AR063805A1 - Derivados de triazol sustituidos como inhibidores de ksp. composiciones farmaceuticas. - Google Patents
Derivados de triazol sustituidos como inhibidores de ksp. composiciones farmaceuticas.Info
- Publication number
- AR063805A1 AR063805A1 ARP070105052A ARP070105052A AR063805A1 AR 063805 A1 AR063805 A1 AR 063805A1 AR P070105052 A ARP070105052 A AR P070105052A AR P070105052 A ARP070105052 A AR P070105052A AR 063805 A1 AR063805 A1 AR 063805A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- group
- heterocycloalkyl
- cycloalkyl
- Prior art date
Links
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical class C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 11
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 8
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 2
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 2
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
- C07D401/12—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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Composiciones de los derivados junto con portadores farmacéuticamente aceptables y usos de los mismos. Reivindicación 1: Un compuesto caracterizado porque tiene fórmula (1), o una sal, éster o prodroga farmacéuticamente aceptable del mismo en donde: R1 se selecciona a partir del grupo consistente en alquilo y alquilo sustituido; R2 se selecciona a partir del grupo consistente en hidrógeno, alquilo y alquilo sustituido; R3 se selecciona a partir del grupo consistente en -L1-A1, donde L1 se selecciona a partir del grupo consistente en -C(O)-, -C(S)-, -S(O)-, y -S(O)2- y A1 se selecciona a partir del grupo consistente en alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido y NR8R9; R4 se selecciona a partir del grupo consistente en hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo y alquinilo sustituido, o R3 y R4, junto con el átomo de nitrógeno al que están unidos, se unen para formar un grupo heterocicloalquilo o heterocicloalquilo sustituido de cinco a siete miembros, donde opcionalmente un átomo adicional del anillo se selecciona a partir del grupo consistente en O, S, o NR11; X es CR5 o N; R5 se selecciona a partir del grupo consistente en hidrógeno, halo, alquilo y alquilo sustituido; R6 se selecciona a partir del grupo consistente en cicloalquilo, heterocicloalquilo, arilo y heteroarilo, todos los cuales pueden estar opcionalmente sustituidos con -(R10)m, donde R10 es el definido en este documento, m es 1, 2, 3 o 4, y cada R10 puede ser el mismo o diferente cuando m es 2, 3 o 4; R7 es -L2-A2, donde l2 es alquileno C1-5 y A2 se selecciona a partir del grupo consistente en arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocicloalquilo y heterocicloalquilo sustituido, siempre que R7 no esté unido a X; R8 se selecciona a partir del grupo consistente en hidrógeno y alquilo; R9 se selecciona a partir del grupo consistente en hidrógeno, hidroxi, alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocicloalquilo y heterocicloalquilo sustituido; o R8 y R9, junto con el átomo de nitrógeno unido a ellos, se unen para formar un heterocicloalquilo o un heterocicloalquilo sustituido; R10 se selecciona a partir del grupo consistente en ciano, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, CF3, alcoxi, alcoxi sustituido, halo e hidroxi; y R11 se selecciona a partir del grupo consistente en hidrógeno, alquilo, alquilo sustituido, -SO2-alquilo y -SO2-alquilo sustituido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85896406P | 2006-11-13 | 2006-11-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR063805A1 true AR063805A1 (es) | 2009-02-18 |
Family
ID=39144618
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070105052A AR063805A1 (es) | 2006-11-13 | 2007-11-13 | Derivados de triazol sustituidos como inhibidores de ksp. composiciones farmaceuticas. |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US7902240B2 (es) |
| EP (1) | EP2091926B1 (es) |
| JP (1) | JP5264755B2 (es) |
| KR (1) | KR20090081020A (es) |
| CN (1) | CN101558049B (es) |
| AR (1) | AR063805A1 (es) |
| AU (1) | AU2007323998B2 (es) |
| BR (1) | BRPI0719002A2 (es) |
| CA (1) | CA2668661A1 (es) |
| CL (1) | CL2007003272A1 (es) |
| CO (1) | CO6382171A2 (es) |
| CR (1) | CR10787A (es) |
| DO (1) | DOP2009000106A (es) |
| EA (1) | EA017748B1 (es) |
| EC (1) | ECSP099326A (es) |
| ES (1) | ES2557478T3 (es) |
| GE (1) | GEP20125389B (es) |
| GT (1) | GT200900122A (es) |
| HN (1) | HN2009000968A (es) |
| IL (1) | IL198471A0 (es) |
| MA (1) | MA30959B1 (es) |
| MX (1) | MX2009005071A (es) |
| NI (1) | NI200900084A (es) |
| NO (1) | NO20092226L (es) |
| NZ (1) | NZ576640A (es) |
| PE (1) | PE20081169A1 (es) |
| SM (1) | SMP200900045B (es) |
| TN (1) | TN2009000178A1 (es) |
| TW (1) | TW200831480A (es) |
| UA (1) | UA97256C2 (es) |
| WO (1) | WO2008063912A1 (es) |
| ZA (1) | ZA200902940B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7902240B2 (en) * | 2006-11-13 | 2011-03-08 | Novartis Ag | Substituted pyrazole and triazole compounds as KSP inhibitors |
| CA2674318A1 (en) * | 2007-01-05 | 2008-07-17 | Novartis Ag | Cyclized derivatives as eg-5 inhibitors |
| WO2011128381A1 (en) * | 2010-04-15 | 2011-10-20 | Novartis Ag | Triazole compounds as ksp inhibitors |
| EP2558452A2 (en) * | 2010-04-15 | 2013-02-20 | Novartis AG | Oxazole and thiazole compounds as ksp inhibitors |
| BR112015012843B8 (pt) * | 2012-12-05 | 2023-04-25 | Merck Sharp & Dohme | Método para sintetizar o composto |
| US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
| CN105451773A (zh) * | 2013-03-15 | 2016-03-30 | 诺华股份有限公司 | 细胞增殖抑制剂及其缀合物 |
| WO2015084763A2 (en) | 2013-12-04 | 2015-06-11 | Merck Sharp & Dohme Corp. | Process for making reverse transcriptase inhibitors |
| US10786578B2 (en) | 2014-08-05 | 2020-09-29 | Novartis Ag | CKIT antibody drug conjugates |
| WO2017097927A1 (en) * | 2015-12-11 | 2017-06-15 | Syngenta Participations Ag | Pesticidally active 1,2,4-triazole derivatives |
| AU2020417293A1 (en) | 2020-01-03 | 2022-09-01 | Berg Llc | Polycyclic amides as UBE2K modulators for treating cancer |
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| US5023252A (en) * | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4837028A (en) | 1986-12-24 | 1989-06-06 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| US5185450A (en) | 1991-02-19 | 1993-02-09 | University Of South Florida | Tetrazolium compounds for cell viability assays |
| AUPP042397A0 (en) * | 1997-11-18 | 1997-12-11 | Fujisawa Pharmaceutical Co., Ltd. | 5-arylpyrazole compounds |
| JP2002541146A (ja) | 1999-04-02 | 2002-12-03 | ニューロゲン コーポレイション | アリールおよびヘテロアリール融合のアミノアルキル−イミダゾール誘導体および糖尿病薬としてのその使用 |
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-
2007
- 2007-11-08 US US11/937,426 patent/US7902240B2/en not_active Expired - Fee Related
- 2007-11-08 UA UAA200904556A patent/UA97256C2/ru unknown
- 2007-11-08 GE GEAP200711253A patent/GEP20125389B/en unknown
- 2007-11-08 BR BRPI0719002-6A patent/BRPI0719002A2/pt not_active IP Right Cessation
- 2007-11-08 AU AU2007323998A patent/AU2007323998B2/en not_active Ceased
- 2007-11-08 KR KR1020097012214A patent/KR20090081020A/ko not_active Application Discontinuation
- 2007-11-08 US US12/312,389 patent/US8129358B2/en not_active Expired - Fee Related
- 2007-11-08 EP EP07844993.1A patent/EP2091926B1/en active Active
- 2007-11-08 MX MX2009005071A patent/MX2009005071A/es active IP Right Grant
- 2007-11-08 CA CA002668661A patent/CA2668661A1/en not_active Abandoned
- 2007-11-08 CN CN2007800456741A patent/CN101558049B/zh not_active Expired - Fee Related
- 2007-11-08 JP JP2009536490A patent/JP5264755B2/ja not_active Expired - Fee Related
- 2007-11-08 EA EA200900631A patent/EA017748B1/ru not_active IP Right Cessation
- 2007-11-08 WO PCT/US2007/084154 patent/WO2008063912A1/en active Application Filing
- 2007-11-08 ES ES07844993.1T patent/ES2557478T3/es active Active
- 2007-11-08 NZ NZ576640A patent/NZ576640A/en not_active IP Right Cessation
- 2007-11-12 TW TW096142719A patent/TW200831480A/zh unknown
- 2007-11-13 AR ARP070105052A patent/AR063805A1/es unknown
- 2007-11-13 CL CL200703272A patent/CL2007003272A1/es unknown
- 2007-11-13 PE PE2007001561A patent/PE20081169A1/es not_active Application Discontinuation
-
2009
- 2009-04-29 ZA ZA200902940A patent/ZA200902940B/xx unknown
- 2009-04-30 IL IL198471A patent/IL198471A0/en unknown
- 2009-05-08 TN TNP2009000178A patent/TN2009000178A1/fr unknown
- 2009-05-08 CR CR10787A patent/CR10787A/es not_active Application Discontinuation
- 2009-05-11 DO DO2009000106A patent/DOP2009000106A/es unknown
- 2009-05-12 CO CO09048059A patent/CO6382171A2/es not_active Application Discontinuation
- 2009-05-12 GT GT200900122A patent/GT200900122A/es unknown
- 2009-05-13 NI NI200900084A patent/NI200900084A/es unknown
- 2009-05-13 EC EC2009009326A patent/ECSP099326A/es unknown
- 2009-05-13 HN HN2009000968A patent/HN2009000968A/es unknown
- 2009-06-01 MA MA31938A patent/MA30959B1/fr unknown
- 2009-06-09 NO NO20092226A patent/NO20092226L/no not_active Application Discontinuation
- 2009-06-10 SM SM200900045T patent/SMP200900045B/it unknown
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