JP2013531627A5 - - Google Patents
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- Publication number
- JP2013531627A5 JP2013531627A5 JP2013511491A JP2013511491A JP2013531627A5 JP 2013531627 A5 JP2013531627 A5 JP 2013531627A5 JP 2013511491 A JP2013511491 A JP 2013511491A JP 2013511491 A JP2013511491 A JP 2013511491A JP 2013531627 A5 JP2013531627 A5 JP 2013531627A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- optionally substituted
- bone
- lower alkyl
- tei
- 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 49
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 210000000988 bone and bone Anatomy 0.000 claims description 13
- 230000002159 abnormal effect Effects 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 11
- 206010017076 Fracture Diseases 0.000 claims description 8
- 150000004663 bisphosphonates Chemical group 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 150000003536 tetrazoles Chemical class 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000003107 substituted aryl group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 5
- 229940122361 Bisphosphonate Drugs 0.000 claims description 4
- 208000006386 Bone Resorption Diseases 0.000 claims description 4
- 206010065687 Bone loss Diseases 0.000 claims description 4
- 208000001132 Osteoporosis Diseases 0.000 claims description 4
- 239000000556 agonist Substances 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 230000024279 bone resorption Effects 0.000 claims description 4
- 230000003913 calcium metabolism Effects 0.000 claims description 4
- 230000007062 hydrolysis Effects 0.000 claims description 4
- 238000006460 hydrolysis reaction Methods 0.000 claims description 4
- 125000001475 halogen functional group Chemical group 0.000 claims description 3
- VZYQAJHQPQELEJ-UHFFFAOYSA-N 1-trityltetrazole Chemical compound C1=NN=NN1C(C=1C=CC=CC=1)(C=1C=CC=CC=1)C1=CC=CC=C1 VZYQAJHQPQELEJ-UHFFFAOYSA-N 0.000 claims description 2
- 208000002679 Alveolar Bone Loss Diseases 0.000 claims description 2
- 208000010392 Bone Fractures Diseases 0.000 claims description 2
- 206010010214 Compression fracture Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000002565 Open Fractures Diseases 0.000 claims description 2
- 208000010191 Osteitis Deformans Diseases 0.000 claims description 2
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims description 2
- 208000003076 Osteolysis Diseases 0.000 claims description 2
- 208000027868 Paget disease Diseases 0.000 claims description 2
- 208000005250 Spontaneous Fractures Diseases 0.000 claims description 2
- 208000008312 Tooth Loss Diseases 0.000 claims description 2
- 230000008416 bone turnover Effects 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000006575 electron-withdrawing group Chemical group 0.000 claims description 2
- 201000003617 glucocorticoid-induced osteoporosis Diseases 0.000 claims description 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 2
- 238000001727 in vivo Methods 0.000 claims description 2
- 125000005647 linker group Chemical group 0.000 claims description 2
- 208000029791 lytic metastatic bone lesion Diseases 0.000 claims description 2
- 208000027202 mammary Paget disease Diseases 0.000 claims description 2
- 230000001394 metastastic effect Effects 0.000 claims description 2
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 2
- 208000028169 periodontal disease Diseases 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 230000008521 reorganization Effects 0.000 claims description 2
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 claims description 2
- 238000001356 surgical procedure Methods 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34969410P | 2010-05-28 | 2010-05-28 | |
| US61/349,694 | 2010-05-28 | ||
| CA2,738,045 | 2011-04-21 | ||
| CA2738045A CA2738045C (en) | 2010-05-28 | 2011-04-21 | Conjugate compounds, methods of making same, and uses thereof |
| PCT/CA2011/000633 WO2011147034A1 (en) | 2010-05-28 | 2011-05-30 | Prostaglandin-bisphosphonate conjugate compounds, methods of making same, and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013531627A JP2013531627A (ja) | 2013-08-08 |
| JP2013531627A5 true JP2013531627A5 (enExample) | 2014-07-17 |
| JP6082692B2 JP6082692B2 (ja) | 2017-02-15 |
Family
ID=45066020
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013511491A Active JP6082692B2 (ja) | 2010-05-28 | 2011-05-30 | プロスタグランジンビスホスホネート結合体化合物およびその作製方法ならびにその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9611284B2 (enExample) |
| EP (1) | EP2576575B1 (enExample) |
| JP (1) | JP6082692B2 (enExample) |
| CA (1) | CA2738045C (enExample) |
| WO (1) | WO2011147034A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2738045C (en) | 2010-05-28 | 2019-02-19 | Simon Fraser University | Conjugate compounds, methods of making same, and uses thereof |
| US9650414B1 (en) | 2014-05-30 | 2017-05-16 | Simon Fraser University | Dual-action EP4 agonist—bisphosphonate conjugates and uses thereof |
| CN107849072B (zh) | 2015-06-12 | 2020-12-15 | 西蒙弗雷泽大学 | 酰胺连接的ep4激动剂-二膦酸盐化合物及其用途 |
| EP3454913A4 (en) | 2016-03-15 | 2019-11-27 | The Regents of the University of California | BONE OBTAINING ANTIBODY CONJUGATE AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| CN108659083A (zh) * | 2017-03-31 | 2018-10-16 | 天津药业研究院有限公司 | 一种依碳氯替泼诺的合成方法 |
| CN108659084A (zh) * | 2017-03-31 | 2018-10-16 | 天津药业研究院有限公司 | 一种17β-羧酸氯甲酯类甾体化合物的制备方法 |
| WO2025024714A2 (en) * | 2023-07-25 | 2025-01-30 | Bioventures, Llc | Bone-targeted canonical notch inhibitor |
| WO2026013441A1 (en) * | 2024-07-10 | 2026-01-15 | Mesentech Inc. | Bisphosphonate-ep4 agonists for selective delivery to damaged muscle |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4320136A (en) * | 1980-08-11 | 1982-03-16 | E. I. Du Pont De Nemours And Company | 8-Aza-16,16-difluoroprostanoids |
| US4922007A (en) | 1989-06-09 | 1990-05-01 | Merck & Co., Inc. | Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof |
| US5019651A (en) | 1990-06-20 | 1991-05-28 | Merck & Co., Inc. | Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP) or salts thereof |
| US5409911A (en) * | 1992-09-11 | 1995-04-25 | Merck & Co., Inc. | Prostaglandin analog for treating osteoporosis |
| TW257765B (enExample) | 1993-08-25 | 1995-09-21 | Merck & Co Inc | |
| US5510517A (en) | 1993-08-25 | 1996-04-23 | Merck & Co., Inc. | Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids |
| JPH10265454A (ja) | 1997-01-27 | 1998-10-06 | Ono Pharmaceut Co Ltd | ３，７−ジチアプロスタン酸誘導体、それらの製造方法およびそれらを有効成分として含有する薬剤 |
| EP1114816A4 (en) | 1998-09-14 | 2002-09-04 | Ono Pharmaceutical Co | SUBSTITUTED PHENYL-PROSTAGLANDIN E DERIVATIVES- $ g (V) AND MEDICINAL PRODUCTS CONTAINING THEM AS ACTIVE INGREDIENT |
| US6121253A (en) * | 1998-11-20 | 2000-09-19 | Merck Frosst Canada & Co. | Prostaglandin conjugates for treating or preventing bone disease |
| AP2002002555A0 (en) | 1999-12-22 | 2002-06-30 | Pfizer Prod Inc | EP4 Receptor selective agonists in the treatment of osteoporosis. |
| ATE327751T1 (de) | 2000-01-31 | 2006-06-15 | Pfizer Prod Inc | Verwendung von aktivatoren des prostaglandinrezeptores 4 zur behandlung von akuter oder chronischer niereninsuffizienz |
| WO2001072268A1 (en) | 2000-03-31 | 2001-10-04 | Toray Industries, Inc. | Hair growth or hair formation controlling agents |
| AU2001290250A1 (en) | 2000-09-21 | 2002-04-02 | Ono Pharmaceutical Co. Ltd. | Ep4 receptor agonists containing 8-azaprostaglandin derivatives as the active ingredient |
| EA200300379A1 (ru) | 2000-11-27 | 2003-08-28 | Пфайзер Продактс Инк. | Селективные агонисты рецептора ep4 в лечении остеопороза |
| WO2003047417A2 (en) | 2001-12-03 | 2003-06-12 | Merck & Co., Inc. | Ep4 receptor agonist, compositions and methods thereof |
| CA2487977A1 (en) * | 2002-06-06 | 2003-12-18 | Merck Frosst Canada & Co./Merck Frosst Canada & Cie | 1,5-disubstituted imidazolidin-2-one derivatives for use as ep4 receptor agonists in the treatment of eye and bone diseases |
| EP1513589B1 (en) * | 2002-06-06 | 2010-11-10 | Merck Frosst Canada Ltd. | 1,5-disubstituted pyrrolid-2-one derivatives for use as ep4 receptor agonists in the treatment of eye diseases such as glaucoma |
| JP2006504679A (ja) | 2002-08-28 | 2006-02-09 | メルク フロスト カナダ アンド カンパニー | 緑内障の治療においてｅｐ４受容体作動薬として使用するためのオキサゾリジン−２−オンおよびチアゾリジン−２−オン誘導体 |
| US7053085B2 (en) * | 2003-03-26 | 2006-05-30 | Merck & Co. Inc. | EP4 receptor agonist, compositions and methods thereof |
| WO2005116010A1 (en) | 2004-05-26 | 2005-12-08 | Merck Frosst Canada Ltd. | Ep4 receptor agonist, compositions and methods thereof |
| US20070232660A1 (en) * | 2006-04-04 | 2007-10-04 | Allergan, Inc. | Therapeutic and delivery methods of prostaglandin ep4 agonists |
| CA2738045C (en) | 2010-05-28 | 2019-02-19 | Simon Fraser University | Conjugate compounds, methods of making same, and uses thereof |
-
2011
- 2011-04-21 CA CA2738045A patent/CA2738045C/en active Active
- 2011-05-30 JP JP2013511491A patent/JP6082692B2/ja active Active
- 2011-05-30 EP EP11785955.3A patent/EP2576575B1/en active Active
- 2011-05-30 WO PCT/CA2011/000633 patent/WO2011147034A1/en not_active Ceased
-
2012
- 2012-11-28 US US13/687,762 patent/US9611284B2/en active Active
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