JP2007509962A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2007509962A5 JP2007509962A5 JP2006538255A JP2006538255A JP2007509962A5 JP 2007509962 A5 JP2007509962 A5 JP 2007509962A5 JP 2006538255 A JP2006538255 A JP 2006538255A JP 2006538255 A JP2006538255 A JP 2006538255A JP 2007509962 A5 JP2007509962 A5 JP 2007509962A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- aza
- androst
- compound
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 144
- 150000001875 compounds Chemical class 0.000 claims 43
- -1 perfluoro Chemical group 0.000 claims 37
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 31
- 125000003118 aryl group Chemical group 0.000 claims 30
- 239000008194 pharmaceutical composition Substances 0.000 claims 30
- 125000003282 alkyl amino group Chemical group 0.000 claims 24
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 23
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 14
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 10
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims 10
- 229910052736 halogen Chemical group 0.000 claims 10
- 150000002367 halogens Chemical group 0.000 claims 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 241000124008 Mammalia Species 0.000 claims 9
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims 9
- 229940011871 estrogen Drugs 0.000 claims 9
- 239000000262 estrogen Substances 0.000 claims 9
- 239000002253 acid Substances 0.000 claims 8
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 8
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 8
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 8
- 239000000199 parathyroid hormone Substances 0.000 claims 8
- 239000011647 vitamin D3 Substances 0.000 claims 8
- 229940021056 vitamin d3 Drugs 0.000 claims 8
- 102000003982 Parathyroid hormone Human genes 0.000 claims 7
- 108090000445 Parathyroid hormone Proteins 0.000 claims 7
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 7
- 229960001319 parathyroid hormone Drugs 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 150000003710 vitamin D derivatives Chemical class 0.000 claims 7
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims 6
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 235000005282 vitamin D3 Nutrition 0.000 claims 6
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 claims 6
- 102100032187 Androgen receptor Human genes 0.000 claims 5
- 125000006598 aminocarbonylamino group Chemical group 0.000 claims 5
- 108010080146 androgen receptors Proteins 0.000 claims 5
- 210000000988 bone and bone Anatomy 0.000 claims 5
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)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]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 5
- 230000006870 function Effects 0.000 claims 5
- 102000055006 Calcitonin Human genes 0.000 claims 4
- 108060001064 Calcitonin Proteins 0.000 claims 4
- 208000001132 Osteoporosis Diseases 0.000 claims 4
- 229930003316 Vitamin D Natural products 0.000 claims 4
- 125000004442 acylamino group Chemical group 0.000 claims 4
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 4
- 229940046836 anti-estrogen Drugs 0.000 claims 4
- 230000001833 anti-estrogenic effect Effects 0.000 claims 4
- 230000002917 arthritic effect Effects 0.000 claims 4
- 229960004015 calcitonin Drugs 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 239000000328 estrogen antagonist Substances 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 210000002997 osteoclast Anatomy 0.000 claims 4
- 239000000583 progesterone congener Substances 0.000 claims 4
- 102000005962 receptors Human genes 0.000 claims 4
- 108020003175 receptors Proteins 0.000 claims 4
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims 4
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims 4
- 239000011710 vitamin D Substances 0.000 claims 4
- 235000019166 vitamin D Nutrition 0.000 claims 4
- 229940046008 vitamin d Drugs 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- 229940121819 ATPase inhibitor Drugs 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 108010007726 Bone Morphogenetic Proteins Proteins 0.000 claims 3
- 102000007350 Bone Morphogenetic Proteins Human genes 0.000 claims 3
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 3
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 3
- 108090000723 Insulin-Like Growth Factor I Proteins 0.000 claims 3
- 102000014429 Insulin-like growth factor Human genes 0.000 claims 3
- 108010047852 Integrin alphaVbeta3 Proteins 0.000 claims 3
- 102000011731 Vacuolar Proton-Translocating ATPases Human genes 0.000 claims 3
- 108010037026 Vacuolar Proton-Translocating ATPases Proteins 0.000 claims 3
- 230000003213 activating effect Effects 0.000 claims 3
- 239000000362 adenosine triphosphatase inhibitor Substances 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 230000004097 bone metabolism Effects 0.000 claims 3
- 229940112869 bone morphogenetic protein Drugs 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 150000004673 fluoride salts Chemical class 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 239000003550 marker Substances 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 150000003180 prostaglandins Chemical class 0.000 claims 3
- 150000003721 vitamin K derivatives Chemical class 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims 2
- LHAPNDAERSFWSC-JGUILPGDSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;1-[2-[4-[(e)-1-(4-methoxyphenyl)-2-nitro-2-phenylethenyl]phenoxy]ethyl]pyrrolidine Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C1=CC(OC)=CC=C1C(\C=1C=CC(OCCN2CCCC2)=CC=1)=C([N+]([O-])=O)\C1=CC=CC=C1 LHAPNDAERSFWSC-JGUILPGDSA-N 0.000 claims 2
- OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical compound NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical group [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 229940123613 Calcium receptor antagonist Drugs 0.000 claims 2
- 229940122156 Cathepsin K inhibitor Drugs 0.000 claims 2
- 108010022452 Collagen Type I Proteins 0.000 claims 2
- 102000012422 Collagen Type I Human genes 0.000 claims 2
- 102000002265 Human Growth Hormone Human genes 0.000 claims 2
- 108010000521 Human Growth Hormone Proteins 0.000 claims 2
- 239000000854 Human Growth Hormone Substances 0.000 claims 2
- SFBODOKJTYAUCM-UHFFFAOYSA-N Ipriflavone Chemical compound C=1C(OC(C)C)=CC=C(C2=O)C=1OC=C2C1=CC=CC=C1 SFBODOKJTYAUCM-UHFFFAOYSA-N 0.000 claims 2
- 102000008108 Osteoprotegerin Human genes 0.000 claims 2
- 108010035042 Osteoprotegerin Proteins 0.000 claims 2
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 2
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 2
- 229940062527 alendronate Drugs 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 239000011575 calcium Substances 0.000 claims 2
- 229910052791 calcium Inorganic materials 0.000 claims 2
- 229940069978 calcium supplement Drugs 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- GKIRPKYJQBWNGO-OCEACIFDSA-N clomifene Chemical compound C1=CC(OCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(\Cl)C1=CC=CC=C1 GKIRPKYJQBWNGO-OCEACIFDSA-N 0.000 claims 2
- 108010049937 collagen type I trimeric cross-linked peptide Proteins 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 239000003102 growth factor Substances 0.000 claims 2
- 229910052500 inorganic mineral Inorganic materials 0.000 claims 2
- 229960005431 ipriflavone Drugs 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 239000011707 mineral Substances 0.000 claims 2
- 235000010755 mineral Nutrition 0.000 claims 2
- XXUPLYBCNPLTIW-UHFFFAOYSA-N octadec-7-ynoic acid Chemical compound CCCCCCCCCCC#CCCCCCC(O)=O XXUPLYBCNPLTIW-UHFFFAOYSA-N 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 2
- 108010068338 p38 Mitogen-Activated Protein Kinases Proteins 0.000 claims 2
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 2
- 229960002797 pitavastatin Drugs 0.000 claims 2
- 239000003909 protein kinase inhibitor Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229960002855 simvastatin Drugs 0.000 claims 2
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims 2
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical group [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims 2
- 206010041569 spinal fracture Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 230000002485 urinary effect Effects 0.000 claims 2
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims 1
- ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 claims 1
- BFPYWIDHMRZLRN-SWBPCFCJSA-N (8r,9s,13s,14s,17s)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SWBPCFCJSA-N 0.000 claims 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 1
- STAHNFFHFRNPMD-OQKDUQJOSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;3-[4-[(z)-1-(4-methoxyphenyl)-2-nitro-2-phenylethenyl]phenoxy]-n,n-dimethylpropan-1-amine Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C1=CC(OC)=CC=C1C(\C=1C=CC(OCCCN(C)C)=CC=1)=C([N+]([O-])=O)/C1=CC=CC=C1 STAHNFFHFRNPMD-OQKDUQJOSA-N 0.000 claims 1
- JWUBBDSIWDLEOM-UHFFFAOYSA-N 25-Hydroxycholecalciferol Natural products C1CCC2(C)C(C(CCCC(C)(C)O)C)CCC2C1=CC=C1CC(O)CCC1=C JWUBBDSIWDLEOM-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 101100219283 Amycolatopsis orientalis cyp165C4 gene Proteins 0.000 claims 1
- 206010002261 Androgen deficiency Diseases 0.000 claims 1
- 208000032467 Aplastic anaemia Diseases 0.000 claims 1
- 102100033367 Appetite-regulating hormone Human genes 0.000 claims 1
- 101710111255 Appetite-regulating hormone Proteins 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 1
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000010392 Bone Fractures Diseases 0.000 claims 1
- 208000006386 Bone Resorption Diseases 0.000 claims 1
- 102100024506 Bone morphogenetic protein 2 Human genes 0.000 claims 1
- 102100024504 Bone morphogenetic protein 3 Human genes 0.000 claims 1
- 102100022526 Bone morphogenetic protein 5 Human genes 0.000 claims 1
- 102100022525 Bone morphogenetic protein 6 Human genes 0.000 claims 1
- 102100022544 Bone morphogenetic protein 7 Human genes 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 102000004171 Cathepsin K Human genes 0.000 claims 1
- 108090000625 Cathepsin K Proteins 0.000 claims 1
- ZQZFYGIXNQKOAV-OCEACIFDSA-N Droloxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=C(O)C=CC=1)\C1=CC=C(OCCN(C)C)C=C1 ZQZFYGIXNQKOAV-OCEACIFDSA-N 0.000 claims 1
- 241000283073 Equus caballus Species 0.000 claims 1
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims 1
- DBVJJBKOTRCVKF-UHFFFAOYSA-N Etidronic acid Chemical compound OP(=O)(O)C(O)(C)P(O)(O)=O DBVJJBKOTRCVKF-UHFFFAOYSA-N 0.000 claims 1
- 102000018233 Fibroblast Growth Factor Human genes 0.000 claims 1
- 108050007372 Fibroblast Growth Factor Proteins 0.000 claims 1
- 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 claims 1
- 102100031706 Fibroblast growth factor 1 Human genes 0.000 claims 1
- 102100024785 Fibroblast growth factor 2 Human genes 0.000 claims 1
- 108090000379 Fibroblast growth factor 2 Proteins 0.000 claims 1
- 206010017076 Fracture Diseases 0.000 claims 1
- 208000036119 Frailty Diseases 0.000 claims 1
- 102000018997 Growth Hormone Human genes 0.000 claims 1
- 108010051696 Growth Hormone Proteins 0.000 claims 1
- 102100035379 Growth/differentiation factor 5 Human genes 0.000 claims 1
- 101000762366 Homo sapiens Bone morphogenetic protein 2 Proteins 0.000 claims 1
- 101000762375 Homo sapiens Bone morphogenetic protein 3 Proteins 0.000 claims 1
- 101000899388 Homo sapiens Bone morphogenetic protein 5 Proteins 0.000 claims 1
- 101000899390 Homo sapiens Bone morphogenetic protein 6 Proteins 0.000 claims 1
- 101000899361 Homo sapiens Bone morphogenetic protein 7 Proteins 0.000 claims 1
- 101001023988 Homo sapiens Growth/differentiation factor 5 Proteins 0.000 claims 1
- 101000599951 Homo sapiens Insulin-like growth factor I Proteins 0.000 claims 1
- 101001135770 Homo sapiens Parathyroid hormone Proteins 0.000 claims 1
- 101001135995 Homo sapiens Probable peptidyl-tRNA hydrolase Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 108700012441 IGF2 Proteins 0.000 claims 1
- MPBVHIBUJCELCL-UHFFFAOYSA-N Ibandronate Chemical compound CCCCCN(C)CCC(O)(P(O)(O)=O)P(O)(O)=O MPBVHIBUJCELCL-UHFFFAOYSA-N 0.000 claims 1
- JJKOTMDDZAJTGQ-DQSJHHFOSA-N Idoxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN2CCCC2)=CC=1)/C1=CC=C(I)C=C1 JJKOTMDDZAJTGQ-DQSJHHFOSA-N 0.000 claims 1
- 102100037852 Insulin-like growth factor I Human genes 0.000 claims 1
- 102000004374 Insulin-like growth factor binding protein 3 Human genes 0.000 claims 1
- 108090000965 Insulin-like growth factor binding protein 3 Proteins 0.000 claims 1
- 229940127449 Integrin Receptor Antagonists Drugs 0.000 claims 1
- DTXXSJZBSTYZKE-ZDQKKZTESA-N Maxacalcitol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](OCCC(C)(C)O)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C DTXXSJZBSTYZKE-ZDQKKZTESA-N 0.000 claims 1
- 206010027304 Menopausal symptoms Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims 1
- LOJFGJZQOKTUBR-XAQOOIOESA-N NC(N)=NCCC[C@@H](C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCC(O)=O)C)CC1=CN=CN1 Chemical compound NC(N)=NCCC[C@@H](C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCC(O)=O)C)CC1=CN=CN1 LOJFGJZQOKTUBR-XAQOOIOESA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims 1
- 208000002500 Primary Ovarian Insufficiency Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- DKJJVAGXPKPDRL-UHFFFAOYSA-N Tiludronic acid Chemical compound OP(O)(=O)C(P(O)(O)=O)SC1=CC=C(Cl)C=C1 DKJJVAGXPKPDRL-UHFFFAOYSA-N 0.000 claims 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 claims 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims 1
- 229930003448 Vitamin K Natural products 0.000 claims 1
- UGEPSJNLORCRBO-UHFFFAOYSA-N [3-(dimethylamino)-1-hydroxy-1-phosphonopropyl]phosphonic acid Chemical compound CN(C)CCC(O)(P(O)(O)=O)P(O)(O)=O UGEPSJNLORCRBO-UHFFFAOYSA-N 0.000 claims 1
- OEKMGABCSLYWOP-DHUJRADRSA-N [4-[(2s)-7-(2,2-dimethylpropanoyloxy)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2h-chromen-3-yl]phenyl] 2,2-dimethylpropanoate Chemical compound C1=CC([C@H]2C(=C(C3=CC=C(OC(=O)C(C)(C)C)C=C3O2)C)C=2C=CC(OC(=O)C(C)(C)C)=CC=2)=CC=C1OCCN1CCCCC1 OEKMGABCSLYWOP-DHUJRADRSA-N 0.000 claims 1
- 210000000579 abdominal fat Anatomy 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- DUYNJNWVGIWJRI-LJAQVGFWSA-N acolbifene Chemical compound C1=CC([C@H]2C(=C(C3=CC=C(O)C=C3O2)C)C=2C=CC(O)=CC=2)=CC=C1OCCN1CCCCC1 DUYNJNWVGIWJRI-LJAQVGFWSA-N 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- DCSBSVSZJRSITC-UHFFFAOYSA-M alendronate sodium trihydrate Chemical compound O.O.O.[Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O DCSBSVSZJRSITC-UHFFFAOYSA-M 0.000 claims 1
- 125000006323 alkenyl amino group Chemical group 0.000 claims 1
- 125000000033 alkoxyamino group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000005157 alkyl carboxy group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 230000001668 ameliorated effect Effects 0.000 claims 1
- 239000003098 androgen Substances 0.000 claims 1
- 230000003042 antagnostic effect Effects 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 206010003549 asthenia Diseases 0.000 claims 1
- 229960005370 atorvastatin Drugs 0.000 claims 1
- 229960000817 bazedoxifene Drugs 0.000 claims 1
- UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical compound C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 claims 1
- 230000033228 biological regulation Effects 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- 229960002882 calcipotriol Drugs 0.000 claims 1
- LWQQLNNNIPYSNX-UROSTWAQSA-N calcipotriol Chemical compound C1([C@H](O)/C=C/[C@@H](C)[C@@H]2[C@]3(CCCC(/[C@@H]3CC2)=C\C=C\2C([C@@H](O)C[C@H](O)C/2)=C)C)CC1 LWQQLNNNIPYSNX-UROSTWAQSA-N 0.000 claims 1
- 229960003773 calcitonin (salmon synthetic) Drugs 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- FNAQSUUGMSOBHW-UHFFFAOYSA-H calcium citrate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O FNAQSUUGMSOBHW-UHFFFAOYSA-H 0.000 claims 1
- 239000001354 calcium citrate Substances 0.000 claims 1
- 125000005026 carboxyaryl group Chemical group 0.000 claims 1
- 229960005110 cerivastatin Drugs 0.000 claims 1
- SEERZIQQUAZTOL-ANMDKAQQSA-N cerivastatin Chemical compound COCC1=C(C(C)C)N=C(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 SEERZIQQUAZTOL-ANMDKAQQSA-N 0.000 claims 1
- ACSIXWWBWUQEHA-UHFFFAOYSA-N clodronic acid Chemical compound OP(O)(=O)C(Cl)(Cl)P(O)(O)=O ACSIXWWBWUQEHA-UHFFFAOYSA-N 0.000 claims 1
- 229960002286 clodronic acid Drugs 0.000 claims 1
- 229960003608 clomifene Drugs 0.000 claims 1
- 230000006999 cognitive decline Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 229940035811 conjugated estrogen Drugs 0.000 claims 1
- 239000007857 degradation product Substances 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 229950004203 droloxifene Drugs 0.000 claims 1
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 claims 1
- 229960002061 ergocalciferol Drugs 0.000 claims 1
- 229960005309 estradiol Drugs 0.000 claims 1
- 229960003399 estrone Drugs 0.000 claims 1
- 229940009626 etidronate Drugs 0.000 claims 1
- 201000003585 eunuchism Diseases 0.000 claims 1
- 208000016253 exhaustion Diseases 0.000 claims 1
- 229940126864 fibroblast growth factor Drugs 0.000 claims 1
- 229960003765 fluvastatin Drugs 0.000 claims 1
- 201000003617 glucocorticoid-induced osteoporosis Diseases 0.000 claims 1
- 239000000122 growth hormone Substances 0.000 claims 1
- 239000003324 growth hormone secretagogue Substances 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 102000058004 human PTH Human genes 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 229940015872 ibandronate Drugs 0.000 claims 1
- 229950002248 idoxifene Drugs 0.000 claims 1
- LWRDQHOZTAOILO-UHFFFAOYSA-N incadronic acid Chemical compound OP(O)(=O)C(P(O)(O)=O)NC1CCCCCC1 LWRDQHOZTAOILO-UHFFFAOYSA-N 0.000 claims 1
- 229950006971 incadronic acid Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229960002367 lasofoxifene Drugs 0.000 claims 1
- GXESHMAMLJKROZ-IAPPQJPRSA-N lasofoxifene Chemical compound C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 GXESHMAMLJKROZ-IAPPQJPRSA-N 0.000 claims 1
- XZEUAXYWNKYKPL-WDYNHAJCSA-N levormeloxifene Chemical compound C1([C@H]2[C@@H](C3=CC=C(C=C3OC2(C)C)OC)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 XZEUAXYWNKYKPL-WDYNHAJCSA-N 0.000 claims 1
- 229950002728 levormeloxifene Drugs 0.000 claims 1
- 229960004844 lovastatin Drugs 0.000 claims 1
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical group C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims 1
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims 1
- 208000037106 male hypogonadism Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229950006319 maxacalcitol Drugs 0.000 claims 1
- 229960004616 medroxyprogesterone Drugs 0.000 claims 1
- FRQMUZJSZHZSGN-HBNHAYAOSA-N medroxyprogesterone Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FRQMUZJSZHZSGN-HBNHAYAOSA-N 0.000 claims 1
- VMMKGHQPQIEGSQ-UHFFFAOYSA-N minodronic acid Chemical compound C1=CC=CN2C(CC(O)(P(O)(O)=O)P(O)(O)=O)=CN=C21 VMMKGHQPQIEGSQ-UHFFFAOYSA-N 0.000 claims 1
- 229950011129 minodronic acid Drugs 0.000 claims 1
- 230000021332 multicellular organism growth Effects 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 201000006938 muscular dystrophy Diseases 0.000 claims 1
- 239000007922 nasal spray Substances 0.000 claims 1
- 229940097496 nasal spray Drugs 0.000 claims 1
- 230000030991 negative regulation of bone resorption Effects 0.000 claims 1
- PUUSSSIBPPTKTP-UHFFFAOYSA-N neridronic acid Chemical compound NCCCCCC(O)(P(O)(O)=O)P(O)(O)=O PUUSSSIBPPTKTP-UHFFFAOYSA-N 0.000 claims 1
- 229950010733 neridronic acid Drugs 0.000 claims 1
- 229940053934 norethindrone Drugs 0.000 claims 1
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- WRUUGTRCQOWXEG-UHFFFAOYSA-N pamidronate Chemical compound NCCC(O)(P(O)(O)=O)P(O)(O)=O WRUUGTRCQOWXEG-UHFFFAOYSA-N 0.000 claims 1
- 229940046231 pamidronate Drugs 0.000 claims 1
- 208000028169 periodontal disease Diseases 0.000 claims 1
- SHUZOJHMOBOZST-UHFFFAOYSA-N phylloquinone Natural products CC(C)CCCCC(C)CCC(C)CCCC(=CCC1=C(C)C(=O)c2ccccc2C1=O)C SHUZOJHMOBOZST-UHFFFAOYSA-N 0.000 claims 1
- VGYFMXBACGZSIL-MCBHFWOFSA-N pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims 1
- RHGYHLPFVJEAOC-FFNUKLMVSA-L pitavastatin calcium Chemical compound [Ca+2].[O-]C(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1.[O-]C(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 RHGYHLPFVJEAOC-FFNUKLMVSA-L 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 229960002965 pravastatin Drugs 0.000 claims 1
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims 1
- 206010036601 premature menopause Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 229960004622 raloxifene Drugs 0.000 claims 1
- 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 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229960000672 rosuvastatin Drugs 0.000 claims 1
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 claims 1
- 108010068072 salmon calcitonin Proteins 0.000 claims 1
- 208000001076 sarcopenia Diseases 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 230000009759 skin aging Effects 0.000 claims 1
- 201000002859 sleep apnea Diseases 0.000 claims 1
- DUYCFMAOEDAKDN-UHFFFAOYSA-M sodium (4-amino-1-hydroxy-1-phosphonobutyl)-hydroxyphosphinate hydrate Chemical compound O.[Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O DUYCFMAOEDAKDN-UHFFFAOYSA-M 0.000 claims 1
- 239000011775 sodium fluoride Substances 0.000 claims 1
- 235000013024 sodium fluoride Nutrition 0.000 claims 1
- NTJHYIRSENEXDR-UHFFFAOYSA-M sodium;fluoro-dioxido-oxo-$l^{5}-phosphane;hydron Chemical compound [Na+].OP([O-])(F)=O NTJHYIRSENEXDR-UHFFFAOYSA-M 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 claims 1
- 239000013589 supplement Substances 0.000 claims 1
- 230000009469 supplementation Effects 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- 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 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 claims 1
- 229940019375 tiludronate Drugs 0.000 claims 1
- 229960005026 toremifene Drugs 0.000 claims 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 claims 1
- 235000013337 tricalcium citrate Nutrition 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 239000011653 vitamin D2 Substances 0.000 claims 1
- 235000019168 vitamin K Nutrition 0.000 claims 1
- 239000011712 vitamin K Substances 0.000 claims 1
- 229940046010 vitamin k Drugs 0.000 claims 1
- XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical class OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 claims 1
- GKIRPKYJQBWNGO-QPLCGJKRSA-N zuclomifene Chemical compound C1=CC(OCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(/Cl)C1=CC=CC=C1 GKIRPKYJQBWNGO-QPLCGJKRSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51642503P | 2003-10-31 | 2003-10-31 | |
| PCT/US2004/035838 WO2005044988A2 (en) | 2003-10-31 | 2004-10-27 | 21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007509962A JP2007509962A (ja) | 2007-04-19 |
| JP2007509962A5 true JP2007509962A5 (cg-RX-API-DMAC7.html) | 2007-12-13 |
Family
ID=34572882
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006538255A Pending JP2007509962A (ja) | 2003-10-31 | 2004-10-27 | アンドロゲン受容体調節剤としての２１−複素環−４−アザステロイド誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US7312229B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP1696925A4 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2007509962A (cg-RX-API-DMAC7.html) |
| CN (1) | CN1871005B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2004288196B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2543956A1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2005044988A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7728026B2 (en) | 2005-04-11 | 2010-06-01 | Abbott Laboratories, Inc. | 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors |
| RU2329035C1 (ru) * | 2006-11-28 | 2008-07-20 | ГУ Научно-исследовательский институт фармакологии Томского научного центра Сибирского отделения Российской академии медицинских наук | Лекарственные средства для профилактики и лечения анемии при невротических воздействиях |
| US20160331729A9 (en) | 2007-04-11 | 2016-11-17 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| US11241420B2 (en) | 2007-04-11 | 2022-02-08 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| EP2612553B1 (en) * | 2007-04-11 | 2016-06-08 | Omeros Corporation | Compositions and Methods for Prophylaxis and Treatment of Addictions |
| JP2013528223A (ja) | 2010-06-10 | 2013-07-08 | アラゴン ファーマシューティカルズ，インク． | エストロゲン受容体モジュレーターおよびその用途 |
| US9193714B2 (en) | 2011-12-14 | 2015-11-24 | Seragon Pharmaceuticals, Inc. | Fluorinated estrogen receptor modulators and uses thereof |
| CN105820206B (zh) * | 2016-04-18 | 2017-08-01 | 广西师范学院 | 22‑降‑豆甾苯并咪唑化合物及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69313114T2 (de) * | 1992-05-20 | 1998-03-19 | Merck & Co Inc | NEUE DELTA-17 UND DELTA-20 UNGESÄTIGTE UND GESATIGTE 17--g(b)-SUBSTITUIERTE-4-AZA-5-g(a)-ANDROSTAN-3-ON VERBINDUNGEN ALS INHIBITOREN VON 5-ALPHA-REDUCTASE |
| ES2158887T3 (es) * | 1992-12-18 | 2001-09-16 | Merck & Co Inc | Procedimiento para tratar la prostatitis cronica con 17 beta-n-terc-butilcarbamoil-4-aza-5 alfa-androst-1-en-ona. |
| US5525608A (en) * | 1994-04-20 | 1996-06-11 | Merck & Co., Inc. | 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors |
| CA2478186C (en) * | 2002-03-13 | 2011-08-23 | Merck & Co., Inc. | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
| CN1849126A (zh) | 2003-09-10 | 2006-10-18 | 默克公司 | 作为雄激素受体调节剂的17－杂环－4－氮杂甾族衍生物 |
-
2004
- 2004-10-27 CA CA002543956A patent/CA2543956A1/en not_active Abandoned
- 2004-10-27 EP EP04796663A patent/EP1696925A4/en not_active Withdrawn
- 2004-10-27 US US10/576,335 patent/US7312229B2/en not_active Expired - Fee Related
- 2004-10-27 JP JP2006538255A patent/JP2007509962A/ja active Pending
- 2004-10-27 WO PCT/US2004/035838 patent/WO2005044988A2/en not_active Ceased
- 2004-10-27 CN CN2004800315580A patent/CN1871005B/zh not_active Expired - Fee Related
- 2004-10-27 AU AU2004288196A patent/AU2004288196B2/en not_active Ceased
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2007505118A5 (cg-RX-API-DMAC7.html) | ||
| JP2005526082A5 (cg-RX-API-DMAC7.html) | ||
| CA2478186A1 (en) | Fluorinated 4-azasteroid derivatives as androgen receptor modulators | |
| JP2005529897A5 (cg-RX-API-DMAC7.html) | ||
| CN1272013C (zh) | 二膦酸盐在制备用于治疗骨更新异常增加的病症的药物中的应用 | |
| EP1260225A1 (en) | A pharmaceutical composition for use in hormone replacement therapy | |
| US20020198179A1 (en) | Selective estrogen receptor modulators in combination with estrogens | |
| US20050065117A1 (en) | Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and a bisphosphonate | |
| PL195772B1 (pl) | Zastosowanie prekursora sterydów płciowych w kombinacji z selektywnym modulatorem receptora estrogenu | |
| JP2007509962A5 (cg-RX-API-DMAC7.html) | ||
| CA2698626C (en) | A combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor | |
| CA2151240A1 (en) | Biophosphonate/estrogen therapy for treating and preventing bone loss | |
| EP1878429B1 (en) | Trenadermal absorption preparation | |
| CA2462456A1 (en) | Androstane 17-beta-carboxamides as androgen receptor modulators | |
| JP2006528686A5 (cg-RX-API-DMAC7.html) | ||
| Sugimoto et al. | Effects of combined treatment with eldecalcitol and alendronate on bone mass, mechanical properties, and bone histomorphometry in ovariectomized rats: a comparison with alfacalcidol and alendronate | |
| CA2472475A1 (en) | 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators | |
| JP2005518404A5 (cg-RX-API-DMAC7.html) | ||
| EP1435967A2 (en) | Methods for preventing and treating bone loss with steroid compounds | |
| US8410171B2 (en) | Adhesive preparation | |
| JP2004026715A (ja) | 骨粗鬆症・骨減少症治療剤 | |
| Hartman et al. | Anti-resorptive and anabolic bone agents | |
| JP2002538122A (ja) | 天然に存在しないｆｐ選択的アゴニストおよび骨吸収抑制化合物を用いる骨体積の増加方法 | |
| AU2006201900A1 (en) | Selective estrogen receptor modulators in combination with estrogens |