HUP0002954A2 - Farnezil-protein transzferáz új N-szubsztituált-karbamid inhibitorai - Google Patents
Farnezil-protein transzferáz új N-szubsztituált-karbamid inhibitoraiInfo
- Publication number
- HUP0002954A2 HUP0002954A2 HU0002954A HUP0002954A HUP0002954A2 HU P0002954 A2 HUP0002954 A2 HU P0002954A2 HU 0002954 A HU0002954 A HU 0002954A HU P0002954 A HUP0002954 A HU P0002954A HU P0002954 A2 HUP0002954 A2 HU P0002954A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- hydrogen
- atom
- oxo
- alkyl
- Prior art date
Links
- 102000004357 Transferases Human genes 0.000 title 1
- 108090000992 Transferases Proteins 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003672 ureas Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 125000000464 thioxo group Chemical group S=* 0.000 abstract 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 2
- 229910052794 bromium Inorganic materials 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- -1 -COR10 Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
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
-
- 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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
Above=16;>(57) A találmány tárgyát az (1.0) általános képletűvegyületek < ahol A nitrogénatom vagy N-oxid-csoport; X nitrogénatom,metincsoport, ha a 11-es szénatomhoz kapcsolódó <-egyes kötés, vagyszénatom, ha a 11-es szénatomhoz kapcsolódó <-kettős kötés; X1 és X2bróm- vagy klóratom; X3 és X4 hidrogén-, bróm- vagy klóratom, azzal amegkötéssel, hogy X3 és X4 legalább egyike hidrogénatom; Y1 és Y2hidrogénatom vagy alkilcsoport; Z oxo- vagy tioxocsoport; R5, R6, R7és R8 hidrogénatom, trifluor-metil-, -COR10, alkil- vagy arilcsoport,valamint R5 és R6 együtt oxo- vagy tioxocsoport és/vagy R7 és R8együtt oxo- vagy tioxocsoport; R10, R19 és R20 hidrogénatom, alkil-,alkoxi-, aril-, aralkil-, heteroaril-, heteroaril-alkil-, cikloalkil-,cikloalkil-alkil-, heterocikloalkil- vagy heteroacikloalkil-alkil-csoport, azzal a megkötéssel, hogy R19 és R20 mindegyike nem lehethidrogénatom; v 0, 1, 2 vagy 3; és w 0 vagy 1 - és gyógyszerészetilegelfogadható sói vagy szolvátjaik, ezeket tartalmazógyógyszerkészítmények, valamint abnormális sejtnövekedés gátlásáravaló alkalmazásuk képezik. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87704997A | 1997-06-17 | 1997-06-17 | |
| PCT/US1998/011507 WO1998057948A1 (en) | 1997-06-17 | 1998-06-15 | Novel n-substituted urea inhibitors of farnesyl-protein transferase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0002954A2 true HUP0002954A2 (hu) | 2001-06-28 |
| HUP0002954A3 HUP0002954A3 (en) | 2002-11-28 |
Family
ID=25369144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0002954A HUP0002954A3 (en) | 1997-06-17 | 1998-06-15 | Novel n-substituted urea inhibitors of farnesyl-protein transferase |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP0989979A1 (hu) |
| JP (1) | JP2002506444A (hu) |
| KR (1) | KR20010013881A (hu) |
| CN (1) | CN1267291A (hu) |
| AR (1) | AR013094A1 (hu) |
| AU (1) | AU8253598A (hu) |
| CA (1) | CA2293706C (hu) |
| CO (1) | CO4940458A1 (hu) |
| HU (1) | HUP0002954A3 (hu) |
| IL (1) | IL133389A0 (hu) |
| NZ (1) | NZ501571A (hu) |
| PE (1) | PE82799A1 (hu) |
| WO (1) | WO1998057948A1 (hu) |
| ZA (1) | ZA985205B (hu) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7342016B2 (en) | 2000-08-30 | 2008-03-11 | Schering Corporation | Farnesyl protein transferase inhibitors as antitumor agents |
| HUP0302913A3 (en) * | 2000-10-05 | 2005-05-30 | Daley George Q Weston | Methods of inducing cancer cell death and tumor regression and preparation of pharmaceutical compositions suitable for treating the same |
| AU2002211427A1 (en) * | 2000-10-05 | 2002-04-15 | Whitehead Institute For Biomedical Research | Effects of combined administration of farnesyl transferase inhibitors and signal transduction inhibitors |
| EP1695961A4 (en) * | 2003-12-17 | 2007-10-24 | Takeda Pharmaceutical | UREA DERIVATIVE, METHOD FOR THE PRODUCTION AND THEIR USE |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| TW201524952A (zh) * | 2013-03-15 | 2015-07-01 | Araxes Pharma Llc | Ｋｒａｓ ｇ１２ｃ之共價抑制劑 |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| US10246424B2 (en) | 2015-04-10 | 2019-04-02 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| ES2856880T3 (es) | 2015-04-15 | 2021-09-28 | Araxes Pharma Llc | Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10875842B2 (en) | 2015-09-28 | 2020-12-29 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3364977A4 (en) | 2015-10-19 | 2019-09-04 | Araxes Pharma LLC | PROCESS FOR SCREENING INHIBITORS OF RAS |
| US10414757B2 (en) | 2015-11-16 | 2019-09-17 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| EP3519402A1 (en) | 2016-09-29 | 2019-08-07 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
| WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| EP3573970A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| EP3573967A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused hetero-hetero bicyclic compounds and methods of use thereof |
| JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| CA3063440A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Covalent inhibitors of kras |
| CN111960990A (zh) * | 2020-07-23 | 2020-11-20 | 宿迁联盛科技股份有限公司 | 一种助剂及其制备方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111235A (en) * | 1993-10-15 | 2001-03-19 | Schering Plough Corp | Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them |
| US5719148A (en) * | 1993-10-15 | 1998-02-17 | Schering Corporation | Tricyclic amide and urea 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 |
| IL125062A (en) * | 1995-12-22 | 2003-11-23 | Schering Corp | Tricyclic amides and pharmaceutical compositions containing them for inhibition of g-protein function and for treatment of proliferative diseases |
| ES2234036T3 (es) * | 1996-09-13 | 2005-06-16 | Schering Corporation | Compuestos utiles para inhibir la farnesil-protein-transferasa. |
| CZ87499A3 (cs) * | 1996-09-13 | 1999-08-11 | Schering Corporation | Substituované deriváty benzocykloheptapyridinu použitelné při léčbě nádorových onemocnění tím, že inhibují farnesylprotein transferázu |
-
1998
- 1998-06-15 EP EP98932717A patent/EP0989979A1/en not_active Withdrawn
- 1998-06-15 PE PE1998000506A patent/PE82799A1/es not_active Application Discontinuation
- 1998-06-15 KR KR1019997011903A patent/KR20010013881A/ko not_active Application Discontinuation
- 1998-06-15 HU HU0002954A patent/HUP0002954A3/hu unknown
- 1998-06-15 CA CA002293706A patent/CA2293706C/en not_active Expired - Fee Related
- 1998-06-15 WO PCT/US1998/011507 patent/WO1998057948A1/en not_active Application Discontinuation
- 1998-06-15 CN CN98808189A patent/CN1267291A/zh active Pending
- 1998-06-15 JP JP50450299A patent/JP2002506444A/ja not_active Ceased
- 1998-06-15 AU AU82535/98A patent/AU8253598A/en not_active Abandoned
- 1998-06-15 IL IL13338998A patent/IL133389A0/xx unknown
- 1998-06-15 ZA ZA985205A patent/ZA985205B/xx unknown
- 1998-06-15 NZ NZ501571A patent/NZ501571A/en unknown
- 1998-06-16 AR ARP980102858A patent/AR013094A1/es unknown
- 1998-06-16 CO CO98034144A patent/CO4940458A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU8253598A (en) | 1999-01-04 |
| IL133389A0 (en) | 2001-04-30 |
| JP2002506444A (ja) | 2002-02-26 |
| WO1998057948A1 (en) | 1998-12-23 |
| CO4940458A1 (es) | 2000-07-24 |
| CA2293706A1 (en) | 1998-12-23 |
| PE82799A1 (es) | 1999-08-26 |
| CN1267291A (zh) | 2000-09-20 |
| NZ501571A (en) | 2002-02-01 |
| ZA985205B (en) | 1998-12-15 |
| KR20010013881A (ko) | 2001-02-26 |
| EP0989979A1 (en) | 2000-04-05 |
| AR013094A1 (es) | 2000-12-13 |
| HUP0002954A3 (en) | 2002-11-28 |
| CA2293706C (en) | 2008-11-18 |
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