HRP20100122T1 - Benzimidazolotiofenski spojevi kao inhibitori plk - Google Patents
Benzimidazolotiofenski spojevi kao inhibitori plk Download PDFInfo
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- HRP20100122T1 HRP20100122T1 HR20100122T HRP20100122T HRP20100122T1 HR P20100122 T1 HRP20100122 T1 HR P20100122T1 HR 20100122 T HR20100122 T HR 20100122T HR P20100122 T HRP20100122 T HR P20100122T HR P20100122 T1 HRP20100122 T1 HR P20100122T1
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- OHNAITIAQLQHJY-UHFFFAOYSA-N 1h-benzimidazole;thiophene Chemical class C=1C=CSC=1.C1=CC=C2NC=NC2=C1 OHNAITIAQLQHJY-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 51
- 150000003839 salts Chemical class 0.000 claims abstract 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract 3
- 229910052799 carbon Inorganic materials 0.000 claims abstract 3
- 241000124008 Mammalia Species 0.000 claims 15
- 239000003814 drug Substances 0.000 claims 10
- 238000004519 manufacturing process Methods 0.000 claims 10
- 229940079593 drug Drugs 0.000 claims 8
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 4
- 206010023774 Large cell lung cancer Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 201000009546 lung large cell carcinoma Diseases 0.000 claims 4
- 208000035269 cancer or benign tumor Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 238000002560 therapeutic procedure Methods 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 230000004663 cell proliferation Effects 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000011278 mitosis Effects 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 230000035755 proliferation Effects 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 206010066476 Haematological malignancy Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 201000003911 head and neck carcinoma Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A61P17/06—Antipsoriatics
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- A61P19/00—Drugs for skeletal disorders
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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Abstract
Spoj, naznačen time što ga se bira između: gdje * označuje kiralni ugljik; i njegove farmaceutski prihvatljive soli. Patent sadrži još 31 patentni zahtjev.
Claims (32)
1. Spoj, naznačen time što ga se bira između:
[image]
[image]
[image]
[image]
gdje * označuje kiralni ugljik;
i njegove farmaceutski prihvatljive soli.
2. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što stereokemija kiralnog ugljika je R.
3. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju A-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
4. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju B-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
5. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju C-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
6. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju D-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju E-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju F-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju G-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Enantiomerno obogaćeni spoj u skladu s patentnim zahtjevom 1, naznačen time što ima apsolutnu stereokemiju opisanu u spoju H-1:
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-10.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 11, naznačen time što još sadrži farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
13. Farmaceutski pripravak u skladu s patentnim zahtjevom 11, naznačen time što još sadrži kemoterapijsko sredstvo.
14. Farmaceutski pripravak, naznačen time što sadrži spoj ili njegovu farmaceutski prihvatljivu sol u skladu s patentnim zahtjevom 5.
15. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta za liječenje stanja kod kojeg posreduje PLK kod sisavca kojem je to potrebno.
16. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta za liječenje osjetljive novotvorine kod sisavca kojem je to potrebno.
17. Upotreba u skladu s patentnim zahtjevom 16, naznačena time što navedenu osjetljivu novotvorinu se bira iz skupine koju čine rak dojke, rak debelog crijeva, rak malih stanica pluća, rak velikih stanica pluća, rak prostate, rak endometrija, rak želuca, melanom, rak jajnika, rak gušterače, karcinom pločastih stanica, karcinom glave i vrata, hepatocelularni karcinom i hematoloških malignoma.
18. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili liječenju raka dojke kod sisavca kojem je to potrebno, gdje se navedeni postupak sastoji u primjeni na sisavcu terapijski djelotvorne količine spoja u skladu s patentnim zahtjevom 1.
19. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili liječenju raka jajnika kod sisavca kojem je to potrebno.
20. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili liječenju raka velikih stanica pluća kod sisavca kojem je to potrebno.
21. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili liječenju raka prostate kod sisavca kojem je to potrebno, gdje se navedeni postupak sastoji u primjeni na sisavcu terapijski djelotvorne količine spoja u skladu s patentnim zahtjevom 1.
22. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili liječenju hematološkog malignoma kod sisavca kojem je to potrebno, gdje se navedeni postupak sastoji u primjeni na sisavcu terapijski djelotvorne količine spoja u skladu s patentnim zahtjevom 1.
23. Upotreba spoja u skladu s patentnim zahtjevima 1-10 u proizvodnji medikamenta ili liječenju stanja, naznačenog time što se odlikuje neodgovarajućom staničnom proliferacijom, kod sisavca kojem je to potrebno.
24. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili inhibiciji stranične proliferacije.
25. Upotreba spoja u skladu s patentnim zahtjevima 1-10, naznačena time što navedeni spoj je namijenjen proizvodnji medikamenta ili inhibiciji stranične mitoze.
26. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen upotrebi u terapiji.
27. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen upotrebi u liječenju stanja kod kojeg posreduje PLK kod sisavca kojem je to potrebno.
28. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen upotrebi u terapiji osjetljive novotvorine, poput raka dojke, raka debelog crijeva, raka malih stanica pluća, raka velikih stanica pluća, raka prostate, raka endometrija, raka želuca, melanoma, raka jajnika, raka gušterače, karcinoma pločastih stanica, karcinoma glave i vrata, hepatocelularnog karcinom i hematoloških malignoma kod sisavca kojem je to potrebno.
29. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, namijenjen upotrebi u liječenju stanja, naznačenog time što se odlikuje neodgovarajućom staničnom proliferacijom, kod sisavca kojem je to potrebno.
30. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen inhibiciji stranične proliferacije.
31. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je namijenjen inhibiciji stranične mitoze.
32. Farmaceutski pripravak koji sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-10, naznačen time što je navedeni spoj namijenjen upotrebi u terapiji osjetljive novotvorine, poput raka dojke, raka jajnika, raka velikih stanica pluća, raka prostate i hematoloških malignoma kod sisavca kojem je to potrebno.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US71433705P | 2005-09-06 | 2005-09-06 | |
US78624406P | 2006-03-27 | 2006-03-27 | |
PCT/US2006/033683 WO2007030361A2 (en) | 2005-09-06 | 2006-08-28 | Benzimidazole thiophene compounds as plk inhibitors |
Publications (1)
Publication Number | Publication Date |
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HRP20100122T1 true HRP20100122T1 (hr) | 2010-05-31 |
Family
ID=37631488
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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HR20100122T HRP20100122T1 (hr) | 2005-09-06 | 2010-03-04 | Benzimidazolotiofenski spojevi kao inhibitori plk |
Country Status (29)
Country | Link |
---|---|
US (2) | US7786127B2 (hr) |
EP (1) | EP1937671B1 (hr) |
JP (1) | JP5002597B2 (hr) |
KR (1) | KR20080047585A (hr) |
AR (1) | AR055616A1 (hr) |
AT (1) | ATE452132T1 (hr) |
AU (1) | AU2006287766B2 (hr) |
BR (1) | BRPI0615668A2 (hr) |
CA (1) | CA2621879A1 (hr) |
CR (1) | CR9786A (hr) |
CY (1) | CY1109916T1 (hr) |
DE (1) | DE602006011192D1 (hr) |
DK (1) | DK1937671T3 (hr) |
EA (1) | EA014111B1 (hr) |
ES (1) | ES2337929T3 (hr) |
HK (1) | HK1117504A1 (hr) |
HR (1) | HRP20100122T1 (hr) |
IL (1) | IL189897A0 (hr) |
JO (1) | JO2578B1 (hr) |
MA (1) | MA29816B1 (hr) |
MX (1) | MX2008003173A (hr) |
NO (1) | NO20081160L (hr) |
NZ (1) | NZ566345A (hr) |
PE (1) | PE20070518A1 (hr) |
PL (1) | PL1937671T3 (hr) |
PT (1) | PT1937671E (hr) |
SI (1) | SI1937671T1 (hr) |
TW (1) | TW200800967A (hr) |
WO (1) | WO2007030361A2 (hr) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101495474A (zh) * | 2006-05-23 | 2009-07-29 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的噻吩-甲酰胺类 |
US7615643B2 (en) | 2006-06-02 | 2009-11-10 | Smithkline Beecham Corporation | Benzimidazole thiophene compounds |
JP2009539771A (ja) * | 2006-06-02 | 2009-11-19 | スミスクライン ビーチャム コーポレーション | 置換ベンゾイミダゾールチオフェンベンジルエーテル化合物 |
AR060979A1 (es) * | 2006-06-02 | 2008-07-23 | Smithkline Beecham Corp | Compuestos de tiofeno de bencimidazol |
EP2123627B1 (en) * | 2007-01-19 | 2013-11-20 | Ube Industries, Ltd. | Process for producing aromatic amine having aralkyloxy or heteroaralkyloxy group |
US8236954B2 (en) | 2007-06-26 | 2012-08-07 | Glaxosmithkline Llc | Processes for preparing benzimidazole thiophenes |
WO2009003911A1 (en) * | 2007-06-29 | 2009-01-08 | 4Sc Ag | Thiophene-imidazopyridines |
EP2100894A1 (en) | 2008-03-12 | 2009-09-16 | 4Sc Ag | Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors |
WO2009151914A1 (en) * | 2008-05-27 | 2009-12-17 | Smithkline Beecham Corporation | Methods for treating neoplasms with a combination of a plk inhibitor and retinoid |
WO2009154645A1 (en) * | 2008-06-20 | 2009-12-23 | Smithkline Beecham Corporation | Methods for the treatment of central nervous system tumors |
JP2012512223A (ja) * | 2008-12-18 | 2012-05-31 | エフ.ホフマン−ラ ロシュ アーゲー | チアゾリル−ベンズイミダゾール類 |
WO2011049625A1 (en) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Method for aflatoxin screening of products |
MY173795A (en) | 2009-11-05 | 2020-02-24 | Incozen Therapeutics Pvt Ltd | Novel benzopyran kinase modulators |
MY168757A (en) | 2011-05-04 | 2018-12-04 | Rhizen Pharmaceuticals S A | Novel compounds as modulators of protein kinases |
SI3260455T1 (sl) | 2012-07-04 | 2019-07-31 | Rhizen Pharmaceuticals S.A. | Selektivni inhibitorji PI3K-delta |
KR102574152B1 (ko) * | 2020-03-27 | 2023-09-05 | (주) 업테라 | Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물 |
KR20210122165A (ko) * | 2020-03-27 | 2021-10-08 | (주) 업테라 | Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물 |
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US5990146A (en) | 1997-08-20 | 1999-11-23 | Warner-Lambert Company | Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation |
US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
JP2002523459A (ja) | 1998-08-31 | 2002-07-30 | メルク エンド カムパニー インコーポレーテッド | 新規血管形成阻害剤 |
WO2004014899A1 (en) * | 2002-08-08 | 2004-02-19 | Smithkline Beecham Corporation | Thiophene compounds |
AU2003903440A0 (en) * | 2003-07-04 | 2003-07-17 | James Hardie International Finance B.V. | Rainscreen apparatus and method |
EP1685128A1 (en) * | 2003-10-16 | 2006-08-02 | Smithkline Beecham Corporation | Process for preparing benzimidazole thiophenes |
JP4721428B2 (ja) | 2003-10-20 | 2011-07-13 | 日本精工株式会社 | ステアリング装置 |
GB0402809D0 (en) * | 2004-02-09 | 2004-03-10 | Glaxo Group Ltd | Chemical compounds |
MX2008003172A (es) * | 2005-09-06 | 2008-03-18 | Smithkline Beecham Corp | Proceso regioselectivo para la preparacion de bencimidazol-tiofenos. |
WO2007030359A1 (en) * | 2005-09-06 | 2007-03-15 | Smithkline Beecham Corporation | Benzimidazole thiophene compounds as plk modulators |
JP5498703B2 (ja) | 2006-01-23 | 2014-05-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド |
AR060979A1 (es) * | 2006-06-02 | 2008-07-23 | Smithkline Beecham Corp | Compuestos de tiofeno de bencimidazol |
JP2009539771A (ja) * | 2006-06-02 | 2009-11-19 | スミスクライン ビーチャム コーポレーション | 置換ベンゾイミダゾールチオフェンベンジルエーテル化合物 |
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