JP2010502651A5 - - Google Patents
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- JP2010502651A5 JP2010502651A5 JP2009526946A JP2009526946A JP2010502651A5 JP 2010502651 A5 JP2010502651 A5 JP 2010502651A5 JP 2009526946 A JP2009526946 A JP 2009526946A JP 2009526946 A JP2009526946 A JP 2009526946A JP 2010502651 A5 JP2010502651 A5 JP 2010502651A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- ring
- heteroalkyl
- independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 40
- -1 C2-C8 heteroalkenyl Chemical group 0.000 claims 39
- 125000004404 heteroalkyl group Chemical group 0.000 claims 30
- 125000001424 substituent group Chemical group 0.000 claims 20
- 125000005843 halogen group Chemical group 0.000 claims 18
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 229910052760 oxygen Inorganic materials 0.000 claims 15
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 12
- 125000006823 (C1-C6) acyl group Chemical group 0.000 claims 11
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 11
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 11
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 11
- 125000002252 acyl group Chemical group 0.000 claims 11
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 238000000034 method Methods 0.000 claims 9
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 239000012661 PARP inhibitor Substances 0.000 claims 6
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 claims 4
- 102100023712 Poly [ADP-ribose] polymerase 1 Human genes 0.000 claims 4
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 230000004663 cell proliferation Effects 0.000 claims 3
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 2
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 claims 2
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 230000033115 angiogenesis Effects 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- ZKHQWZAMYRWXGA-KQYNXXCUSA-J ATP(4-) Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]1O ZKHQWZAMYRWXGA-KQYNXXCUSA-J 0.000 claims 1
- ZKHQWZAMYRWXGA-UHFFFAOYSA-N Adenosine triphosphate Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP(O)(=O)OP(O)(O)=O)C(O)C1O ZKHQWZAMYRWXGA-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 150000007942 carboxylates Chemical class 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 150000001735 carboxylic acids Chemical class 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- 0 *C1NC(*=**)=C(*=C)c2c1c(*)c(*)[s]2 Chemical compound *C1NC(*=**)=C(*=C)c2c1c(*)c(*)[s]2 0.000 description 4
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84206106P | 2006-09-01 | 2006-09-01 | |
| US60/842,061 | 2006-09-01 | ||
| US84454206P | 2006-09-13 | 2006-09-13 | |
| US60/844,542 | 2006-09-13 | ||
| US84668306P | 2006-09-22 | 2006-09-22 | |
| US60/846,683 | 2006-09-22 | ||
| US87393606P | 2006-12-07 | 2006-12-07 | |
| US60/873,936 | 2006-12-07 | ||
| US89571607P | 2007-03-19 | 2007-03-19 | |
| US60/895,716 | 2007-03-19 | ||
| PCT/US2007/077464 WO2008028168A2 (en) | 2006-09-01 | 2007-08-31 | Serine-threonine protein kinase and parp modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010502651A JP2010502651A (ja) | 2010-01-28 |
| JP2010502651A5 true JP2010502651A5 (https=) | 2010-07-29 |
| JP5399905B2 JP5399905B2 (ja) | 2014-01-29 |
Family
ID=39136972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009526946A Active JP5399905B2 (ja) | 2006-09-01 | 2007-08-31 | セリン−トレオニンタンパク質キナーゼおよびｐａｒｐ調節因子 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US7956064B2 (https=) |
| EP (1) | EP2061765B1 (https=) |
| JP (1) | JP5399905B2 (https=) |
| KR (1) | KR20090050094A (https=) |
| AU (1) | AU2007289065B2 (https=) |
| BR (1) | BRPI0719123A2 (https=) |
| CA (2) | CA2974246C (https=) |
| DK (1) | DK2061765T3 (https=) |
| ES (1) | ES2528316T3 (https=) |
| IL (1) | IL197088A0 (https=) |
| MX (1) | MX2009002298A (https=) |
| NO (1) | NO20090854L (https=) |
| PL (1) | PL2061765T3 (https=) |
| PT (1) | PT2061765E (https=) |
| RU (1) | RU2681209C2 (https=) |
| WO (1) | WO2008028168A2 (https=) |
Families Citing this family (104)
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| US9512125B2 (en) * | 2004-11-19 | 2016-12-06 | The Regents Of The University Of California | Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents |
| WO2007114926A2 (en) | 2006-04-04 | 2007-10-11 | The Regents Of The University Of California | Kinase antagonists |
| US7956064B2 (en) | 2006-09-01 | 2011-06-07 | Cylene Pharmaceuticals, Inc. | Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators |
| GB2467670B (en) | 2007-10-04 | 2012-08-01 | Intellikine Inc | Chemical entities and therapeutic uses thereof |
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| EP3613743B1 (en) | 2008-01-04 | 2022-03-16 | Intellikine, LLC | Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives |
| AU2009219154A1 (en) * | 2008-02-29 | 2009-09-03 | Cylene Pharmaceuticals, Inc. | Protein kinase modulators |
| US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
| US8637542B2 (en) * | 2008-03-14 | 2014-01-28 | Intellikine, Inc. | Kinase inhibitors and methods of use |
| EP2303890A4 (en) * | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
| JP5788316B2 (ja) * | 2008-07-08 | 2015-09-30 | インテリカイン， エルエルシー | キナーゼインヒビターおよび使用方法 |
| US20110224223A1 (en) * | 2008-07-08 | 2011-09-15 | The Regents Of The University Of California, A California Corporation | MTOR Modulators and Uses Thereof |
| AU2009289317A1 (en) | 2008-09-02 | 2010-03-11 | Novartis Ag | Heterocyclic PIM-kinase inhibitors |
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| WO2010045542A2 (en) | 2008-10-16 | 2010-04-22 | The Regents Of The University Of California | Fused ring heteroaryl kinase inhibitors |
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- 2007-08-31 US US11/849,230 patent/US7956064B2/en active Active
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- 2007-08-31 WO PCT/US2007/077464 patent/WO2008028168A2/en not_active Ceased
- 2007-08-31 DK DK07841767.2T patent/DK2061765T3/en active
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