SK36397A3 - Use of aromatase inhibitors in the preparation of a drug for treating a relative androgen deficiency in men - Google Patents
Use of aromatase inhibitors in the preparation of a drug for treating a relative androgen deficiency in men Download PDFInfo
- Publication number
- SK36397A3 SK36397A3 SK363-97A SK36397A SK36397A3 SK 36397 A3 SK36397 A3 SK 36397A3 SK 36397 A SK36397 A SK 36397A SK 36397 A3 SK36397 A3 SK 36397A3
- Authority
- SK
- Slovakia
- Prior art keywords
- men
- testosterone
- androgen
- aromatase inhibitors
- estrogen
- Prior art date
Links
- 239000003886 aromatase inhibitor Substances 0.000 title claims abstract description 29
- 206010002261 Androgen deficiency Diseases 0.000 title claims abstract description 15
- 239000003814 drug Substances 0.000 title claims abstract description 8
- 229940046844 aromatase inhibitors Drugs 0.000 title abstract description 18
- 229940079593 drug Drugs 0.000 title abstract 3
- PEPMWUSGRKINHX-TXTPUJOMSA-N atamestane Chemical compound C1C[C@@H]2[C@@]3(C)C(C)=CC(=O)C=C3CC[C@H]2[C@@H]2CCC(=O)[C@]21C PEPMWUSGRKINHX-TXTPUJOMSA-N 0.000 claims abstract description 6
- 229950004810 atamestane Drugs 0.000 claims abstract description 5
- OSVMTWJCGUFAOD-KZQROQTASA-N formestane Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1O OSVMTWJCGUFAOD-KZQROQTASA-N 0.000 claims abstract description 5
- CLPFFLWZZBQMAO-UHFFFAOYSA-N 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1C1N2C=NC=C2CCC1 CLPFFLWZZBQMAO-UHFFFAOYSA-N 0.000 claims abstract description 3
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims abstract description 3
- 229940078010 arimidex Drugs 0.000 claims abstract description 3
- 229960003881 letrozole Drugs 0.000 claims abstract description 3
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims abstract description 3
- XLMPPFTZALNBFS-INIZCTEOSA-N vorozole Chemical compound C1([C@@H](C2=CC=C3N=NN(C3=C2)C)N2N=CN=C2)=CC=C(Cl)C=C1 XLMPPFTZALNBFS-INIZCTEOSA-N 0.000 claims abstract description 3
- 229960004421 formestane Drugs 0.000 claims abstract 2
- 238000011282 treatment Methods 0.000 claims description 17
- 229940122815 Aromatase inhibitor Drugs 0.000 claims description 11
- 238000004519 manufacturing process Methods 0.000 claims description 8
- -1 Pentrozole Chemical compound 0.000 claims description 2
- 229950011548 fadrozole Drugs 0.000 claims description 2
- CWRVKFFCRWGWCS-UHFFFAOYSA-N Pentrazole Chemical compound C1CCCCC2=NN=NN21 CWRVKFFCRWGWCS-UHFFFAOYSA-N 0.000 abstract 1
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 58
- 229960003604 testosterone Drugs 0.000 description 29
- 239000003098 androgen Substances 0.000 description 27
- 229940011871 estrogen Drugs 0.000 description 21
- 239000000262 estrogen Substances 0.000 description 21
- 230000007423 decrease Effects 0.000 description 15
- 210000002966 serum Anatomy 0.000 description 12
- 230000000694 effects Effects 0.000 description 10
- 229940046836 anti-estrogen Drugs 0.000 description 8
- 230000001833 anti-estrogenic effect Effects 0.000 description 8
- 239000000328 estrogen antagonist Substances 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 7
- 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 description 6
- 229960005309 estradiol Drugs 0.000 description 6
- 229930182833 estradiol Natural products 0.000 description 6
- 102000014654 Aromatase Human genes 0.000 description 4
- 108010078554 Aromatase Proteins 0.000 description 4
- 239000000902 placebo Substances 0.000 description 4
- 229940068196 placebo Drugs 0.000 description 4
- 206010060862 Prostate cancer Diseases 0.000 description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 3
- 229940030486 androgens Drugs 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 230000003054 hormonal effect Effects 0.000 description 3
- 230000007774 longterm Effects 0.000 description 3
- 230000004060 metabolic process Effects 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 230000002829 reductive effect Effects 0.000 description 3
- 150000003431 steroids Chemical class 0.000 description 3
- 150000003515 testosterones Chemical class 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 description 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 description 2
- 230000002411 adverse Effects 0.000 description 2
- 230000032683 aging Effects 0.000 description 2
- 230000002280 anti-androgenic effect Effects 0.000 description 2
- 239000000051 antiandrogen Substances 0.000 description 2
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 230000018109 developmental process Effects 0.000 description 2
- 230000001076 estrogenic effect Effects 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000000366 juvenile effect Effects 0.000 description 2
- 230000002045 lasting effect Effects 0.000 description 2
- 238000011866 long-term treatment Methods 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 230000001568 sexual effect Effects 0.000 description 2
- 230000003637 steroidlike Effects 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 230000002381 testicular Effects 0.000 description 2
- DKVSUQWCZQBWCP-QAGGRKNESA-N (8R,9S,10R,13S,14S)-10,13-dimethyl-9,10,11,12,13,14,15,16-octahydro-3H-cyclopenta[alpha]phenanthrene-3,17(8H)-dione Natural products O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3C=CC2=C1 DKVSUQWCZQBWCP-QAGGRKNESA-N 0.000 description 1
- YEWSFUFGMDJFFG-QAGGRKNESA-N (8r,9s,10r,13s,14s)-10,13-dimethyl-2,8,9,11,12,14,15,16-octahydro-1h-cyclopenta[a]phenanthrene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3C=CC2=C1 YEWSFUFGMDJFFG-QAGGRKNESA-N 0.000 description 1
- YEWSFUFGMDJFFG-UHFFFAOYSA-N (9beta,10alpha)-Androsta-4,6-diene-3,17-dione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3C=CC2=C1 YEWSFUFGMDJFFG-UHFFFAOYSA-N 0.000 description 1
- HVZFAUANDOETNZ-UHFFFAOYSA-N 4-[cyano-phenyl-(1,2,4-triazol-1-yl)methyl]benzonitrile Chemical compound C1=CC(C#N)=CC=C1C(C#N)(N1N=CN=C1)C1=CC=CC=C1 HVZFAUANDOETNZ-UHFFFAOYSA-N 0.000 description 1
- OSVMTWJCGUFAOD-UHFFFAOYSA-N 4-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthrene-3,17-dione Chemical compound O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1O OSVMTWJCGUFAOD-UHFFFAOYSA-N 0.000 description 1
- RLJHZHFTUDAXCF-UHFFFAOYSA-N 5-[cyclopentylidene(imidazol-1-yl)methyl]thiophene-2-carbonitrile Chemical compound S1C(C#N)=CC=C1C(N1C=NC=C1)=C1CCCC1 RLJHZHFTUDAXCF-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 229910002012 Aerosil® Inorganic materials 0.000 description 1
- 240000001851 Artemisia dracunculus Species 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 108010044091 Globulins Proteins 0.000 description 1
- 102000006395 Globulins Human genes 0.000 description 1
- 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 1
- LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 108010089417 Sex Hormone-Binding Globulin Proteins 0.000 description 1
- 102100030758 Sex hormone-binding globulin Human genes 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000001548 androgenic effect Effects 0.000 description 1
- 229960003473 androstanolone Drugs 0.000 description 1
- 229960005471 androstenedione Drugs 0.000 description 1
- 230000008687 biosynthesis inhibition Effects 0.000 description 1
- 230000037182 bone density Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 229940097647 casodex Drugs 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- RGLYKWWBQGJZGM-ISLYRVAYSA-N diethylstilbestrol Chemical compound C=1C=C(O)C=CC=1C(/CC)=C(\CC)C1=CC=C(O)C=C1 RGLYKWWBQGJZGM-ISLYRVAYSA-N 0.000 description 1
- 229960000452 diethylstilbestrol Drugs 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 102000015694 estrogen receptors Human genes 0.000 description 1
- 108010038795 estrogen receptors Proteins 0.000 description 1
- 230000008713 feedback mechanism Effects 0.000 description 1
- 208000000509 infertility Diseases 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 231100000535 infertility Toxicity 0.000 description 1
- LRDFRRGEGBBSRN-UHFFFAOYSA-N isobutyronitrile Chemical compound CC(C)C#N LRDFRRGEGBBSRN-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 229940126601 medicinal product Drugs 0.000 description 1
- UXYRZJKIQKRJCF-TZPFWLJSSA-N mesterolone Chemical compound C1C[C@@H]2[C@@]3(C)[C@@H](C)CC(=O)C[C@@H]3CC[C@H]2[C@@H]2CC[C@H](O)[C@]21C UXYRZJKIQKRJCF-TZPFWLJSSA-N 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000036314 physical performance Effects 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 230000001817 pituitary effect Effects 0.000 description 1
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- AOJFQRQNPXYVLM-UHFFFAOYSA-N pyridine hydrochloride Substances [Cl-].C1=CC=[NH+]C=C1 AOJFQRQNPXYVLM-UHFFFAOYSA-N 0.000 description 1
- 239000003087 receptor blocking agent Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000003270 steroid hormone Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229960001603 tamoxifen Drugs 0.000 description 1
- 229960005353 testolactone Drugs 0.000 description 1
- BPEWUONYVDABNZ-DZBHQSCQSA-N testolactone Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(OC(=O)CC4)[C@@H]4[C@@H]3CCC2=C1 BPEWUONYVDABNZ-DZBHQSCQSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4435368A DE4435368A1 (de) | 1994-09-22 | 1994-09-22 | Verwendung von Aromatasehemmern zur Herstellung eines Arzneimittels zur Behandlung eines relativen Androgenmangels beim Mann |
| PCT/EP1995/003733 WO1996009057A1 (de) | 1994-09-22 | 1995-09-22 | Verwendung von aromatasehemmern zur herstellung eines arzneimittels zur behandlung eines relativen androgenmangels beim mann |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK36397A3 true SK36397A3 (en) | 1997-08-06 |
Family
ID=6529877
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK363-97A SK36397A3 (en) | 1994-09-22 | 1995-09-22 | Use of aromatase inhibitors in the preparation of a drug for treating a relative androgen deficiency in men |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US5861389A (sv) |
| EP (1) | EP0782450B1 (sv) |
| JP (1) | JPH10505848A (sv) |
| KR (1) | KR100387345B1 (sv) |
| CN (1) | CN1104243C (sv) |
| AT (1) | ATE241989T1 (sv) |
| AU (1) | AU707997B2 (sv) |
| BR (1) | BR9509155A (sv) |
| CA (1) | CA2200195C (sv) |
| CZ (1) | CZ76097A3 (sv) |
| DE (2) | DE4435368A1 (sv) |
| DK (1) | DK0782450T3 (sv) |
| ES (1) | ES2199255T3 (sv) |
| FI (1) | FI971207A0 (sv) |
| HU (1) | HUT76981A (sv) |
| MX (1) | MX9702170A (sv) |
| NO (1) | NO971349L (sv) |
| PL (1) | PL182909B1 (sv) |
| PT (1) | PT782450E (sv) |
| SK (1) | SK36397A3 (sv) |
| WO (1) | WO1996009057A1 (sv) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19610645A1 (de) | 1996-03-06 | 1997-09-11 | Schering Ag | Kombination von Dehydroepiandrosteron und Aromatasehemmern und Verwendung dieser Kombination zur Herstellung eines Arzeimittels zur Behandlung eines relativen und absoluten Androgenmangels beim Mann |
| US5972921A (en) * | 1997-12-12 | 1999-10-26 | Hormos Medical Oy Ltd. | Use of an aromatase inhibitor in the treatment of decreased androgen to estrogen ratio and detrusor urethral sphincter dyssynergia in men |
| CA2409647C (en) | 2000-05-26 | 2012-07-03 | Harry Fisch | Methods of treating androgen deficiency in men using selective antiestrogens |
| US7067557B2 (en) * | 2000-05-26 | 2006-06-27 | Harry Fisch | Methods of treating androgen deficiency in men using selective antiestrogens |
| US7547728B2 (en) * | 2001-12-06 | 2009-06-16 | University Of Tennessee Research Foundation | Treating muscle wasting with selective androgen receptor modulators |
| US6607755B2 (en) * | 2001-06-21 | 2003-08-19 | Michael Donald Farley | Anti-aromatase pharmaceutical composition for controlling testosterone/estrone ratios |
| WO2003005954A2 (en) * | 2001-07-09 | 2003-01-23 | Zonagen, Inc. | Methods and materials for the treatment of testosterone deficiency in men |
| US7173064B2 (en) * | 2001-07-09 | 2007-02-06 | Repros Therapeutics Inc. | Methods and compositions with trans-clomiphene for treating wasting and lipodystrophy |
| US7737185B2 (en) * | 2001-07-09 | 2010-06-15 | Repros Therapeutics Inc. | Methods and compositions with trans-clomiphene |
| US6586417B1 (en) | 2002-04-22 | 2003-07-01 | Nutrisport Pharmacal, Inc. | Ester and ether derivatives of 4-hydroxy 4-androstene-3,17-dione and a method for the regulation of athletic function in humans |
| AU2003203010A1 (en) * | 2003-01-13 | 2004-08-13 | Michael Donald Farley | Improvements in or relating to anti-aromatase composition |
| EP1624863A1 (en) * | 2003-01-13 | 2006-02-15 | Michael Farley | Improvements in or relating to anti-aromatase composition |
| US20040248989A1 (en) | 2003-06-05 | 2004-12-09 | Risto Santti | Method for the treatment or prevention of lower urinary tract symptoms |
| MX2007000050A (es) * | 2004-07-14 | 2007-07-10 | Repros Therapeutics Inc | Trans-clomifeno para el tratamiento de hipertrofia de prostata benigna, cancer de prostata, hipogonadismo, trigliceridos elevados y colesterol elevado. |
| PL219509B1 (pl) * | 2005-02-04 | 2015-05-29 | Repros Therapeutics Inc | Zastosowanie kompozycji zawierającej trans-klomifen |
| WO2006102232A2 (en) * | 2005-03-22 | 2006-09-28 | Repros Therapeutics Inc. | Dosing regimes for trans-clomiphene |
| WO2007135547A2 (en) | 2006-05-22 | 2007-11-29 | Hormos Medical Ltd. | Selective estrogen receptor modulators or aromatase inhibitors for treating chronic nonbacterial prostatitis |
| NZ585389A (en) | 2007-10-16 | 2011-10-28 | Repros Therapeutics Inc | Trans-clomiphene for metabolic syndrome |
| WO2009066712A1 (ja) * | 2007-11-21 | 2009-05-28 | Kracie Pharma, Ltd. | アロマターゼ阻害剤 |
| US20090215733A1 (en) * | 2008-02-26 | 2009-08-27 | Michael Charles Scally | Therapy for the prophylaxis or treatment of adverse body composition changes and/or decreased muscle strength after androgen or gnrh analogue intake |
| WO2011016814A1 (en) * | 2009-08-07 | 2011-02-10 | Kneller Bruce W | 5α-ANDROSTANE-3,6,17-TRIONE (KNELLER'S TRIONE) AND METHODS OF USE THEREFOR |
| US20090306031A1 (en) * | 2009-08-07 | 2009-12-10 | Kneller Bruce W | 5alpha-ANDROSTANE-3,6,17-TRIONE (KNELLER'S TRIONE) AND METHODS OF USE THEREFOR |
| UA113291C2 (xx) | 2011-08-04 | 2017-01-10 | Метаболіти транскломіфену і їх застосування | |
| WO2013020215A1 (en) * | 2011-08-09 | 2013-02-14 | Adams Kenneth W | Use of aromatase inhibitor or estrogen blocker for increasing spermatogenesis or testosterone levels in males |
| AU2012304693B2 (en) * | 2011-09-08 | 2016-03-31 | Mereo Biopharma 2 Limited | Use of an aromatase inhibitor for the treatment of hypogonadism and related diseases |
| CN102641502A (zh) * | 2012-04-25 | 2012-08-22 | 中国农业大学 | 芳香酶抑制剂的新用途 |
| US9687458B2 (en) | 2012-11-02 | 2017-06-27 | Repros Therapeutics Inc. | Trans-clomiphene for use in cancer therapy |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4289762A (en) * | 1980-06-27 | 1981-09-15 | Merrell Dow Pharmaceuticals Inc. | 10-(1,2-Propadienyl) steroids as irreversible aromatase inhibitors |
| US4322416A (en) * | 1980-06-27 | 1982-03-30 | Merrell Dow Pharmaceuticals Inc. | 10-Alkynyl steroids |
| EP0100566B1 (en) * | 1982-07-14 | 1986-02-19 | Akzo N.V. | Novel 19-thio-androstane derivatives |
| DE3322285A1 (de) * | 1983-06-18 | 1984-12-20 | Schering AG, 1000 Berlin und 4709 Bergkamen | 1-alkyl-androsta-1,4-dien-3,17-dione, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3539244A1 (de) * | 1985-11-01 | 1987-05-07 | Schering Ag | 1-methyl-15(alpha)-alkyl-androsta- 1,4-dien-3,17-dione, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| GB8531745D0 (en) * | 1985-12-24 | 1986-02-05 | Erba Farmitalia | 10beta-alkynyl-4-9(11)-estradiene derivatives |
| GB8615092D0 (en) * | 1986-06-20 | 1986-07-23 | Erba Farmitalia | Androst-4-ene-317-diones |
| DE3705990A1 (de) * | 1987-02-20 | 1988-09-01 | Schering Ag | 1-methyl-15(alpha)-(1-oxyalkyl)-androsta-1,4-dien- 3,17-dione, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3926365A1 (de) * | 1989-08-04 | 1991-02-07 | Schering Ag | Cycloalkylenazole, verfahren zu deren herstellung, pharmazeutische praeparate, die diese enthalten sowie ihre verwendung zur herstellung von arzneimitteln |
| GB9226620D0 (en) * | 1992-12-21 | 1993-02-17 | Fujisawa Pharmaceutical Co | A new compound fr 901537,production thereof and use thereof |
-
1994
- 1994-09-22 DE DE4435368A patent/DE4435368A1/de not_active Withdrawn
-
1995
- 1995-09-22 CA CA002200195A patent/CA2200195C/en not_active Expired - Fee Related
- 1995-09-22 CZ CZ97760A patent/CZ76097A3/cs unknown
- 1995-09-22 WO PCT/EP1995/003733 patent/WO1996009057A1/de not_active Application Discontinuation
- 1995-09-22 AU AU36518/95A patent/AU707997B2/en not_active Ceased
- 1995-09-22 CN CN95195216A patent/CN1104243C/zh not_active Expired - Fee Related
- 1995-09-22 BR BR9509155A patent/BR9509155A/pt not_active Application Discontinuation
- 1995-09-22 ES ES95934094T patent/ES2199255T3/es not_active Expired - Lifetime
- 1995-09-22 DK DK95934094T patent/DK0782450T3/da active
- 1995-09-22 SK SK363-97A patent/SK36397A3/sk unknown
- 1995-09-22 KR KR1019970701850A patent/KR100387345B1/ko not_active IP Right Cessation
- 1995-09-22 EP EP95934094A patent/EP0782450B1/de not_active Expired - Lifetime
- 1995-09-22 US US08/809,582 patent/US5861389A/en not_active Expired - Fee Related
- 1995-09-22 JP JP8510608A patent/JPH10505848A/ja active Pending
- 1995-09-22 PL PL95319299A patent/PL182909B1/pl not_active IP Right Cessation
- 1995-09-22 HU HU9701697A patent/HUT76981A/hu unknown
- 1995-09-22 AT AT95934094T patent/ATE241989T1/de not_active IP Right Cessation
- 1995-09-22 PT PT95934094T patent/PT782450E/pt unknown
- 1995-09-22 DE DE59510714T patent/DE59510714D1/de not_active Expired - Fee Related
- 1995-09-22 MX MX9702170A patent/MX9702170A/es not_active IP Right Cessation
-
1997
- 1997-03-21 FI FI971207A patent/FI971207A0/sv not_active IP Right Cessation
- 1997-03-21 NO NO971349A patent/NO971349L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2199255T3 (es) | 2004-02-16 |
| CA2200195C (en) | 2008-04-22 |
| AU3651895A (en) | 1996-04-09 |
| WO1996009057A1 (de) | 1996-03-28 |
| ATE241989T1 (de) | 2003-06-15 |
| PL319299A1 (en) | 1997-08-04 |
| DK0782450T3 (da) | 2003-08-18 |
| CZ76097A3 (en) | 1997-07-16 |
| EP0782450B1 (de) | 2003-06-04 |
| JPH10505848A (ja) | 1998-06-09 |
| FI971207A (sv) | 1997-03-21 |
| NO971349L (no) | 1997-05-16 |
| DE4435368A1 (de) | 1996-03-28 |
| CN1104243C (zh) | 2003-04-02 |
| KR100387345B1 (ko) | 2003-08-30 |
| EP0782450A1 (de) | 1997-07-09 |
| BR9509155A (pt) | 1997-10-14 |
| CN1158570A (zh) | 1997-09-03 |
| AU707997B2 (en) | 1999-07-29 |
| DE59510714D1 (de) | 2003-07-10 |
| FI971207A0 (sv) | 1997-03-21 |
| CA2200195A1 (en) | 1996-03-28 |
| US5861389A (en) | 1999-01-19 |
| MX9702170A (es) | 1998-04-30 |
| KR970706002A (ko) | 1997-11-03 |
| HUT76981A (hu) | 1998-01-28 |
| PT782450E (pt) | 2003-09-30 |
| NO971349D0 (no) | 1997-03-21 |
| PL182909B1 (pl) | 2002-04-30 |
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