Tetracyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/284)
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Patent number: 5994362Abstract: Disclosed is a new treatment for men with prostatic cancer involving combination therapy of a 5.alpha.-reductase inhibitor, i.e., a 17.beta.-substituted 4-azasteroid, a 17.beta.-substituted non-azasteroid, 17.beta.-acyl-3-carboxyandrost-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylamino-phenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an antiandrogen, i.e. flutamide. Pharmaceutical compositions useful for treatment are also disclosed.Type: GrantFiled: June 2, 1995Date of Patent: November 30, 1999Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Elizabeth Stoner
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Patent number: 5994363Abstract: Symptoms of Parkinson's disease and psychogenic male erectile dysfunction (MED) can be ameliorated through the use of apomorphine. The adverse side effects of apomorphine administration, such as nausea, vomiting, yawning, and cardiovascular effects, can be significantly reduced by a dose escalating method of acclimatization. An initial dose of apomorphine is administered to the patient, and subsequently increased over a period of time until a final apomorphine dose in excess of a desired therapeutic dose has been received by the patient. Thereafter a therapeutic dose of apomorphine, less than the final apomorphine dose, is administered to the patient with attendant reduced side effects.Type: GrantFiled: August 24, 1998Date of Patent: November 30, 1999Assignee: Pentech Pharmaceuticals, Inc.Inventors: Ragab El-Rashidy, Bruce Ronsen
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Patent number: 5985889Abstract: Psychogenic impotence or erectile dysfunction can be identified in psychogenic male patients and can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms so as to maintain a plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter.Type: GrantFiled: June 22, 1998Date of Patent: November 16, 1999Assignees: Pentech Pharmaceuticals, Inc., Queen's University at KingstonInventors: Ragab El-Rashidy, Jeremy P. W. Heaton, Alvaro Morales, Michael A. Adams
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Patent number: 5981541Abstract: The present invention provides compounds of formula (I): ##STR1## wherein R.sub.1 -R.sub.7, W, X, Y, and Z have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are are useful as anticancer agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.Type: GrantFiled: September 23, 1997Date of Patent: November 9, 1999Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Leroy Fong Liu, Darshan B. Makhey
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Patent number: 5981543Abstract: The instant invention involves a method of treating and/or reversing androgenic alopecia and promoting hair growth, and methods of treating acne vulgaris, seborrhea, and female hirsutism, by administering to a patient in need of such treatment a 5.alpha.-reductase 2 inhibitor such as finasteride, in a dosage amount under 5 mgs/day.Type: GrantFiled: June 22, 1998Date of Patent: November 9, 1999Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Keith D. Kaufman, Elizabeth Stoner, Joanne Waldstreicher
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Patent number: 5977127Abstract: Solid and liquid pharmaceutical preparations containing cilansetron or its acid addition salts as active substance which include an amount sufficient to stabilize cilansetron against racemization, of a physiologically compatible water-soluble acid additive selected from monobasic or multibasic organic acids having 2 to 12 carbon atoms with a first p.sub.s value between 1.1 and 4.8, acid salts of the aforementioned multibasic organic acids, and acid salts of multibasic mineral acids having a first available pK.sub.s value between 1.5 and 7.5, as well as the use of such acid additives for stabilizing cilansetron against racemization in pharmaceutical preparations.Type: GrantFiled: July 31, 1998Date of Patent: November 2, 1999Assignee: Solvay Pharmaceuticals GmbHInventors: Ingo Bonnacker, Hartmut Koehn, Gerhard Kristen, Christine Reichel
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Patent number: 5977126Abstract: The present invention relates to methods for preparing and using compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) wherein X, W, Z, R.sup.4, and R.sup.5, are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: May 14, 1998Date of Patent: November 2, 1999Assignee: Glaxo Wellcome Inc.Inventors: Kenneth William Batchelor, Stephen Vernon Frye
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Patent number: 5962442Abstract: The invention concerns the treatment of hyderandrogenic conditions in humans by the formation of a novel mechanism-based irreversible inhibitor of human 5.alpha.-reductase enzymes from 3-oxo-4-azasteroids having a 1,2-double bond and the pyridine-nucleotide cofactor of the 5.alpha.-reductase enzyme, NADPH. Until the present invention, it was not know or predicted that 3-oxo-4-azasteroids having 1,2-double bond would form a complex with NADPH by the mechanism of 5.alpha.-reductase in vivo. The invention further relates to the novel inhibitor-cofactor complex and pharmaceutical compositions containing the complex.Type: GrantFiled: May 5, 1997Date of Patent: October 5, 1999Assignee: Merck & Co., INc.Inventors: Herb G. Bull, Georgianna S. Harris
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Patent number: 5962463Abstract: Stimulating non-amyloidogenic processing by the activation of cell surface serotonin receptors linked to phospholipase and protein kinase C is described. Activation of the cell surface serotonin receptors is accomplished by contacting the cell with an agent which is a serotonin agonist or which increases the intrasynaptic concentration of serotonin. Also described is the activation of cell surface serotonin receptors by dexnorfenfluramine. Agents which cause the activation of cell surface serotonin receptors can be administered to an individual to stimulate non-amyloidogenic processing in the brain of the individual, thereby inhibiting the deposition of amyloid in the brain of the individual.Type: GrantFiled: January 27, 1997Date of Patent: October 5, 1999Assignee: Massachusetts Institute Of TechnologyInventors: Roger M. Nitsch, Richard J. Wurtman
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Patent number: 5958890Abstract: Compounds the formula ##STR1## their use as farnesyl transferase protein inhibitors and pharmaceutical compositions containing them are disclosed, especially compounds of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are halo, A and B are each H.sub.2, and R is as defined in the specification.Type: GrantFiled: September 11, 1997Date of Patent: September 28, 1999Assignee: Schering CorporationInventors: Dinanath F. Rane, Alan K. Mallams, Arthur G. Taveras, F. George Njoroge
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Patent number: 5945412Abstract: The present invention provides for a method of inhibiting bone loss in a subject in need of such treatment comprising administration to the subject of a therapeutically effective amount of a compound of structural formula I: ##STR1## The present invention further provides for a method for treating and preventing osteoporosis and osteopenia and other diseases where inhibiting bone loss may be beneficial, including: Paget's disease, malignant hypercalcemia, periodontal disease, joint loosening and metastatic bone disease, comprising administration of therapeutically effective amount of a compound of structural formula I to the subject.Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for inhibiting bone loss and treating or preventing osteoporosis and osteopenia.Type: GrantFiled: December 3, 1997Date of Patent: August 31, 1999Assignee: Merck & Co., Inc.Inventors: Vivian L. Fuh, Keith D. Kaufman, Joanne Waldstreicher
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Patent number: 5942519Abstract: This invention is concerned with the prevention of precipitated acute urinary retention in a subject male susceptible thereto by the administration of an inhibitor of 5.alpha.-reductase to the subject. The present invention also provides for a method of reducing the risk of precipitated acute urinary retention by the administration of a 5.alpha.-reductase inhibitor to the subject at risk therefor.Type: GrantFiled: October 23, 1998Date of Patent: August 24, 1999Assignee: Merck & Co., Inc.Inventor: Joanne Waldstreicher
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Patent number: 5935968Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: ##STR1## to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).Type: GrantFiled: March 12, 1998Date of Patent: August 10, 1999Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
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Patent number: 5925647Abstract: Novel cryptolepine analogs useful as hypoglycemic agents and methods for their use as hypoglycemic agents, for example, in the treatment of diabetes, and a method for their synthesis are described. As hypoglycemic agents, the novel cryptolepine analogs are useful for the treatment of insulin-dependent diabetes mellitus (IDDM or Type I) and non-insulin dependent diabetes mellitus (NIDDM or Type II).Type: GrantFiled: October 20, 1997Date of Patent: July 20, 1999Assignee: Shaman Pharmaceuticals, Inc.Inventor: Donald E. Bierer
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Patent number: 5922728Abstract: Compounds of formula (I), wherein: the symbol represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.Type: GrantFiled: May 13, 1997Date of Patent: July 13, 1999Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
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Patent number: 5886184Abstract: Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.Type: GrantFiled: March 26, 1997Date of Patent: March 23, 1999Assignee: Merck & Co., Inc.Inventors: Ulf H. Dolling, James A. McCauley, Richard J. Varsolona
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Patent number: 5886005Abstract: Compounds of the formula ##STR1## are inhibitors of 5.alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: May 6, 1997Date of Patent: March 23, 1999Assignee: Merck & Co., Inc.Inventors: Susan D. Aster, Donald W. Graham
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Patent number: 5872126Abstract: The present invention provides for a method of treating preterm labor in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of 5.alpha.-reductase type 1 to the subject. The present invention further provides for a method of preventing premature labor in a subject susceptible thereto comprising administration of a labor-preventive amount of an inhibitor of 5.alpha.-reductase type 1 to the subject. Further, the present invention also relates to a method of reducing the risk of premature labor in a subject at risk therefor. The present invention also provides for a method for stopping labor preparatory (i.e., prior) to Cesarean delivery in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of 5.alpha.-reductase type 1 to the subject.Type: GrantFiled: August 29, 1997Date of Patent: February 16, 1999Assignee: Merck & Co., Inc.Inventors: Mark A. Cukierski, Stanley G. Spence, Joanne Waldstreicher
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Patent number: 5861411Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.Type: GrantFiled: April 10, 1996Date of Patent: January 19, 1999Assignee: Mitsubishi Chemical CorporationInventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
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Patent number: 5854273Abstract: A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.Type: GrantFiled: July 23, 1997Date of Patent: December 29, 1998Assignee: ADIR et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
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Patent number: 5846976Abstract: The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: August 22, 1996Date of Patent: December 8, 1998Assignee: Glaxo Wellcome Inc.Inventors: Kenneth William Batchelor, Stephen Vernon Frye, George F. Dorsey, Jr., Robert A. Mook, Jr.
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Patent number: 5843953Abstract: Compounds of formula (I) wherein: the dotted line indicates that a double bond may be present or absent; R.sup.1 is H, methyl or ethyl; R.sup.2 is .alpha.- or .beta.-C.sub.1-10 straight or branched alkyl; R.sup.3 is CO.sub.2 H, CN, CO.sub.2 R.sup.4, COHNR.sup.4, or CON(R.sup.4).sub.2 ; R.sup.4 is H, C.sub.1-10 straight or branched alky, aryl, heteroaryl, or aralkyl; Aryl is phenyl, substituted phenyl, naphthyl, or biphenyl; Heteroaryl is pyridil, pyrrolyl, thienyl, furanyl or quinolinyl; and Aralkyl is C.sub.1-10 alkyl substituted with one to three phenyl or substituted phenyl moieties; and their pharmaceutically acceptable salts are described. These compounds are 5.alpha.-reductase type 1 inhibitors. They may be used for treating conditions associated with an excess of DHT, either alone or in combination with other 5.alpha.-reductase inhibitors.Type: GrantFiled: March 24, 1997Date of Patent: December 1, 1998Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Josephine R. Carlin, Richard L. Tolman, Shuet-Hing Lee Chiu
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Patent number: 5824686Abstract: The instant invention involves a method of treating and/or reversing androgenic alopecia and promoting hair growth, and methods of treating acne vulgaris, seborrhea, and female hirsutism, by administering to a patient in need of such treatment a 5.alpha.-reductase 2 inhibitor such as finasteride, in a dosage amount under 5 mgs/day.Type: GrantFiled: February 20, 1996Date of Patent: October 20, 1998Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Keith D. Kaufman, Elizabeth Stoner, Joanne Waldstreicher
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Patent number: 5817818Abstract: The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) or (B) wherein X, W, Z, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: March 14, 1996Date of Patent: October 6, 1998Assignee: Glaxo Wellcome Inc.Inventors: Kenneth William Batchelor, Stephen Vernon Frye
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Patent number: 5770606Abstract: Psychogenic impotence or erectile dysfunction can be identified in psychogenic male patients and can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms so as to maintain a plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter.Type: GrantFiled: October 20, 1995Date of Patent: June 23, 1998Assignees: Pentech Pharmaceuticals, Inc., Queen's University at KingstonInventors: Ragab El-Rashidy, Jeremy P. W. Heaton, Alvaro Morales, Michael A. Adams
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Patent number: 5763453Abstract: A condensed indan derivative represented by the formula (1) ##STR1## wherein the ring A is an optionally substituted benzene ring or a benzene ring which has lower alkylenedioxy group(s), the ring B is an optionally substituted benzene ring or a benzene ring which has lower alkylene dioxy group(s), and R is a group --NR.sub.1 R.sub.2, an optionally substituted nitrogen-containing heterocyclic group, a group --OR.sub.3 or a group --SR.sub.4 (wherein R.sub.1 and R.sub.2 are the same or different and each represent a hydrogen atom, a phenyl group, an optionally substituted nitrogen-containing heterocyclic group, or a lower alkyl group which may be substituted by optionally substituted amino group(s), lower alkoxy group(s), phenyl group(s), nitrogen-containing heterocyclic group(s) or hydroxyl group(s), and R.sub.3 and R.sub.Type: GrantFiled: April 3, 1997Date of Patent: June 9, 1998Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shinji Okazaki, Tetsuji Asao, Teruhiro Utsugi, Yuji Yamada
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Patent number: 5763361Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase, particularly 5.alpha.-reductase type 1. The compounds of formula I are useful in the systemic, including oral, or parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostafic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula I.Type: GrantFiled: October 21, 1996Date of Patent: June 9, 1998Assignee: Merck & Co., Inc.Inventors: Georgianna Harris, Richard L. Tolman, Soumya P. Sahoo
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Patent number: 5760046Abstract: The instant invention involves a method of treating and/or reversing androgenic alopecia and promoting hair growth, and methods of treating acne vulgaris, seborrhea, and female hirsutism, by administering to a patient in need of such treatment a 5.alpha.-reductase 2 inhibitor, such as finasteride, in a dosage amount under 5 mgs/day.Type: GrantFiled: February 14, 1996Date of Patent: June 2, 1998Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Keith D. Kaufman, Elizabeth Stoner, Joanne Waldstreicher
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Patent number: 5760045Abstract: Described are new delta-17 and delta-20 olefic and saturated 17.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds and the use of such compounds as 5.alpha.-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.Type: GrantFiled: February 6, 1996Date of Patent: June 2, 1998Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Susan D. Aster, Richard L. Tolman
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Patent number: 5756483Abstract: The invention relates to pharmaceutical compositions for the intranasal administration of dihydroergotamine, apomorphine and morphine comprising one of these pharmacologically active ingredients in combination with a cyclodextrin and/or a disaccharide and/or a polysaccharide and/or a sugar alcohol.Type: GrantFiled: December 4, 1995Date of Patent: May 26, 1998Inventor: Franciscus W. H. M. Merkus
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Patent number: 5756453Abstract: There is disclosed a method for vascularizing tissue, a method for improving vascularization of ischemic tissue, and a method for improving the viability of grafted tissue or tissue survival in gradient ischemia of heart, brain or skin, comprising administering locally to the grafted or ischemic tissue or the site of the graft an effective amount of a compound comprising an alk-1-enyl glycerol derivative.Type: GrantFiled: January 31, 1996Date of Patent: May 26, 1998Assignee: Cell Therapeutics, Inc.Inventors: Nicholas B. Vedder, Edward D. Nudelman
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Patent number: 5744476Abstract: This invention provides for a method of raising extracellular brain acetylcholine levels to improve cognition by the administration to a warm-blooded animal of a pharmaceutical composition comprising an effective amount of a dopamine D.sub.1 agonist.Type: GrantFiled: June 27, 1994Date of Patent: April 28, 1998Assignee: Interneuron Pharmaceuticals, Inc.Inventors: Kenneth Walter Locke, Thomas David Steele
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Patent number: 5741795Abstract: Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.Type: GrantFiled: October 17, 1996Date of Patent: April 21, 1998Assignee: Merck & Co., Inc.Inventors: Susan D. Aster, Donald W. Graham, Derek J. Von Langen
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Patent number: 5739137Abstract: Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: February 28, 1996Date of Patent: April 14, 1998Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
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Patent number: 5733918Abstract: A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## wherein ring A represents an optionally substituted benzene ring or naphthalene ring, or a benzene ring having a lower alkylenedioxy group, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR=N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.Type: GrantFiled: January 19, 1996Date of Patent: March 31, 1998Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shinji Okazaki, Tetsuji Asao, Motoji Wakida, Keisuke Ishida, Masato Washinosu, Teruhiro Utsugi, Yuji Yamada
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Patent number: 5730964Abstract: The instant invention involves methods of treating sweat related conditions with compounds that are 5.alpha.-reductase inhibitors. The 5.alpha.-reductase inhibitors may be administered alone or in combination with other active agents to treat conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa.Type: GrantFiled: December 9, 1996Date of Patent: March 24, 1998Assignee: Merck & Co., Inc.Inventor: Joanne Waldstreicher
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Patent number: 5731317Abstract: The present invention is directed to certain novel compounds identified as bridged piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.1a, R.sup.2a, R.sup.3, R.sup.3a,R.sup.4, R.sup.5, A, X, and Y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: March 10, 1995Date of Patent: March 24, 1998Assignee: Merck & Co., Inc.Inventors: Zhijian Lu, Arthur A. Patchett, James R. Tata
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Patent number: 5719158Abstract: Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: June 5, 1995Date of Patent: February 17, 1998Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek von Langen
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Patent number: 5719159Abstract: The present invention provides compounds of formula (D wherein the symbol - - - represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain; B is a straight or branched C.sub.1 -C.sub.12 alkylene group optionally substituted by one or more aryl groups or fluorine atoms; W is a group R.sub.1 or (a) wherein R.sub.1 is a straight or branched C.sub. -C.sub.6 alkyl group unsubstituted or substituted by one or more fluorine atoms, provided that at least a fluorine atom is present in B or W. The compounds of the invention are useful as testosterone 5.alpha.-reductase inhibitors.Type: GrantFiled: May 31, 1996Date of Patent: February 17, 1998Assignee: Pharmacia S.p.A.Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
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Patent number: 5710275Abstract: Described are new 7.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.Type: GrantFiled: April 3, 1995Date of Patent: January 20, 1998Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gary H. Rasmusson, Richard L. Tolman, Gool F. Patel, Georgianna S. Harris, Donald W. Graham, Bruce E. Witzel
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Patent number: 5708001Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R.sup.1 and R.sup.2 i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, or ii) taken together are a --CH.sub.2 -- group forming a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond; R.sup.3 is preferably hydrogen, halogen or lower alkyl, R.sup.4 is preferably hydrogen or lower alkyl, X is preferably CH.sub.2, Y is preferably hydrogen and Z is preferably CONR.sup.14 R.sup.15 and R.sup.14 and R.sup.15 are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Glaxo Wellcome Inc.Inventors: Robert Carl Andrews, Cynthia Markert Cribbs, Stephen Vernon Frye, Curt Dale Haffner, Patrick Reed Maloney
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Patent number: 5703089Abstract: Novel bis-1,2-dihydro-3H-dibenzisoquinoline-1,3-diones and their salts, processes for their preparation, pharmaceutical compositions containing them and methods of using them to treat malignancies, mainly human solid tumor carcinomas.Type: GrantFiled: August 19, 1996Date of Patent: December 30, 1997Assignee: Knoll AktiengesellschaftInventors: Miguel Fernandez Brana, Jose Maria Castellano Berlanga, Cynthia Romerdahl
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Patent number: 5696128Abstract: Disclosed are methods for rectifying or ameliorating abnormal responses of mammalian immune systems. Also disclosed are methods for modifying normal responses of the mammalian immune system. Further disclosed are methods for accomplishing the foregoing by administering to a mammal a prolactin reducer and/or enhancer at a pre-determined time or times during a 24-hour period that results in modification of the mammal's abnormal prolactin profile so that it approaches or conforms to the prolactin profile of a young, healthy mammal of the same species (or to a standard profile generated from such individuals). Additionally, methods of upregulating or augmenting an immune response in a mammal are disclosed.Type: GrantFiled: July 7, 1994Date of Patent: December 9, 1997Assignees: The Board of Supervisors of Louisiana University and Agricultural and Mechanical College, The General Hospital CorporationInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5693809Abstract: Described are new 16-substituted and 7,16-disubstituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.Type: GrantFiled: May 12, 1995Date of Patent: December 2, 1997Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William Hagmann, Gary H. Rasmusson, Richard L. Tolman, Ihor E. Kopka, Soumya P. Sahoo, Craig K. Esser, Nathan G. Steinberg, Donald W. Graham, Bruce E. Witzel
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Patent number: 5693810Abstract: Described are new 17.beta.-carboxanilides of 4-aza-5.alpha.-androstan-3-ones and related compounds of structural formula I: ##STR1## and the use of such compounds as 5.alpha.-reductase inhibitors for treatment of benign prostatic hyperplasia acne, seborrhea, female hirsutism, prostatitis, and prostatic carcinoma and other hyperandrogenetic related disorders.Type: GrantFiled: March 21, 1995Date of Patent: December 2, 1997Assignee: Merck & Co., Inc.Inventors: Gary H. Rasmusson, Raman K. Bakshi, Gool F. Patel
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Patent number: 5663178Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.Type: GrantFiled: February 6, 1995Date of Patent: September 2, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
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Patent number: 5661163Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Mark G. Bock, Roger M. Freidinger, Rose Ann Ponticello
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Patent number: 5658922Abstract: Compounds of formula (I), wherein: R.sup.1 is selected from the group consisting of hydrogen and methyl; R.sup.2 is selected from the group consisting of methyl and ethyl; R.sup.3 is selected from the group consisting of hydrogen and methyl; and the C1-C2 carbon-carbon bond may be a single or double bond. Such compounds are useful in the treatment of pathologic conditions that benefit from blockade of isozymes of 5.alpha.-reductase.Type: GrantFiled: October 31, 1995Date of Patent: August 19, 1997Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Soumya P. Sahoo
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Patent number: 5648380Abstract: This invention pertains to therapeutic anti-inflammatory-wound healing compositions. The compositions comprise a therapeutically effective amount of one or more anti-inflammatory agents and a wound healing composition. In one embodiment the wound healing composition comprises (a) pyruvate; (b) an antioxidant; and (c) a mixture of saturated and unsaturated fatty acids. The therapeutic anti-inflammatory-wound healing compositions may be utilized in a wide variety of topical and ingestible pharmaceutical products. This invention also relates to methods for preparing and using the therapeutic anti-inflammatory-wound healing compositions and the pharamceutical products in which the therapeutic compositions may be used.Type: GrantFiled: May 22, 1995Date of Patent: July 15, 1997Assignee: Warner-Lambert CompanyInventor: Alain Martin
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Patent number: 5643914Abstract: This invention relates to a compound of formula 1 ##STR1## or an N-oxide, or a pharmaceutically acceptable salt, where A is CH.sub.2 and Z is S(O).sub.q where q is 0, 1 or 2, CH.sub.2, CHOH, CO, NR.sub.x, or O, orA is C.dbd.O and Z is NR.sub.x ;m is 0-5;R.sub.x is hydrogen or lower alkyl;R is C.sub.1 to C.sub.20 -aliphatic, unsubstituted or substituted five-membered heteroaryl-C.sub.1 to C.sub.10 -aliphatic-O--, unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic where substituted p from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo, or R is C.sub.1 to C.sub.20 -aliphatic-O--, or R is unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic-O-- where substituted phenyl has one or more radicals selected from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo;R.sub.1 is R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)CHO, --(C.sub.1 to C.sub.5 aliphatic)CH.sub.2 OR.sub.5;R.sub.2 and R.sub.Type: GrantFiled: December 19, 1994Date of Patent: July 1, 1997Assignee: SmithKline Beecham CorporationInventor: Robert A. Daines