JP2005526082A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005526082A5 JP2005526082A5 JP2003575972A JP2003575972A JP2005526082A5 JP 2005526082 A5 JP2005526082 A5 JP 2005526082A5 JP 2003575972 A JP2003575972 A JP 2003575972A JP 2003575972 A JP2003575972 A JP 2003575972A JP 2005526082 A5 JP2005526082 A5 JP 2005526082A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- oxo
- aza
- carboxamide
- fluoro
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 125
- -1 (2) naphthyl Chemical group 0.000 claims description 115
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 51
- 125000003545 alkoxy group Chemical group 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 21
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 10
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 10
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 10
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 10
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 10
- 125000004414 alkyl thio group Chemical group 0.000 claims description 10
- 125000006598 aminocarbonylamino group Chemical group 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims description 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 10
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 10
- 125000001424 substituent group Chemical group 0.000 claims description 10
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims description 5
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims description 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 5
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 claims description 5
- 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 description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 5
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims description 5
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims description 5
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims description 5
- 125000003282 alkyl amino group Chemical group 0.000 claims description 5
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims description 5
- 125000004429 atom Chemical group 0.000 claims description 5
- 125000005602 azabenzimidazolyl group Chemical group 0.000 claims description 5
- 150000001721 carbon Chemical group 0.000 claims description 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000002541 furyl group Chemical group 0.000 claims description 5
- 125000002883 imidazolyl group Chemical group 0.000 claims description 5
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 5
- 125000005956 isoquinolyl group Chemical group 0.000 claims description 5
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 5
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 5
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 5
- 125000002971 oxazolyl group Chemical group 0.000 claims description 5
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 5
- 125000004076 pyridyl group Chemical group 0.000 claims description 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 5
- 125000005493 quinolyl group Chemical group 0.000 claims description 5
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 5
- 125000000335 thiazolyl group Chemical group 0.000 claims description 5
- 125000001544 thienyl group Chemical group 0.000 claims description 5
- 125000001425 triazolyl group Chemical group 0.000 claims description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims 35
- 238000000034 method Methods 0.000 claims 12
- 229940011871 estrogen Drugs 0.000 claims 11
- 239000000262 estrogen Substances 0.000 claims 11
- 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 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
- 239000000199 parathyroid hormone Substances 0.000 claims 9
- 241000124008 Mammalia Species 0.000 claims 8
- 102000003982 Parathyroid hormone Human genes 0.000 claims 8
- 108090000445 Parathyroid hormone Proteins 0.000 claims 8
- 229960001319 parathyroid hormone Drugs 0.000 claims 8
- 239000011647 vitamin D3 Substances 0.000 claims 8
- 229940021056 vitamin d3 Drugs 0.000 claims 8
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 7
- 229940122361 Bisphosphonate Drugs 0.000 claims 7
- 150000004663 bisphosphonates Chemical class 0.000 claims 7
- 210000000988 bone and bone Anatomy 0.000 claims 7
- 210000002997 osteoclast Anatomy 0.000 claims 7
- 150000003710 vitamin D derivatives Chemical class 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- 229940046836 anti-estrogen Drugs 0.000 claims 5
- 230000001833 anti-estrogenic effect Effects 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
- 239000000328 estrogen antagonist Substances 0.000 claims 5
- 239000000583 progesterone congener Substances 0.000 claims 5
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims 5
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims 5
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 4
- 229940121819 ATPase inhibitor Drugs 0.000 claims 4
- 102000055006 Calcitonin Human genes 0.000 claims 4
- 108060001064 Calcitonin Proteins 0.000 claims 4
- 229940122156 Cathepsin K inhibitor Drugs 0.000 claims 4
- 108010047852 Integrin alphaVbeta3 Proteins 0.000 claims 4
- 102000011731 Vacuolar Proton-Translocating ATPases Human genes 0.000 claims 4
- 108010037026 Vacuolar Proton-Translocating ATPases Proteins 0.000 claims 4
- 229930003316 Vitamin D Natural products 0.000 claims 4
- 239000000362 adenosine triphosphatase inhibitor Substances 0.000 claims 4
- 229960004015 calcitonin Drugs 0.000 claims 4
- 229940044551 receptor antagonist Drugs 0.000 claims 4
- 239000002464 receptor antagonist 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
- 102100032187 Androgen receptor Human genes 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
- 208000001132 Osteoporosis Diseases 0.000 claims 3
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 3
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 3
- 108010080146 androgen receptors Proteins 0.000 claims 3
- 239000005557 antagonist 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
- 239000000203 mixture Substances 0.000 claims 3
- 230000000921 morphogenic effect Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003180 prostaglandins Chemical class 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 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 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
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 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
- 102100033367 Appetite-regulating hormone Human genes 0.000 claims 2
- 101710111255 Appetite-regulating hormone Proteins 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
- 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
- 108010016731 PPAR gamma Proteins 0.000 claims 2
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 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
- 229930003448 Vitamin K Natural products 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 229940062527 alendronate Drugs 0.000 claims 2
- 239000003098 androgen Substances 0.000 claims 2
- 230000008485 antagonism Effects 0.000 claims 2
- 230000002917 arthritic effect Effects 0.000 claims 2
- 229940069978 calcium supplement Drugs 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
- 239000003324 growth hormone secretagogue Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 229960005431 ipriflavone Drugs 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 230000001404 mediated effect Effects 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
- 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
- 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
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 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
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 206010002261 Androgen deficiency Diseases 0.000 claims 1
- 208000032467 Aplastic anaemia Diseases 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
- 208000010392 Bone Fractures 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
- 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
- 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
- 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
- 101001135770 Homo sapiens Parathyroid hormone Proteins 0.000 claims 1
- 101001135995 Homo sapiens Probable peptidyl-tRNA hydrolase Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010021118 Hypotonia Diseases 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
- 102000048143 Insulin-Like Growth Factor II Human genes 0.000 claims 1
- 108090001117 Insulin-Like Growth Factor II Proteins 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
- 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
- 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
- 208000007379 Muscle Hypotonia Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- 102000008108 Osteoprotegerin Human genes 0.000 claims 1
- 108010035042 Osteoprotegerin Proteins 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
- 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
- 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
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims 1
- 102100030742 Transforming growth factor beta-1 proprotein Human genes 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
- 239000002253 acid Substances 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
- 230000032683 aging Effects 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- DCSBSVSZJRSITC-UHFFFAOYSA-M alendronate sodium trihydrate Chemical group O.O.O.[Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O DCSBSVSZJRSITC-UHFFFAOYSA-M 0.000 claims 1
- 230000001668 ameliorated effect Effects 0.000 claims 1
- 206010003246 arthritis 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
- 230000008416 bone turnover 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
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 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
- 159000000007 calcium salts Chemical class 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
- 229940035811 conjugated estrogen Drugs 0.000 claims 1
- 235000015872 dietary supplement Nutrition 0.000 claims 1
- 229950004203 droloxifene Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 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
- 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
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 102000058004 human PTH Human genes 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
- 229910052500 inorganic mineral Inorganic materials 0.000 claims 1
- 208000018937 joint inflammation Diseases 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
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 208000037106 male hypogonadism Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000003550 marker Substances 0.000 claims 1
- 229950006319 maxacalcitol Drugs 0.000 claims 1
- 229960002985 medroxyprogesterone acetate Drugs 0.000 claims 1
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 claims 1
- 239000011707 mineral Substances 0.000 claims 1
- 235000010755 mineral Nutrition 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
- 229940074371 monofluorophosphate Drugs 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
- 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
- 229960001652 norethindrone acetate 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
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- XXUPLYBCNPLTIW-UHFFFAOYSA-N octadec-7-ynoic acid Chemical compound CCCCCCCCCCC#CCCCCCC(O)=O XXUPLYBCNPLTIW-UHFFFAOYSA-N 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
- 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
- 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
- 229940089617 risedronate Drugs 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
- 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
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims 1
- 206010041569 spinal fracture Diseases 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 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
- 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
- 210000004291 uterus Anatomy 0.000 claims 1
- 239000011653 vitamin D2 Substances 0.000 claims 1
- 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 1
- 229960004276 zoledronic acid Drugs 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 |
|---|---|---|---|
| US36382202P | 2002-03-13 | 2002-03-13 | |
| PCT/US2003/008277 WO2003077919A1 (en) | 2002-03-13 | 2003-03-07 | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010055367A Division JP5268975B2 (ja) | 2002-03-13 | 2010-03-12 | アンドロゲン受容体モジュレーターとしてのフッ化４−アザステロイド誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005526082A JP2005526082A (ja) | 2005-09-02 |
| JP2005526082A5 true JP2005526082A5 (https=) | 2006-04-13 |
| JP4516316B2 JP4516316B2 (ja) | 2010-08-04 |
Family
ID=28041817
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003575972A Expired - Fee Related JP4516316B2 (ja) | 2002-03-13 | 2003-03-07 | アンドロゲン受容体モジュレーターとしてのフッ化４−アザステロイド誘導体 |
| JP2010055367A Expired - Fee Related JP5268975B2 (ja) | 2002-03-13 | 2010-03-12 | アンドロゲン受容体モジュレーターとしてのフッ化４−アザステロイド誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010055367A Expired - Fee Related JP5268975B2 (ja) | 2002-03-13 | 2010-03-12 | アンドロゲン受容体モジュレーターとしてのフッ化４−アザステロイド誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7186838B2 (https=) |
| EP (1) | EP1485095A4 (https=) |
| JP (2) | JP4516316B2 (https=) |
| KR (1) | KR100938136B1 (https=) |
| CN (1) | CN1652786A (https=) |
| AU (1) | AU2003218235B2 (https=) |
| BR (1) | BR0308355A (https=) |
| CA (1) | CA2478186C (https=) |
| EC (1) | ECSP045287A (https=) |
| HR (1) | HRP20040822A2 (https=) |
| IL (2) | IL163825A0 (https=) |
| IS (1) | IS7425A (https=) |
| MA (1) | MA27112A1 (https=) |
| MX (1) | MXPA04008800A (https=) |
| NO (1) | NO20044312L (https=) |
| NZ (1) | NZ534946A (https=) |
| PL (1) | PL372920A1 (https=) |
| RU (1) | RU2320670C2 (https=) |
| UA (1) | UA78029C2 (https=) |
| WO (1) | WO2003077919A1 (https=) |
| ZA (1) | ZA200406843B (https=) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7622503B2 (en) | 2000-08-24 | 2009-11-24 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| US8853266B2 (en) | 2001-12-06 | 2014-10-07 | University Of Tennessee Research Foundation | Selective androgen receptor modulators for treating diabetes |
| US7772433B2 (en) | 2002-02-28 | 2010-08-10 | University Of Tennessee Research Foundation | SARMS and method of use thereof |
| PL372920A1 (en) * | 2002-03-13 | 2005-08-08 | Merck & Co,Inc. | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
| RU2387451C2 (ru) * | 2002-05-10 | 2010-04-27 | Ф.Хоффманн-Ля Рош Аг | Бисфосфоновые кислоты, предназначенные для лечения и профилактики остеопороза |
| US8309603B2 (en) | 2004-06-07 | 2012-11-13 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US20070088042A1 (en) * | 2004-09-09 | 2007-04-19 | Meissner Robert S | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
| US7446110B2 (en) * | 2003-09-10 | 2008-11-04 | Merck & Co., Inc. | 17-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
| WO2005037201A2 (en) * | 2003-10-14 | 2005-04-28 | Gtx, Inc. | Treating bone-related disorders with selective androgen receptor modulators |
| WO2005044988A2 (en) * | 2003-10-31 | 2005-05-19 | Merck & Co., Inc. | 21-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
| RU2397176C2 (ru) | 2004-01-07 | 2010-08-20 | Эндорешерш, Инк. | Стероидные фармацевтические продукты, направленные на спираль 12 |
| EP1734963A4 (en) * | 2004-04-02 | 2008-06-18 | Merck & Co Inc | METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER |
| WO2005105091A1 (en) * | 2004-04-28 | 2005-11-10 | Merck & Co., Inc. | Fluorinated 4-azasteroids 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 |
| JP2008510811A (ja) * | 2004-08-25 | 2008-04-10 | メルク エンド カムパニー インコーポレーテッド | アンドロゲン受容体モジュレーター |
| CA2602386A1 (en) * | 2005-03-25 | 2006-10-05 | Merck & Co., Inc. | Method of treating men with testosterone supplement and 5alpha-reductase inhibitor |
| US7301026B2 (en) * | 2005-05-05 | 2007-11-27 | Merck & Co., Inc | Process for making fluorinated 4-azasteroid derivatives |
| TW200730505A (en) * | 2005-12-07 | 2007-08-16 | Merck & Co Inc | Polymorphs of an androgen receptor modulator |
| US9730908B2 (en) | 2006-08-24 | 2017-08-15 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US9844528B2 (en) | 2006-08-24 | 2017-12-19 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US10010521B2 (en) | 2006-08-24 | 2018-07-03 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| EP2269611B1 (en) | 2006-11-16 | 2016-03-23 | Gemmus Pharma Inc. | EP2 and EP4 agonists as agents for the treatment of influenza A viral infection |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| EP2222636B1 (en) | 2007-12-21 | 2013-04-10 | Ligand Pharmaceuticals Inc. | Selective androgen receptor modulators (sarms) and uses thereof |
| JP2011511085A (ja) * | 2008-02-07 | 2011-04-07 | ブリストル−マイヤーズ スクイブ カンパニー | グルココルチコイド受容体、ＡＰ−１、および／またはＮＦ−κＢ活性の縮合ヘテロアリール修飾因子並びにその使用 |
| EP2149552A1 (de) | 2008-07-30 | 2010-02-03 | Bayer Schering Pharma AG | 5,6 substituierte Benzamid-Derivate als Modulatoren des EP2-Rezeptors |
| EP2149551A1 (de) | 2008-07-30 | 2010-02-03 | Bayer Schering Pharma AG | N-(Indol-3-ylalkyl)-(hetero)arylamidderivate als Modulatoren des EP2-Rezeptors |
| EP2149554A1 (de) | 2008-07-30 | 2010-02-03 | Bayer Schering Pharma Aktiengesellschaft | Indolylamide als Modulatoren des EP2-Rezeptors |
| RS56042B1 (sr) | 2010-06-10 | 2017-09-29 | Seragon Pharmaceuticals Inc | Modulatori estrogenih receptora i njihove upotrebe |
| DE102010027016A1 (de) | 2010-07-09 | 2012-01-12 | Universitätsklinikum Jena | Steroid-Styrylfarbstoff-Konjugate zur Simulation und direkten lichtoptischen Detektion des Verhaltens von Steroiden im lebenden biologischen Gewebe und in Gegenwart von steroidbindenden Proteinen |
| WO2013090829A1 (en) | 2011-12-14 | 2013-06-20 | Aragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| LT2872482T (lt) | 2012-07-13 | 2020-12-28 | Oncternal Therapeutics, Inc. | Krūties vėžių gydymo būdas selektyviu androgeno receptoriaus moduliatoriumi |
| 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) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (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) |
| 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) |
| US9566310B2 (en) | 2012-09-10 | 2017-02-14 | Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Reno | Methods of treating muscular dystrophy |
| US9707210B2 (en) | 2013-03-15 | 2017-07-18 | Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Reno | Methods of treating muscular dystrophy |
| US10441567B2 (en) | 2014-01-17 | 2019-10-15 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| KR101586345B1 (ko) * | 2014-08-06 | 2016-01-18 | 한국생명공학연구원 | 에스트라디올 벤조에이트(Estradiol benzoate) 또는 이의 약학적으로 허용 가능한 염을 포함하는 근력약화 관련 질환의 예방 또는 치료용 약학적 조성물 |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| BR112020006677A2 (pt) | 2017-10-05 | 2020-10-06 | Fulcrum Therapeutics, Inc. | uso de inibidores p38 para reduzir a expressão de dux4 |
| WO2019154257A1 (zh) | 2018-02-11 | 2019-08-15 | 江苏豪森药业集团有限公司 | 一种甾族类衍生物调节剂及其制备方法和应用 |
| WO2020214834A1 (en) | 2019-04-19 | 2020-10-22 | Ligand Pharmaceuticals Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
| CN118027131A (zh) | 2019-08-07 | 2024-05-14 | 上海翰森生物医药科技有限公司 | 一种甾族类衍生物调节剂的盐及其晶型 |
| US11904006B2 (en) | 2019-12-11 | 2024-02-20 | University Of Iowa Research Foundation | Poly(diaminosulfide) particle-based vaccine |
| CN112851745B (zh) * | 2021-01-25 | 2021-11-16 | 广西民族大学 | 氮杂甾体吡啶类化合物及其合成与应用 |
| US20240293322A1 (en) | 2021-06-23 | 2024-09-05 | University Of Iowa Research Foundation | Sustained release formulations comprising a selective androgen receptor modulator |
| CN115558013B (zh) * | 2021-07-02 | 2025-02-18 | 石家庄迪斯凯威医药科技有限公司 | 一种甾体磷酸酯化合物及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5187278A (en) * | 1990-08-27 | 1993-02-16 | Merck & Co., Inc. | Trialkylsilyl trifluoromethanesulfonate mediated α-methylenic carbon functionalization of 4-aza-5α-androstan-3-one steroids |
| IE76452B1 (en) * | 1990-10-29 | 1997-10-22 | Sankyo Co | Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use |
| GB9216284D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives |
| TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
| JPH11512434A (ja) * | 1995-09-15 | 1999-10-26 | メルク エンド カンパニー インコーポレーテッド | アンドロゲン過剰状態治療用の４−アザステロイド |
| WO1998025623A1 (en) * | 1996-12-09 | 1998-06-18 | Merck & Co., Inc. | Methods and compositions for preventing and treating bone loss |
| PL372920A1 (en) * | 2002-03-13 | 2005-08-08 | Merck & Co,Inc. | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
-
2003
- 2003-03-07 PL PL03372920A patent/PL372920A1/xx not_active Application Discontinuation
- 2003-03-07 US US10/507,239 patent/US7186838B2/en not_active Expired - Fee Related
- 2003-03-07 BR BR0308355-1A patent/BR0308355A/pt not_active IP Right Cessation
- 2003-03-07 MX MXPA04008800A patent/MXPA04008800A/es active IP Right Grant
- 2003-03-07 HR HR20040822A patent/HRP20040822A2/hr not_active Application Discontinuation
- 2003-03-07 IL IL16382503A patent/IL163825A0/xx unknown
- 2003-03-07 WO PCT/US2003/008277 patent/WO2003077919A1/en not_active Ceased
- 2003-03-07 CA CA2478186A patent/CA2478186C/en not_active Expired - Fee Related
- 2003-03-07 EP EP03714228A patent/EP1485095A4/en not_active Withdrawn
- 2003-03-07 NZ NZ534946A patent/NZ534946A/en not_active IP Right Cessation
- 2003-03-07 KR KR1020047014281A patent/KR100938136B1/ko not_active Expired - Fee Related
- 2003-03-07 CN CNA038104857A patent/CN1652786A/zh active Pending
- 2003-03-07 AU AU2003218235A patent/AU2003218235B2/en not_active Ceased
- 2003-03-07 JP JP2003575972A patent/JP4516316B2/ja not_active Expired - Fee Related
- 2003-03-07 RU RU2004130452/04A patent/RU2320670C2/ru not_active IP Right Cessation
- 2003-07-03 UA UA20041008266A patent/UA78029C2/uk unknown
-
2004
- 2004-08-26 IS IS7425A patent/IS7425A/is unknown
- 2004-08-27 ZA ZA200406843A patent/ZA200406843B/en unknown
- 2004-08-31 IL IL163825A patent/IL163825A/en not_active IP Right Cessation
- 2004-09-10 EC EC2004005287A patent/ECSP045287A/es unknown
- 2004-10-07 MA MA27893A patent/MA27112A1/fr unknown
- 2004-10-12 NO NO20044312A patent/NO20044312L/no unknown
-
2010
- 2010-03-12 JP JP2010055367A patent/JP5268975B2/ja not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2005526082A5 (https=) | ||
| CA2478186A1 (en) | Fluorinated 4-azasteroid derivatives as androgen receptor modulators | |
| JP2005529897A5 (https=) | ||
| JP2007505118A5 (https=) | ||
| KR20160048054A (ko) | 골 성장의 촉진을 위한 방법, 시스템 및 조성물 | |
| Rubin et al. | New anabolic therapies in osteoporosis | |
| EP1260225A1 (en) | A pharmaceutical composition for use in hormone replacement therapy | |
| RU2469042C2 (ru) | Терапевтически активные триазолы и их использование | |
| CN1620300A (zh) | 二膦酸盐的给药方法 | |
| CA2462456A1 (en) | Androstane 17-beta-carboxamides as androgen receptor modulators | |
| EP1878429B1 (en) | Trenadermal absorption preparation | |
| AU2007223981A1 (en) | HMG Co-A reductase inhibitor enhancement of bone and cartilage | |
| CA2838089A1 (en) | Methods for treating cancer comprising the administration of a vitamin d compound and an additional therapeutic agent, and compositions containing the same | |
| JP2006528686A5 (https=) | ||
| JP2002506030A (ja) | 骨再吸収の阻害方法 | |
| AU7945898A (en) | A combined pharmaceutical preparation comprising parathyroid hormone and a bone resorption inhibitor | |
| CA2524409A1 (en) | Androgen receptor modulators and methods of use thereof | |
| JP2007509962A5 (https=) | ||
| US20190270767A1 (en) | Oxysterol-therapeutic agent derivative for bone healing | |
| CA2472475A1 (en) | 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators | |
| JP2005518404A5 (https=) | ||
| US20010003745A1 (en) | Combination of an agent that binds to the androgen receptor and a bisphosphonic acid in the prevention and/or treatment of diseases involving calcium or phosphate metabolism | |
| KR20050032507A (ko) | 스테로이드 화합물을 이용한 골소실의 예방 및 치료 방법 | |
| Geusens et al. | Newer drug treatments: their effects on fracture prevention | |
| JP2004026715A (ja) | 骨粗鬆症・骨減少症治療剤 |