IL105240A - The use of melatonin in the preparation of a drug for the treatment of benign prostatic hyperplasia - Google Patents

The use of melatonin in the preparation of a drug for the treatment of benign prostatic hyperplasia

Info

Publication number: IL105240A
Authority: IL; Israel
Prior art keywords: melatonin; profile; formulation; use according; bph
Prior art date: 1992-04-07

Application number

IL10524093A

Other languages

English (en)

Hebrew (he)

Other versions

IL105240A0 (en

Inventor

Zisapel Nava

Original Assignee

Neurim Pharma 1991

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.)

1992-04-07

Filing date

1993-03-31

Publication date

1999-04-11

1993-03-31 Application filed by Neurim Pharma 1991 filed Critical Neurim Pharma 1991

1993-07-08 Publication of IL105240A0 publication Critical patent/IL105240A0/xx

1997-11-24 Priority to US08/976,508 priority Critical patent/US6048888A/en

1999-04-11 Publication of IL105240A publication Critical patent/IL105240A/en

Links

229960003987 melatonin Drugs 0.000 title claims abstract description 152
YJPIGAIKUZMOQA-UHFFFAOYSA-N Melatonin Natural products COC1=CC=C2N(C(C)=O)C=C(CCN)C2=C1 YJPIGAIKUZMOQA-UHFFFAOYSA-N 0.000 title claims abstract description 145
DRLFMBDRBRZALE-UHFFFAOYSA-N melatonin Chemical compound COC1=CC=C2NC=C(CCNC(C)=O)C2=C1 DRLFMBDRBRZALE-UHFFFAOYSA-N 0.000 title claims abstract description 145
206010004446 Benign prostatic hyperplasia Diseases 0.000 title claims abstract description 27
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QKNYBSVHEMOAJP-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;hydron;chloride Chemical compound Cl.OCC(N)(CO)CO QKNYBSVHEMOAJP-UHFFFAOYSA-N 0.000 description 1
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Epidemiology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Urology & Nephrology (AREA)
Endocrinology (AREA)
Reproductive Health (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

IL10524093A 1992-04-07 1993-03-31 The use of melatonin in the preparation of a drug for the treatment of benign prostatic hyperplasia IL105240A (en)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
US08/976,508 US6048888A (en)	1992-04-07	1997-11-24	Method and pharmaceutical formulation for treating benign prostatic hyperplasia

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US86468492A	1992-04-07	1992-04-07

Publications (2)

Publication Number	Publication Date
IL105240A0 IL105240A0 (en)	1993-07-08
IL105240A true IL105240A (en)	1999-04-11

Family

ID=25343832

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL10524093A IL105240A (en)	1992-04-07	1993-03-31	The use of melatonin in the preparation of a drug for the treatment of benign prostatic hyperplasia

Country Status (11)

Country	Link
US (2)	US5750557A (de)
EP (1)	EP0565296B1 (de)
JP (1)	JPH0640939A (de)
AT (1)	ATE141051T1 (de)
DE (1)	DE69303919T2 (de)
DK (1)	DK0565296T3 (de)
ES (1)	ES2090861T3 (de)
GR (1)	GR3021258T3 (de)
HK (1)	HK1006681A1 (de)
IL (1)	IL105240A (de)
SG (1)	SG41955A1 (de)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
AU2109695A (en)	1994-03-30	1995-10-23	Novartis Ag	Screening method using the rzr receptor family
EP0748627A3 (de) *	1995-06-14	1997-05-21	Lilly Co Eli	Melatoninagonisten zur Behandlung von gutartigen Hyperplasieformen der Prostata
DK0973790T3 (da) *	1997-04-07	2003-09-22	Wyeth Corp	Estra-5(10),7-diener med østrogen aktivitet
PT1272177E (pt) *	2000-01-05	2007-07-11	Neurim Pharma 1991	Método e formulação para o tratamento da resistência aos antihipertensos e condições associadas.
RU2221567C2 (ru) *	2000-08-25	2004-01-20	Санкт-Петербургская медицинская академия последипломного образования	Способ нормализации уровней клеточных факторов роста у мужчин с возрастным андрогенным дефицитом
IL144900A (en) *	2001-08-14	2013-12-31	Neurim Pharma 1991	Melatonin and drugs containing it for use in the treatment of primary insomnia, and the manufacture of those drugs
TWI271402B (en) *	2002-10-15	2007-01-21	Tanabe Seiyaku Co	Large conductance calcium-activated K channel opener
IL155666A (en) *	2003-04-29	2013-12-31	Neurim Pharma 1991	Insomnia treatment
US9119846B2 (en)	2003-04-29	2015-09-01	Neurim Pharmaceuticals (1991) Ltd.	Method and composition for enhancing cognition in alzheimer's patients
MXPA06009377A (es) *	2004-02-20	2007-03-07	Lifescape Biosciences Inc	Composiciones y metodos para regulacion del sueno.
US8940326B2 (en)	2007-03-19	2015-01-27	Vita Sciences Llc	Transdermal patch and method for delivery of vitamin B12
SG11201903829PA (en)	2016-10-31	2019-05-30	Neurim Pharma 1991	Melatonin mini-tablets and method of manufacturing the same
US10849856B2 (en)	2016-10-31	2020-12-01	Neurim Pharmaceuticals Ltd.	Melatonin mini-tablets and method of manufacturing the same
CN114982720B (zh) *	2022-07-26	2024-02-13	贵州省人民医院	一种建立小鼠或大鼠雌雄激素失调型前列腺增生模型的方法
US12274680B2 (en)	2022-09-13	2025-04-15	II George William Creasy	Treatment of benign prostatic hypertrophy with capsinoids

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4600723A (en) *	1983-05-18	1986-07-15	Monash University	Method for minimizing disturbances in circadian rhythms of bodily performance and function
US4654361A (en) *	1986-01-27	1987-03-31	State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University	Method of lowering intraocular pressure using melatonin
EP0330652A1 (de) *	1987-02-13	1989-09-06	GRAZIOSI, Maurizio	System um schuhunterteile atoxisch zu machen
US4855305A (en) *	1987-03-23	1989-08-08	Applied Medical Research	Compositions and methods of effecting contraception utilizing melatonin
GB8727099D0 (en) *	1987-11-19	1987-12-23	Cellena Cell Eng A G	Compositions containing melantonin/homologues
US4945103A (en) *	1989-01-17	1990-07-31	Michael Cohen	Method of treating pre-menstrual syndrome
IN171596B (de)	1989-06-27	1992-11-21	Cohen Michael
ATE181670T1 (de)	1991-05-09	1999-07-15	Neurim Pharma 1991	Melatonin enthaltende arzneimittel
US5196435A (en) *	1991-11-21	1993-03-23	Eli Lilly And Company	Melatonin derivatives and combinations with antiestrogen compounds for treating mammalian breast carcinoma

1993
- 1993-03-31 DK DK93302513.2T patent/DK0565296T3/da active
- 1993-03-31 DE DE69303919T patent/DE69303919T2/de not_active Expired - Fee Related
- 1993-03-31 EP EP93302513A patent/EP0565296B1/de not_active Expired - Lifetime
- 1993-03-31 IL IL10524093A patent/IL105240A/en not_active IP Right Cessation
- 1993-03-31 AT AT93302513T patent/ATE141051T1/de not_active IP Right Cessation
- 1993-03-31 SG SG1995002001A patent/SG41955A1/en unknown
- 1993-03-31 ES ES93302513T patent/ES2090861T3/es not_active Expired - Lifetime
- 1993-04-07 JP JP5080753A patent/JPH0640939A/ja active Pending
- 1993-08-24 US US08/111,014 patent/US5750557A/en not_active Expired - Fee Related
1996
- 1996-10-04 GR GR960402609T patent/GR3021258T3/el unknown
1997
- 1997-11-24 US US08/976,508 patent/US6048888A/en not_active Expired - Fee Related
1998
- 1998-06-23 HK HK98106095A patent/HK1006681A1/en not_active IP Right Cessation

Also Published As

Publication number	Publication date
DK0565296T3 (da)	1996-12-09
DE69303919T2 (de)	1997-01-30
US6048888A (en)	2000-04-11
GR3021258T3 (en)	1997-01-31
ATE141051T1 (de)	1996-08-15
EP0565296B1 (de)	1996-08-07
EP0565296A1 (de)	1993-10-13
SG41955A1 (en)	1997-08-15
JPH0640939A (ja)	1994-02-15
ES2090861T3 (es)	1996-10-16
DE69303919D1 (de)	1996-09-12
US5750557A (en)	1998-05-12
IL105240A0 (en)	1993-07-08
HK1006681A1 (en)	1999-03-12

Legal Events

Date	Code	Title
1999-08-17	FF	Patent granted
2000-02-17	KB	Patent renewed
2003-06-24	KB	Patent renewed
2008-01-06	MM9K	Patent not in force due to non-payment of renewal fees

Publication	Publication Date	Title
EP0565296B1 (de)	1996-08-07	Verwendung von Melatonin zur Herstellung eines Arzneimittels zur Behandlung der gutartigen Prostatahyperplasie
Cardinali	1981	Melatonin. A mammalian pineal hormone
Frye et al.	2000	Anti-seizure effects of progesterone and 3α, 5α-THP in kainic acid and perforant pathway models of epilepsy
Preslock	1984	The pineal gland: basic implications and clinical correlations
Pang et al.	2020	Melatonin secretion and its rhythms in biological fluids
Traish et al.	2003	Effects of medical or surgical castration on erectile function in an animal model
HK1006681B (en)	1999-03-12	Use of melatonin for the manufacture of a medicament for the treatment of benign prostatic hyperplasia
US5877183A (en)	1999-03-02	Treatment of lipid and glucose metabolism disorders with dopamine and serotonin agonists
US6855707B2 (en)	2005-02-15	Method for the treatment of lipid and glucose metabolism disorders
DK170513B1 (da)	1995-10-09	Topiske præparater omfattende melatoninforbindelser samt anvendelsen af disse
US5792748A (en)	1998-08-11	Method for inhibiting neoplastic disease in mammals
EP0934069A1 (de)	1999-08-11	Verfahren und zusammensetzung zur behandlung von stoerungen des fett- und glukosemetabolismus
Masson-Pévet et al.	2004	Seasonality and melatonin receptors in the pars tuberalis in some long day breeders
WO1987000432A2 (en)	1987-01-29	Use of melatonin or related compounds for the treatment of psoriasis
Hastings et al.	1985	Melatonin and the brain in photoperiodic mammals
Jonakait et al.	1981	Elevation of maternal glucocorticoid hormones alters neurotransmitter phenotypic expression in embryos
Bagdy et al.	1991	Circadian patterns of plasma immunoreactive corticotropin, beta-endorphin, corticosterone and prolactin after immunoneutralization of corticotropin-releasing hormone
WO1997046239A1 (en)	1997-12-11	Treatment of lipid and glucose metabolism disorders with dopamine and serotonin agonists
JP2007291139A (ja)	2007-11-08	脂質及びグルコースの代謝疾患治療剤及び組成物
Kumanov et al.	2005	Altered melatonin secretion in hypogonadal men: clinical evidence
Salzman et al.	1987	Treatment of experimental spinal trauma with thyrotropin-releasing hormone: central serotonergic and vascular mechanisms of action
Gibbs et al.	2006	Effects of Long‐Term Hormone Treatment and of Tibolone on Monoamines and Monoamine Metabolites in the Brains of Ovariectomised, Cynomologous Monkeys
EP3773599A1 (de)	2021-02-17	Gaba-a antagonisten zur behandlung von entzugsstörungen
Claustrat	2013	Melatonin: an introduction to its physiological and pharmacological effects in humans
Dejana et al.	2021	Challenges in Establishing a Relevant Model of Polycystic Ovary Syndrome in Rats–A Mini Review