JP2015523368A5 - - Google Patents
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- Publication number
- JP2015523368A5 JP2015523368A5 JP2015520686A JP2015520686A JP2015523368A5 JP 2015523368 A5 JP2015523368 A5 JP 2015523368A5 JP 2015520686 A JP2015520686 A JP 2015520686A JP 2015520686 A JP2015520686 A JP 2015520686A JP 2015523368 A5 JP2015523368 A5 JP 2015523368A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- compound
- aryl
- alkyl chain
- alkyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 200
- 125000000217 alkyl group Chemical group 0.000 claims description 120
- 125000003118 aryl group Chemical group 0.000 claims description 118
- 125000001072 heteroaryl group Chemical group 0.000 claims description 112
- 150000003839 salts Chemical class 0.000 claims description 106
- -1 nitro, carboxy Chemical group 0.000 claims description 90
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 84
- 125000005843 halogen group Chemical group 0.000 claims description 83
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 83
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 79
- 229920006395 saturated elastomer Polymers 0.000 claims description 73
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 59
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 claims description 55
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 53
- 125000005862 (C1-C6)alkanoyl group Chemical group 0.000 claims description 38
- 125000004423 acyloxy group Chemical group 0.000 claims description 38
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 37
- 241001465754 Metazoa Species 0.000 claims description 28
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 26
- 239000003814 drug Substances 0.000 claims description 19
- 102100039291 Geranylgeranyl pyrophosphate synthase Human genes 0.000 claims description 12
- 108010066605 Geranylgeranyl-Diphosphate Geranylgeranyltransferase Proteins 0.000 claims description 12
- 230000002401 inhibitory effect Effects 0.000 claims description 12
- 230000001225 therapeutic effect Effects 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 125000005505 thiomorpholino group Chemical group 0.000 claims description 8
- 102100035111 Farnesyl pyrophosphate synthase Human genes 0.000 claims description 6
- 101710125754 Farnesyl pyrophosphate synthase Proteins 0.000 claims description 6
- 108010022535 Farnesyl-Diphosphate Farnesyltransferase Proteins 0.000 claims description 6
- 206010022489 Insulin Resistance Diseases 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 208000008589 Obesity Diseases 0.000 claims description 6
- 208000030852 Parasitic disease Diseases 0.000 claims description 6
- 102100037997 Squalene synthase Human genes 0.000 claims description 6
- 208000021017 Weight Gain Diseases 0.000 claims description 6
- 206010003119 arrhythmia Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 235000020824 obesity Nutrition 0.000 claims description 6
- 230000003449 preventive effect Effects 0.000 claims description 6
- 125000006413 ring segment Chemical group 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 235000019786 weight gain Nutrition 0.000 claims description 6
- 230000035558 fertility Effects 0.000 claims description 5
- 238000000338 in vitro Methods 0.000 claims description 5
- 238000001727 in vivo Methods 0.000 claims description 5
- 210000002997 osteoclast Anatomy 0.000 claims description 5
- 230000000069 prophylactic effect Effects 0.000 claims description 5
- 230000002381 testicular Effects 0.000 claims description 5
- 230000004584 weight gain Effects 0.000 claims description 5
- 125000001041 indolyl group Chemical group 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 230000002141 anti-parasite Effects 0.000 claims description 2
- 238000003745 diagnosis Methods 0.000 claims description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 244000045947 parasite Species 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 39
- 125000006755 (C2-C20) alkyl group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 230000037396 body weight Effects 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 15
- 230000001105 regulatory effect Effects 0.000 description 4
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 241000124008 Mammalia Species 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261668299P | 2012-07-05 | 2012-07-05 | |
| US61/668,299 | 2012-07-05 | ||
| PCT/US2013/049341 WO2014008407A1 (en) | 2012-07-05 | 2013-07-03 | Therapeutic bisphosphonates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015523368A JP2015523368A (ja) | 2015-08-13 |
| JP2015523368A5 true JP2015523368A5 (https=) | 2016-08-04 |
| JP6226974B2 JP6226974B2 (ja) | 2017-11-08 |
Family
ID=48790678
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015520686A Expired - Fee Related JP6226974B2 (ja) | 2012-07-05 | 2013-07-03 | 治療用ビスホスホネート |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9745331B2 (https=) |
| EP (1) | EP2870168B1 (https=) |
| JP (1) | JP6226974B2 (https=) |
| CN (1) | CN104822695B (https=) |
| AU (1) | AU2013286683B2 (https=) |
| CA (1) | CA2878413A1 (https=) |
| ES (1) | ES2617448T3 (https=) |
| WO (1) | WO2014008407A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2946430B2 (ja) | 1990-12-21 | 1999-09-06 | 近藤運輸機工株式会社 | 圧縮故紙緊締ワイヤの処理装置 |
| CA2910572A1 (en) * | 2013-04-25 | 2014-10-30 | University Of Iowa Research Foundation | Methods to modulate rac1 import and to treat pulmonary fibrosis |
| CN110573518A (zh) | 2017-01-26 | 2019-12-13 | 尤拉·S·赞特里佐斯 | 被取代的双环嘧啶基化合物及其组合物和用途 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2489711A1 (fr) | 1980-04-21 | 1982-03-12 | Minemet Rech Sa | Compositions echangeuses de cations metalliques |
| JPS57106688A (en) * | 1980-12-20 | 1982-07-02 | Lion Corp | 1-methacryloxyethane-1,1-diphosphonic acid |
| US4559157A (en) | 1983-04-21 | 1985-12-17 | Creative Products Resource Associates, Ltd. | Cosmetic applicator useful for skin moisturizing |
| LU84979A1 (fr) | 1983-08-30 | 1985-04-24 | Oreal | Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux |
| GB8419489D0 (en) * | 1984-07-31 | 1984-09-05 | Leo Pharm Prod Ltd | Chemical compounds |
| IL77243A (en) | 1984-12-21 | 1996-11-14 | Procter & Gamble | Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds |
| US4820508A (en) | 1987-06-23 | 1989-04-11 | Neutrogena Corporation | Skin protective composition |
| US4992478A (en) | 1988-04-04 | 1991-02-12 | Warner-Lambert Company | Antiinflammatory skin moisturizing composition and method of preparing same |
| US4938949A (en) | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| US5739313A (en) | 1995-11-13 | 1998-04-14 | Regents Of The University Of Minnesota | Radionuclide labeling of vitamin B12 and coenzymes thereof |
| IT1276162B1 (it) | 1995-11-23 | 1997-10-27 | Baldacci Lab Spa | Geranilgeranil-derivati,procedimento per la loro preparazione e relative composizioni farmaceutiche |
| US6727234B2 (en) | 2001-04-03 | 2004-04-27 | University Of Iowa Research Foundation | Isoprenoid analog compounds and methods of making and use thereof |
| WO2006026380A2 (en) | 2004-08-25 | 2006-03-09 | University Of Iowa Research Foundation | Geranylgeranyl pyrophosphate synthase inhibitors |
| EP1802641B8 (en) * | 2004-10-08 | 2012-03-07 | The Board Of Trustees Of The University Of Illinois | Bisphosphonate compounds and methods for bone resorption diseases, cancer, bone pain, immune disorders, and infectious diseases |
| US8363849B2 (en) | 2006-08-31 | 2013-01-29 | Omniphase Research Laboratories, Inc. | Automated interferometric noise measurement |
| US20080200679A1 (en) * | 2007-01-22 | 2008-08-21 | University Of Southern California | Alpha-HYDROXY, alpha-SUBSTITUTED METHYLENEBISPHOSPHONATES AND PHOSPHONOACETATES |
| CN101679466A (zh) * | 2007-04-12 | 2010-03-24 | 伊利诺伊大学评议会 | 对包括fpps、ggpps和dpps在内的多靶点效力提高的二膦酸盐化合物及方法 |
-
2013
- 2013-07-03 ES ES13737116.7T patent/ES2617448T3/es active Active
- 2013-07-03 CA CA2878413A patent/CA2878413A1/en not_active Abandoned
- 2013-07-03 CN CN201380046344.XA patent/CN104822695B/zh not_active Expired - Fee Related
- 2013-07-03 US US14/412,578 patent/US9745331B2/en not_active Expired - Fee Related
- 2013-07-03 AU AU2013286683A patent/AU2013286683B2/en not_active Ceased
- 2013-07-03 EP EP13737116.7A patent/EP2870168B1/en not_active Not-in-force
- 2013-07-03 JP JP2015520686A patent/JP6226974B2/ja not_active Expired - Fee Related
- 2013-07-03 WO PCT/US2013/049341 patent/WO2014008407A1/en not_active Ceased
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