JP2017530180A5 - - Google Patents
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- Publication number
- JP2017530180A5 JP2017530180A5 JP2017518905A JP2017518905A JP2017530180A5 JP 2017530180 A5 JP2017530180 A5 JP 2017530180A5 JP 2017518905 A JP2017518905 A JP 2017518905A JP 2017518905 A JP2017518905 A JP 2017518905A JP 2017530180 A5 JP2017530180 A5 JP 2017530180A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- osteoporosis
- compound
- pharmaceutically acceptable
- acceptable salt
- 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 34
- 150000003839 salts Chemical class 0.000 claims description 30
- 208000001132 Osteoporosis Diseases 0.000 claims description 21
- 239000003814 drug Substances 0.000 claims description 17
- 210000002997 osteoclast Anatomy 0.000 claims description 9
- 230000015572 biosynthetic process Effects 0.000 claims description 5
- 208000001685 postmenopausal osteoporosis Diseases 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 238000011282 treatment Methods 0.000 claims description 5
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 4
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 4
- 206010065687 Bone loss Diseases 0.000 claims description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 3
- 239000011575 calcium Substances 0.000 claims description 3
- 229910052791 calcium Inorganic materials 0.000 claims description 3
- 230000004069 differentiation Effects 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 229910052708 sodium Inorganic materials 0.000 claims description 3
- 239000011734 sodium Substances 0.000 claims description 3
- OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical compound NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 2
- 229940122361 Bisphosphonate Drugs 0.000 claims description 2
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims description 2
- DBVJJBKOTRCVKF-UHFFFAOYSA-N Etidronic acid Chemical compound OP(=O)(O)C(O)(C)P(O)(O)=O DBVJJBKOTRCVKF-UHFFFAOYSA-N 0.000 claims description 2
- 208000029663 Hypophosphatemia Diseases 0.000 claims description 2
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- 208000010191 Osteitis Deformans Diseases 0.000 claims description 2
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims description 2
- 206010031264 Osteonecrosis Diseases 0.000 claims description 2
- 208000027067 Paget disease of bone Diseases 0.000 claims description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 2
- IIDJRNMFWXDHID-UHFFFAOYSA-N Risedronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CC1=CC=CN=C1 IIDJRNMFWXDHID-UHFFFAOYSA-N 0.000 claims description 2
- 108010049264 Teriparatide Proteins 0.000 claims description 2
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 2
- 229940062527 alendronate Drugs 0.000 claims description 2
- 150000004663 bisphosphonates Chemical class 0.000 claims description 2
- 208000016738 bone Paget disease Diseases 0.000 claims description 2
- 229910052802 copper Inorganic materials 0.000 claims description 2
- 239000010949 copper Substances 0.000 claims description 2
- 229960001251 denosumab Drugs 0.000 claims description 2
- 229940009626 etidronate Drugs 0.000 claims description 2
- 229910052742 iron Inorganic materials 0.000 claims description 2
- 229910052744 lithium Inorganic materials 0.000 claims description 2
- 239000011777 magnesium Substances 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- WPBNNNQJVZRUHP-UHFFFAOYSA-L manganese(2+);methyl n-[[2-(methoxycarbonylcarbamothioylamino)phenyl]carbamothioyl]carbamate;n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[S-]C(=S)NCCNC([S-])=S.COC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OC WPBNNNQJVZRUHP-UHFFFAOYSA-L 0.000 claims description 2
- 229910052751 metal Inorganic materials 0.000 claims description 2
- 239000002184 metal Substances 0.000 claims description 2
- 230000011164 ossification Effects 0.000 claims description 2
- 210000000963 osteoblast Anatomy 0.000 claims description 2
- 208000005368 osteomalacia Diseases 0.000 claims description 2
- 208000002865 osteopetrosis Diseases 0.000 claims description 2
- WRUUGTRCQOWXEG-UHFFFAOYSA-N pamidronate Chemical compound NCCC(O)(P(O)(O)=O)P(O)(O)=O WRUUGTRCQOWXEG-UHFFFAOYSA-N 0.000 claims description 2
- 229940046231 pamidronate Drugs 0.000 claims description 2
- 229910052700 potassium Inorganic materials 0.000 claims description 2
- 239000011591 potassium Substances 0.000 claims description 2
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims description 2
- 229960004622 raloxifene Drugs 0.000 claims description 2
- 229940089617 risedronate Drugs 0.000 claims description 2
- 229960001603 tamoxifen Drugs 0.000 claims description 2
- OGBMKVWORPGQRR-UMXFMPSGSA-N teriparatide Chemical compound C([C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CNC=N1 OGBMKVWORPGQRR-UMXFMPSGSA-N 0.000 claims description 2
- 229960005460 teriparatide Drugs 0.000 claims description 2
- 239000011701 zinc Substances 0.000 claims description 2
- 229910052725 zinc Inorganic materials 0.000 claims description 2
- XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 claims description 2
- 229960004276 zoledronic acid Drugs 0.000 claims description 2
- 230000000638 stimulation Effects 0.000 claims 2
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- 230000033558 biomineral tissue development Effects 0.000 claims 1
- 230000030991 negative regulation of bone resorption Effects 0.000 claims 1
- 230000010938 positive regulation of bone remodeling Effects 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 37
- 125000000217 alkyl group Chemical group 0.000 description 14
- 210000000988 bone and bone Anatomy 0.000 description 6
- 102000013462 Interleukin-12 Human genes 0.000 description 4
- 108010065805 Interleukin-12 Proteins 0.000 description 4
- 102100032236 Tumor necrosis factor receptor superfamily member 11B Human genes 0.000 description 4
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 210000002449 bone cell Anatomy 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 229940117681 interleukin-12 Drugs 0.000 description 4
- 230000004936 stimulating effect Effects 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000002243 precursor Substances 0.000 description 3
- GZCWLCBFPRFLKL-UHFFFAOYSA-N 1-prop-2-ynoxypropan-2-ol Chemical compound CC(O)COCC#C GZCWLCBFPRFLKL-UHFFFAOYSA-N 0.000 description 2
- 102000013563 Acid Phosphatase Human genes 0.000 description 2
- 108010051457 Acid Phosphatase Proteins 0.000 description 2
- 102000011690 Adiponectin Human genes 0.000 description 2
- 108010076365 Adiponectin Proteins 0.000 description 2
- 102000008186 Collagen Human genes 0.000 description 2
- 108010035532 Collagen Proteins 0.000 description 2
- 108010057466 NF-kappa B Proteins 0.000 description 2
- 102100023050 Nuclear factor NF-kappa-B p105 subunit Human genes 0.000 description 2
- 108010035042 Osteoprotegerin Proteins 0.000 description 2
- 102000014128 RANK Ligand Human genes 0.000 description 2
- 108010025832 RANK Ligand Proteins 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 2
- 229920001436 collagen Polymers 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- XXUPLYBCNPLTIW-UHFFFAOYSA-N octadec-7-ynoic acid Chemical compound CCCCCCCCCCC#CCCCCCC(O)=O XXUPLYBCNPLTIW-UHFFFAOYSA-N 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 208000006386 Bone Resorption Diseases 0.000 description 1
- 102000004160 Phosphoric Monoester Hydrolases Human genes 0.000 description 1
- 108090000608 Phosphoric Monoester Hydrolases Proteins 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 230000010072 bone remodeling Effects 0.000 description 1
- 230000024279 bone resorption Effects 0.000 description 1
- 230000002308 calcification Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000019734 interleukin-12 production Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462062597P | 2014-10-10 | 2014-10-10 | |
| US62/062,597 | 2014-10-10 | ||
| PCT/CA2015/000540 WO2016054728A1 (en) | 2014-10-10 | 2015-10-08 | Substituted aromatic compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017530180A JP2017530180A (ja) | 2017-10-12 |
| JP2017530180A5 true JP2017530180A5 (enExample) | 2018-11-22 |
| JP6700639B2 JP6700639B2 (ja) | 2020-05-27 |
Family
ID=55652429
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017518905A Expired - Fee Related JP6700639B2 (ja) | 2014-10-10 | 2015-10-08 | 骨粗しょう症の予防及び治療用の置換芳香族化合物ならびに医薬組成物 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US20180228750A1 (enExample) |
| EP (1) | EP3203999B1 (enExample) |
| JP (1) | JP6700639B2 (enExample) |
| KR (1) | KR20170066476A (enExample) |
| CN (1) | CN106999456B (enExample) |
| AR (1) | AR102246A1 (enExample) |
| AU (1) | AU2015330645B2 (enExample) |
| BR (1) | BR112017007426A2 (enExample) |
| CA (1) | CA2963354A1 (enExample) |
| DK (1) | DK3203999T3 (enExample) |
| ES (1) | ES2785317T3 (enExample) |
| IL (1) | IL251404B (enExample) |
| MX (1) | MX376873B (enExample) |
| MY (1) | MY194308A (enExample) |
| PH (1) | PH12017500638A1 (enExample) |
| PL (1) | PL3203999T3 (enExample) |
| PT (1) | PT3203999T (enExample) |
| RU (1) | RU2709205C2 (enExample) |
| SG (1) | SG11201702868VA (enExample) |
| TW (1) | TWI699200B (enExample) |
| UY (1) | UY36356A (enExample) |
| WO (1) | WO2016054728A1 (enExample) |
| ZA (1) | ZA201702639B (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016054725A1 (en) * | 2014-10-10 | 2016-04-14 | Prometic Biosciences Inc. | Phenylketone carboxylate compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis |
| AU2015345943B2 (en) * | 2014-11-12 | 2020-03-19 | Liminal Biosciences Limited | Substituted aromatic compounds and pharmaceutical compositions for tissue self-repair and regeneration |
| CN107683135A (zh) | 2015-03-09 | 2018-02-09 | 因特克林医疗有限公司 | 用于治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法 |
| KR20190065252A (ko) * | 2016-08-18 | 2019-06-11 | 인테크린 테라퓨틱스, 아이엔씨. | 골 질환 치료용 PPARγ 작용제 |
| AU2018249822A1 (en) | 2017-04-03 | 2019-10-31 | Coherus Biosciences Inc. | PPArgamma agonist for treatment of progressive supranuclear palsy |
| AU2021356346A1 (en) * | 2020-10-06 | 2023-06-15 | Pharmaceutique Ingenew Inc. | Substituted aromatic compounds and pharmaceutical compositions thereof |
| MX2024005982A (es) * | 2021-11-17 | 2024-05-30 | Natreon Inc | Withania somnifera y asparagus racemosus en el tratamiento de enfermedades posmenopausicas. |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200720256A (en) * | 2005-05-13 | 2007-06-01 | Synta Pharmaceuticals Corp | IL-12 modulatory compounds |
| EP2427416B1 (en) * | 2009-05-04 | 2016-03-09 | Prometic Pharma Smt Limited | Substituted aromatic compounds and pharmaceutical uses thereof |
| BRPI1015118A2 (pt) * | 2009-05-04 | 2016-04-12 | Prometic Biosciences Inc | sais de ácido pentilfenilacético e usos farmacêuticos dos mesmos |
| PH12013500763B1 (en) * | 2010-10-27 | 2018-07-04 | Prometic Pharma Smt Ltd | Phenylketone carboxylate compounds and pharmaceutical uses thereof |
| CN105997967B (zh) * | 2010-10-27 | 2019-08-23 | 普罗米蒂克医药Smt有限公司 | 用于治疗癌症的化合物和组合物 |
| TWI742541B (zh) * | 2013-03-15 | 2021-10-11 | 英商邊緣生物科技有限公司 | 用於治療肺纖維化、肝纖維化、皮膚纖維化及心臟纖維化之經取代之芳族化合物 |
| TWI689490B (zh) * | 2013-03-15 | 2020-04-01 | 英商邊緣生物科技有限公司 | 用於治療纖維化之經取代之芳族化合物及相關方法 |
| WO2016054725A1 (en) * | 2014-10-10 | 2016-04-14 | Prometic Biosciences Inc. | Phenylketone carboxylate compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis |
-
2015
- 2015-10-08 PL PL15849675T patent/PL3203999T3/pl unknown
- 2015-10-08 EP EP15849675.2A patent/EP3203999B1/en active Active
- 2015-10-08 JP JP2017518905A patent/JP6700639B2/ja not_active Expired - Fee Related
- 2015-10-08 WO PCT/CA2015/000540 patent/WO2016054728A1/en not_active Ceased
- 2015-10-08 TW TW104133254A patent/TWI699200B/zh not_active IP Right Cessation
- 2015-10-08 MX MX2017004733A patent/MX376873B/es active IP Right Grant
- 2015-10-08 KR KR1020177011332A patent/KR20170066476A/ko not_active Ceased
- 2015-10-08 RU RU2017116178A patent/RU2709205C2/ru active
- 2015-10-08 PT PT158496752T patent/PT3203999T/pt unknown
- 2015-10-08 AU AU2015330645A patent/AU2015330645B2/en not_active Ceased
- 2015-10-08 SG SG11201702868VA patent/SG11201702868VA/en unknown
- 2015-10-08 DK DK15849675.2T patent/DK3203999T3/da active
- 2015-10-08 CA CA2963354A patent/CA2963354A1/en not_active Abandoned
- 2015-10-08 BR BR112017007426-5A patent/BR112017007426A2/pt not_active Application Discontinuation
- 2015-10-08 CN CN201580058623.7A patent/CN106999456B/zh not_active Expired - Fee Related
- 2015-10-08 US US15/516,643 patent/US20180228750A1/en not_active Abandoned
- 2015-10-08 MY MYPI2017000520A patent/MY194308A/en unknown
- 2015-10-08 ES ES15849675T patent/ES2785317T3/es active Active
- 2015-10-13 UY UY0001036356A patent/UY36356A/es not_active Application Discontinuation
- 2015-10-13 AR ARP150103294A patent/AR102246A1/es unknown
-
2017
- 2017-03-27 IL IL251404A patent/IL251404B/en active IP Right Grant
- 2017-04-06 PH PH12017500638A patent/PH12017500638A1/en unknown
- 2017-04-12 ZA ZA2017/02639A patent/ZA201702639B/en unknown
-
2020
- 2020-04-09 US US16/844,813 patent/US11185521B2/en not_active Expired - Fee Related
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