10-10 1999-04-22 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
CA2336054A1 (en) 1998-07-02 2000-01-13 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
EP1090011A4 (en) 1998-07-02 2005-04-06 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
AU7124000A (en) * 1999-09-09 2001-04-10 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
US7417026B2 (en) 2003-08-13 2008-08-26 Children's Hospital Medical Center Mobilization of hematopoietic cells
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
TW200804345A (en) 2005-08-30 2008-01-16 Novartis Ag Substituted benzimidazoles and methods of preparation
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
AU2007237904B2 (en) 2006-04-19 2011-03-03 Novartis Ag 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
AU2007300627B2 (en) 2006-09-22 2012-02-16 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
EP2805945B1 (en) 2007-01-10 2019-04-03 MSD Italia S.r.l. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
EP2132177B1 (en) 2007-03-01 2013-07-17 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
EP3103791B1 (en) 2007-06-27 2018-01-31 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
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
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
CN103080093A (zh) 2010-03-16 2013-05-01 达纳－法伯癌症研究所公司 吲唑化合物及其应用
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
EP2601293B1 (en) 2010-08-02 2017-12-06 Sirna Therapeutics, Inc. RNA INTERFERENCE MEDIATED INHIBITION OF CATENIN (CADHERIN-ASSOCIATED PROTEIN), BETA 1 (CTNNB1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
CN103282497B (zh) 2010-08-17 2018-07-10 瑟纳治疗公司 使用短干扰核酸(siNA)的乙型肝炎病毒(HBV)基因表达的RNA干扰介导的抑制
WO2012027236A1 (en) 2010-08-23 2012-03-01 Schering Corporation 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
ES2663009T3 (es) 2010-10-29 2018-04-10 Sirna Therapeutics, Inc. Inhibición de la expresión génica mediada por interferencia por ARN utilizando ácidos nucleicos de interferencia cortos (ANic)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2012143879A1 (en) 2011-04-21 2012-10-26 Piramal Healthcare Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
AU2013323508B2 (en) 2012-09-28 2017-11-02 Merck Sharp & Dohme Corp. Novel compounds that are ERK inhibitors
WO2014063068A1 (en) 2012-10-18 2014-04-24 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
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
JP6290237B2 (ja) 2012-11-28 2018-03-07 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 癌を処置するための組成物および方法
WO2014100065A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
AU2014337044A1 (en) 2013-10-18 2016-05-05 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
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
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
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
WO2017044858A2 (en) 2015-09-09 2017-03-16 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
IL315837A (en) 2017-04-13 2024-11-01 Sairopa B V Anti-SIRP-alpha antibodies
WO2019094312A1 (en) 2017-11-08 2019-05-16 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
CA3099763A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
KR20210046009A (ko) 2018-08-07 2021-04-27 머크 샤프 앤드 돔 코포레이션 Prmt5 억제제
JP7660063B2 (ja) 2018-12-28 2025-04-10 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７のインヒビターおよびそれらの使用
WO2021126729A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
AU2024228641A1 (en) 2023-03-02 2025-07-24 Carcimun Biotech Gmbh Means and methods for diagnosing cancer and/or an acute inflammatory disease
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
ATE139447T1 (de) * 1990-12-18 1996-07-15 Wellcome Found Mittel zur verstaerkung der wirkung von antitumoralen mittel und zur widerstandsbekaempfung von vielfachdrogen

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ZA947970B (en) 1996-07-12
TW308594B (cg-RX-API-DMAC10.html) 1997-06-21
DE69429438T2 (de) 2002-08-08
JPH08510759A (ja) 1996-11-12
HUT76066A (en) 1997-06-30
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HU9600963D0 (en) 1996-06-28
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