JP2004502730A - ビスホスホネート、エストロゲン剤および所望によるエストロゲンの組み合わせ - Google Patents

ビスホスホネート、エストロゲン剤および所望によるエストロゲンの組み合わせ Download PDF

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Publication number: JP2004502730A
Authority: JP; Japan
Prior art keywords: alkyl; pharmaceutically acceptable; phenyl; hydroxy; acceptable salt
Prior art date: 2000-07-06
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

Application number

JP2002508431A

Other languages

English (en)

Japanese (ja)

Inventor

サイモン・ニコラス・ジェンキンズ

バリー・サミュエル・コム

クリストファー・ポール・ミラー

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Wyeth LLC

Original Assignee

Wyeth LLC

Priority date (The priority date 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 date listed.)

2000-07-06

Filing date

2001-06-29

Publication date

2004-01-29

2001-06-29 Application filed by Wyeth LLC filed Critical Wyeth LLC

2004-01-29 Publication of JP2004502730A publication Critical patent/JP2004502730A/ja

Status Pending legal-status Critical Current

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229940122361 Bisphosphonate Drugs 0.000 title claims abstract description 27
150000004663 bisphosphonates Chemical class 0.000 title claims abstract description 25
239000000262 estrogen Substances 0.000 title claims description 43
229940011871 estrogen Drugs 0.000 title claims description 41
150000003839 salts Chemical class 0.000 claims abstract description 68
238000000034 method Methods 0.000 claims abstract description 45
125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 37
229910052736 halogen Inorganic materials 0.000 claims abstract description 30
150000002367 halogens Chemical class 0.000 claims abstract description 30
125000000217 alkyl group Chemical group 0.000 claims abstract description 24
208000020084 Bone disease Diseases 0.000 claims abstract description 21
150000002148 esters Chemical class 0.000 claims abstract description 21
150000005215 alkyl ethers Chemical class 0.000 claims abstract description 19
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 17
125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims abstract description 11
SMYMDRJWEFCCCI-UHFFFAOYSA-N trichloro(trichloromethoxy)methane Chemical compound ClC(Cl)(Cl)OC(Cl)(Cl)Cl SMYMDRJWEFCCCI-UHFFFAOYSA-N 0.000 claims abstract description 3
WZEOZJQLTRFNCU-UHFFFAOYSA-N trifluoro(trifluoromethoxy)methane Chemical compound FC(F)(F)OC(F)(F)F WZEOZJQLTRFNCU-UHFFFAOYSA-N 0.000 claims abstract description 3
-1 C 1 -C 4 alkyl Chemical group 0.000 claims description 77
150000001875 compounds Chemical class 0.000 claims description 40
229910052739 hydrogen Inorganic materials 0.000 claims description 31
125000004953 trihalomethyl group Chemical group 0.000 claims description 25
125000001424 substituent group Chemical group 0.000 claims description 23
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 20
239000001257 hydrogen Substances 0.000 claims description 19
125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims description 18
125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims description 18
241000124008 Mammalia Species 0.000 claims description 18
125000003282 alkyl amino group Chemical group 0.000 claims description 18
125000005843 halogen group Chemical group 0.000 claims description 18
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 18
125000004951 trihalomethoxy group Chemical group 0.000 claims description 18
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 description 15
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 description 14
229910052799 carbon Inorganic materials 0.000 claims description 14
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 13
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 12
DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims description 10
125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
DBVJJBKOTRCVKF-UHFFFAOYSA-N Etidronic acid Chemical compound OP(=O)(O)C(O)(C)P(O)(O)=O DBVJJBKOTRCVKF-UHFFFAOYSA-N 0.000 claims description 10
239000008194 pharmaceutical composition Substances 0.000 claims description 10
229940009626 etidronate Drugs 0.000 claims description 9
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 9
OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical compound NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims description 8
208000001132 Osteoporosis Diseases 0.000 claims description 8
NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
IIDJRNMFWXDHID-UHFFFAOYSA-N Risedronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CC1=CC=CN=C1 IIDJRNMFWXDHID-UHFFFAOYSA-N 0.000 claims description 8
JICOGKJOQXTAIP-UHFFFAOYSA-N 2-(4-hydroxyphenyl)-3-methyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]indol-5-ol Chemical compound C=1C=C(OCCN2CCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 JICOGKJOQXTAIP-UHFFFAOYSA-N 0.000 claims description 7
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 description 7
210000000988 bone and bone Anatomy 0.000 claims description 7
125000000623 heterocyclic group Chemical group 0.000 claims description 7
229940089617 risedronate Drugs 0.000 claims description 7
229940062527 alendronate Drugs 0.000 claims description 6
ACSIXWWBWUQEHA-UHFFFAOYSA-N clodronic acid Chemical compound OP(O)(=O)C(Cl)(Cl)P(O)(O)=O ACSIXWWBWUQEHA-UHFFFAOYSA-N 0.000 claims description 6
229960002286 clodronic acid Drugs 0.000 claims description 6
229960005309 estradiol Drugs 0.000 claims description 6
125000005842 heteroatom Chemical group 0.000 claims description 6
229950006971 incadronic acid Drugs 0.000 claims description 6
229920006395 saturated elastomer Polymers 0.000 claims description 6
229940019375 tiludronate Drugs 0.000 claims description 6
MPBVHIBUJCELCL-UHFFFAOYSA-N Ibandronate Chemical compound CCCCCN(C)CCC(O)(P(O)(O)=O)P(O)(O)=O MPBVHIBUJCELCL-UHFFFAOYSA-N 0.000 claims description 5
208000010191 Osteitis Deformans Diseases 0.000 claims description 5
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 description 5
239000003937 drug carrier Substances 0.000 claims description 5
229940015872 ibandronate Drugs 0.000 claims description 5
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 description 5
229950011129 minodronic acid Drugs 0.000 claims description 5
WRUUGTRCQOWXEG-UHFFFAOYSA-N pamidronate Chemical compound NCCC(O)(P(O)(O)=O)P(O)(O)=O WRUUGTRCQOWXEG-UHFFFAOYSA-N 0.000 claims description 5
229940046231 pamidronate Drugs 0.000 claims description 5
XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 claims description 5
229960004276 zoledronic acid Drugs 0.000 claims description 5
NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims description 4
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 description 4
BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 claims description 4
206010028980 Neoplasm Diseases 0.000 claims description 4
208000027868 Paget disease Diseases 0.000 claims description 4
HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims description 4
229960003399 estrone Drugs 0.000 claims description 4
VKYKSIONXSXAKP-UHFFFAOYSA-N hexamethylenetetramine Chemical compound C1N(C2)CN3CN1CN2C3 VKYKSIONXSXAKP-UHFFFAOYSA-N 0.000 claims description 4
229940088597 hormone Drugs 0.000 claims description 4
239000005556 hormone Substances 0.000 claims description 4
208000027202 mammary Paget disease Diseases 0.000 claims description 4
RYWZPRVUQHMJFF-BZSNNMDCSA-N (13s,14s,17s)-13-methyl-11,12,14,15,16,17-hexahydrocyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2C(CC[C@]3([C@H]4CC[C@@H]3O)C)=C4C=CC2=C1 RYWZPRVUQHMJFF-BZSNNMDCSA-N 0.000 claims description 3
RYWZPRVUQHMJFF-KSZLIROESA-N 17alpha-Dihydroequilenin Chemical compound OC1=CC=C2C(CC[C@]3([C@H]4CC[C@H]3O)C)=C4C=CC2=C1 RYWZPRVUQHMJFF-KSZLIROESA-N 0.000 claims description 3
RYWZPRVUQHMJFF-UHFFFAOYSA-N 17alpha-Dihydroequilenin Natural products OC1=CC=C2C(CCC3(C4CCC3O)C)=C4C=CC2=C1 RYWZPRVUQHMJFF-UHFFFAOYSA-N 0.000 claims description 3
BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 claims description 3
WKRLQDKEXYKHJB-UHFFFAOYSA-N Equilin Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3=CCC2=C1 WKRLQDKEXYKHJB-UHFFFAOYSA-N 0.000 claims description 3
WKRLQDKEXYKHJB-HFTRVMKXSA-N equilin Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 WKRLQDKEXYKHJB-HFTRVMKXSA-N 0.000 claims description 3
229960002568 ethinylestradiol Drugs 0.000 claims description 3
230000003211 malignant effect Effects 0.000 claims description 3
230000000010 osteolytic effect Effects 0.000 claims description 3
238000002360 preparation method Methods 0.000 claims description 3
PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 claims description 2
HWCYISVQOIISSU-HULBTWJISA-N (8R,9R,10S,13R)-13-methyl-1,2,3,4,5,6,7,8,9,10,11,12-dodecahydrocyclopenta[a]phenanthrene Chemical compound C([C@@H]12)CCCC1CC[C@@H]1[C@@H]2CC[C@@]2(C)C1=CC=C2 HWCYISVQOIISSU-HULBTWJISA-N 0.000 claims description 2
HVDGDHBAMCBBLR-UHFFFAOYSA-N Enterolactone Natural products OC1=CC=CC(CC2C(C(=O)OC2)CC=2C=C(O)C=CC=2)=C1 HVDGDHBAMCBBLR-UHFFFAOYSA-N 0.000 claims description 2
241000282816 Giraffa camelopardalis Species 0.000 claims description 2
206010027476 Metastases Diseases 0.000 claims description 2
201000011510 cancer Diseases 0.000 claims description 2
125000004432 carbon atom Chemical group C* 0.000 claims description 2
230000015556 catabolic process Effects 0.000 claims description 2
PDRGHUMCVRDZLQ-UHFFFAOYSA-N d-equilenin Natural products OC1=CC=C2C(CCC3(C4CCC3=O)C)=C4C=CC2=C1 PDRGHUMCVRDZLQ-UHFFFAOYSA-N 0.000 claims description 2
238000006731 degradation reaction Methods 0.000 claims description 2
HVDGDHBAMCBBLR-WMLDXEAASA-N enterolactone Chemical compound OC1=CC=CC(C[C@@H]2[C@H](C(=O)OC2)CC=2C=C(O)C=CC=2)=C1 HVDGDHBAMCBBLR-WMLDXEAASA-N 0.000 claims description 2
ADFCQWZHKCXPAJ-GFCCVEGCSA-N equol Chemical compound C1=CC(O)=CC=C1[C@@H]1CC2=CC=C(O)C=C2OC1 ADFCQWZHKCXPAJ-GFCCVEGCSA-N 0.000 claims description 2
235000019126 equol Nutrition 0.000 claims description 2
NLLMJANWPUQQTA-SPUZQDLCSA-N estra-1,3,5(10),7-tetraene-3,17alpha-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@@H](CC4)O)[C@@H]4C3=CCC2=C1 NLLMJANWPUQQTA-SPUZQDLCSA-N 0.000 claims description 2
PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 claims description 2
229960001348 estriol Drugs 0.000 claims description 2
ADFCQWZHKCXPAJ-UHFFFAOYSA-N indofine Natural products C1=CC(O)=CC=C1C1CC2=CC=C(O)C=C2OC1 ADFCQWZHKCXPAJ-UHFFFAOYSA-N 0.000 claims description 2
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125000004435 hydrogen atom Chemical class [H]* 0.000 claims 6
125000006662 (C2-C4) acyloxy group Chemical group 0.000 claims 2
LWRDQHOZTAOILO-UHFFFAOYSA-N incadronic acid Chemical compound OP(O)(=O)C(P(O)(O)=O)NC1CCCCCC1 LWRDQHOZTAOILO-UHFFFAOYSA-N 0.000 claims 2
VOEBBZZZNRIFGA-UHFFFAOYSA-N CC1=CN(C2=C1C=C(C=C2)O)C3=CC=CC=C3O Chemical compound CC1=CN(C2=C1C=C(C=C2)O)C3=CC=CC=C3O VOEBBZZZNRIFGA-UHFFFAOYSA-N 0.000 claims 1
125000004429 atom Chemical group 0.000 claims 1
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PDRGHUMCVRDZLQ-WMZOPIPTSA-N equilenin Chemical compound OC1=CC=C2C(CC[C@]3([C@H]4CCC3=O)C)=C4C=CC2=C1 PDRGHUMCVRDZLQ-WMZOPIPTSA-N 0.000 claims 1
238000006467 substitution reaction Methods 0.000 claims 1
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract description 3
150000002170 ethers Chemical class 0.000 abstract description 2
239000008280 blood Substances 0.000 abstract 1
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239000000203 mixture Substances 0.000 description 70
238000009472 formulation Methods 0.000 description 54
150000002475 indoles Chemical class 0.000 description 23
ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 18
CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 17
239000007884 disintegrant Substances 0.000 description 17
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SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 13
150000002431 hydrogen Chemical class 0.000 description 13
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229910019142 PO4 Inorganic materials 0.000 description 12
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235000021317 phosphate Nutrition 0.000 description 12
239000000546 pharmaceutical excipient Substances 0.000 description 10
150000003013 phosphoric acid derivatives Chemical class 0.000 description 10
150000003467 sulfuric acid derivatives Chemical class 0.000 description 10
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239000000945 filler Substances 0.000 description 9
239000011734 sodium Substances 0.000 description 9
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DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 8
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HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
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QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 4
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150000007524 organic acids Chemical class 0.000 description 4
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Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Epidemiology (AREA)
Physical Education & Sports Medicine (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Orthopedic Medicine & Surgery (AREA)
Rheumatology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

JP2002508431A 2000-07-06 2001-06-29 ビスホスホネート、エストロゲン剤および所望によるエストロゲンの組み合わせ Pending JP2004502730A (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US21606900P	2000-07-06	2000-07-06
US21618800P	2000-07-06	2000-07-06
PCT/US2001/020970 WO2002003976A2 (fr)	2000-07-06	2001-06-29	Combinaisons de bisphosphonates, de substances a action oestrogenique et eventuellement d'oestrogenes

Publications (1)

Publication Number	Publication Date
JP2004502730A true JP2004502730A (ja)	2004-01-29

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JP2002508431A Pending JP2004502730A (ja)	2000-07-06	2001-06-29	ビスホスホネート、エストロゲン剤および所望によるエストロゲンの組み合わせ

Country Status (8)

Country	Link
EP (1)	EP1299093A2 (fr)
JP (1)	JP2004502730A (fr)
CN (1)	CN1450913A (fr)
AU (1)	AU2001273125A1 (fr)
BR (1)	BR0112364A (fr)
CA (1)	CA2415052A1 (fr)
MX (1)	MXPA02012897A (fr)
WO (1)	WO2002003976A2 (fr)

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WO2002003989A2 (fr) *	2000-07-06	2002-01-17	Wyeth	Therapie permettant d'inhiber l'incontinence du sphincter
US6376486B1 (en)	2000-07-06	2002-04-23	American Home Products Corporation	Methods of inhibiting sphincter incontinence
EP1545206B1 (fr)	2002-07-24	2020-03-04	Children's Hospital Medical Center	Compositions et produits contenant de l'equol enantiomere, et procedes de fabrication
US8668914B2 (en)	2002-07-24	2014-03-11	Brigham Young University	Use of equol for treating skin diseases
US8580846B2 (en)	2002-10-29	2013-11-12	Brigham Young University	Use of equol for ameliorating or preventing neuropsychiatric and neurodegenerative diseases or disorders
CA2504682A1 (fr)	2002-10-29	2004-05-13	Colorado State University Research Foundation	Utilisation d'equol dans le traitement de maladies d'origine androgenique
ES2291749T5 (es)	2002-12-20	2011-07-21	F. Hoffmann-La Roche Ag	Formulación de altas dosis de ibandronato.
US7781478B2 (en)	2004-07-14	2010-08-24	Ptc Therapeutics, Inc.	Methods for treating hepatitis C
KR102710603B1 (ko)	2015-10-01	2024-09-27	올레마 파마슈티컬스 인코포레이티드	테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물
SMT202300018T1 (it)	2015-12-09	2023-03-17	Univ Illinois	Downregolatori del recettore degli estrogeni a base di benzotiofene
CN109790143A (zh)	2016-05-10	2019-05-21	C4医药公司	用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
EP4491236A3 (fr)	2016-05-10	2025-04-02	C4 Therapeutics, Inc.	Dégronimères hétérocycliques pour la dégradation de protéines cibles
EP3454862B1 (fr)	2016-05-10	2024-09-11	C4 Therapeutics, Inc.	Dégronimères spirocycliques pour la dégradation de protéines cibles
CN109641874A (zh)	2016-05-10	2019-04-16	C4医药公司	用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
EP3858835A1 (fr)	2016-07-01	2021-08-04	G1 Therapeutics, Inc.	Agents antiprolifératifs à base de pyrimidine
WO2018081168A2 (fr)	2016-10-24	2018-05-03	The Board Of Trustees Of The University Of Illinois	Répresseurs du récepteur oestrogénique sélectifs mixtes à base de benzothiophène
EP3565558B1 (fr)	2017-01-06	2023-12-06	G1 Therapeutics, Inc.	Polythérapie avec un composé serd et un inhibiteur cdk4/6 pour le traitement du cancer
KR20190117582A (ko)	2017-02-10	2019-10-16	쥐원 쎄라퓨틱스, 인크.	벤조티오펜 에스트로겐 수용체 조정제
EP4717317A2 (fr)	2017-06-20	2026-04-01	C4 Therapeutics, Inc.	Dégrons et dégrons liés à n/o pour dégradation protéique
FI3645001T3 (fi)	2017-06-29	2024-09-25	G1 Therapeutics Inc	Git38:n morfisia muotoja ja niiden valmistusmenetelmiä
CN120698983A (zh)	2018-12-20	2025-09-26	C4医药公司	靶向蛋白降解
MX2022000279A (es)	2019-07-07	2022-02-03	Olema Pharmaceuticals Inc	Regimenes de antagonistas del receptor de estrogeno.
BR112022011827A2 (pt)	2019-12-20	2022-08-30	C4 Therapeutics Inc	Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção
AU2021231898A1 (en)	2020-03-05	2022-10-27	C4 Therapeutics, Inc.	Compounds for targeted degradation of BRD9
EP4192458A4 (fr)	2020-08-05	2024-09-04	C4 Therapeutics, Inc.	Composés pour la dégradation ciblée de ret
WO2022261250A1 (fr)	2021-06-08	2022-12-15	C4 Therapeutics, Inc.	Agents thérapeutiques pour la dégradation de braf mutante
JP2025525917A (ja)	2022-08-03	2025-08-07	ブリストル－マイヤーズスクイブカンパニー	Ｒｅｔタンパク質を調節するための化合物
CN120530116A (zh)	2022-11-04	2025-08-22	百时美施贵宝公司	Ret-ldd蛋白抑制剂
CN120569388A (zh)	2022-11-04	2025-08-29	百时美施贵宝公司	Ret-ldd蛋白降解剂
WO2025006753A2 (fr)	2023-06-30	2025-01-02	Merck Patent Gmbh	Composés hétérobifonctionnels pour la dégradation de la protéine kras

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CA2331318A1 (fr) *	1998-05-15	1999-11-25	James Harrison Pickar	Compositions comprenant des composes a base de 2-phenyl-indole et de formulations d'oestrogenes
ID26890A (id) *	1998-05-15	2001-02-15	American Home Prod	2-fenil-1-(4-(2-aminoetoksi) -benzil)-indol dalam kombinasinya dengan estrogen
US6465445B1 (en) *	1998-06-11	2002-10-15	Endorecherche, Inc.	Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

2001
- 2001-06-29 MX MXPA02012897A patent/MXPA02012897A/es unknown
- 2001-06-29 BR BR0112364-5A patent/BR0112364A/pt not_active Application Discontinuation
- 2001-06-29 EP EP01952365A patent/EP1299093A2/fr not_active Withdrawn
- 2001-06-29 CA CA002415052A patent/CA2415052A1/fr not_active Abandoned
- 2001-06-29 WO PCT/US2001/020970 patent/WO2002003976A2/fr not_active Ceased
- 2001-06-29 AU AU2001273125A patent/AU2001273125A1/en not_active Abandoned
- 2001-06-29 CN CN01815091A patent/CN1450913A/zh active Pending
- 2001-06-29 JP JP2002508431A patent/JP2004502730A/ja active Pending

Also Published As

Publication number	Publication date
AU2001273125A1 (en)	2002-01-21
MXPA02012897A (es)	2003-10-24
WO2002003976A3 (fr)	2003-01-03
WO2002003976A2 (fr)	2002-01-17
CN1450913A (zh)	2003-10-22
EP1299093A2 (fr)	2003-04-09
BR0112364A (pt)	2003-07-29
CA2415052A1 (fr)	2002-01-17

Publication	Publication Date	Title
JP2004502730A (ja)	2004-01-29	ビスホスホネート、エストロゲン剤および所望によるエストロゲンの組み合わせ
JP2004502731A (ja)	2004-01-29	スタチン、エストロゲン剤および所望によるエストロゲンの組み合わせ
WO2002003992A2 (fr)	2002-01-17	Therapie pour degenerescence osseuse en rapport avec une prothese
US6358991B2 (en)	2002-03-19	Methods of treating neuropeptide Y-related conditions
JP2004502729A (ja)	2004-01-29	Ｓｓｒｉおよびエストロゲン剤の組み合わせ
US20020028805A1 (en)	2002-03-07	Methods of inhibiting uterotrophic effects of estrogenic agents
US20020016318A1 (en)	2002-02-07	Methods of treating breast disorders
JP2004502733A (ja)	2004-01-29	エストロゲン剤の医薬組成物
US6509332B2 (en)	2003-01-21	Methods of treating excessive intraocular pressure
WO2002003989A2 (fr)	2002-01-17	Therapie permettant d'inhiber l'incontinence du sphincter
US20020022617A1 (en)	2002-02-21	Methods for increasing nitric oxide synthase activity
US6455568B2 (en)	2002-09-24	Combination therapy for inhibiting sphincter incontinence
US6369051B1 (en)	2002-04-09	Combinations of SSRI and estrogenic agents
US20020028792A1 (en)	2002-03-07	Combinations of bisphosphonates, estrogens and estrogenic agents
US20020019373A1 (en)	2002-02-14	Combinations of bisphosphonates and estrogenic agents
US20020025952A1 (en)	2002-02-28	Combinations of statins, estrogens and estrogenic agents
US6635660B2 (en)	2003-10-21	Methods of inhibiting sphincter incontinence
US20020028800A1 (en)	2002-03-07	Combination therapy for prosthesis-related bone degeneration
US6465454B2 (en)	2002-10-15	Combinations of statins and estrogenic agents
US20020022613A1 (en)	2002-02-21	Methods of treating prosthesis-related bone degeneration
EP1656938A1 (fr)	2006-05-17	Combinaisons d'inhibiteurs spécifiques du recaptage de la sérotonine avec des agents oestrogéniques
HK1089695A (en)	2006-12-08	Combinations of ssri and estrogenic agents