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EP About this file: EP0624594

EP0624594 - Monomeric bile acid derivatives, a process for their production, and their use as medicines [Right-click to bookmark this link]
Status	No opposition filed within time limit Status updated on 09.06.2000 Database last updated on 08.04.2026
Most recent event Tooltip	09.06.2000	No opposition filed within time limit	published on 26.07.2000 [2000/30]
Applicant(s)	For all designated states HOECHST AKTIENGESELLSCHAFT Brüningstrasse 50 65929 Frankfurt am Main / DE
	[1999/32]
Former [1994/46]	For all designated states HOECHST AKTIENGESELLSCHAFT Brüningstrasse 50 D-65929 Frankfurt am Main / DE
Inventor(s)	01 / Glombik, Heiner, Dr. Südhang 16 D-65719 Hofheim am Taunus / DE
	02 / Enhsen, Alfons, Dr. Odenwaldstrasse 19 D-64572 Büttelborn / DE
	03 / Kramer, Werner, Dr. Dr. Henry-Moisand-Strasse 19 D-55130 Mainz / DE
	04 / Wess, Günther, Dr. Langenselbolder Weg 35 D-63526 Erlensee / DE
	[1994/46]
Application number, filing date	94106845.4	02.05.1994
	[1994/46]
Priority number, date	DE19934315439	08.05.1993 Original published format: DE 4315439
	[1994/46]
Filing language	DE
Procedural language	DE
Publication	Type:	A2 Application without search report
	No.:	EP0624594
	Date:	17.11.1994
	Language:	DE
	[1994/46]
	Type:	A3 Search report
	No.:	EP0624594
	Date:	01.05.1996
	[1996/18]
	Type:	B1 Patent specification
	No.:	EP0624594
	Date:	11.08.1999
	Language:	DE
	[1999/32]
Search report(s)	(Supplementary) European search report - dispatched on:	EP	13.03.1996
Classification	IPC:	C07J9/00, A61K31/575, C07J41/00, // C07J31/00, C07J51/00, C07J43/00	[1995/22]
	CPC:	C07J51/00 (EP,US); A61P3/06 (EP); A61P9/10 (EP); C07J31/006 (EP,US); C07J41/0055 (EP,US); C07J41/0088 (EP,US); (+) C07J43/003 (EP,US); C07J9/005 (EP,US) (-)
	Former IPC [1994/46]	C07J9/00, C07J41/00, A61K31/575, // C07J31/00, C07J51/00, C07J43/00
Designated contracting states	AT, BE, CH, DE, DK, ES, FR, GB, GR, IE, IT, LI, LU, NL, PT, SE [1994/46]
Title	German:	Monomere Gallensäurederivate, Verfahren zu ihrer Herstellung und Verwendung dieser Verbindungen als Arzneimittel	[1994/46]
	English:	Monomeric bile acid derivatives, a process for their production, and their use as medicines	[1994/46]
	French:	Dérivés des acides biliaires monomères, un procédé pour leur production et leur utilisation comme médicaments	[1994/46]
Examination procedure	04.11.1996	Examination requested [1997/01]
	28.02.1997	Despatch of a communication from the examining division (Time limit: M04)
	11.06.1997	Reply to a communication from the examining division
	11.07.1997	Despatch of a communication from the examining division (Time limit: M04)
	05.11.1997	Reply to a communication from the examining division
	08.06.1998	Despatch of a communication from the examining division (Time limit: M02)
	04.08.1998	Reply to a communication from the examining division
	06.10.1998	Despatch of communication of intention to grant (Approval: Yes)
	03.02.1999	Communication of intention to grant the patent
	14.05.1999	Fee for grant paid
	14.05.1999	Fee for publishing/printing paid
Opposition(s)	12.05.2000	No opposition filed within time limit [2000/30]
Fees paid	Renewal fee
	31.05.1996	Renewal fee patent year 03
	02.06.1997	Renewal fee patent year 04
	02.06.1998	Renewal fee patent year 05
	31.05.1999	Renewal fee patent year 06
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	[XY] G. WESS ET AL: "Modified bile acids: preparation of 7.alpha.,12.alpha.-dihydroxy-3.beta.- and 7.alpha.,12.alpha.-dihydroxy-3.alpha.-(2-hydroxyethoxy)-5.beta.-cholanic acid and their biological activity", TETRAHEDRON LETTERS, vol. 33, no. 2, OXFORD GB, pages 195 - 198, XP002001751 [X] 1-4 * Seite 195, Verbindungen 2 und 3 * [Y] 1-4
		[X] R. PELLICCIARI ET AL: "Bile Acids with a Cyclopropyl-Containing Side Chain. 1. Preparation and Properties of 3.alpha.,7.beta.-Dihydroxy-22,23-methylene-5.beta.-cholan-24-oic Acid", JOURNAL OF MEDICINAL CHEMISTRY, vol. 27, no. 6, WASHINGTON US, pages 746 - 749 [X] 1-4 * the whole document *
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		[X] BIOCHIM. BIOPHYS. ACTA, vol. 754, no. 1, pages 101 - 109
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		[X] BIOMED. MASS SPECTROM., vol. 7, no. 11/12, pages 515 - 520
		[X] "CHEMICAL ABSTRACTS TENTH COLLECTIVE INDEX, FORMULAS C23H21N3O7 - C28H22NP", CHEMICAL ABSTRACTS, COLUMBUS, OHIO, USA * page 15553F, column 3, line 44 - line 46 *
		[X] CHEMICAL ABSTRACTS, vol. 103, no. 1, 8 July 1985, Columbus, Ohio, US; abstract no. 004386, AMMON H V ET AL: "Effects of sulfodeoxycholate on rat and rabbit small intestine" page 404; column 1; [X] 1,2 * abstract *
		[X] AM. J. PHYSIOL., vol. 248, no. 4 pt 1, pages G485 - G493
		[X] N. MURATA ET AL: "DETERMINATION OF SULFATED AND NONSULFATED BILE ACIDS IN SERUM BY MASS FRAGMENTOGRAPHY", STEROIDS, vol. 42, no. 5, SAN FRANCISCO US, pages 575 - 592, XP023581546, DOI: doi:10.1016/0039-128X(83)90121-6 [X] 1,2 * page 577; figure 1 * DOI: http://dx.doi.org/10.1016/0039-128X(83)90121-6
		[X] CHEMICAL ABSTRACTS, vol. 092, no. 9, 3 March 1980, Columbus, Ohio, US; abstract no. 073345, DE WITT E H ET AL: "Effects of sulfation patterns on intestinal transport of bile salt sulfate esters" page 404; column 2; [X] 1,2 * abstract *
		[X] AM. J. PHYSIOL., vol. 238, no. 1, pages G34 - G39
		[X] T. BANDIERA ET AL: "A CONVENIENT PROCEDURE FOR THE SYNTHESIS OF URSODEOXYCHOLIC ACID SULFATED DERIVATIVES", SYNTHETIC COMMUNICATIONS, vol. 17, no. 9, pages 1111 - 1117, XP000564355, DOI: doi:10.1080/00397918708078793 [X] 1,2 * the whole document * DOI: http://dx.doi.org/10.1080/00397918708078793
		[X] J. C. BABCOCK ET AL: "Reductive Methylation of Steroid Ketones", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 74, no. 21, 5 November 1952 (1952-11-05), DC US, pages 5472 - 5474, XP002260967, DOI: doi:10.1021/ja01141a073 [X] 1,2 * page 5474, column 2, paragraph B * DOI: http://dx.doi.org/10.1021/ja01141a073
		[X] I. MAZUMDER ET AL: "Bile acid transformations by Alcaligenes recti", STEROIDS: STRUCTURE, FUNCTION, AND REGULATION, vol. 58, no. 2, MA US, pages 79 - 86, XP023431415, DOI: doi:10.1016/0039-128X(93)90057-T [X] 1,2 * page 80, column 1 - page 81, column 2 * DOI: http://dx.doi.org/10.1016/0039-128X(93)90057-T
		[XY] G. WESS ET AL: "Preparation of 3.alpha.- and 3.beta.-(.omega.-aminoalkoxy)-7.alpha.,12.alpha.-dihydroxy-5.beta.-cholanoic acid esters: versatile shuttles for drug targeting", TETRAHEDRON LETTERS, vol. 34, no. 5, 29 January 1993 (1993-01-29), OXFORD GB, pages 817 - 818 [X] 1,2 * Seite 817, Verbindungen 4 und 8; Seite 818, Verbindungen 10, 12 und 14 *[Y] 1-4
		[X] S. YAMADA ET AL: "Mild oxidation of aldehydes to the corresponding carboxylic acids and esters: alkaline iodine oxidation revisited", TETRAHEDRON LETTERS, vol. 33, no. 30, OXFORD GB, pages 4329 - 4332, XP028085739, DOI: doi:10.1016/S0040-4039(00)74252-3 [X] 1,2 * page 4330 - page 4331 * DOI: http://dx.doi.org/10.1016/S0040-4039(00)74252-3
		[X] W. ZHOU ET AL: "Studies of steroidal plant-growth regulator 25. Concise stereoselective construction of side chain of brassinosteroid from the intact side chain of hyodeoxycholic acid: formal synthesis of brassinolide, 25-methylbrassinolide, 26,27-dimethylbrassinolide and their related compounds", TETRAHEDRON, (INCL TETRAHEDRON REPORTS), vol. 48, no. 10, OXFORD GB, pages 1837 - 1852 [X] 1,2 * Seite 1839, Verbindung 9 *
		[X] CHEMICAL ABSTRACTS, vol. 55, no. 4, 20 February 1961, Columbus, Ohio, US; abstract no. 3648c, S. YASUO ET AL: "Basic bile acids. I. Synthesis and configuration of 3.alpha.aminocholanic acid" column 3648; [X] 1,2 * abstract *
		[X] NIPPON KAGAKU ZASSHI, vol. 80, pages 1310 - 1312
		[X] "CHEMICAL ABSTRACTS, SIXTH COLLECTIVE INDEX, FORMULAS C20-Z", CHEMICAL ABSTRACTS, EASTON, PENNSYLVANIA, USA * page 3222F, column 1, line 64 *
		[X] J. REDEL ET AL: "Amines cycliques des acides biliaires. Premire partie : Monoamines", BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE (MEMOIRES), PARIS FR, pages 877 - 883 [X] 1,2 * page 880, column 2 *
		[X] R. A. HILL ET AL: "DICTIONARY OF STEROIDS, INDEXES", CHAPMAN & HALL, LONDON, GB [X] 1,2 * page 386, column 2 - page 387, column 2 *
		[Y] W. KRAMER ET AL: "Liver specific drug targeting by coupling to bile acids", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 267, no. 26, MD US, pages 18598 - 18604 [Y] 1-4 * Seite 18600, Verbindung S-2539; Seite 18601, Fig 4 *
		[Y] WESS G ET AL: "Synthesis of bile acid - drug conjugates: potential drug shuttles for liver specific targeting", TETRAHEDRON LETTERS, vol. 34, no. 5, OXFORD GB, pages 819 - 822, XP000335946, DOI: doi:10.1016/0040-4039(93)89021-H [Y] 1-4 * the whole document * DOI: http://dx.doi.org/10.1016/0040-4039(93)89021-H
		[Y] MUELLNER S ET AL: "Synthesis of affinity chromatography and electrophoresis matrixes for the purification of bile acid transport proteins", CHROMATOGRAPHIA, vol. 32, no. 5/6, pages 265 - 268 [Y] 1-4 * the whole document *
		[Y] QUACKENBUSH F W ET AL: "Arylsulfonate esters of fatty alcohols. II. Structural relation to hypocholesterolemic activity", ARTERY (LEONIDAS, MICH.), vol. 3, no. 6, pages 553 - 575, XP000564780 [Y] 1-4 * Seite 566, Verbindung 52 *
		[Y] CHEMICAL ABSTRACTS, vol. 110, no. 4, 23 January 1989, Columbus, Ohio, US; abstract no. 28956, N. HO ET AL: "Utilising bile acid carrier mechanisms to enhance liver and small intestine absoprtion" page 330; column 2; [Y] 1-4 * abstract *
		[Y] ANN. N. Y. ACAD. SCI. (BIOL. APPROACHES CONTROLLED DELIVERY DRUGS), vol. 507, pages 315 - 329
		[Y] SHERMAN I A ET AL: "Hepatic transport of fluorescent molecules: in vivo studies using intravital TV microscopy", HEPATOLOGY (BALTIMORE), vol. 6, no. 3, pages 444 - 449, XP000564785, DOI: doi:10.1002/hep.1840060321 [Y] 1-4 * page 445, column 2, paragraph 1 * * page 448, column 1, paragraph 1 * DOI: http://dx.doi.org/10.1002/hep.1840060321
		[Y] B. PALMIERI ET AL: "Clinical Research into the Hypolipemic and Platelet Antiaggregant Activity of Plafibride, Carried out in Double.blind Conditions and in Comparison with Clofibrate", ARZNEIMITTEL FORSCHUNG DRUG RESEARCH., vol. 31, no. 10a, AULENDORF DE, pages 1863 - 1866 [Y] 1-4 * the whole document *
		[Y] SHIN-ICHI MORISHITA ET AL: "Synthesis and Hypolipidemic Activity of 2-Substituted Isobutyric Acid Derivatives", JOURNAL OF MEDICINAL CHEMISTRY, vol. 31, no. 6, WASHINGTON US, pages 1205 - 1209, XP002003702, DOI: doi:10.1021/jm00401a022 [Y] 1-4 * page 1207; table II * DOI: http://dx.doi.org/10.1021/jm00401a022
		[Y] J. M. CHAPMAN ET AL: "Hypolipidemic Activity of Phthalimide Derivatives V: Reduced and Hydrolytic Products of Simple Cyclic Imides", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 73, no. 10, WASHINGTON US, pages 1482 - 1484, XP009103639, DOI: doi:10.1002/jps.2600731041 [Y] 1-4 * page 1483; table 1 * DOI: http://dx.doi.org/10.1002/jps.2600731041
		[Y] CHEMICAL ABSTRACTS, vol. 073, no. 3, Columbus, Ohio, US; abstract no. 013070, KOCIAN J ET AL: "Effect of oral calcium administration on the cholesterol and phospholipid serum levels" page 220; column 1; [Y] 1-4 * abstract *
		[Y] CAS. LEK. CESK., vol. 109, no. 8, pages 175 - 179
		[Y] HARDISON W G M ET AL: "Specificity of an sodium-dependent taurocholate transport site in isolated rat hepatocytes", AM. J. PHYSIOL. GASTROINTESTINAL AND LIVER PHYSIOLOGY, vol. 9, no. 5, pages G477 - G483, XP000564784 [Y] 1-4 * page 482, column 1, paragraph 2 - column 2, paragraph 1 *
		[A] K. GREISEN ET AL: "Inhibition of 3H-Glibenclamide Binding to Sulfonylurea Receptors by Oral Antidiabetics", ARZNEIMITTEL FORSCHUNG DRUG RESEARCH., vol. 35, no. 4, AULENDORF DE, pages 707 - 712 [A] 1-4 * page 708, column 2; example HB985 *
		[A] CHEMICAL ABSTRACTS, vol. 112, no. 21, 21 May 1990, Columbus, Ohio, US; abstract no. 193405, A. VILLEGAS-NAVARRO: "9-Anthracenecarboxylic acid and hematological and biochemical variables in the rat" page 230; column 1; [A] 1-4 * abstract *
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		[A] J. M. CRAWFORD ET AL: "Physical and biological properties of fluorescent dansylated bile salt derivatives: the role of steroid ring hydroxylation", BIOCHIMICA ET BIOPHYSICA ACTA, vol. 1085, no. 2, pages 223 - 234, XP023577840, DOI: doi:10.1016/0005-2760(91)90098-3 [A] 1-4 * the whole document * DOI: http://dx.doi.org/10.1016/0005-2760(91)90098-3
		[PX] WESS G ET AL: "Specific Inhibitors of Ileal Bile Acid Transport", JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, no. 7, 1 April 1994 (1994-04-01), WASHINGTON US, pages 873 - 875 [PX] 1,2 * Seite 874, Verbindung (7) *
		[PY] DONG-CHOOL KIM ET AL: "Evaluation of the Bile Acid Transporter in Enhancing Intestinal Permeability to Renin-Inhibitory Peptides", JOURNAL OF DRUG TARGETING, vol. 1, no. 4, pages 347 - 359, XP000564343 [PY] 1-4 * the whole document *

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.