CO4940458A1 - Novedosos inhibidores de urea n-sustituida de transferasa de proteina farnesilo - Google Patents
Novedosos inhibidores de urea n-sustituida de transferasa de proteina farnesiloInfo
- Publication number
- CO4940458A1 CO4940458A1 CO98034144A CO98034144A CO4940458A1 CO 4940458 A1 CO4940458 A1 CO 4940458A1 CO 98034144 A CO98034144 A CO 98034144A CO 98034144 A CO98034144 A CO 98034144A CO 4940458 A1 CO4940458 A1 CO 4940458A1
- Authority
- CO
- Colombia
- Prior art keywords
- hydrogen
- farnesilo
- alkyl
- protein transferase
- independently selected
- Prior art date
Links
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
Un compuesto de fórmula (1.0) o una sal o solvatofarmacéuticamente aceptable del mismo, en donde A representa N o N-óxido; X representa N, CH ó C, de manera que cuando X es N ó CH, hay un único enlace al átomo de carbono 11 según se representa por la línea sólida; o cuando X es C, hay un doble enlace al átomo de carbono 11, según se representa por las líneas punteada y sólida; X1 y X2 son independientemente seleccionados entre bromo o cloro, y X3 y X4 son independientemente seleccionados entre hidrógeno, bromo o cloro siempre que por lo menos uno de X3 y X4 sea hidrógeno; Y1 y Y2 son independientemente seleccionados entre hidrógeno o alquilo; Z es =O ó =S; R5 , R6 , R7 y R8 cada uno representa independientemente hidrógeno, -CF3 , -COR10 , alquilo o arilo, y adicionalmente en donde R5 puede combinarse con R6 para representar =O ó =S y/o R7 puede combinarse con R8 para representar =O ó =S; R10 , R19 y R20 representan independientemente hidrógeno, alquilo, alcoxi, arilo, aralquilo, heteroarilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo y heterocicloalquilalquilo, con la condición de que R19 y R20 no sean ambos hidrógeno; V es cero, 1, 2 ó 3 y W es cero ó 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87704997A | 1997-06-17 | 1997-06-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO4940458A1 true CO4940458A1 (es) | 2000-07-24 |
Family
ID=25369144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO98034144A CO4940458A1 (es) | 1997-06-17 | 1998-06-16 | Novedosos inhibidores de urea n-sustituida de transferasa de proteina farnesilo |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP0989979A1 (es) |
| JP (1) | JP2002506444A (es) |
| KR (1) | KR20010013881A (es) |
| CN (1) | CN1267291A (es) |
| AR (1) | AR013094A1 (es) |
| AU (1) | AU8253598A (es) |
| CA (1) | CA2293706C (es) |
| CO (1) | CO4940458A1 (es) |
| HU (1) | HUP0002954A3 (es) |
| IL (1) | IL133389A0 (es) |
| NZ (1) | NZ501571A (es) |
| PE (1) | PE82799A1 (es) |
| WO (1) | WO1998057948A1 (es) |
| ZA (1) | ZA985205B (es) |
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 |
| NZ501571A (en) | 2002-02-01 |
| AU8253598A (en) | 1999-01-04 |
| KR20010013881A (ko) | 2001-02-26 |
| HUP0002954A3 (en) | 2002-11-28 |
| HUP0002954A2 (hu) | 2001-06-28 |
| CA2293706A1 (en) | 1998-12-23 |
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