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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (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)
- Plural Heterocyclic 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 |
| 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 |
| CA2424797C (en) | 2000-10-05 | 2009-12-29 | George Q. Daley | Methods of inducing cancer cell death and tumor regression |
| WO2005058823A1 (ja) * | 2003-12-17 | 2005-06-30 | Takeda Pharmaceutical Company Limited | ウレア誘導体、その製造法及び用途 |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| JP6473133B2 (ja) * | 2013-03-15 | 2019-02-20 | アラクセス ファーマ エルエルシー | Ｋｒａｓｇ１２ｃの共有結合性阻害剤 |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| 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 |
| CN107849022A (zh) | 2015-04-10 | 2018-03-27 | 亚瑞克西斯制药公司 | 取代的喹唑啉化合物和其使用方法 |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method 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 |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | 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 |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| CN110312711A (zh) | 2016-10-07 | 2019-10-08 | 亚瑞克西斯制药公司 | 作为ras抑制剂的杂环化合物及其使用方法 |
| US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole 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 |
| US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
| WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| TW201906832A (zh) | 2017-05-25 | 2019-02-16 | 美商亞瑞克西斯製藥公司 | 用於癌症治療之化合物及其使用方法 |
| EP3630747A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| CN110869358A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
| 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| JP3193725B2 (ja) * | 1995-12-22 | 2001-07-30 | シェーリング コーポレイション | Ｇ―タンパク質機能の阻害および増殖性疾患の処置に有用な三環式アミド |
| ATE286044T1 (de) * | 1996-09-13 | 2005-01-15 | Schering Corp | Trizyklische verbindungen mit farnesyl protein transferase inhibierender wirkung |
| IL128929A0 (en) * | 1996-09-13 | 2000-02-17 | Schering Corp | Substituted benzocycloheptapyridine derivatives useful for inhibition of farnesyl protein transferase |
-
1998
- 1998-06-15 CA CA002293706A patent/CA2293706C/en not_active Expired - Fee Related
- 1998-06-15 NZ NZ501571A patent/NZ501571A/en unknown
- 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 IL IL13338998A patent/IL133389A0/xx unknown
- 1998-06-15 AU AU82535/98A patent/AU8253598A/en not_active Abandoned
- 1998-06-15 ZA ZA985205A patent/ZA985205B/xx unknown
- 1998-06-15 WO PCT/US1998/011507 patent/WO1998057948A1/en not_active Application Discontinuation
- 1998-06-15 JP JP50450299A patent/JP2002506444A/ja not_active Ceased
- 1998-06-15 HU HU0002954A patent/HUP0002954A3/hu unknown
- 1998-06-15 CN CN98808189A patent/CN1267291A/zh active Pending
- 1998-06-16 CO CO98034144A patent/CO4940458A1/es unknown
- 1998-06-16 AR ARP980102858A patent/AR013094A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0989979A1 (en) | 2000-04-05 |
| IL133389A0 (en) | 2001-04-30 |
| JP2002506444A (ja) | 2002-02-26 |
| CA2293706C (en) | 2008-11-18 |
| AR013094A1 (es) | 2000-12-13 |
| PE82799A1 (es) | 1999-08-26 |
| CN1267291A (zh) | 2000-09-20 |
| WO1998057948A1 (en) | 1998-12-23 |
| ZA985205B (en) | 1998-12-15 |
| CO4940458A1 (es) | 2000-07-24 |
| NZ501571A (en) | 2002-02-01 |
| AU8253598A (en) | 1999-01-04 |
| KR20010013881A (ko) | 2001-02-26 |
| HUP0002954A3 (en) | 2002-11-28 |
| CA2293706A1 (en) | 1998-12-23 |
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