IL126345A - For bormeloxifene crystalline pomarate - Google Patents

For bormeloxifene crystalline pomarate

Info

Publication number: IL126345A
Authority: IL; Israel
Prior art keywords: phenyl; crystalline; trans; pyrrolidin; methoxy
Prior art date: 1996-05-08

Application number

IL12634597A

Other languages

English (en)

Hebrew (he)

Other versions

IL126345A0 (en

Original Assignee

Novo Nordisk As

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.)

1996-05-08

Filing date

1997-05-07

Publication date

2001-07-24

1997-05-07 Application filed by Novo Nordisk As filed Critical Novo Nordisk As

1999-05-09 Publication of IL126345A0 publication Critical patent/IL126345A0/xx

2001-07-24 Publication of IL126345A publication Critical patent/IL126345A/en

Links

CKDZFQCZLXNLRD-JJGRXVLVSA-N (e)-but-2-enedioic acid;1-[2-[4-[(3r,4r)-7-methoxy-2,2-dimethyl-3-phenyl-3,4-dihydrochromen-4-yl]phenoxy]ethyl]pyrrolidine Chemical compound OC(=O)\C=C\C(O)=O.C1([C@H]2[C@@H](C3=CC=C(C=C3OC2(C)C)OC)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 CKDZFQCZLXNLRD-JJGRXVLVSA-N 0.000 title description 6
150000001875 compounds Chemical class 0.000 claims description 17
VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 14
VZCYOOQTPOCHFL-OWOJBTEDSA-M fumarate(1-) Chemical compound OC(=O)\C=C\C([O-])=O VZCYOOQTPOCHFL-OWOJBTEDSA-M 0.000 claims description 13
238000000034 method Methods 0.000 claims description 12
125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 11
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
239000008194 pharmaceutical composition Substances 0.000 claims description 10
206010065687 Bone loss Diseases 0.000 claims description 9
238000002360 preparation method Methods 0.000 claims description 8
150000003839 salts Chemical class 0.000 claims description 8
239000002904 solvent Substances 0.000 claims description 6
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 6
239000003085 diluting agent Substances 0.000 claims description 5
239000003814 drug Substances 0.000 claims description 5
239000003937 drug carrier Substances 0.000 claims description 4
239000001530 fumaric acid Substances 0.000 claims description 4
208000001132 Osteoporosis Diseases 0.000 claims description 3
230000002265 prevention Effects 0.000 claims description 3
210000000988 bone and bone Anatomy 0.000 claims 1
229910052739 hydrogen Inorganic materials 0.000 abstract description 3
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract description 2
239000001257 hydrogen Substances 0.000 abstract description 2
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 16
239000000203 mixture Substances 0.000 description 12
239000000243 solution Substances 0.000 description 11
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 6
239000003826 tablet Substances 0.000 description 6
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 5
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 4
239000002775 capsule Substances 0.000 description 4
238000001914 filtration Methods 0.000 description 4
229950002728 levormeloxifene Drugs 0.000 description 4
239000000725 suspension Substances 0.000 description 4
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 3
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
BTANRVKWQNVYAZ-UHFFFAOYSA-N butan-2-ol Chemical compound CCC(C)O BTANRVKWQNVYAZ-UHFFFAOYSA-N 0.000 description 3
239000001506 calcium phosphate Substances 0.000 description 3
239000013078 crystal Substances 0.000 description 3
239000003995 emulsifying agent Substances 0.000 description 3
-1 fatty acid monoglycerides Chemical class 0.000 description 3
238000009472 formulation Methods 0.000 description 3
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 description 3
239000000546 pharmaceutical excipient Substances 0.000 description 3
239000003755 preservative agent Substances 0.000 description 3
239000000126 substance Substances 0.000 description 3
239000000454 talc Substances 0.000 description 3
235000012222 talc Nutrition 0.000 description 3
229910052623 talc Inorganic materials 0.000 description 3
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
201000009273 Endometriosis Diseases 0.000 description 2
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
229920002472 Starch Polymers 0.000 description 2
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
239000011230 binding agent Substances 0.000 description 2
230000000740 bleeding effect Effects 0.000 description 2
239000000872 buffer Substances 0.000 description 2
235000011010 calcium phosphates Nutrition 0.000 description 2
239000000969 carrier Substances 0.000 description 2
239000004359 castor oil Substances 0.000 description 2
235000019438 castor oil Nutrition 0.000 description 2
HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
238000004040 coloring Methods 0.000 description 2
238000013270 controlled release Methods 0.000 description 2
238000007796 conventional method Methods 0.000 description 2
238000001816 cooling Methods 0.000 description 2
235000014113 dietary fatty acids Nutrition 0.000 description 2
239000002552 dosage form Substances 0.000 description 2
230000002500 effect on skin Effects 0.000 description 2
230000000694 effects Effects 0.000 description 2
239000000839 emulsion Substances 0.000 description 2
239000000194 fatty acid Substances 0.000 description 2
229930195729 fatty acid Natural products 0.000 description 2
239000012458 free base Substances 0.000 description 2
ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 2
ZSIAUFGUXNUGDI-UHFFFAOYSA-N hexan-1-ol Chemical compound CCCCCCO ZSIAUFGUXNUGDI-UHFFFAOYSA-N 0.000 description 2
239000007943 implant Substances 0.000 description 2
230000002401 inhibitory effect Effects 0.000 description 2
239000008101 lactose Substances 0.000 description 2
239000007788 liquid Substances 0.000 description 2
235000019359 magnesium stearate Nutrition 0.000 description 2
239000000463 material Substances 0.000 description 2
BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 2
239000003921 oil Substances 0.000 description 2
235000019198 oils Nutrition 0.000 description 2
230000003287 optical effect Effects 0.000 description 2
239000007787 solid Substances 0.000 description 2
238000001179 sorption measurement Methods 0.000 description 2
239000003381 stabilizer Substances 0.000 description 2
239000008107 starch Substances 0.000 description 2
235000019698 starch Nutrition 0.000 description 2
239000006188 syrup Substances 0.000 description 2
235000020357 syrup Nutrition 0.000 description 2
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical class [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 2
239000000080 wetting agent Substances 0.000 description 2
CMIBUZBMZCBCAT-HOTGVXAUSA-N (2s,3s)-2,3-bis[(4-methylbenzoyl)oxy]butanedioic acid Chemical compound C1=CC(C)=CC=C1C(=O)O[C@H](C(O)=O)[C@@H](C(O)=O)OC(=O)C1=CC=C(C)C=C1 CMIBUZBMZCBCAT-HOTGVXAUSA-N 0.000 description 1
DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 description 1
FXNSRODXMVUCNJ-TYYBGVCCSA-N (e)-but-2-enedioic acid;hydrochloride Chemical compound Cl.OC(=O)\C=C\C(O)=O FXNSRODXMVUCNJ-TYYBGVCCSA-N 0.000 description 1
WMJNKBXKYHXOHC-UHFFFAOYSA-N 2,3-dihydroxy-2,3-bis(2-methylbenzoyl)butanedioic acid Chemical compound CC1=CC=CC=C1C(=O)C(O)(C(O)=O)C(O)(C(O)=O)C(=O)C1=CC=CC=C1C WMJNKBXKYHXOHC-UHFFFAOYSA-N 0.000 description 1
OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 1
229920001817 Agar Polymers 0.000 description 1
208000024827 Alzheimer disease Diseases 0.000 description 1
229920000856 Amylose Polymers 0.000 description 1
201000001320 Atherosclerosis Diseases 0.000 description 1
206010003694 Atrophy Diseases 0.000 description 1
208000006386 Bone Resorption Diseases 0.000 description 1
206010006187 Breast cancer Diseases 0.000 description 1
208000026310 Breast neoplasm Diseases 0.000 description 1
235000019739 Dicalciumphosphate Nutrition 0.000 description 1
206010014733 Endometrial cancer Diseases 0.000 description 1
206010014759 Endometrial neoplasm Diseases 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
208000032843 Hemorrhage Diseases 0.000 description 1
241000282412 Homo Species 0.000 description 1
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
206010020584 Hypercalcaemia of malignancy Diseases 0.000 description 1
208000031226 Hyperlipidaemia Diseases 0.000 description 1
201000002980 Hyperparathyroidism Diseases 0.000 description 1
206010020880 Hypertrophy Diseases 0.000 description 1
240000007472 Leucaena leucocephala Species 0.000 description 1
235000010643 Leucaena leucocephala Nutrition 0.000 description 1
206010027304 Menopausal symptoms Diseases 0.000 description 1
NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 description 1
UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 description 1
208000008589 Obesity Diseases 0.000 description 1
208000010191 Osteitis Deformans Diseases 0.000 description 1
208000027868 Paget disease Diseases 0.000 description 1
235000019483 Peanut oil Nutrition 0.000 description 1
206010036049 Polycystic ovaries Diseases 0.000 description 1
239000002202 Polyethylene glycol Substances 0.000 description 1
206010060862 Prostate cancer Diseases 0.000 description 1
235000021355 Stearic acid Nutrition 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
206010046798 Uterine leiomyoma Diseases 0.000 description 1
239000000654 additive Substances 0.000 description 1
239000008272 agar Substances 0.000 description 1
235000010419 agar Nutrition 0.000 description 1
230000002513 anti-ovulatory effect Effects 0.000 description 1
239000008346 aqueous phase Substances 0.000 description 1
239000007864 aqueous solution Substances 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
230000037444 atrophy Effects 0.000 description 1
239000012752 auxiliary agent Substances 0.000 description 1
230000033228 biological regulation Effects 0.000 description 1
208000034158 bleeding Diseases 0.000 description 1
230000024279 bone resorption Effects 0.000 description 1
229910000389 calcium phosphate Inorganic materials 0.000 description 1
CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
235000013539 calcium stearate Nutrition 0.000 description 1
239000008116 calcium stearate Substances 0.000 description 1
OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 1
150000001720 carbohydrates Chemical class 0.000 description 1
235000014633 carbohydrates Nutrition 0.000 description 1
210000000748 cardiovascular system Anatomy 0.000 description 1
230000004663 cell proliferation Effects 0.000 description 1
230000015271 coagulation Effects 0.000 description 1
238000005345 coagulation Methods 0.000 description 1
229940125773 compound 10 Drugs 0.000 description 1
238000002425 crystallisation Methods 0.000 description 1
230000008025 crystallization Effects 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
229940038472 dicalcium phosphate Drugs 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
239000007884 disintegrant Substances 0.000 description 1
238000004090 dissolution Methods 0.000 description 1
239000008298 dragée Substances 0.000 description 1
230000002357 endometrial effect Effects 0.000 description 1
239000000945 filler Substances 0.000 description 1
235000019253 formic acid Nutrition 0.000 description 1
239000000499 gel Substances 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
201000000079 gynecomastia Diseases 0.000 description 1
208000008750 humoral hypercalcemia of malignancy Diseases 0.000 description 1
229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
238000002513 implantation Methods 0.000 description 1
ZLVXBBHTMQJRSX-VMGNSXQWSA-N jdtic Chemical compound C1([C@]2(C)CCN(C[C@@H]2C)C[C@H](C(C)C)NC(=O)[C@@H]2NCC3=CC(O)=CC=C3C2)=CC=CC(O)=C1 ZLVXBBHTMQJRSX-VMGNSXQWSA-N 0.000 description 1
201000010260 leiomyoma Diseases 0.000 description 1
230000006372 lipid accumulation Effects 0.000 description 1
239000002502 liposome Substances 0.000 description 1
230000005923 long-lasting effect Effects 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
208000027202 mammary Paget disease Diseases 0.000 description 1
230000004060 metabolic process Effects 0.000 description 1
210000004400 mucous membrane Anatomy 0.000 description 1
235000020824 obesity Nutrition 0.000 description 1
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
239000004006 olive oil Substances 0.000 description 1
235000008390 olive oil Nutrition 0.000 description 1
239000003960 organic solvent Substances 0.000 description 1
230000003204 osmotic effect Effects 0.000 description 1
230000011164 ossification Effects 0.000 description 1
230000001009 osteoporotic effect Effects 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
239000000312 peanut oil Substances 0.000 description 1
239000001814 pectin Substances 0.000 description 1
235000010987 pectin Nutrition 0.000 description 1
229920001277 pectin Polymers 0.000 description 1
239000000825 pharmaceutical preparation Substances 0.000 description 1
239000012071 phase Substances 0.000 description 1
201000010065 polycystic ovary syndrome Diseases 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
229920001592 potato starch Polymers 0.000 description 1
239000000843 powder Substances 0.000 description 1
210000002307 prostate Anatomy 0.000 description 1
201000001514 prostate carcinoma Diseases 0.000 description 1
238000001953 recrystallisation Methods 0.000 description 1
238000010992 reflux Methods 0.000 description 1
239000012266 salt solution Substances 0.000 description 1
RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
235000012239 silicon dioxide Nutrition 0.000 description 1
210000000329 smooth muscle myocyte Anatomy 0.000 description 1
229910000029 sodium carbonate Inorganic materials 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000000829 suppository Substances 0.000 description 1
238000001356 surgical procedure Methods 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
201000005665 thrombophilia Diseases 0.000 description 1
208000010579 uterine corpus leiomyoma Diseases 0.000 description 1
201000007954 uterine fibroid Diseases 0.000 description 1
239000006213 vaginal ring Substances 0.000 description 1
229940124549 vasodilator Drugs 0.000 description 1
239000003071 vasodilator agent Substances 0.000 description 1
239000003981 vehicle Substances 0.000 description 1
230000003442 weekly effect Effects 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Physical Education & Sports Medicine (AREA)
Pharmacology & Pharmacy (AREA)
General Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Bioinformatics & Cheminformatics (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Orthopedic Medicine & Surgery (AREA)
Rheumatology (AREA)
Obesity (AREA)
Diabetes (AREA)
Hematology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Pyrane Compounds (AREA)
Pyrrole Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

IL12634597A 1996-05-08 1997-05-07 For bormeloxifene crystalline pomarate IL126345A (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
DK55296		1996-05-08
PCT/DK1997/000211 WO1997042184A1 (en)	1996-05-08	1997-05-07	Crystalline (-)-3r,4r-trans-7-methoxy-2,2-dimethyl-3-phenyl-4-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}chromane, hydrogen fumarate

Publications (2)

Publication Number	Publication Date
IL126345A0 IL126345A0 (en)	1999-05-09
IL126345A true IL126345A (en)	2001-07-24

Family

ID=8094838

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL12634597A IL126345A (en)	1996-05-08	1997-05-07	For bormeloxifene crystalline pomarate

Country Status (17)

Country	Link
EP (1)	EP0912543B1 (de)
JP (1)	JP2951410B2 (de)
KR (1)	KR20000010644A (de)
CN (1)	CN1218462A (de)
AT (1)	ATE262516T1 (de)
AU (1)	AU710334B2 (de)
BR (1)	BR9709060A (de)
CA (1)	CA2253284A1 (de)
CZ (1)	CZ359898A3 (de)
DE (1)	DE69728271D1 (de)
HU (1)	HUP9901738A3 (de)
IL (1)	IL126345A (de)
NO (1)	NO985205D0 (de)
PL (1)	PL329624A1 (de)
RU (1)	RU2182149C2 (de)
WO (1)	WO1997042184A1 (de)
ZA (1)	ZA973961B (de)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
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1997
- 1997-05-07 JP JP9539447A patent/JP2951410B2/ja not_active Expired - Fee Related
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- 1997-05-07 AU AU27638/97A patent/AU710334B2/en not_active Ceased
- 1997-05-07 DE DE69728271T patent/DE69728271D1/de not_active Expired - Lifetime
- 1997-05-07 HU HU9901738A patent/HUP9901738A3/hu unknown
- 1997-05-07 KR KR1019980708596A patent/KR20000010644A/ko not_active Ceased
- 1997-05-07 CA CA002253284A patent/CA2253284A1/en not_active Abandoned
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- 1997-05-07 RU RU98121844/04A patent/RU2182149C2/ru not_active IP Right Cessation
- 1997-05-07 BR BR9709060A patent/BR9709060A/pt not_active Application Discontinuation
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- 1997-05-07 WO PCT/DK1997/000211 patent/WO1997042184A1/en not_active Ceased
- 1997-05-07 CN CN97194453A patent/CN1218462A/zh active Pending
- 1997-05-08 ZA ZA9703961A patent/ZA973961B/xx unknown
1998
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Publication number	Publication date
ATE262516T1 (de)	2004-04-15
BR9709060A (pt)	1999-08-03
NO985205L (no)	1998-11-06
JPH11501953A (ja)	1999-02-16
IL126345A0 (en)	1999-05-09
AU710334B2 (en)	1999-09-16
KR20000010644A (ko)	2000-02-25
AU2763897A (en)	1997-11-26
CZ359898A3 (cs)	1999-05-12
CN1218462A (zh)	1999-06-02
PL329624A1 (en)	1999-03-29
DE69728271D1 (en)	2004-04-29
HUP9901738A3 (en)	2000-12-28
JP2951410B2 (ja)	1999-09-20
HUP9901738A2 (en)	2000-07-28
CA2253284A1 (en)	1997-11-13
RU2182149C2 (ru)	2002-05-10
EP0912543B1 (de)	2004-03-24
WO1997042184A1 (en)	1997-11-13
EP0912543A1 (de)	1999-05-06
NO985205D0 (no)	1998-11-06
ZA973961B (en)	1997-12-04

Legal Events

Date	Code	Title
2002-02-10	FF	Patent granted
2002-02-10	KB	Patent renewed
2003-07-06	KB	Patent renewed
2007-07-06	KB	Patent renewed
2011-05-31	KB	Patent renewed
2017-12-31	EXP	Patent expired

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EP1546138B1 (de)	2012-01-18	Raloxifene-l-lactat oder ein hemihydrat davon, deren verwendungen, pharmazeutischen zusammensetzungen und herstellungsverfahren
RU2102392C1 (ru)	1998-01-20	Пиперидилметилзамещенные производные хромана и их соли с неорганическими кислотами
CN102803247B (zh)	2014-11-05	组胺h3受体拮抗剂的新颖富马酸盐
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