HRP20170003T1 - Uporaba inhibitora aromataze za liječenje hipogenadizma i srodnih bolesti - Google Patents
Uporaba inhibitora aromataze za liječenje hipogenadizma i srodnih bolesti Download PDFInfo
- Publication number
- HRP20170003T1 HRP20170003T1 HRP20170003TT HRP20170003T HRP20170003T1 HR P20170003 T1 HRP20170003 T1 HR P20170003T1 HR P20170003T T HRP20170003T T HR P20170003TT HR P20170003 T HRP20170003 T HR P20170003T HR P20170003 T1 HRP20170003 T1 HR P20170003T1
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- Croatia
- Prior art keywords
- compound
- treatment
- dose
- use according
- hypogonadism
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Links
- 206010058359 Hypogonadism Diseases 0.000 title claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 4
- 229940122815 Aromatase inhibitor Drugs 0.000 title 1
- 239000003886 aromatase inhibitor Substances 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 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 claims 8
- 230000003247 decreasing effect Effects 0.000 claims 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 4
- 210000002966 serum Anatomy 0.000 claims 4
- 229960003604 testosterone Drugs 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 3
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 210000003205 muscle Anatomy 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 206010017076 Fracture Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- 206010027940 Mood altered Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 210000000579 abdominal fat Anatomy 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 231100000502 fertility decrease Toxicity 0.000 claims 1
- 230000004153 glucose metabolism Effects 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 201000003368 hypogonadotropic hypogonadism Diseases 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 230000007510 mood change Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008183 oral pharmaceutical preparation Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000036314 physical performance Effects 0.000 claims 1
- 230000002829 reductive effect Effects 0.000 claims 1
- 230000002269 spontaneous effect Effects 0.000 claims 1
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- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4833—Encapsulating processes; Filling of capsules
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Inorganic Chemistry (AREA)
- Psychiatry (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Dermatology (AREA)
- Nutrition Science (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (9)
1. Spoj 4,4’-[fluoro-(1-H-1,2,4-triazol-1-il)metilen]bisbenzonitril za uporabu u liječenju hipogonadizma u muškog subjekta s ukupnom razinom testosterona u serumu ispod 400 ng/dl, gdje spoj dolazi u obliku koji sadrži od oko 0.001 mg do oko 1.0 mg 4,4’-[fluoro-(1-H-1,2,4-triazol-1-il)metilen]bisbenzonitrila po dozi, i gdje je spoj za primjenu prema režimu doziranja u kojem je periodičnost doziranja u rasponu od jedne doze dnevno do jedne doze svakih 60 dana.
2. Spoj za uporabu prema zahtjevu 1, gdje je liječenje za prekomjerno teškog ili pretilog muškog subjekta, poželjno bolesnog muškarca.
3. Spoj za uporabu prema zahtjevu 1 ili 2, gdje je liječenje za hipogonadotropni hipogonadizam.
4. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 3, gdje muški bolesnik ima ukupnu razinu serumskog testosterona ispod 300 ng/dl.
5. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje je spoj za (i) prevenciju ili liječenje jednog ili više poremećaja odabranog između metaboličkih sindroma, dijabetesa tipa II, pretilosti i kardiovaskularne bolesti, (ii) prevenciju ili liječenje jednog ili više poremećaja odabranog između inzulinske rezistencije, intolerancije glukoze i dislipidemije, (iii) poboljšanje osjetljivosti na inzulin i/ili metabolizma glukoze i/ili lipidnog profila, i/ili (iv) prevenciju ili liječenje jednog ili više poremećaja odabranog iz skupine koju čine smanjeni libido, smanjene spontane erekcije, erektilna disfunkcija, smanjena plodnost, gubitak dlaka, smanjeno brijanje, nedostatak energije, umor, kognitivni poremećaj, depresija, promjene raspoloženja, niska gustoća kostiju, povećani rizik od prijeloma, smanjena mišićna masa, smanjena mišićna snaga, povećano abdominalno masno tkivo i ograničeni kapacitet tjelesnih performansi.
6. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje spoj spoj dolazi u obliku koji sadrži od oko 0.005 mg do oko 0.5 mg, najpoželjnije od oko 0.01 mg do oko 0.1 mg, ili od oko 0.005 mg do manje od 0.05 mg 4,4’-[fluoro-(1-H-1,2,4-triazol-1-il)metilen]bisbenzonitrila po dozi.
7. Spoj za uporabu prema bilo kojem od prethodnih zahtjeva, gdje je spoj za primjenu prema režimu doziranja u kojem je periodičnost doziranja od oko jedne doze jednom tjedno.
8. Oralni farmaceutski pripravak koji sadrži od oko 0.001 mg do oko 1.0 mg 4,4’-[fluoro-(1-H-1,2,4-triazol-1-il)metilen]bisbenzonitrila po dozi, po izboru u kombinaciji s jednom ili više farmaceutski prikladnih pomoćnih tvari, za uporabu u liječenju hipogonadizma u muškog bolesnika s ukupnom razinom testosterona u serumu ispod 400 ng/dl, i gdje je pripravak za primjenu prema režimu doziranja u kojem je periodičnost doziranja od jedne doze dnevno do jedne doze svakih 60 dana.
9. Set dijelova za uporabu u liječenju hipogonadizma u muškog bolesnika s ukupnom razinom testosterona u serumu ispod 400 ng/dl, gdje set sadrži:
(i) farmaceutski pripravak koji sadrži oko 0.001 mg do oko 1.0 mg 4,4’-[fluoro-(1-H-1,2,4-triazol-1-il)-metilen]-bisbenzonitrila; zajedno s
(ii) uputama kako primijeniti taj farmaceutski pripravak, gdje upute navode kako se pripravak treba primjenjivati prema režimu doziranja u kojem je periodičnost doziranja u rasponu od jedne doze dnevno do jedne doze svakih 60 dana.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161532459P | 2011-09-08 | 2011-09-08 | |
| US201261638588P | 2012-04-26 | 2012-04-26 | |
| EP12758965.3A EP2753312B1 (en) | 2011-09-08 | 2012-09-06 | Use of an aromatase inhibitor for the treatment of hypogonadism and related diseases |
| PCT/US2012/053844 WO2013036562A1 (en) | 2011-09-08 | 2012-09-06 | Use of an aromatase inhibitor for the treatment of hypogonadism and related diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170003T1 true HRP20170003T1 (hr) | 2017-03-10 |
Family
ID=46846026
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170003TT HRP20170003T1 (hr) | 2011-09-08 | 2017-01-03 | Uporaba inhibitora aromataze za liječenje hipogenadizma i srodnih bolesti |
| HRP20170002TT HRP20170002T1 (hr) | 2011-09-08 | 2017-01-03 | Farmaceutski pripravci koji sadrže inhibitor aromataze |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170002TT HRP20170002T1 (hr) | 2011-09-08 | 2017-01-03 | Farmaceutski pripravci koji sadrže inhibitor aromataze |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US9370505B2 (hr) |
| EP (2) | EP2753312B1 (hr) |
| JP (2) | JP6051467B2 (hr) |
| KR (3) | KR101872561B1 (hr) |
| CN (2) | CN103781476B (hr) |
| AR (1) | AR087790A1 (hr) |
| AU (2) | AU2012304693B2 (hr) |
| BR (2) | BR112014005434B1 (hr) |
| CA (2) | CA2845929C (hr) |
| CL (1) | CL2014000552A1 (hr) |
| CY (2) | CY1118461T1 (hr) |
| DK (2) | DK2753313T3 (hr) |
| ES (2) | ES2613667T3 (hr) |
| HR (2) | HRP20170003T1 (hr) |
| HU (2) | HUE031435T2 (hr) |
| IL (1) | IL231234A (hr) |
| IN (1) | IN2014DN01619A (hr) |
| LT (2) | LT2753313T (hr) |
| MX (2) | MX360315B (hr) |
| PE (1) | PE20141584A1 (hr) |
| PL (2) | PL2753312T3 (hr) |
| PT (2) | PT2753313T (hr) |
| RU (2) | RU2617510C2 (hr) |
| SG (2) | SG2014012132A (hr) |
| SI (2) | SI2753313T1 (hr) |
| TN (1) | TN2014000059A1 (hr) |
| TW (1) | TW201316987A (hr) |
| UY (1) | UY34315A (hr) |
| WO (2) | WO2013036563A1 (hr) |
| ZA (1) | ZA201401040B (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE031435T2 (en) * | 2011-09-08 | 2017-07-28 | Mereo Biopharma 2 Ltd | Pharmaceutical compositions comprising an aromatase inhibitor |
| WO2015148549A1 (en) * | 2014-03-26 | 2015-10-01 | The Regents Of The University Of California | Ultrasensitive androgen receptor bioassay |
| MX2016017315A (es) * | 2014-07-07 | 2017-04-27 | Novartis Ag | Formas de dosificacion farmaceutica. |
| GB201614179D0 (en) * | 2016-08-19 | 2016-10-05 | Mereo Biopharma 2 Ltd | Dosage regimen for the treatment of endometriosis |
| EP3592338A1 (en) * | 2017-03-08 | 2020-01-15 | ARIAD Pharmaceuticals, Inc. | Pharmaceutical formulations comprising 5-chloro-n4 |
| USD894149S1 (en) * | 2018-08-16 | 2020-08-25 | Alibaba Group Holding Limited | Information terminal for payment |
| USD894148S1 (en) * | 2018-08-16 | 2020-08-25 | Alibaba Group Holding Limited | Information terminal for payment |
| JP7121999B2 (ja) * | 2019-09-26 | 2022-08-19 | 学校法人九州文化学園 | 男性性腺機能低下症治療剤 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4749713A (en) | 1986-03-07 | 1988-06-07 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| TW210334B (hr) * | 1990-12-12 | 1993-08-01 | Ciba Geigy Ag | |
| DE4435368A1 (de) * | 1994-09-22 | 1996-03-28 | Schering Ag | Verwendung von Aromatasehemmern zur Herstellung eines Arzneimittels zur Behandlung eines relativen 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 |
| AU2001271162A1 (en) * | 2000-07-05 | 2002-01-14 | Astrazeneca Ab | Pharmaceutical combination of an anti-androgen and letrozole for providing an anit-androgenic effect and aromatase inhibition |
| DK1381431T3 (da) * | 2001-04-17 | 2007-10-08 | Ares Trading Sa | Aromatase-inhibition for at foröge implantationsrate |
| US7101573B2 (en) * | 2001-09-28 | 2006-09-05 | Mcneil-Pcc, Inc. | Simethicone solid oral dosage form |
| US20040235812A1 (en) * | 2002-04-03 | 2004-11-25 | Caspers Robert F | Pharmaceutical composition comprisng an aromatase inhibitor and an estrogen suitable for hormone replacement therapy for a male |
| EP1937251A2 (en) * | 2005-04-25 | 2008-07-02 | Pfizer Products Inc. | Pharmaceutical compositions and methods comprising a combination of a selective estrogen receptor modulator and an aromatase inhibitor |
| CN102335219A (zh) * | 2007-11-21 | 2012-02-01 | 客乐谐制药株式会社 | 芳香酶抑制剂 |
| HUE031435T2 (en) * | 2011-09-08 | 2017-07-28 | Mereo Biopharma 2 Ltd | Pharmaceutical compositions comprising an aromatase inhibitor |
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2012
- 2012-09-06 HU HUE12758966A patent/HUE031435T2/en unknown
- 2012-09-06 WO PCT/US2012/053846 patent/WO2013036563A1/en active Application Filing
- 2012-09-06 US US14/342,813 patent/US9370505B2/en active Active
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