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4746675 External pharmaceutical composition
New Patents
group; whereas Y stands for -NH- when R5 stands for a hydrogen atom and a valence bond exists between the C2, and C7, atoms, as well as their acid addition salts and pharmaceutical preparations containing these compounds. Further on, the invention relates to a process for preparing these compounds and preparations. The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
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4746671 PHARMACEUTICAL USE OF (3-PYRIDINYL-METHYLENAMINO-OXY)ALKANOIC ACIDS AND ESTERS Eddy J Freyne, Alfons H M Raeymaekers, Victor Sipido, Marc G Venet, Rumst, Belgium assigned to Janssen Pharmaceutica N V Novel (3-pyridinyl-methylen-aminooxy)alkanoic acids and esters, compositions containing the same, and methods of treating clinical conditions related with the production of thromboxane A2, prostacyclin and/or prostaglandins D2, E2 and F2 alpha.
4746667 PHARMACEUTICAL COMPOSITION CONTAINING 2-(2-BENZIMIDAZOLYL THIOMETHYL) PYRIDINE Enar I Carlsson, Hakan S Larsson, Sundell Gunhild W yon Wittken, Viola SamuelssonJunggren, Kenneth Lundstrom, VFr Sweded assigned to Aktiebolaget Hassle A pharmaceutical preparation containing as active ingredient a compound of the formula See Patent for Chemical Structure or a therapeutically acceptable salt thereof in which formula R1 and R2 are the same or different and each selected from the group consisting of H, CF3, NO2, -COOCH3, -COOC2H5, alkyl containing 1-7 carbon atoms, halogen, alkoxy, containing 1-5 carbon atoms, and alkanoyl containing 1-4 carbon atoms; R is selected from the group consisting of H, alkanoyl containing 14 carbon atoms, and carboalkoxy containing 2-6 carbon atoms; and R3, R4 and RS, which are the same or different, are each selected from the group consisting of H, CH3, C2H5, OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3; provided that (a) at least one of R3, R4 and R5 is selected from the group consisting of CH3, C2H5, OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3, and (b) when two of R3, R4 and R5 are H, then the remaining radical R3, R4 or R5 is selected from the group consisting of OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3; the use of the compounds for inhibiting gastric acid secretion; compounds included in the formula I, and processes for their preparation.
4746672 OXIDES OF 1,2,5-THIADIAZOLES, THEIR USE IN PHARMACEUTICAL COMPOSITIONS Tobias O Yellin, Philip Edwards, Michael Large assigned to ICI Americas Inc Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: See Patent for Chemical Structure I in which R1 and R2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 414C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, CI or Br atoms, provided that one of R 1 and R2 is halogen substituted; ring X is a heterocyclie ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R3 is a variety of radicals described in the specification; and the pharmaceuticaUy-aggqftable acid-addition salts thereof. M a~md~cturing processes for the derivatives, :-'-rmediates and pharmaceutical compositions are also part of the invention.
4746675 EXTERNAL PHARMACEUTICAL COMPOSITION Yuji Makino, Yoshiki Suzuki, Hino, Japan assigned to Teijin Limited A pharmaceutical composition for external use with the enhanced penetration of a pharma-
iv
New Patents
cologically active agent through the skin or mucosa of a warm-blooded animal, said composition comprising (A) a pharmaceutically effective amount of the pharmacologically active agent such as antiinflammatory agent, etc., and (B) a penetration enhancer of the following formula (1) See Patent for Chemical Structure (1) wherein R1 and R2 are identical or different and each represents H, a C1-25 alkyl, C2-25 alkenyl, a (C1-24 alkyl)carbonyl or a (C2-24 alkenyl)carbonyl, provided that RI and R2 are not H at the same time, or R1 and R2, taken together, may form a group of the following formula (a) See Patent for Chemical Structure (a) in which R3 and R4 are identical or different and each represents H, C1-24 alkyl or CI-24 alkenyl.
within 4 hours which comprises coating the particles of the active ingredient in a liquid medium with a water insoluble polymer-preferably with an ethyl cellulose polymer film-and thereafter admixing the coated crystals with at least one disintegrating agent being capable of swelling in aqueous medium and other auxiliary agents conventionally used in pharmaceutical industry and pressing the mixture into tablets. The advantage of the process of the present invention is that it is readily feasible with a very wide range of active ingredients and provides sustained release tablets having a high active ingredient content.
~481~ 4746679 NOVEL PHARMACEUTICAL COMPOSITIONS IMPROVING THE PSYCHOMOTOR PERFORMANCES AND A PROCESS FOR PRODUCING THE SAME Anne Rolland, 75018 Paris, France There is provided a method for alleviating the decrease of psychomotor performance~ in depressed or tired humans in need of such alleviation which consists in administering to such humans a safe but effective amount of 2,2-bis phenoxy-N,N-dimethyl ethylamine or an acid addition salt thereof.
ANGIOTENSIN CONVERTING ENZYME INHIBITORS AND THEIR FORMULATION AND USE AS PHARMACEUTICALS Colin Bennion, David P Marriott, Anthony Cook, David H Robinson, Loughborough, United Kingdom assigned to Fisons plc There are described compounds of formula I, See Patent for Tabular Presentation PS where the substituents are defined in the disclosure. There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.
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4748023 PROCESS FOR THE PREPARATION OF SUSTAINED RELEASE PHARMACEUTICAL COMPOSITIONS HAVING A HIGH ACTIVE INGREDIENT CONTENT Ev Tamas, Pa Fekete, Tibor Kovacs, Denes Bezzegh, nee Baumgartner Ilona Bor, Zoltan Toth, nee Sumeg Katalin Zukovics, Ghungara assigned to EGYT Gyogyszervegyeszeti Gyar The invention relates to a process for the preparation of sustained release solid pharmaceutical compositions having an active ingredient content of at least 80% and possessing a structure which loosens in aqueous medium but does not disintegrate to discrete particles
BICYCLIC BENZONOID ALKYLENE AMINO THIENO (3,4-D) I S O T H I A Z O L E E T H E R S AND THIOETHETHERS, PHARMACEUTICAL COMPOSITIONS AND USE Donald E Kuhla, Henry F Campbell, William L Studt assigned to Rorer Pharmaceutical Corporation A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including antisecretory and anti-ulcero-genic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
group; whereas Y stands for -NH- when R5 stands for a hydrogen atom and a valence bond exists between the C2, and C7, atoms, as well as their acid addition salts and pharmaceutical preparations containing these compounds. Further on, the invention relates to a process for preparing these compounds and preparations. The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
iii
4746671 PHARMACEUTICAL USE OF (3-PYRIDINYL-METHYLENAMINO-OXY)ALKANOIC ACIDS AND ESTERS Eddy J Freyne, Alfons H M Raeymaekers, Victor Sipido, Marc G Venet, Rumst, Belgium assigned to Janssen Pharmaceutica N V Novel (3-pyridinyl-methylen-aminooxy)alkanoic acids and esters, compositions containing the same, and methods of treating clinical conditions related with the production of thromboxane A2, prostacyclin and/or prostaglandins D2, E2 and F2 alpha.
4746667 PHARMACEUTICAL COMPOSITION CONTAINING 2-(2-BENZIMIDAZOLYL THIOMETHYL) PYRIDINE Enar I Carlsson, Hakan S Larsson, Sundell Gunhild W yon Wittken, Viola SamuelssonJunggren, Kenneth Lundstrom, VFr Sweded assigned to Aktiebolaget Hassle A pharmaceutical preparation containing as active ingredient a compound of the formula See Patent for Chemical Structure or a therapeutically acceptable salt thereof in which formula R1 and R2 are the same or different and each selected from the group consisting of H, CF3, NO2, -COOCH3, -COOC2H5, alkyl containing 1-7 carbon atoms, halogen, alkoxy, containing 1-5 carbon atoms, and alkanoyl containing 1-4 carbon atoms; R is selected from the group consisting of H, alkanoyl containing 14 carbon atoms, and carboalkoxy containing 2-6 carbon atoms; and R3, R4 and RS, which are the same or different, are each selected from the group consisting of H, CH3, C2H5, OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3; provided that (a) at least one of R3, R4 and R5 is selected from the group consisting of CH3, C2H5, OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3, and (b) when two of R3, R4 and R5 are H, then the remaining radical R3, R4 or R5 is selected from the group consisting of OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3; the use of the compounds for inhibiting gastric acid secretion; compounds included in the formula I, and processes for their preparation.
4746672 OXIDES OF 1,2,5-THIADIAZOLES, THEIR USE IN PHARMACEUTICAL COMPOSITIONS Tobias O Yellin, Philip Edwards, Michael Large assigned to ICI Americas Inc Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: See Patent for Chemical Structure I in which R1 and R2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 414C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, CI or Br atoms, provided that one of R 1 and R2 is halogen substituted; ring X is a heterocyclie ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R3 is a variety of radicals described in the specification; and the pharmaceuticaUy-aggqftable acid-addition salts thereof. M a~md~cturing processes for the derivatives, :-'-rmediates and pharmaceutical compositions are also part of the invention.
4746675 EXTERNAL PHARMACEUTICAL COMPOSITION Yuji Makino, Yoshiki Suzuki, Hino, Japan assigned to Teijin Limited A pharmaceutical composition for external use with the enhanced penetration of a pharma-
iv
New Patents
cologically active agent through the skin or mucosa of a warm-blooded animal, said composition comprising (A) a pharmaceutically effective amount of the pharmacologically active agent such as antiinflammatory agent, etc., and (B) a penetration enhancer of the following formula (1) See Patent for Chemical Structure (1) wherein R1 and R2 are identical or different and each represents H, a C1-25 alkyl, C2-25 alkenyl, a (C1-24 alkyl)carbonyl or a (C2-24 alkenyl)carbonyl, provided that RI and R2 are not H at the same time, or R1 and R2, taken together, may form a group of the following formula (a) See Patent for Chemical Structure (a) in which R3 and R4 are identical or different and each represents H, C1-24 alkyl or CI-24 alkenyl.
within 4 hours which comprises coating the particles of the active ingredient in a liquid medium with a water insoluble polymer-preferably with an ethyl cellulose polymer film-and thereafter admixing the coated crystals with at least one disintegrating agent being capable of swelling in aqueous medium and other auxiliary agents conventionally used in pharmaceutical industry and pressing the mixture into tablets. The advantage of the process of the present invention is that it is readily feasible with a very wide range of active ingredients and provides sustained release tablets having a high active ingredient content.
~481~ 4746679 NOVEL PHARMACEUTICAL COMPOSITIONS IMPROVING THE PSYCHOMOTOR PERFORMANCES AND A PROCESS FOR PRODUCING THE SAME Anne Rolland, 75018 Paris, France There is provided a method for alleviating the decrease of psychomotor performance~ in depressed or tired humans in need of such alleviation which consists in administering to such humans a safe but effective amount of 2,2-bis phenoxy-N,N-dimethyl ethylamine or an acid addition salt thereof.
ANGIOTENSIN CONVERTING ENZYME INHIBITORS AND THEIR FORMULATION AND USE AS PHARMACEUTICALS Colin Bennion, David P Marriott, Anthony Cook, David H Robinson, Loughborough, United Kingdom assigned to Fisons plc There are described compounds of formula I, See Patent for Tabular Presentation PS where the substituents are defined in the disclosure. There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.
47~1~
4748023 PROCESS FOR THE PREPARATION OF SUSTAINED RELEASE PHARMACEUTICAL COMPOSITIONS HAVING A HIGH ACTIVE INGREDIENT CONTENT Ev Tamas, Pa Fekete, Tibor Kovacs, Denes Bezzegh, nee Baumgartner Ilona Bor, Zoltan Toth, nee Sumeg Katalin Zukovics, Ghungara assigned to EGYT Gyogyszervegyeszeti Gyar The invention relates to a process for the preparation of sustained release solid pharmaceutical compositions having an active ingredient content of at least 80% and possessing a structure which loosens in aqueous medium but does not disintegrate to discrete particles
BICYCLIC BENZONOID ALKYLENE AMINO THIENO (3,4-D) I S O T H I A Z O L E E T H E R S AND THIOETHETHERS, PHARMACEUTICAL COMPOSITIONS AND USE Donald E Kuhla, Henry F Campbell, William L Studt assigned to Rorer Pharmaceutical Corporation A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including antisecretory and anti-ulcero-genic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.