JP2007505118A5 - - Google Patents
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- JP2007505118A5 JP2007505118A5 JP2006526181A JP2006526181A JP2007505118A5 JP 2007505118 A5 JP2007505118 A5 JP 2007505118A5 JP 2006526181 A JP2006526181 A JP 2006526181A JP 2006526181 A JP2006526181 A JP 2006526181A JP 2007505118 A5 JP2007505118 A5 JP 2007505118A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylamino
- cycloalkyl
- aryl
- carbonyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 300
- 125000003118 aryl group Chemical group 0.000 claims 59
- 125000000623 heterocyclic group Chemical group 0.000 claims 59
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 56
- 125000003282 alkyl amino group Chemical group 0.000 claims 56
- -1 aminocarbonyloxy Chemical group 0.000 claims 55
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 51
- 125000003545 alkoxy group Chemical group 0.000 claims 45
- 150000001875 compounds Chemical class 0.000 claims 40
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 37
- 229910052736 halogen Chemical group 0.000 claims 27
- 150000002367 halogens Chemical group 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 20
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 20
- 238000000034 method Methods 0.000 claims 19
- 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 18
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 12
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 12
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 12
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 241000124008 Mammalia Species 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
- 125000004442 acylamino group Chemical group 0.000 claims 10
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000006598 aminocarbonylamino group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 229940011871 estrogen Drugs 0.000 claims 9
- 239000000262 estrogen Substances 0.000 claims 9
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 8
- 125000000449 nitro group Chemical class [O-][N+](*)=O 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
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 229960001319 parathyroid hormone Drugs 0.000 claims 7
- 150000003710 vitamin D derivatives Chemical class 0.000 claims 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- 101100219283 Amycolatopsis orientalis cyp165C4 gene Proteins 0.000 claims 6
- 229940122361 Bisphosphonate Drugs 0.000 claims 6
- 150000004663 bisphosphonates Chemical class 0.000 claims 6
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 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
- 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 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
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 210000002997 osteoclast Anatomy 0.000 claims 5
- 102000055006 Calcitonin Human genes 0.000 claims 4
- 108060001064 Calcitonin Proteins 0.000 claims 4
- 229930003316 Vitamin D Natural products 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 229940046836 anti-estrogen Drugs 0.000 claims 4
- 230000001833 anti-estrogenic effect Effects 0.000 claims 4
- 229960004015 calcitonin Drugs 0.000 claims 4
- 239000000328 estrogen antagonist Substances 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 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
- 150000003721 vitamin K derivatives Chemical class 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
- 229940122156 Cathepsin K inhibitor Drugs 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
- 208000001132 Osteoporosis Diseases 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
- 239000000362 adenosine triphosphatase inhibitor Substances 0.000 claims 3
- 125000000033 alkoxyamino group Chemical group 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 230000002917 arthritic effect Effects 0.000 claims 3
- 230000004097 bone metabolism Effects 0.000 claims 3
- 229940112869 bone morphogenetic protein Drugs 0.000 claims 3
- 229940069978 calcium supplement Drugs 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000005026 carboxyaryl group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 150000004673 fluoride salts Chemical class 0.000 claims 3
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 3
- 239000003550 marker Substances 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003180 prostaglandins Chemical class 0.000 claims 3
- 229940044551 receptor antagonist Drugs 0.000 claims 3
- 239000002464 receptor antagonist Substances 0.000 claims 3
- 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
- OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical compound NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 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
- 108010022452 Collagen Type I Proteins 0.000 claims 2
- 102000012422 Collagen Type I Human genes 0.000 claims 2
- 102000018997 Growth Hormone Human genes 0.000 claims 2
- 108010051696 Growth Hormone Proteins 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
- 208000004403 Prostatic Hyperplasia Diseases 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
- 229930003448 Vitamin K Natural products 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 2
- 229940062527 alendronate Drugs 0.000 claims 2
- 125000005157 alkyl carboxy group Chemical group 0.000 claims 2
- 239000003098 androgen Substances 0.000 claims 2
- 230000003042 antagnostic effect Effects 0.000 claims 2
- 239000005557 antagonist 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
- 239000003102 growth factor Substances 0.000 claims 2
- 239000000122 growth hormone Substances 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 239000003112 inhibitor 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
- 239000000203 mixture Substances 0.000 claims 2
- XXUPLYBCNPLTIW-UHFFFAOYSA-N octadec-7-ynoic acid Chemical compound CCCCCCCCCCC#CCCCCCC(O)=O XXUPLYBCNPLTIW-UHFFFAOYSA-N 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
- 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 2
- 229960002797 pitavastatin Drugs 0.000 claims 2
- 239000003909 protein kinase inhibitor Substances 0.000 claims 2
- 230000028327 secretion Effects 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
- 230000002485 urinary effect Effects 0.000 claims 2
- 235000019168 vitamin K Nutrition 0.000 claims 2
- 239000011712 vitamin K Substances 0.000 claims 2
- 229940046010 vitamin k Drugs 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
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 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
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- 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
- 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
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- 206010006895 Cachexia Diseases 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 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
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- 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 claims 1
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- 101000762366 Homo sapiens Bone morphogenetic protein 2 Proteins 0.000 claims 1
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- 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
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- 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
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- 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
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- 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
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- 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
- 102000015433 Prostaglandin Receptors Human genes 0.000 claims 1
- 108010050183 Prostaglandin Receptors Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 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 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
- 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
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| EP1696925A4 (en) | 2003-10-31 | 2009-11-18 | Merck & Co Inc | 21-Heterocyclic 4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| US9889110B2 (en) | 2004-06-07 | 2018-02-13 | University Of Tennessee Research Foundation | Selective androgen receptor modulator for treating hormone-related conditions |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| KR101595238B1 (ko) | 2007-12-21 | 2016-02-18 | 리간드 파마슈티칼스 인코포레이티드 | 선택적 안드로겐 수용체 조절제(ｓａｒｍ) 및 이의 용도 |
| WO2011150360A1 (en) | 2010-05-28 | 2011-12-01 | The Board Of Regents Of The University Of Texas System | Oligo-benzamide compounds and their use |
| HUE033581T2 (hu) | 2010-06-10 | 2017-12-28 | Seragon Pharmaceuticals Inc | Ösztrogén receptor modulátorok és alkalmazásaik |
| WO2013078288A1 (en) | 2011-11-23 | 2013-05-30 | The Board Of Regents Of The University Of Texas System | Oligo-benzamide compounds for use in treating cancers |
| US8754124B2 (en) | 2011-11-23 | 2014-06-17 | Board Of Regents, The University Of Texas System | Oligo-benzamide compounds and their use in treating cancers |
| JP6112625B2 (ja) | 2011-12-14 | 2017-04-12 | セラゴン ファーマシューティカルズ，インク． | フッ素化したエストロゲン受容体モジュレーターおよびその使用 |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| PT2872482T (pt) | 2012-07-13 | 2020-09-22 | Oncternal Therapeutics Inc | Método de tratamento de cancro de mama com modulador seletivo do recetor de andrógeno (sarm) |
| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US9622992B2 (en) | 2012-07-13 | 2017-04-18 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| EP3094323A4 (en) | 2014-01-17 | 2017-10-11 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| US9974767B2 (en) * | 2014-07-14 | 2018-05-22 | University Of Washington | Statins in the treatment of muscular dystrophies and myopathies |
| CN107312056B (zh) * | 2017-08-24 | 2019-10-25 | 广西师范学院 | 2-(3’-羟基-17’-孕甾烷基)-5-氟苯并咪唑的合成方法 |
| JP7640458B2 (ja) | 2018-10-05 | 2025-03-05 | アンナプルナ バイオ インコーポレイテッド | Ａｐｊ受容体活性に関連する状態を処置するための化合物および組成物 |
| AU2020257397B2 (en) | 2019-04-19 | 2026-02-26 | Ligand Pharmaceuticals Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
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| US5525608A (en) | 1994-04-20 | 1996-06-11 | Merck & Co., Inc. | 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors |
| GB9727522D0 (en) | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Process for preparing carboxamido-4-azasteroids |
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- 2004-09-02 US US10/569,303 patent/US7217720B2/en not_active Expired - Fee Related
- 2004-09-02 AU AU2004272004A patent/AU2004272004B2/en not_active Ceased
- 2004-09-02 WO PCT/US2004/028641 patent/WO2005025579A1/en not_active Ceased
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