Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/100)
  • Patent number: 5700789
    Abstract: This invention provides an antiallergic composition which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl.
    Type: Grant
    Filed: July 18, 1996
    Date of Patent: December 23, 1997
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Sakaue, Shogo Sameshima
  • Patent number: 5660976
    Abstract: This invention provides a hepatic graft preservative composition containing a phosphoric acid diester compound of the formula: ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group) or a pharmacologically acceptable salt thereof and a method for viable preservation of the hepatic graft using the above substance.The hepatic graft preservative composition and hepatic graft preserving method of this invention inhibit hepatic microcirculation disturbance following cold storage-reperfusion of the liver to effectively prevent necrosis of hepatocytes and is, therefore, useful for the preservation of the hepatic graft.
    Type: Grant
    Filed: June 13, 1995
    Date of Patent: August 26, 1997
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Yuzuru Ishimura, Makoto Suematsu, Kenichi Yoshida
  • Patent number: 5656618
    Abstract: The present invention relates to the use of an .alpha.-tocopherol phosphate, especially in its dl or d form, or an ester thereof, of the general formula ##STR1## in which: R.sub.1 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, or an .alpha.-tocopheryl radical; and R.sub.2 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as a methyl or ethyl radical in particular, or an oxyethylene chain of the formula ##STR2## in which R.sub.3 and R.sub.4 independently are a hydrogen atom or a methyl radical and n is an integer greater than or equal to 1, or a salt thereof, for preparing a pharmaceutical, dermatological or cosmetic composition for the prevention or treatment of allergic manifestations such as skin allergy or bronchial asthma, or inflammatory manifestations, or for the prevention or treatment of the harmful effects of free radicals.
    Type: Grant
    Filed: October 24, 1994
    Date of Patent: August 12, 1997
    Assignee: LVMH Recherche
    Inventors: Alain Meybeck, Frederic Bonte, Christian Marechal
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5650404
    Abstract: This invention provides a therapeutic composition for pancreatitis which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl. The pharmaceutical composition of this invention can be used with advantage in the prevention and treatment of pancreatitis.
    Type: Grant
    Filed: July 18, 1995
    Date of Patent: July 22, 1997
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Sakaue, Shinya Ogino, Sachiko Matsuura, Rie Nagao
  • Patent number: 5643597
    Abstract: Use of a tocopherol phosphate, other than alpha-tocopherol phosphate, especially in its dl or d form, or one of its esters having general formula (I) in which: R' is hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, R'O is a tocopheryl radical; R" is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, or R"O is an oxyethylene chain, of formula (a) in which R.sub.4 and R.sub.5 are independently a hydrogen atom or a methyl radical, and n is an integer of 1 or over; R.sub.1, R.sub.2 and R.sub.3 are independently a hydrogen atom or a methyl radical, it being understood that R.sub.1, R.sub.2 and R.sub.3 cannot simultaneously be a methyl radical. A represents the groups (b), or (c).
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 1, 1997
    Assignee: LVMH Recherche
    Inventors: Alain Meybeck, Marc Dumas, Frederic Bonte, Christian Marechal
  • Patent number: 5627173
    Abstract: Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and prophylaxis of degenerative joint disorders, of rheumatic disorders accompanied by cartilage breakdown, such as rheumatoid arthritis, joint trauma and chondrolysis as a consequence of prolonged immobilization of the joint, of inflammations, septic shock, disorders with impaired leukocyte adhesion, disorders caused by an elevated concentration of tumor necrosis factor alpha, such as cachexia or Crohn's disease.
    Type: Grant
    Filed: January 23, 1996
    Date of Patent: May 6, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Graeve, Werner Thorwart, Ruth Raiss, Klaus U. Weithmann, Stefan M ullner
  • Patent number: 5612323
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventor: Raj N. Misra
  • Patent number: 5612370
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or --N(O)-- and the others are carbon atoms; Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)--; and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventor: Karnail S. Atwal
  • Patent number: 5580863
    Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: December 3, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Patent number: 5563170
    Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.
    Type: Grant
    Filed: August 15, 1991
    Date of Patent: October 8, 1996
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5556842
    Abstract: This invention provides a lung graft preservative composition comprising a phosphoric acid diester compound of the formula: ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group) or a pharmaceutically acceptable salt thereof and a method for the preservation of the lung graft using the compound.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: September 17, 1996
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Nobuyoshi Shimizu, Kouzi Uno, Motoi Aoe, Kenichi Yoshida
  • Patent number: 5552389
    Abstract: The present invention provides suppressory compositions against hepatic metastases of tumors which comprise a phosphoric acid diester compound of the formula: ##STR1## (wherein R.sub.1 and R.sub.2 each is the same as or different from the other and represents hydrogen or methyl) or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: September 3, 1996
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Tetsuya Toge, Toshihiro Hirai, Akihiro Yoshimoto, Kenichi Yoshida
  • Patent number: 5527786
    Abstract: The present invention provides a phosphonic diester derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and they each represent a hydrogen atom, a lower alkyl group, a halogen atom, a cyano group, a hydroxyl group, or a lower alkoxy group optionally having a halogen atom, a phenyl group or a hydroxypiperidino group as a substituent; R.sup.4 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group optionally having a halogen atom or a cyano group as a substituent; and R.sup.5 and R.sup.6 are the same or different and they each represent a hydrogen atom or a lower alkyl group.The derivative of the present invention has excellent hypolipidemic, vasodepressor and hypoglycemic activities and is useful as therapeutic and preventive agents for hyperlipidemic diseases, hypertension and diabetes.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: June 18, 1996
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kazuyoshi Miyata, Yasuhisa Kurogi, Yoshihiko Tsuda, Kazuhiko Tsutsumi, Takeshi Iwamoto, Chieko Naba
  • Patent number: 5523296
    Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5, R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CHOR.sub.9 O, --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: June 4, 1996
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5500418
    Abstract: Compounds of formula I ##STR1## wherein R is diethoxymethyl, R.sub.1 is hydrogen, R.sub.2 is pyrid-3-ylmethyl and R.sub.3 is hydrogen, or R is cyclohexylmethyl, R.sub.1 is hydrogen and R.sub.2 is quinolin-4-ylmethyl, or R.sub.1 is hydroxy and R.sub.2 is 3,4-methylenedioxybenzyl, 1-(3,4-methylenedioxyphenyl)ethyl, and R.sub.3 is hydrogen, or R is benzyl, R.sub.1 is hydroxy, R.sub.2 is 1-(3,4-methylenedioxyphenyl)ethyl, and R.sub.3 is hydrogen, and salts thereof have GABA.sub.B -antagonistic properties and can be used for the treatment of diseases responsive to GABA.sub.B -antagonists.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: March 19, 1996
    Assignee: Ciba-Geigy Corporation
    Inventor: Stuart J. Mickel
  • Patent number: 5489576
    Abstract: A therapeutic agent for hemorrhoidal diseases, comprising, as an active ingredient, a diester phosphate compound of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom or a methyl, or a pharmacologically acceptable salt thereof, and a method for treating hemorrhoidal diseases, comprising administering a pharmaceutically effective amount of said diester phosphate compound or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: February 6, 1996
    Assignees: Senju Pharmaceutical Co., Ltd., Amato Pharmaceutical Products, Ltd.
    Inventors: Kenichi Yoshida, Etsunosuke Noda
  • Patent number: 5478815
    Abstract: A liver protectant comprising a phosphoric diester compound of the following formula (wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl) or a pharmacologically acceptable salt thereof. ##STR1## The liver protectant composition of this invention effectively inhibits the elevation of GOT and GPT, among other parameters, so that it is useful for the prevention and therapy , of acute liver disorder, chronic liver disorder and fuminant liver disorder. It can also be used in cirrhosis of the liver with success. The liver protectant composition of this invention can be used with advantage in liver damage associated with alcohol intake and hepatic impairment due to acetaminophen and other drugs. Furthermore, the liver protectant composition of this invention is of value in acute intrahepatic cholestasis.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: December 26, 1995
    Assignee: Senji Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Sakaue, Sachiko Matsuura, Rie Nagao, Shinya Ogino
  • Patent number: 5474992
    Abstract: A pharmaceutical composition for renal disorder and a dialysis solution for extracorporeal hemodialysis which comprise a phosphoric acid diester of the following formula: ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group) or a pharmacologically acceptable salt thereof.Since the composition of this invention inhibits the formation of free radicals in the body, it can be advantageously used for the prophylaxis and treatment of various renal disorders such as glomerulonephritis, acute renal failure, uremia, adriamycin nephrosis, puromycin nephrosis, gentamicin- and cisplatin-induced disorders of the kidney, renal impairment due to paraquat and other agricultural chemicals, and immune complex nephritis. Moreover, the composition of this invention is also of use as a dialysis solution for extracorporeal hemodialysis with the propylactic/therapeutic effect on dialysis amyloidosis.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: December 12, 1995
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Sakaue, Noriko Saito, Sachiko Matsuura, Rie Nagao, Shinya Ogino
  • Patent number: 5474991
    Abstract: This invention relates to a lipid metabolism improving medicinal composition containing a phosphoric acid diester compound of the formula or a pharmacologically acceptable salt thereof. ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group.The lipid metabolism improving medicinal composition of this invention lowers the plasma levels of triglycerides (TG), non-esterified fatty acids (NEFA), total cholesterol (T-ch), esterified cholesterol (E-ch), free cholesterol (F-ch), total lipid (TL) and lipid peroxides (LPO) and, among cholesterol fractions, increases the high-density lipoprotein (HDL) fraction and reduces the low-density ipoprotein (VLDL) fractions. Therefore, the composition can be used with advantage for the amelioration of hyperlipidemia associated with arteriosclerotic diseases such as myocardial infarction, angina pectoris, cerebral infarction, cerebral arteriosclerosis, etc.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: December 12, 1995
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Sakaue, Yasuko Umegaki, Rie Nagao
  • Patent number: 5470845
    Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R.sup.4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: November 28, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
  • Patent number: 5453421
    Abstract: Novel compounds useful, for example, for the treatment of ischemic conditions and arrhythmia are disclosed. The compounds have the formula ##STR1## wherein X is oxygen or sulfur and the R groups are as defined herein.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: September 26, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail S. Atwal, Syed Z. Ahmed, Dinos P. Santafianos
  • Patent number: 5447922
    Abstract: .alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: September 5, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: R. Michael Lawrence, Scott A. Biller, Olga M. Fryszman
  • Patent number: 5436245
    Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: July 25, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 5428027
    Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: June 27, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: John P. Daub, George P. Lahm, Bradford S. Marlin
  • Patent number: 5387579
    Abstract: The present invention relates to the use of an .alpha.-tocopherol phosphate, especially in its dl or d form, or an ester thereof, of the general formula ##STR1## in which: R.sub.1 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, or an .alpha.-tocopheryl radical; and R.sub.2 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as a methyl or ethyl radical in particular, or an oxyethylene chain of the formula ##STR2## in which R.sub.3 and R.sub.4 independently are a hydrogen atom or a methyl radical and n is an integer greater than or equal to 1, or a salt thereof, for preparing a pharmaceutical, dermatological or cosmetic composition for the prevention or treatment of allergic manifestations such as skin allergy or bronchial asthma, or inflammatory manifestations, or for the prevention or treatment of the harmful effects of free radicals.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: February 7, 1995
    Assignee: Lvmh Recherche
    Inventors: Alain Meybeck, Frederic Bonte, Christian Marechal
  • Patent number: 5356621
    Abstract: A method of attracting flies of the Muscidae or Muscinae families comprising providing in a locus where the flies exist a fly attractant composition which contains as an active ingredient a composition extracted from a bamboo with an extractive solvent such as water or C.sub.1 -C.sub.4 alcohol.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: October 18, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Yuichiro Tabaru, Akio Saito
  • Patent number: 5306713
    Abstract: A highly active antioxidant composed of a diester of phosphoric acid with tocopherol and ascorbic acid or a salt thereof used to stabilize other materials.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: April 26, 1994
    Assignees: Shiseido Company Ltd., Senju Pharmaceutical Co, Ltd.
    Inventors: Keiko Suetsugu, Kazumi Ogata, Kenichi Yoshida, Keiichi Uehara, Kenichi Tomita
  • Patent number: 5306495
    Abstract: Compounds containing substituted piperidine groups, of the general formula (I) ##STR1## in which n is e.g. 1, 2 or 3, R.sub.1 is e.g. hydrogen or methyl, R.sub.2 is e.g. ethylene or trimethylene and if n is 1, A is e.g. hydrogen, --COOC.sub.18 H.sub.37 --n or --COC.sub.11 H.sub.23 --n, if n is 2, A is e.g. ##STR2## and if n is 3, A is e.g. ##STR3## are effective stabilizers for organic materials, especially synthetic polymers, which are subject to the action of light, heat and oxidation.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: April 26, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Giuseppe Cantatore, Graziano Vignali
  • Patent number: 5268388
    Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 7, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: John P. Daub, George P. Lahm, Bradford S. Marlin
  • Patent number: 5229375
    Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: July 20, 1993
    Assignee: Scripps Clinic and Research Foundation
    Inventors: Peter E. Maligres, Kyriacos C. Nicolaou
  • Patent number: 5204334
    Abstract: Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I ##STR1## wherein R.sub.1 and R.sub.2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alk.sub.1 and alk.sub.2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula ##STR2## wherein R.sub.1, R.sub.2, n, m, m', X, Y, alk.sub.1 and alk.sub.2 are as defined above, R'.sub.3 is one of the groups R.sub.3 mentioned above or is an amino-protecting group R.sub.0, Z.sub.1 is a functionally modified phosphono group, and Z.sub.2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z.sub.
    Type: Grant
    Filed: September 25, 1991
    Date of Patent: April 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Frostl, Knut A. Jaeggi
  • Patent number: 5202313
    Abstract: Complexes between natural or synthetic phospholipids and bilobalide, a sesquiterpene extracted from the leaves of Gingko biloba, are disclosed, as well as the preparation thereof and their therapeutic application as antiinflammatory agents and as agents for the treatment of disorders associated with inflammatory or traumatic neuritic processes. These new compounds, which exhibit a different bioavailability compared with free bilobalide, are suitable for incorporation into pharmaceutical formulations for systemic and topical administration: the latter route has been found to be particularly useful for the treatment of common peripheral disorders associated with inflammatory or neurodystrophic alterations.
    Type: Grant
    Filed: February 6, 1991
    Date of Patent: April 13, 1993
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Giuseppe Mustich
  • Patent number: 5190929
    Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 2, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Gregory W. Canute
  • Patent number: 5151442
    Abstract: Compounds of the formula ##STR1## in which: Z represents a halogen or a cyano, acetyl, trifluoroacetyl, nitro, C.sub.1 -C.sub.4 alkylthio, carboxyl, phosphono, dialkoxyphosphonyl or alkoxycarbonyl group, the alkylthio and alkoxy groups containing from 1 to 3 carbon atoms;R.sub.1 denotes a hydroxyl group and R.sub.2 represents hydrogen, or R.sub.1 and R.sub.2 taken together form an additional bond between the carbon atoms by which they are carried; andR.sub.3 representsa group NH--X--R.sub.4, in which X denotes a direct bond or an SO.sub.2 group and R.sub.4 represents a phenyl group which is unsubstituted or monosubstituted or disubstituted by a halogen, a nitro group, a C.sub.1 -C.sub.4 group, a trifluoromethyl group, an amino group, a group --N(Alk).sub.2, a group --COOAlk or a group OAlk, Alk denoting a C.sub.1 -C.sub.4 Alkyl group;a group --S--R.sub.5, in which R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.
    Type: Grant
    Filed: October 23, 1991
    Date of Patent: September 29, 1992
    Assignee: Sanofi
    Inventors: Georges Garcia, Alain Di Malta, Philippe Soubrie
  • Patent number: 5147866
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein a and b together form an --O-- or --CH.sub.2 -- linkage or a bond;either Y is N and R.sub.2 is hydrogen; orY is C-R.sub.1whereineither one of R.sub.1 and R.sub.2 is hydrogen and the other is nitro, cyano, halo, --CF.sub.3, C.sub.2 F.sub.5, formyl aldoxime, CF.sub.3 O, NO.sub.2 --CH.dbd.CH--, NC--CH.dbd.CH--; a group R.sub.x X-- wherein R.sub.x is C.sub.1-6 alkyl, aryl or heteroaryl either of which may be optionally substituted by one, two or three of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, halo, CF.sub.3 and cyano; and X is C.dbd.O, O.C.dbd.O, C.dbd.O.O, CHOH, SO, SO.sub.2, O.SO, O.SO.sub.2, CONH, O.CONH, C.dbd.S, O.C.dbd.S, C.dbd.S.O, CH.SH, SONH, SO.sub.2 NH, O.SONH, O.SO.sub.2 NH, CO--CH.dbd.CH, C.dbd.NHOH, C.dbd.NNH.sub.2 ; or a group R.sub.y R.sub.z NZ-- wherein R.sub.y and R.sub.z are independently hydrogen or C.sub.1-6 alkyl and Z is C.dbd.O, SO or SO.sub.2 ; or a group (R.sub.w O).sub.2 P(O)W wherein R.sub.
    Type: Grant
    Filed: October 29, 1990
    Date of Patent: September 15, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Geoffrey Stemp, Gordon Burrell
  • Patent number: 5145990
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: September 8, 1992
    Assignee: Merck & Co., Inc.
    Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
  • Patent number: 5100667
    Abstract: A method of making, without use of a solvent, insecticidal pellet compositions of N-hydrocarboyl phosphoroamidothioates and phosphoroamidodithioates is provided.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: March 31, 1992
    Assignee: Chevron Research and Technology Company
    Inventors: Jim H. Chan, Kent A. Hasse, Roderick I. Satre, James H. Trusler
  • Patent number: 4985414
    Abstract: New 1-naphtholphthalein monophosphates of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen or halogen, and each of M.sup.1 and M.sup.2 is a proton or an alkali metal, alkaline earth metal, ammonium, dicyclohexylammonium, tetraalkylammonium or alkanolammonium cation, and the tautomeric transformation products thereof, are useful as substrates for detection and photometric determination of alkaline phosphotase.
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: January 15, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Werner Guethlein, Hartmut Merdes
  • Patent number: 4963537
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: April 26, 1989
    Date of Patent: October 16, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4948786
    Abstract: The present invention relates to a pharmaceutical composition for the prophylaxis and treatment of ischemic disorder in mammalian organs which contains, as an ingredient, a compound of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the methyl group or a hydrogen atom, or a salt thereof.
    Type: Grant
    Filed: January 10, 1989
    Date of Patent: August 14, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Norio Shimamoto, Kazumi Ogata
  • Patent number: 4939128
    Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, carboxylic acid acyl or carbamoyl which may be substituted; R is an aliphatic hydrocarbon group which may be substituted or alicylic hydrocarbon group which may be substituted, or a salt thereof.The compound of the present invention has the effects to prevent and improve dysfunctions caused by oxygen free radicals, and can be used as preventive and therapeutic drugs against dysfunctions in the circulatory system.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: July 3, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Norio Shimamoto
  • Patent number: 4937237
    Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: June 26, 1990
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4937257
    Abstract: New flavanone derivatives of the formula I ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each phenyl which is unsubstituted or monosubstituted to trisubstituted by OH, alkyl, alkoxy, acylamino, halogen, COOalkyl and/or NO.sub.2 and/or substituted by a methylenedioxy group, and the alkyl, alkoxy and acyl groups each have 1-7 C atoms, but wherein the HO group is only in the 6-position if at least one of the radicals Ar.sup.1 and Ar.sup.2 is substituted phenyl, and the phosphoric acid esters thereof and the salts of these compounds display antiallergic effects. Salts of the I-phosphoric acid esters with aminoglycoside antibiotics are outstandingly stable and possess advantageous kinetics of liberation.
    Type: Grant
    Filed: August 28, 1985
    Date of Patent: June 26, 1990
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rolf Gericke, Helmut Wahlig, Elvira Dingeldein
  • Patent number: 4914197
    Abstract: Novel phosphoric diesters of general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each means a methyl group or a hydrogen atom, provided that at least one of R.sub.1 and R.sub.2 is a hydrogen atom, or a salt thereof which can be produced by reacting .beta., .gamma. or .delta.-tocopherol with a halophosphorylating agent such as phosphorus oxychloride, reacting the resultant product with ascorbic acid whereof hydroxyl groups at 5- and 6-positions are protected, and then removing protected groups from the hydroxyl groups. The phosphoric diester has antiinflammatory activity.
    Type: Grant
    Filed: March 4, 1987
    Date of Patent: April 3, 1990
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Itaru Yamamoto, Kazumi Ogata
  • Patent number: 4902696
    Abstract: Herein is described an ocular composition comprising an ocular decongestant such as phenylephrine and certain labdane derivatives which are intraocular pressure lowering agents. The composition not only markedly reduces the ocular reddening otherwise produced by such labdane compounds, but also unexpectedly prolongs and frequently potentiates their intraocular pressure lowering effect. Both of these effects are very beneficial to the use of such labdanes for the treatment of glaucoma.
    Type: Grant
    Filed: October 8, 1987
    Date of Patent: February 20, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Paul G. Conway, Grover C. Helsley
  • Patent number: 4897402
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.
    Type: Grant
    Filed: June 29, 1988
    Date of Patent: January 30, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 4888329
    Abstract: A composition comprising a compound of the following formula or a salt thereof ##STR1## wherein R.sub.1 and R.sub.2 each represent a hydrogen atom or a methyl group. The composition is highly safe and useful as an antiulcer agent.
    Type: Grant
    Filed: April 27, 1988
    Date of Patent: December 19, 1989
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Takahiro Ogawa, Takahiro Sakaue
  • Patent number: 4886791
    Abstract: Novel water-soluble derivatives of silybin of enhanced activity are provided as well as methods of preparing the derivatives and pharmaceutical compositions containing them. The novel derivatives according to the invention have the following general formula (I); ##STR1## where: R=H or PO(OH).sub.2 and R'=PO(OH).sub.2 The compounds of the invention are useful inter alia in therapy of liver disorders and other applications where an anti-radical effect is required. They have the advantages of high hydrophilicity and are soluble at approximately pH 4, compared to prior art compounds which are water-soluble only at higher pH and enhanced stability.
    Type: Grant
    Filed: July 13, 1988
    Date of Patent: December 12, 1989
    Assignee: Inverni della Beffa S.p.A.
    Inventors: Raffaello Giorgi, Marisa Conti, Giorgio Pifferi
  • Patent number: 4882319
    Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: November 21, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf