BRPI0416852A - inibidores da quinase akt - Google Patents
inibidores da quinase aktInfo
- Publication number
- BRPI0416852A BRPI0416852A BRPI0416852-6A BRPI0416852A BRPI0416852A BR PI0416852 A BRPI0416852 A BR PI0416852A BR PI0416852 A BRPI0416852 A BR PI0416852A BR PI0416852 A BRPI0416852 A BR PI0416852A
- Authority
- BR
- Brazil
- Prior art keywords
- kinase inhibitors
- akt kinase
- present
- akt
- compounds
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- -1 enantiomers Chemical class 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 125000005647 linker group Chemical group 0.000 abstract 1
- 239000003909 protein kinase inhibitor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B41—PRINTING; LINING MACHINES; TYPEWRITERS; STAMPS
- B41M—PRINTING, DUPLICATING, MARKING, OR COPYING PROCESSES; COLOUR PRINTING
- B41M3/00—Printing processes to produce particular kinds of printed work, e.g. patterns
- B41M3/008—Sequential or multiple printing, e.g. on previously printed background; Mirror printing; Recto-verso printing; using a combination of different printing techniques; Printing of patterns visible in reflection and by transparency; by superposing printed artifacts
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B44—DECORATIVE ARTS
- B44F—SPECIAL DESIGNS OR PICTURES
- B44F1/00—Designs or pictures characterised by special or unusual light effects
- B44F1/08—Designs or pictures characterised by special or unusual light effects characterised by colour effects
- B44F1/10—Changing, amusing, or secret pictures
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/28—Cinnolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- G—PHYSICS
- G09—EDUCATION; CRYPTOGRAPHY; DISPLAY; ADVERTISING; SEALS
- G09F—DISPLAYING; ADVERTISING; SIGNS; LABELS OR NAME-PLATES; SEALS
- G09F13/00—Illuminated signs; Luminous advertising
- G09F13/16—Signs formed of or incorporating reflecting elements or surfaces, e.g. warning signs having triangular or other geometrical shape
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/24—Structurally defined web or sheet [e.g., overall dimension, etc.]
- Y10T428/24802—Discontinuous or differential coating, impregnation or bond [e.g., artwork, printing, retouched photograph, etc.]
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/24—Structurally defined web or sheet [e.g., overall dimension, etc.]
- Y10T428/24802—Discontinuous or differential coating, impregnation or bond [e.g., artwork, printing, retouched photograph, etc.]
- Y10T428/24851—Intermediate layer is discontinuous or differential
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/25—Web or sheet containing structurally defined element or component and including a second component containing structurally defined particles
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/31504—Composite [nonstructural laminate]
- Y10T428/31507—Of polycarbonate
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/31504—Composite [nonstructural laminate]
- Y10T428/31551—Of polyamidoester [polyurethane, polyisocyanate, polycarbamate, etc.]
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/31504—Composite [nonstructural laminate]
- Y10T428/31786—Of polyester [e.g., alkyd, etc.]
-
- 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/31504—Composite [nonstructural laminate]
- Y10T428/31855—Of addition polymer from unsaturated monomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Physics & Mathematics (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Geometry (AREA)
- Theoretical Computer Science (AREA)
- General Physics & Mathematics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Quinoline Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
"INIBIDORES DA QUINASE AKT". A presente invenção proporciona compostos, incluindo enantiómeros, diastereómeros, solvatos e sais farmaceuticamente aceitáveis decompostos dos mesmos, compreendendo a Fórmula: A-L-CR, em que CR é um grupo com núcleo cíclico, L é um grupo de ligação e A é conforme definido aqui. Também proporcionados são métodos de uso dos compostos da presente invenção como inibidores da quinase de proteína AKT e para o tratamento de doenças hiperproliferativas, tal como câncer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US52400303P | 2003-11-21 | 2003-11-21 | |
| PCT/US2004/039094 WO2005051304A2 (en) | 2003-11-21 | 2004-11-19 | Akt protein kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0416852A true BRPI0416852A (pt) | 2007-02-27 |
Family
ID=34632854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0416852-6A BRPI0416852A (pt) | 2003-11-21 | 2004-11-19 | inibidores da quinase akt |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US20050130954A1 (pt) |
| EP (1) | EP1684694A2 (pt) |
| JP (1) | JP2007512364A (pt) |
| KR (2) | KR20110137838A (pt) |
| CN (2) | CN102786482A (pt) |
| AU (1) | AU2004293026B2 (pt) |
| BR (1) | BRPI0416852A (pt) |
| CA (1) | CA2546754A1 (pt) |
| IL (2) | IL175221A (pt) |
| NO (1) | NO20062884L (pt) |
| NZ (2) | NZ547327A (pt) |
| PH (1) | PH12012501891A1 (pt) |
| RU (1) | RU2006121990A (pt) |
| WO (1) | WO2005051304A2 (pt) |
| ZA (1) | ZA200604069B (pt) |
Families Citing this family (106)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2080757A1 (en) * | 2003-07-24 | 2009-07-22 | Euro-Celtique S.A. | Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain |
| PT2017276E (pt) * | 2003-09-22 | 2011-04-05 | Euro Celtique Sa | Compostos de fenilcarboxamida úteis para o tratamento da dor |
| US7402652B2 (en) * | 2004-09-14 | 2008-07-22 | Miller Landon C G | Baclofen conjugate and a pharmaceutical composition for treatment of neuronal disorders |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| AU2005310490B2 (en) | 2004-12-02 | 2012-01-19 | Daiichi Sankyo Company, Limited | 7-membered ring compound, process for producing the same, and medicinal use thereof |
| US7994172B2 (en) | 2004-12-28 | 2011-08-09 | Exelixis, Inc. | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| KR20070116060A (ko) * | 2005-03-01 | 2007-12-06 | 와이어쓰 | 신놀린 화합물 및 간 x 수용체 조절제로서의 이의 용도 |
| EP1702916A1 (en) * | 2005-03-18 | 2006-09-20 | Santhera Pharmaceuticals (Schweiz) GmbH | DPP-IV inhibitors |
| KR20080016659A (ko) * | 2005-05-20 | 2008-02-21 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제의 억제제로서 유용한 피롤로피리딘 |
| US7825244B2 (en) | 2005-06-10 | 2010-11-02 | Janssen Pharmaceutica Nv | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis |
| US8071768B2 (en) | 2005-06-10 | 2011-12-06 | Janssen Pharmaceutica, N.V. | Alkylquinoline and alkylquinazoline kinase modulators |
| GB0516967D0 (en) * | 2005-08-18 | 2005-09-28 | Univ Southampton | Inhibitors |
| JP4935675B2 (ja) | 2005-08-25 | 2012-05-23 | 宇部興産株式会社 | 光学活性(S又はR)−α−アミノ酸及び光学活性(R又はS)−α−アミノ酸エステルの製造方法 |
| CA2623034A1 (en) * | 2005-09-27 | 2007-04-05 | Novartis Ag | Carboxyamine compounds and their use in the treatment of hdac dependent diseases |
| EP1948185A4 (en) * | 2005-11-10 | 2010-04-21 | Glaxosmithkline Llc | INHIBITORS OF AKT ACTIVITY |
| WO2007058879A2 (en) * | 2005-11-10 | 2007-05-24 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| EP1962851A2 (en) * | 2005-12-22 | 2008-09-03 | SmithKline Beecham Corporation | Compounds |
| EP1968568A4 (en) * | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
| US20090099175A1 (en) * | 2006-03-01 | 2009-04-16 | Arrington Mark P | Phosphodiesterase 10 inhibitors |
| JP5606734B2 (ja) | 2006-04-25 | 2014-10-15 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| US20090124610A1 (en) * | 2006-04-25 | 2009-05-14 | Gordon Saxty | Pharmaceutical compounds |
| CN101528039A (zh) | 2006-05-26 | 2009-09-09 | 路易斯维尔大学研究基金会公司 | 巨噬细胞迁移抑制因子拮抗剂及其应用方法 |
| JP5117382B2 (ja) * | 2006-05-31 | 2013-01-16 | 第一三共株式会社 | 7員環化合物の製造方法 |
| US8063050B2 (en) * | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| CN101511842B (zh) * | 2006-07-06 | 2012-10-31 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶 |
| ATE532789T1 (de) * | 2006-07-06 | 2011-11-15 | Array Biopharma Inc | Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren |
| AU2014201211B2 (en) * | 2006-07-06 | 2016-04-14 | Array Biopharma Inc. | Hydroxylated and methoxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
| UA95641C2 (xx) * | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы |
| WO2008006032A1 (en) * | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
| US20080051410A1 (en) * | 2006-08-02 | 2008-02-28 | Northwestern University | Protein Kinase Targeted Therapeutics |
| CA2663436A1 (en) * | 2006-10-04 | 2008-04-10 | Pfizer Products Inc. | Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists |
| WO2008070823A2 (en) * | 2006-12-07 | 2008-06-12 | University Of South Florida | Substrate-mimetic akt inhibitor |
| UY30892A1 (es) * | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008109104A1 (en) * | 2007-03-07 | 2008-09-12 | The Regents Of The University Of California | Bivalent inhibitors of akt protein kinase |
| US8618097B2 (en) * | 2007-07-05 | 2013-12-31 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| SI2173723T1 (sl) * | 2007-07-05 | 2011-12-30 | Array Biopharma Inc | Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze |
| PT2188289E (pt) * | 2007-08-08 | 2015-12-21 | Lexicon Pharmaceuticals Inc | (7h-pirrolo[2,3-d]pirimidin-4-il)piperazinas como inibidores de quinases para o tratamento de cancro e de inflamação |
| BRPI0818533B8 (pt) | 2007-10-11 | 2021-05-25 | Astrazeneca Ab | composto, composição farmacêutica, uso de um composto, e, processo para a preparação de um composto |
| CN101959887B (zh) * | 2008-01-08 | 2013-07-31 | 阵列生物制药公司 | 作为激酶抑制剂的吡咯并吡啶 |
| CA2711782C (en) | 2008-01-09 | 2017-01-03 | Array Biopharma Inc. | 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors |
| JP5346345B2 (ja) * | 2008-01-09 | 2013-11-20 | アレイ バイオファーマ、インコーポレイテッド | Aktタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン類 |
| EP2240455B1 (en) * | 2008-01-09 | 2012-12-26 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor |
| TW200940542A (en) | 2008-01-09 | 2009-10-01 | Array Biopharma Inc | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| EP2242757B1 (en) * | 2008-01-09 | 2012-08-01 | Array Biopharma, Inc. | Pyrazolopyridines as kinase inhibitors |
| CA2711759A1 (en) * | 2008-01-30 | 2009-08-06 | Genentech, Inc. | Pyrazolopyrimidine pi3k inhibitor compounds and methods of use |
| EP2297153B1 (en) * | 2008-04-21 | 2015-05-27 | Lexicon Pharmaceuticals, Inc. | Limk2 inhibitors, compositions comprising them, and methods of their use |
| CA2731095A1 (en) * | 2008-08-05 | 2010-02-11 | Abbott Laboratories | Compounds useful as inhibitors of protein kinases |
| US8110578B2 (en) * | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| CA2744154A1 (en) | 2008-11-20 | 2010-05-27 | Genentech, Inc. | Pyrazolopyridine pi3k inhibitor compounds and methods of use |
| CA2750565C (en) * | 2009-01-30 | 2015-10-20 | Glaxosmithkline Llc | Crystalline n-{(1s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride |
| EP2270002A1 (en) * | 2009-06-18 | 2011-01-05 | Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg | Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders |
| BR112012000422A2 (pt) | 2009-07-08 | 2017-05-09 | Leo Pharma As | composto, composição farmacêutica, uso de um composto, e, método para a prevenir tratar ou melhorar doenças do sistema imune |
| WO2011038234A2 (en) * | 2009-09-24 | 2011-03-31 | University Of Louisville Research Foundation, Inc. | Novel iodo pyrimidine derivatives useful for the treatment of macrophage migration inhibitory factor (mif)-implicated diseases and conditions |
| US9155790B2 (en) | 2010-05-20 | 2015-10-13 | University of Lousiville Research Foundation, Inc. | Methods and compositions for modulating ocular damage |
| US20140221370A1 (en) * | 2010-07-09 | 2014-08-07 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
| KR20140058402A (ko) | 2011-01-07 | 2014-05-14 | 레오 파마 에이/에스 | 단백질 티로신 키나제 억제제로서의 신규한 설파미드 피페라진 유도체 및 이의 약제학적 용도 |
| WO2012131399A1 (en) | 2011-04-01 | 2012-10-04 | Astrazeneca Ab | Therapeutic treatment |
| ES2620644T3 (es) | 2011-04-01 | 2017-06-29 | Genentech, Inc. | Combinaciones de compuestos inhibidores de AKT y agentes quimioterapéuticos, y métodos de uso |
| KR20140022053A (ko) | 2011-04-01 | 2014-02-21 | 제넨테크, 인크. | Akt 및 mek 억제제 화합물의 조합물, 및 사용 방법 |
| SG2014009260A (en) | 2011-09-12 | 2014-09-26 | Merck Patent Gmbh | Aminopyrimidine derivatives for use as modulators of kinase activity |
| WO2013062071A1 (ja) * | 2011-10-27 | 2013-05-02 | 大鵬薬品工業株式会社 | ピペラジン誘導体及びその塩 |
| PT2785349T (pt) | 2011-11-30 | 2019-12-11 | Astrazeneca Ab | Tratamento combinado de cancro |
| GB201201566D0 (en) * | 2012-01-30 | 2012-03-14 | Vernalis R&D Ltd | New chemical compounds |
| EP2809668B1 (en) | 2012-02-02 | 2017-04-12 | Actelion Pharmaceuticals Ltd. | 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives |
| AU2013204533B2 (en) | 2012-04-17 | 2017-02-02 | Astrazeneca Ab | Crystalline forms |
| DK2858989T3 (da) | 2012-05-17 | 2020-06-02 | Genentech Inc | Amorf form af en AKT-hæmmende pyrimidinyl-cyclopentan-forbindelse, sammensætninger deraf og fremgangsmåder dertil |
| JP6214636B2 (ja) | 2012-05-17 | 2017-10-18 | アレイ バイオファーマ、インコーポレイテッド | ヒドロキシル化シクロペンチルピリミジン化合物を作製するためのプロセス |
| WO2013182612A1 (en) * | 2012-06-07 | 2013-12-12 | Bayer Pharma Aktiengesellschaft | Glucose transport inhibitors |
| AU2013277154A1 (en) | 2012-06-20 | 2014-12-18 | Jonathan E. Grob | Complement pathway modulators and uses thereof |
| CN104981247A (zh) * | 2012-09-06 | 2015-10-14 | 普莱希科公司 | 用于激酶调节的化合物和方法及其适应症 |
| SG11201600504TA (en) | 2013-07-22 | 2016-02-26 | Actelion Pharmaceuticals Ltd | 1-(piperazin-1-yl)-2-([1,2,4]triazol-1-yl)-ethanone derivatives |
| AR099789A1 (es) | 2014-03-24 | 2016-08-17 | Actelion Pharmaceuticals Ltd | Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina |
| JP6418679B2 (ja) * | 2014-09-09 | 2018-11-07 | 学校法人明治大学 | ヘテロアリール化合物の製造方法 |
| MA41169A (fr) * | 2014-12-17 | 2017-10-24 | Acraf | Composés antibactériens à large spectre d'activité |
| TWI693221B (zh) | 2015-01-15 | 2020-05-11 | 瑞士商愛杜西亞製藥有限公司 | 作為cxcr3受體調節劑之羥烷基六氫吡衍生物 |
| AR103399A1 (es) | 2015-01-15 | 2017-05-10 | Actelion Pharmaceuticals Ltd | Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3 |
| CN104876933A (zh) * | 2015-05-12 | 2015-09-02 | 烟台万润药业有限公司 | 一种含氮杂环酰基哌嗪类化合物及其制备方法与应用 |
| CN104876934B (zh) * | 2015-05-12 | 2017-08-11 | 山东大学 | 一种含氮杂环苯基哌啶类化合物及其制备方法与应用 |
| WO2017004133A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| TW201734002A (zh) * | 2015-12-11 | 2017-10-01 | 拜耳作物科學股份有限公司 | 作為殺蟲劑之經取代的丙二醯胺類 |
| CN109843856B (zh) * | 2016-05-18 | 2023-05-02 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| AU2017348322B8 (en) | 2016-10-28 | 2021-12-23 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating EZH2-mediated cancer |
| CN108503645A (zh) * | 2018-03-01 | 2018-09-07 | 山东大学 | 含氨甲基的哌嗪酮类化合物及其制备方法和应用 |
| WO2019173516A1 (en) * | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| CN108997351A (zh) * | 2018-07-18 | 2018-12-14 | 山东大学 | 含取代对氯苯乙酰基哌嗪类化合物及其制备方法与应用 |
| CN108752351A (zh) * | 2018-09-13 | 2018-11-06 | 遵义医学院 | 一种含哌嗪的吡唑并嘧啶类化合物或其药用盐及其制备方法与应用 |
| PL3919491T3 (pl) * | 2019-01-29 | 2025-10-20 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | Inhibitor akt |
| US12465648B2 (en) | 2019-05-06 | 2025-11-11 | Icahn School Of Medicine At Mount Sinai | Heterobifunctional compounds as degraders of HPK1 |
| WO2021228223A1 (zh) * | 2020-05-15 | 2021-11-18 | 南京正大天晴制药有限公司 | 氘代akt激酶抑制剂 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| JP2023529867A (ja) | 2020-06-05 | 2023-07-12 | キネート バイオファーマ インク. | 線維芽細胞増殖因子受容体キナーゼの阻害剤 |
| WO2022015375A1 (en) * | 2020-07-16 | 2022-01-20 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| AU2021314419B2 (en) * | 2020-07-22 | 2023-12-07 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | Salt of dihydropyrido[2,3-d]pyrimidinone derivative, preparation method therefor, and use thereof |
| US20230271958A1 (en) * | 2020-07-22 | 2023-08-31 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | SALT AND CRYSTAL FORM OF DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATE |
| CA3186565A1 (en) * | 2020-07-22 | 2022-01-27 | Lei Miao | Unit dosage composition of akt inhibitor |
| CN114380841B (zh) * | 2020-10-19 | 2025-12-30 | 南京正大天晴制药有限公司 | 作为akt抑制剂的三环喹唑啉或二氢喹唑啉化合物 |
| JP7756374B2 (ja) * | 2021-03-08 | 2025-10-20 | 曁南大学 | ピリドピリミジン系化合物及びその使用 |
| CA3213079A1 (en) | 2021-04-13 | 2022-10-20 | Kristin Lynne ANDREWS | Amino-substituted heterocycles for treating cancers with egfr mutations |
| CN115716840B (zh) * | 2021-08-24 | 2024-07-23 | 昆药集团股份有限公司 | 一种具有kras突变蛋白抑制作用的杂环化合物及其药物组合和用途 |
| AR129965A1 (es) * | 2022-07-20 | 2024-10-16 | Sanofi Sa | Compuestos de imidazopiridina, preparación de los mismos y usos terapéuticos de los mismos |
| WO2024249604A2 (en) * | 2023-06-02 | 2024-12-05 | Purdue Research Foundation | Covalent inhibitors as anti-malarial agents |
| CN121419774A (zh) * | 2023-06-14 | 2026-01-27 | 南京正大天晴制药有限公司 | Akt抑制剂在制备预防或治疗卵巢癌药物中的用途 |
| CN119040500B (zh) * | 2024-07-18 | 2026-04-17 | 中国农业科学院作物科学研究所 | 与大豆种子油份、蛋白含量和百粒重相关的snp分子标记与应用 |
Family Cites Families (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3885035A (en) | 1972-04-05 | 1975-05-20 | Sandoz Ag | Method for treating arrhythmia by using 1,4-bis(4 quinazolinyl) piperazines |
| US3956495A (en) * | 1973-10-30 | 1976-05-11 | Eli Lilly And Company | 2,4-Diaminoquinazolines as antithrombotic agents |
| US3966936A (en) * | 1974-02-21 | 1976-06-29 | Pfizer Inc. | Piperazino quinazoline bronchodilators |
| US4060615A (en) * | 1976-02-18 | 1977-11-29 | Mead Johnson & Company | 2-Piperazinyl-6,7-dimethoxyquinazolines |
| JPS5991408A (ja) * | 1982-11-18 | 1984-05-26 | Nippon Kogaku Kk <Nikon> | ビハインド絞りレンズ |
| MX19185A (es) * | 1989-01-20 | 1993-12-01 | Pfizer | Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas. |
| HU207859B (en) | 1990-08-31 | 1993-06-28 | Alkaloida Vegyeszeti Gyar | Process for producing new amino-quinoline derivatives and pharmaceutical compositions containing them |
| WO1995003286A1 (en) | 1993-07-23 | 1995-02-02 | The Green Cross Corporation | Triazole derivative and pharmaceutical use thereof |
| WO1995034311A1 (en) | 1994-06-13 | 1995-12-21 | Merck & Co., Inc. | Piperazine compounds promote release of growth hormone |
| GB9416189D0 (en) * | 1994-08-10 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
| US5525625A (en) * | 1995-01-24 | 1996-06-11 | Warner-Lambert Company | 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders |
| ZA979961B (en) * | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| US6506798B1 (en) * | 1997-07-01 | 2003-01-14 | Warner-Lambert Company | 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors |
| US6310060B1 (en) * | 1998-06-24 | 2001-10-30 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors |
| AU757046B2 (en) | 1997-07-01 | 2003-01-30 | Warner-Lambert Company | 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
| US6821963B2 (en) * | 1997-07-01 | 2004-11-23 | Warner-Lambert Company | 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
| JP2002509536A (ja) | 1997-07-01 | 2002-03-26 | ワーナー−ランバート・カンパニー | 2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用 |
| AU3053999A (en) * | 1998-03-31 | 1999-10-25 | Kyowa Hakko Kogyo Co. Ltd. | Nitrogenous heterocyclic compounds |
| AU2203800A (en) | 1999-01-07 | 2000-07-24 | Warner-Lambert Company | Antiviral method using mek inhibitors |
| DE69924641D1 (de) | 1999-01-07 | 2005-05-12 | Warner Lambert Company Llc Mor | Behandlung von asthma anhand von mek-inhibitoren |
| CA2348236A1 (en) | 1999-01-13 | 2000-07-20 | Stephen Douglas Barrett | 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors |
| CA2349467A1 (en) * | 1999-01-13 | 2000-07-20 | Warner-Lambert Company | Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors |
| CA2349180A1 (en) | 1999-01-13 | 2000-07-20 | Stephen Douglas Barrett | Anthranilic acid derivatives |
| AU2201500A (en) * | 1999-01-13 | 2000-08-01 | Warner-Lambert Company | Benzenesulfonamide derivatives and their use as mek inhibitors |
| IL144214A0 (en) | 1999-01-13 | 2002-05-23 | Warner Lambert Co | Benzoheterocycles and their use as mek inhibitors |
| GEP20032999B (en) | 1999-01-13 | 2003-06-25 | Warner Lambert Co | 1-Heterocycle Substituted Diarylamines |
| GB9903548D0 (en) | 1999-02-16 | 1999-04-07 | Novartis Ag | Organic compounds |
| GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| EP1202732A2 (en) | 1999-07-16 | 2002-05-08 | Warner-Lambert Company Llc | Method for treating chronic pain using mek inhibitors |
| AU6068600A (en) | 1999-07-16 | 2001-02-05 | Warner-Lambert Company | Method for treating chronic pain using mek inhibitors |
| KR20020012315A (ko) | 1999-07-16 | 2002-02-15 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | Mek 저해제를 사용한 만성 통증의 치료 방법 |
| DK1202724T3 (da) | 1999-07-16 | 2004-01-26 | Warner Lambert Co | Fremgangsmåde til behandling af kronisk smerte under anvendelse af mek-inhibitorer |
| UA75055C2 (uk) | 1999-11-30 | 2006-03-15 | Пфайзер Продактс Інк. | Похідні бензоімідазолу, що використовуються як антипроліферативний засіб, фармацевтична композиція на їх основі |
| AU2001247372A1 (en) | 2000-03-15 | 2001-09-24 | Warner Lambert Company | 5-amide substituted diarylamines as mex inhibitors |
| WO2002006213A2 (en) | 2000-07-19 | 2002-01-24 | Warner-Lambert Company | Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids |
| KR20030059115A (ko) | 2000-08-25 | 2003-07-07 | 워너-램버트 캄파니 엘엘씨 | N-아릴-안트라닐산 및 그의 유도체의 제조 방법 |
| AU2002210714A1 (en) | 2000-11-02 | 2002-06-11 | Astrazeneca Ab | Substituted quinolines as antitumor agents |
| WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| JP4310109B2 (ja) * | 2001-04-26 | 2009-08-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾリル基を置換基として有する含窒素縮合環化合物およびその医薬組成物 |
| UY27304A1 (es) | 2001-05-24 | 2002-12-31 | Avanir Pharmaceuticals | Inhibidores del factor inhibidor de la migración de los macrófagos y métodos para su identificación |
| US7115741B2 (en) | 2001-09-06 | 2006-10-03 | Levy Daniel E | 4-thieno[2,3-D]pyrimidin-4-YL piperazine compounds |
| US20030187026A1 (en) * | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| WO2003077855A2 (en) | 2002-03-13 | 2003-09-25 | Array Biopharma, Inc | N3 alkylated benzimidazole derivatives as mek inhibitors |
| US7235537B2 (en) * | 2002-03-13 | 2007-06-26 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as MEK inhibitors |
| TWI343377B (en) | 2002-03-13 | 2011-06-11 | Array Biopharma Inc | N3 alkylated benzimidazole derivatives as mek inhibitors |
| WO2003086279A2 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| WO2003086394A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| US7273869B2 (en) | 2002-04-08 | 2007-09-25 | Merck & Co., Inc. | Inhibitors of Akt activity |
| WO2003086403A1 (en) | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| MXPA04012393A (es) | 2002-06-12 | 2005-06-17 | Chemocentryx | Derivados de piperazina 1-aril-4-substituidos para utilizar como antagonistas ccr1 para tratamiento de inflamacion y desordenes inmunes. |
| AU2003247772A1 (en) | 2002-06-27 | 2004-01-19 | Schering Aktiengesellschaft | Substituted quinoline ccr5 receptor antagonists |
| WO2004018453A1 (ja) | 2002-08-23 | 2004-03-04 | Dainippon Pharmaceutical Co., Ltd. | プロリン誘導体 |
| MXPA05009459A (es) | 2003-03-03 | 2006-05-17 | Array Biopharma Inc | Inhibidores de p38 y sus metodos de uso. |
| MXPA06002853A (es) | 2003-09-11 | 2006-06-14 | Kemia Inc | Inhibidores citoquina. |
-
2004
- 2004-11-19 US US10/993,173 patent/US20050130954A1/en not_active Abandoned
- 2004-11-19 NZ NZ547327A patent/NZ547327A/xx not_active IP Right Cessation
- 2004-11-19 KR KR1020117028995A patent/KR20110137838A/ko not_active Ceased
- 2004-11-19 WO PCT/US2004/039094 patent/WO2005051304A2/en not_active Ceased
- 2004-11-19 JP JP2006541594A patent/JP2007512364A/ja not_active Withdrawn
- 2004-11-19 CN CN2012102808790A patent/CN102786482A/zh active Pending
- 2004-11-19 CN CNA2004800342342A patent/CN1882347A/zh active Pending
- 2004-11-19 RU RU2006121990/04A patent/RU2006121990A/ru not_active Application Discontinuation
- 2004-11-19 BR BRPI0416852-6A patent/BRPI0416852A/pt not_active Application Discontinuation
- 2004-11-19 EP EP04811755A patent/EP1684694A2/en not_active Withdrawn
- 2004-11-19 CA CA002546754A patent/CA2546754A1/en not_active Abandoned
- 2004-11-19 PH PH1/2012/501891A patent/PH12012501891A1/en unknown
- 2004-11-19 AU AU2004293026A patent/AU2004293026B2/en not_active Ceased
- 2004-11-19 KR KR1020067009848A patent/KR101223914B1/ko not_active Expired - Fee Related
- 2004-11-19 NZ NZ590160A patent/NZ590160A/en not_active IP Right Cessation
-
2006
- 2006-04-26 IL IL175221A patent/IL175221A/en not_active IP Right Cessation
- 2006-05-19 ZA ZA200604069A patent/ZA200604069B/xx unknown
- 2006-06-20 NO NO20062884A patent/NO20062884L/no not_active Application Discontinuation
-
2009
- 2009-09-25 US US12/567,258 patent/US8680114B2/en not_active Expired - Fee Related
-
2010
- 2010-10-06 IL IL208520A patent/IL208520A0/en unknown
-
2014
- 2014-01-31 US US14/170,272 patent/US20160152576A9/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| NZ547327A (en) | 2009-08-28 |
| JP2007512364A (ja) | 2007-05-17 |
| WO2005051304A3 (en) | 2006-07-27 |
| IL175221A (en) | 2015-05-31 |
| CN102786482A (zh) | 2012-11-21 |
| US8680114B2 (en) | 2014-03-25 |
| RU2006121990A (ru) | 2007-12-27 |
| US20100168123A1 (en) | 2010-07-01 |
| KR20110137838A (ko) | 2011-12-23 |
| AU2004293026B2 (en) | 2012-01-19 |
| PH12012501891A1 (en) | 2013-09-02 |
| NZ590160A (en) | 2012-07-27 |
| US20160152576A9 (en) | 2016-06-02 |
| US20140148436A1 (en) | 2014-05-29 |
| CA2546754A1 (en) | 2005-06-09 |
| US20050130954A1 (en) | 2005-06-16 |
| KR101223914B1 (ko) | 2013-01-18 |
| KR20070026332A (ko) | 2007-03-08 |
| EP1684694A2 (en) | 2006-08-02 |
| AU2004293026A1 (en) | 2005-06-09 |
| NO20062884L (no) | 2006-08-18 |
| CN1882347A (zh) | 2006-12-20 |
| IL175221A0 (en) | 2006-10-31 |
| ZA200604069B (en) | 2009-04-29 |
| WO2005051304A2 (en) | 2005-06-09 |
| IL208520A0 (en) | 2010-12-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PH12012501891A1 (en) | Akt protein kinase inhibitors | |
| BRPI0713923B8 (pt) | compostos de ciclopentanos de pirimidila hidroxilados e metoxilados, composição farmacêutica compreendendo os referidos compostos, método de preparação de um composto, e uso dos mesmos | |
| BRPI0407699A (pt) | Inibidores de rna-polimerase dependente de rna de vìrus de hepatite c e composições e tratamentos que os utilizam | |
| BRPI0713555A2 (pt) | ciclopenta [d] pirimidinas como inibidores de akt protéina cinase | |
| MX2010010151A (es) | Moduladores de cinasa aurora y metodo de uso. | |
| ATE493418T1 (de) | Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren | |
| EA201400111A1 (ru) | Ингибиторы mek и способы их применения | |
| EA200501849A1 (ru) | Производные пиразолохиназолина: способ получения и применение в качестве ингибиторов киназ | |
| BRPI0416692A (pt) | inibidores heterocìclicos de mek e métodos de emprego destes | |
| BRPI0413152A (pt) | derivados de benzimidazol alquilado por n3 como inibidores de mek | |
| DK2054418T3 (da) | Dihydrothieno-pyrimidiner som AKT-proteinkinase-inhibitorer | |
| BRPI0414111A (pt) | inibidores heterocìclicos de mek e métodos de uso dos mesmos | |
| BRPI0414533A (pt) | composto, composição farmacêutica, e, métodos para inibir um hsp90 e para tratar um indivìduo tendo um distúrbio mediado por hsp90 | |
| BRPI0312464B8 (pt) | compostos inibidores de tirosina quinases, composições farmacêuticas compreendendo os mesmos, processos para fabricação e usos dos mesmos | |
| BRPI0410669A (pt) | inibidores de caspase e usos dos mesmo | |
| BR0208373A (pt) | Inibidores da tirosina cinase | |
| BR0014073A (pt) | Pirazolopirimidinas como agentes terapêuticos | |
| DE60206911D1 (de) | Imidazol-2-carbonsäureamid derivate als raf-kinase-inhibitoren | |
| BR0315580A (pt) | Derivados de metileno uréia | |
| BRPI0411891A (pt) | pirazol[3,4-b]piridin-6-onas como inibidores de gsk-3 | |
| BR9908125A (pt) | Composto, composto dimérico, composição farmacêutica, uso do composto, processo compreendendo inibir células de câncer, e, processo terapêutico | |
| BRPI0513513A (pt) | composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, métodos para produzir um efeito inibitório de eg5 e um efeito anticáncer em um animal de sangue quente, e para tratar carcinomas em um animal de sangue quente | |
| BR9911559A (pt) | Processo para a preparação de um composto, composto, processo para o tratamento de tumores resistentes a medicamento múltiplo, uso de um composto, e, agente e composição para tratar tumores resistentes a medicamento múltiplo. | |
| BRPI0415678A (pt) | compostos de pirimidina para o tratamento de inflamação | |
| EP1453507A4 (en) | SOLUBILIZED TOPOISOMERASE GIFT MEDIUM |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |