Deutsch English Français

Contact

EP2810938

European procedure

Quick help

Maintenance news

Scheduled maintenance

Regular maintenance outages:
between 05.00 and 05.15 hrs CET (Monday to Sunday).

Other outages
Availability
Register Forum

2022.02.11

More...

News flashes

News flashes

New version of the European Patent Register - SPC information for Unitary Patents.

2024-03-06

More...

Extract from the Register of European Patents

EP About this file: EP2810938

EP2810938 - N-PHENYLPIPERAZINE DERIVATIVES THAT ARE ANTAGONISTS OF A1A, A1D ADRENOCEPTORS AND 5-HT1A RECEPTORS FOR THE TREATMENT OF BENIGN PROSTATE HYPERPLASIA, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME [Right-click to bookmark this link]
Status	The application is deemed to be withdrawn Status updated on 22.07.2016 Database last updated on 26.06.2024
Most recent event Tooltip	22.07.2016	Application deemed to be withdrawn	published on 24.08.2016 [2016/34]
Applicant(s)	For all designated states Universidade Federal Do Rio De Janeiro - UFRJ Av. Pedro Calmon, nº. 550 - 2° Andar Prédio da Reitoria - Illha do Fundão Cidade Universitária 21941-901 Rio De Janeiro - RJ / BR
	For all designated states Uniao Brasiliense de Educacao e Cultura- UBEC SMPW Quadra 5 Conjunto 13, lote 08 71.735-513 Nucleo Bandeirante (Brasilia - DF) / BR
	[2014/50]
Inventor(s)	01 / MARTINS DA SILVA, Claudia Lucia Rua Juraci Camargo 600/901 Jardim Guanabara Rio de Janeiro - RJ / BR
	02 / CHAGAS DA SILVA, Fernanda Rua Mora 403 Campo Grande CEP: 23013-620 Rio de Janeiro - RJ / BR
	03 / CHAVES BARBERATO, Luana CBN 11 Lote 09 sala 101 Taguatinga Norte CEP: 72115-115 Brasília - DF / BR
	04 / DE CAMARGO NASCENTE, Luciana Colônoa Agrícola Vicente Pires Chácara 291 Lote 08-Vicente Pires CEP: 72110-800 Brasília - DF / BR
	05 / BARBOSA DO NASCIMENTO VIANA, Jessica Rua Almirante Tamandaré 59/702 Flamngo CEP: 22210-060 Rio de Janeiro - RJ / BR
	06 / OLIVEIRA SILVA, Renata QNA 09 casa 32 - Taguatinga Norte CEP: 72110-090 Barsília - DF / BR
	07 / NUNES LEMES, Laís Flávia QNM 08 Conjunto F casa 03 Ceilândia Norte CEP: 72210-086 Brasília - DF / BR
	08 / GERMAN NOËL, François Rua Mathias Antonio dos Santos 354/103 21940-380 Rio de Janeiro / BR
	09 / SOARES ROMEIRO, Luís Antônio Av. Parque das Aguas Claras lote 3465 Ap. 101 Águas Claras Norte CEP: 71906-500 Brasília - DF / BR
	[2014/52]
Former [2014/50]	01 / MARTINS DA SILVA, Claudia Lucia Rua Juraci Camargo 600/901 Jardim Guanabara Rio de Janeiro - RJ / BR
	02 / CHAGAS DA SILVA, Fernanda Rua Mora 403 Campo Grande CEP: 23013-620 Rio de Janeiro - RJ / BR
	03 / CHAVES BARBERATO, Luana CBN 11 Lote 09 sala 101 Taguatinga Norte CEP: 72115-115 Brasília - DF / BR
	04 / DE CAMARGO NASCENTE, Luciana Colônoa Agrícola Vicente Pires Chácara 291 Lote 08-Vicente Pires CEP: 72110-800 Brasília - DF / BR
	05 / BARBOSA DO NASCIMENTO VIANA, Jessica Rua Almirante Tamandaré 59/702 Flamngo CEP: 22210-060 Rio de Janeiro - RJ / BR
	06 / OLIVEIRA SILVA, Renata QNA 09 casa 32 - Taguatinga Norte CEP: 72110-090 Barsília - DF / BR
	07 / NUNES LEMES, Laís Flávia QNM 08 Conjunto F casa 03 Ceilândia Norte CEP: 72210-086 Brasília - DF / BR
	08 / GERMAN NOËL, François Rua Mathias Antonio dos Santos 354/103 CEP: 21940-380 Jardim Guanabara - RJ / BE
	09 / SOARES ROMEIRO, Luís Antônio Av. Parque das Aguas Claras lote 3465 Ap. 101 Águas Claras Norte CEP: 71906-500 Brasília - DF / BR
Representative(s)	KATZAROV S.A. Geneva Business Center 12 Avenue des Morgines 1213 Petit-Lancy / CH
	[N/P]
Former [2014/50]	KATZAROV S.A. European Patent Attorneys 19, rue des Epinettes 1227 Genève / CH
Application number, filing date	13733873.7	04.01.2013
	WO2013BR00003
Priority number, date	BR20121000187	05.01.2012 Original published format: BR102012000187
	[2014/50]
Filing language	PT
Procedural language	EN
Publication	Type:	A1 Application with search report
	No.:	WO2013102249
	Date:	11.07.2013
	Language:	PT
	[2013/28]
	Type:	A1 Application with search report
	No.:	EP2810938
	Date:	10.12.2014
	Language:	EN
	[2014/50]
Search report(s)	International search report - published on:	BR	11.07.2013
	(Supplementary) European search report - dispatched on:	EP	26.06.2015
Classification	IPC:	C07D295/096, A61K31/473, A61P35/00, C07D317/58, A61K31/495, A61K31/496	[2015/31]
	CPC:	C07D317/58 (EP,CN,US); A61K31/496 (US); A61K31/495 (US); A61P13/02 (EP); A61P13/08 (EP); A61P35/00 (EP); (+) C07D295/033 (CN); C07D295/096 (EP,CN,US) (-)
	Former IPC [2014/50]	C07D219/00, A61K31/473, A61P35/00
Designated contracting states	AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LI, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR [2014/50]
Title	German:	N-PHENYLPIPERAZINDERIVATE ALS ANTAGONISTEN VON A1A-, A1D-ADRENOREZEPTOREN UND 5-HT1A-REZEPTOREN ZUR BEHANDLUNG VON BENIGNER PROSTATAHYPERPLASIE, PHARMAZEUTISCHE ZUSAMMENSETZUNGEN DAMIT	[2014/50]
	English:	N-PHENYLPIPERAZINE DERIVATIVES THAT ARE ANTAGONISTS OF A1A, A1D ADRENOCEPTORS AND 5-HT1A RECEPTORS FOR THE TREATMENT OF BENIGN PROSTATE HYPERPLASIA, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME	[2014/50]
	French:	DÉRIVÉS N-PHÉNYLPIPÉRAZINIQUES ANTAGONISTES D'ADRÉNORÉCEPTEURS A1A, A1D ET DE RÉCEPTEURS 5-HT1A DANS LE TRAITEMENT DE L'HYPERPLASIE BÉNIGNE DE LA PROSTATE, ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT	[2014/50]
Entry into regional phase	30.07.2014	Translation filed
	30.07.2014	National basic fee paid
	30.07.2014	Search fee paid
	30.07.2014	Designation fee(s) paid
	30.07.2014	Examination fee paid
Examination procedure	27.08.2013	Request for preliminary examination filed International Preliminary Examining Authority: BR
	30.07.2014	Amendment by applicant (claims and/or description)
	30.07.2014	Examination requested [2014/50]
	26.01.2016	Application deemed to be withdrawn, date of legal effect [2016/34]
	01.03.2016	Despatch of communication that the application is deemed to be withdrawn, reason: reply to the communication from the examining division not received in time [2016/34]
Fees paid	Renewal fee
	17.12.2014	Renewal fee patent year 03
	Penalty fee
	Additional fee for renewal fee
	31.01.2016	04 M06 Not yet paid
Opt-out from the exclusive Tooltip competence of the Unified Patent Court	See the Register of the Unified Patent Court for opt-out data
	Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court.
Documents cited:	Search	[X]EP0624584 (DAIICHI SEIYAKU CO [JP]) [X] 1,2 * example 100 *;
		[X]WO9936412 (HOECHST RES & TECH GMBH & CO [DE], et al) [X] 1,2 * example 6 *;
		[X]WO2005112538 (UNIV RIO DE JANEIRO [BR], et al) [X] 1-4 * 1-(1,3-benzodioxol-5-ilethyl)-4-(2-methoxyphenyl)piperazine (LASSbio 772); page 10, line 1 - line 6; claims 1, 5, 6 *;
		[X]US2009093493 (BERARDI FRANCESCO [IT], et al) [X] 1,2 * claim 5; compounds EC52, EC65, EC74 *;
		[X] - MOKROSZ M J ET AL, "STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS, PART 32 EFFECT OF STRUCTURAL MODIFICATIONS IN 1-ARYLPIPERAZINE DERIVATIVES ON ALPHA1-ADRENORCEPTOR AFFINITY", ARCHIV DER PHARMAZIE, WILEY VERLAG, WEINHEIM, (19970601), vol. 330, no. 6, doi:10.1002/ARDP.19973300605, ISSN 0365-6233, pages 177 - 180, XP001033771 [X] 1,2 * table 2; compounds 8b, 9b * DOI: http://dx.doi.org/10.1002/ardp.19973300605
		[X] - RATOUIS R ET AL, "Synthesis and pharmacological STUDY OF NEW PIPERAZINE DERIVATIVES. II. PHENETHYLPIPERAZINES", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, (19650101), vol. 8, doi:10.1021/JM00325A021, ISSN 0022-2623, pages 104 - 107, XP002315168 [X] 1,2 * table 1; compound 17 * DOI: http://dx.doi.org/10.1021/jm00325a021
		[X] - ENZA LACIVITA ET AL, "Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT1A receptors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, (20101101), vol. 20, no. 22, doi:10.1016/j.bmcl.2010.09.027, ISSN 0960-894X, pages 6628 - 6632, XP055196122 [X] 1,2 * page 6629, column lhc; figure 1; compounds 3, 5 * DOI: http://dx.doi.org/10.1016/j.bmcl.2010.09.027
		[X] - MOKROSZ J L ET AL, "QUANTITIVE ANALYSIS OF THE ALKYL CHAIN EFFECTS ON THE 5-HT1A AND 5-HT2 RECEPTOR AFFINITIES OF 4-ALKYL-1-ARYLPIPERAZINES AND THEIR ANALOGS", ARCHIV DER PHARMAZIE, WILEY VERLAG, WEINHEIM, (19950201), vol. 328, no. 2, ISSN 0365-6233, pages 143 - 148, XP002041901 [X] 1,2 * examples 1b, 4b, 4e-4g; tables 1, 2 *
		[X] - C. L. KUO ET AL, "G-protein coupled receptors: SAR analyses of neurotransmitters and antagonists", JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS, (20040601), vol. 29, no. 3, doi:10.1111/j.1365-2710.2004.00563.x, ISSN 0269-4727, pages 279 - 298, XP055180749 [X] 1,2 * figure 9; example 19; table 8a * DOI: http://dx.doi.org/10.1111/j.1365-2710.2004.00563.x
		[X] - JERZY L. MOKROSZ ET AL, "Structure-Activity Relationship Studies of Central Nervous System Agents. 13.4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a New Putative 5-HT1A Receptor Antagonist, and Its Analogs", JOURNAL OF MEDICINAL CHEMISTRY, (19940801), vol. 37, no. 17, doi:10.1021/jm00043a014, ISSN 0022-2623, pages 2754 - 2760, XP055196206 [X] 1,2 * examples 6-8; table 1 * DOI: http://dx.doi.org/10.1021/jm00043a014
	International search	[Y]JPH0324014 (BOEHRINGER MANNHEIM GMBH);
		[X]WO9504049 (RECORDATI CHEM PHARM [IT], et al);
		[Y]JPH09227380 (MITSUBISHI CHEM CORP);
		[A]WO03043983 (SCHERING AG [DE]);
		[Y] - PULITO VL ET AL., "Investigation of the Uroselective Properties of Four Novel alfala-Adrenergic Receptor Subtype-Selective Antagonists", J PHARM EXP THER., (2000), vol. 292, no. 1, pages 224 - 229, XP055158067
		[A] - BRADBURY RH ET AL., "Small-molecule androgen receptor downregulators as an approach to 'treatment of advanced prostate cancer", BIOORG MED CHEM LETTERS, (2011), vol. 21, pages 5442 - 5445, XP028267883 DOI: http://dx.doi.org/10.1016/j.bmcl.2011.06.122
		[A] - KUMAR CSA ET AL., "Synthesis and in vitro antiproliferative activity of novel 1-benzhydrylpiperazine derivatives against human cancer cell lines", EUR J MED CHEM, (2009), vol. 44, pages 1223 - 1229, XP025989475 DOI: http://dx.doi.org/10.1016/j.ejmech.2008.09.025
	by applicant	- OLDHAM; HA MM, NATURE, (2008), vol. 9, pages 60 - 71
		- FREDRIKSSON ET AL., MOL. PHARMACOL., (2003), vol. 63, pages 1256 - 1272
		- NAT. REV. DRUG DISCOV, (2006), vol. 5, no. 12, pages 993 - 996
		- BJARNAD6TTIR RN ET AL., GENOMICS, (2006), vol. 88, pages 263 - 273
		- OLDHAM; HAMM, NATURE, (2008), vol. 9, pages 60 - 71
		- AVELLAR ET AL., AN. ACAD. BRAS. CIENC., (2009), vol. 81, no. 3, pages 321 - 344
		- WESS, PHARMACOL. THER, (1998), vol. 80, no. 3, pages 231 - 264
		- FREDRIKSSON ET AL., MOL PHARMACOL, (2003), vol. 63, pages 1256 - 1272
		- HIEBLE ET AL., PHARMACOL REV, (1995), vol. 45, pages 267 - 270
		- MICHEL ET AL., NAUNYN SCHMIEDEBERGS ARCH PHARMACOL, (1995), vol. 352, no. 1, pages 1 - 10
		- LANGER, EUR. J. UROL, (1999), vol. 36, pages 2 - 6
		- VARMA; DENG, CAN. J. PHYSIOL. PHARMACOL., (2000), vol. 78, pages 267 - 292
		- ZHONG; MINNEMAN, EUR. J. PHARMACOL., (1999), vol. 375, pages 261 - 276
		- HUH ET AL., GENES GENET. SYST, (2010), vol. 85, no. 1, pages 65 - 73
		- SCOFIELD ET AL., J. PHARMACOL. EXP. THER, (1995), vol. 275, pages 1035 - 1042
		- HIEBLE, PHARM. ACTA. HELV., (2000), vol. 74, no. 2-3, pages 163 - 171
		- MICHELOTTI ET AL., PHARMACOL. THER, (2000), vol. 88, pages 281 - 309
		- FORRAY ET AL., MOL. PHARMACOL., (1994), vol. 45, no. 4, pages 703 - 708
		- HATANO ET AL., BR. J. PHARMACOL, (1994), vol. 113, no. 3, pages 723 - 728
		- MARSHALL ET AL., J. PHARMACOL, (1995), vol. 115, no. 5, pages 781 - 786
		- HIEBLE; RUFFOLO, EXPERT OPIN INVESTIG DRUGS, (1997), vol. 6, no. 4, pages 367 - 387
		- MALLOY ET AL., J. UROL., (199809), vol. 160, pages 937 - 943
		- MURAMATSU ET AL., BR J. UROL., (1994), vol. 74, no. 5, pages 572 - 578
		- HIEBLE ET AL., PHARMACOL. REV., (1995), vol. 45, pages 267 - 270
		- CHEN ET AL., J. UROL, (2005), vol. 174, pages 370 - 374
		- MCNEAL, UROL. CLIN. NORTH AM., (1990), vol. 17, pages 477 - 486
		- COCKETT ET AL., PROG. UROL, (1991), vol. 1, no. 6, pages 957 - 72
		- PRICE ET AL., MOL PHARMACOL, (1994), vol. 46, pages 221 - 226
		- TSENG-CRANK ET AL., J. PHARMACOL, (1995), vol. 115, pages 1475 - 1485
		- LEPOR ET AL., J. UROL, (1993), vol. 149, pages 640 - 642
		- MICHEL ET AL., J. AUTON PHARMACOL, (1996), vol. 16, pages 21 - 28
		- KOJIMA ET AL., PROSTATE, (2006), vol. 66, pages 761 - 767
		- CHAPPLE, BR J UROL, (1995), vol. 76, no. 1, pages 47 - 56
		- SHIBATA ET AL., MOL. PHARMACOL, (1995), vol. 48, pages 250 - 258
		- GOETZ ET AL., EUR. J. PHARMACOL, (1995), vol. 272, no. 2-3, pages R5 - 6
		- CHAPUT; MONTIGNI, J. PHARMACOL. THER, (1988), vol. 246, no. 1, pages 359 - 370
		- HOYER ET AL., PHARMACOL REV, (1994), vol. 46, pages 157 - 203
		- HOYER; MARTIN, NEUROPHARMACOLOGY, (1997), vol. 36, pages 419 - 428
		- SAXENA ET AL., TRENDS PHARMACOL SCI, (1998), vol. 19, pages 311 - 316
		- VILLALON ET AL., DRUG DISCOV TODAY, (1997), vol. 2, pages 294 - 300
		- VILLALON; CENTURION, NAUNYN. SCHMIEDEBERGS ARCH PHARMACOL, (2007), vol. 376, no. 1-2, pages 45 - 63
		- FREDRIKSSON ET AL., MOL PHARMACOL., (2003), vol. 1256-127, page 63
		- TRUMPP-KALLMEYER ET AL., J. MED., (1992), vol. 35, no. 19, pages 3448 - 3462
		- BARNES; SHARP, NEUROPHARMACOLOGY, (1999), vol. 38, pages 1083 - 1152
		- KOBILKA ET AL., NATURE, (1987), vol. 329, pages 75 - 79
		- FARGIN ET AL., NATURE, (1988), vol. 335, no. 6188, pages 358 - 360
		- PUCADYIL; CHATTOPADHYAY, PROGR. LIPID RES., (2006), vol. 45, pages 295 - 333
		- ABDUL ET AL., ANTICANCER RES, (1994), vol. 14, no. 3A, pages 1215 - 1220
		- DIZEYI ET AL., PROSTATE, (2004), vol. 59, no. 3, pages 328 - 336
		- ABDUL, ANTICANCER RES, (1994), vol. 14, no. 3A, pages 1215 - 1220
		- TATE; SCHERTLER, CURR OPIN STRUCT BIOL, (2009), vol. 19, no. 4, pages 386 - 395
		- KOBILKA; SCHERTLER, TRENDS PHARMACOL SCI, (2008), vol. 29, no. 2, pages 79 - 83
		- THIEL, NAT BIOTECHNOL, (2004), vol. 22, pages 513 - 519
		- PEREZ, BIOCHEM PHARMACOL, (2007), vol. 73, no. 8, pages 1051 - 1062
		- WAUGH ET AL., J. BIOL CHEM, (2001), vol. 276, no. 27, pages 25366 - 2537
		- L6PEZ-RODRIGUEZ ET AL., J. MED . CHEM, (1997), vol. 40, pages 2653 - 2656
		- LI ET AL., J. MOL. MODEL, (2008), vol. 14, no. 10, pages 957 - 966
		- LOPEZ-RODRIGUEZ ET AL., MOLPHARMACOL, (2002), vol. 62, no. 1, pages 15 - 21
		- KUBINYI., PHARMAZIE, (1995), vol. 50, pages 647 - 662
		- HUBER ET AL., BIOCHEMISTRY, (2008), vol. 47, no. 42, pages 11013 - 1 1023
		- FORRAY ET AL., PHARMACOL., (1994), vol. 45, no. 4, pages 703 - 708
		- HATANO ET AL., J. PHARMACOL, (1994), vol. 113, no. 3, pages 723 - 728
		- MARSHALL ET AL., BR J PHARMACOL, (1995), vol. 115, no. 5, pages 1 - 786 78
		- MALLOY ET AL., UROL, J., (1998), vol. 160, pages 937 - 943
	- MURAMATSU ET AL., BR J UROL., (1994), vol. 74, no. 5, pages 572 - 578
	- HIEBLE ET AL., PHARMACOL REV., (1995), vol. 45, pages 267 - 270
	- HIEBLE, PHARMA HELV ACTA, (2000), vol. 74, no. 2-3, pages 163 - 171
	- MTCHELOTTI ET AL., PHARMACOL. THER., (2000), vol. 88, pages 281 - 309
	- DIZEYL ET AL., PROSTATE, (2004), vol. 59, no. 3, pages 328 - 336
	- RATOUIS ET AL., J. MED., (1965), vol. 8, pages 271 - 273
	- LEOPOLD ET AL., J PHARM. PHARMACOL, (2003), vol. 56, no. 2, pages 247 - 255
	- MOKROSZ ET AL., ARCH PHARM, (1995), vol. 328, pages 143 - 148
	- MOKROSZ ET AL., J MED CHEM, (1996), vol. 39, pages 1125 - 1129
	- LOWRY ET AL., J. BIOL. CHEM, (1951), vol. 193, no. 1, pages 265 - 275
	- RICHARDS, J PHARMACOL, (1990), vol. 99, pages 753 - 761
	- CASTOLDI, LIFE SCI, (2006), vol. 78, pages 1915 - 1924
	- NEVES ET AL., BIOORG MED. CHEM, (2010), vol. 18, no. 5, pages 1925 - 1935
	- NIZNIK ET AL., NAUNYN-SCHMIEDEBERGS ARCH.. PHARMACOL, (1985), vol. 329, pages 333 - 343
	- TERAI ET AL., EUR J PHARMACOL, (1989), vol. 173, page 177
	- HAMDI ET AL., LIFE SCI, (1992), vol. 50, pages 1529 - 1534
	- NEVES ET AL., BIOORG. MED., (2010), vol. 18, no. 5, pages 1925 - 1935
	- DE LEAN ET AL., MOL PHARMACOL., (1982), vol. 21, no. 1, page 5 IT
	- MOSMANN, T., IMMUNOL METHODS., (19821216), vol. 65, no. 1 -2, pages 55 - 63
	- LORKE, D., ARCH TOXICOL, (1983), vol. 54, no. 4, pages 275 - 87
	- SCOFIELD ET AL., J. PHARMACOL EXP THER, (1995), vol. 275, pages 1035 - 1042
	- TESTA ET AL., LIFE SCI, (1995), vol. 57, no. 13, pages PL159 - 63
	- BANES ET AL., J. PHARMACOL EXP THER, (1999), vol. 291, pages 1179 - 1187
	- CARROLL ET AL., BIOORG MED CHEM LETT, (2001), vol. 11, pages 1119 - 1121
	- SHIBATA, MOL. PHARMACOL., (1995), vol. 48, pages 250 - 258
	- NEVES ET AL., BIOORG MED CHEM, (2010), vol. 18, no. 5, pages 1925 - 1935
	- NEVES ET AL., BIOORG. MED. CHEM, (2010), vol. 18, no. 5, pages 1925 - 1935
	- CHENG; PRUSOFF, BIOCHEM. PHARMACOL, (1973), vol. 22, pages 3099 - 3108
	- KOJIMA A, PROSTATE, (2006), vol. 66, pages 761 - 767

The EPO accepts no responsibility for the accuracy of data originating from other authorities; in particular, it does not guarantee that it is complete, up to date or fit for specific purposes.

Legal notice
Terms of use
24.1.24; 34p