PE20081850A1 - Derivados ciclizados como inhibidores de la eg-5 - Google Patents
Derivados ciclizados como inhibidores de la eg-5Info
- Publication number
- PE20081850A1 PE20081850A1 PE2008000091A PE2008000091A PE20081850A1 PE 20081850 A1 PE20081850 A1 PE 20081850A1 PE 2008000091 A PE2008000091 A PE 2008000091A PE 2008000091 A PE2008000091 A PE 2008000091A PE 20081850 A1 PE20081850 A1 PE 20081850A1
- Authority
- PE
- Peru
- Prior art keywords
- independently
- rent
- inhibitors
- ona
- dimethylpropyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 2
- RAXXELZNTBOGNW-UHFFFAOYSA-O Imidazolium Chemical compound C1=C[NH+]=CN1 RAXXELZNTBOGNW-UHFFFAOYSA-O 0.000 abstract 1
- 102000010638 Kinesin Human genes 0.000 abstract 1
- 108010063296 Kinesin Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE IMIDAZOL DE FORMULA (I), EN DONDE R1 ES ALQUILO OPCIONALMENTE SUSTITUIDO; R2 ES H, ALQUILO OPCIONALMENTE SUSTITUIDO; L ES -O-, -OCH2-, -CH2OCH2-, -C(O)NR7, -CH2O-, ENTRE OTROS; R3 Y R4 SON INDEPENDIENTEMENTE HALO, ALQUILO OPCIONALMENTE SUSTITUIDO; R5 Y R6 SON INDEPENDIENTEMENTE CIANO, ALQUILO OPCIONALMENTE SUSTITUIDO, ALCOXI, ENTRE OTROS; m Y n SON INDEPENDIENTEMENTE DE 0 A 3; p ES 0 O 1. SON SELECCIONADOS: (S)-5-(AMINOMETIL)-3-((R)-1-(1-BENCIL-4-(2,5-DIFLUOROFENIL)-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL)OXAZOLIDIN-2-ONA, (5S)-5-(AMINOMEIL)-3-[(1R)-1-(1-BENCIL-4-FENIL-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL]-1,3-OXAZIN-2-ONA, ENTRE OTROS. TAMBIEN SE RERIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE PROTEINAS DE KINESINAS (KSP) EN ESPECIAL DE EG-5, POR LO QUE SON UTILES EN EL TRATAMIENTO DE UNA ENFERMEDAD DE PROLIFERACION CELULAR TAL COMO EL CANCER
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88374007P | 2007-01-05 | 2007-01-05 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20081850A1 true PE20081850A1 (es) | 2009-02-05 |
Family
ID=39577804
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2008000091A PE20081850A1 (es) | 2007-01-05 | 2008-01-04 | Derivados ciclizados como inhibidores de la eg-5 |
Country Status (30)
Country | Link |
---|---|
US (3) | US7820646B2 (es) |
EP (1) | EP2106399A2 (es) |
JP (1) | JP2010515687A (es) |
KR (1) | KR20090097210A (es) |
CN (1) | CN101622247A (es) |
AR (1) | AR064760A1 (es) |
AU (1) | AU2008205169B2 (es) |
BR (1) | BRPI0806264A2 (es) |
CA (1) | CA2674318A1 (es) |
CL (1) | CL2008000029A1 (es) |
CO (1) | CO6561828A2 (es) |
CR (1) | CR10879A (es) |
DO (1) | DOP2009000169A (es) |
EA (1) | EA200900924A1 (es) |
EC (1) | ECSP099485A (es) |
GE (1) | GEP20125415B (es) |
GT (1) | GT200900192A (es) |
HN (1) | HN2009001262A (es) |
MA (1) | MA31080B1 (es) |
MX (1) | MX2009007260A (es) |
NI (1) | NI200900134A (es) |
NZ (1) | NZ577727A (es) |
PE (1) | PE20081850A1 (es) |
SM (1) | SMP200900065B (es) |
SV (1) | SV2009003325A (es) |
TN (1) | TN2009000287A1 (es) |
TW (1) | TW200836722A (es) |
UA (1) | UA97821C2 (es) |
WO (1) | WO2008086122A2 (es) |
ZA (1) | ZA200904175B (es) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8252832B2 (en) | 2007-12-14 | 2012-08-28 | Novartis Ag | Kinesin inhibitors as cancer therapeutics |
EP2558452A2 (en) * | 2010-04-15 | 2013-02-20 | Novartis AG | Oxazole and thiazole compounds as ksp inhibitors |
WO2011128381A1 (en) | 2010-04-15 | 2011-10-20 | Novartis Ag | Triazole compounds as ksp inhibitors |
EP2390247A1 (en) | 2010-05-26 | 2011-11-30 | Netherlands Organisation for Scientific Research (Advanced Chemical Technologies for Sustainability) | Preparation of caprolactone, caprolactam, 2,5-tetrahydrofuran dimethanol, 1,6-hexanediol or 1,2,6-hexanetriol from 5-hydroxymethyl-2-furfuraldehyde |
GB201113538D0 (en) | 2011-08-04 | 2011-09-21 | Karobio Ab | Novel estrogen receptor ligands |
US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
EP2968591A1 (en) * | 2013-03-15 | 2016-01-20 | Novartis AG | Cell proliferation inhibitors and conjugates thereof |
SG11201604758PA (en) * | 2013-12-23 | 2016-07-28 | Bayer Pharma AG | Antibody drug conjugates (adcs) with kinesin spindel protein (ksp) |
MX2017017172A (es) * | 2015-06-22 | 2018-02-23 | Bayer Pharma AG | Conjugados de ligador-principio activo (adcs) y conjugados de ligador-profarmaco (apdcs) con grupos enzimaticamente escindibles. |
CN105367506B (zh) * | 2015-12-08 | 2021-02-05 | 华润双鹤药业股份有限公司 | 手性高哌嗪环的制备方法 |
CN105330657B (zh) * | 2015-12-08 | 2019-05-21 | 华润双鹤药业股份有限公司 | 5-氯-2-[5-(r)-甲基-1,4-二氮杂环庚烷-1-]苯并恶唑的制备方法 |
JP7022707B2 (ja) | 2016-06-15 | 2022-02-18 | バイエル・ファルマ・アクティエンゲゼルシャフト | Ksp阻害剤および抗cd123抗体を含む特異的抗体-薬物-コンジュゲート(adc) |
CA3047522A1 (en) | 2016-12-21 | 2018-06-28 | Bayer Pharma Aktiengesellschaft | Specific antibody drug conjugates (adcs) having ksp inhibitors |
WO2018114578A1 (de) | 2016-12-21 | 2018-06-28 | Bayer Pharma Aktiengesellschaft | Binder-wirkstoff-konjugate (adcs) mit enzymatisch spaltbaren gruppen |
CA3103327A1 (en) | 2018-06-18 | 2019-12-26 | Bayer Aktiengesellschaft | Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile |
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-
2008
- 2008-01-03 CN CN200880007148A patent/CN101622247A/zh active Pending
- 2008-01-03 GE GEAP200811346A patent/GEP20125415B/en unknown
- 2008-01-03 BR BRPI0806264-1A patent/BRPI0806264A2/pt not_active IP Right Cessation
- 2008-01-03 EA EA200900924A patent/EA200900924A1/ru unknown
- 2008-01-03 US US11/969,164 patent/US7820646B2/en not_active Expired - Fee Related
- 2008-01-03 WO PCT/US2008/050149 patent/WO2008086122A2/en active Application Filing
- 2008-01-03 NZ NZ577727A patent/NZ577727A/en not_active IP Right Cessation
- 2008-01-03 CA CA002674318A patent/CA2674318A1/en not_active Abandoned
- 2008-01-03 JP JP2009544977A patent/JP2010515687A/ja active Pending
- 2008-01-03 EP EP08705667A patent/EP2106399A2/en not_active Withdrawn
- 2008-01-03 MX MX2009007260A patent/MX2009007260A/es not_active Application Discontinuation
- 2008-01-03 KR KR1020097016289A patent/KR20090097210A/ko not_active Application Discontinuation
- 2008-01-03 AU AU2008205169A patent/AU2008205169B2/en not_active Ceased
- 2008-01-04 CL CL200800029A patent/CL2008000029A1/es unknown
- 2008-01-04 PE PE2008000091A patent/PE20081850A1/es not_active Application Discontinuation
- 2008-01-04 AR ARP080100042A patent/AR064760A1/es not_active Application Discontinuation
- 2008-01-04 TW TW097100432A patent/TW200836722A/zh unknown
- 2008-03-01 UA UAA200906929A patent/UA97821C2/ru unknown
-
2009
- 2009-06-15 ZA ZA200904175A patent/ZA200904175B/xx unknown
- 2009-06-19 CR CR10879A patent/CR10879A/es unknown
- 2009-06-30 MA MA32061A patent/MA31080B1/fr unknown
- 2009-07-02 DO DO2009000169A patent/DOP2009000169A/es unknown
- 2009-07-02 CO CO09068496A patent/CO6561828A2/es not_active Application Discontinuation
- 2009-07-02 NI NI200900134A patent/NI200900134A/es unknown
- 2009-07-03 EC EC2009009485A patent/ECSP099485A/es unknown
- 2009-07-03 SV SV2009003325A patent/SV2009003325A/es not_active Application Discontinuation
- 2009-07-03 TN TNP2009000287A patent/TN2009000287A1/fr unknown
- 2009-07-03 GT GT200900192A patent/GT200900192A/es unknown
- 2009-07-03 HN HN2009001262A patent/HN2009001262A/es unknown
- 2009-07-23 SM SM200900065T patent/SMP200900065B/it unknown
-
2010
- 2010-09-15 US US12/882,473 patent/US20110003791A1/en not_active Abandoned
-
2012
- 2012-04-03 US US13/438,569 patent/US20120189623A1/en not_active Abandoned
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