Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
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Patent number: 6476019Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.Type: GrantFiled: August 7, 2000Date of Patent: November 5, 2002Assignee: Sepracor Inc.Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
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Publication number: 20020161005Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.Type: ApplicationFiled: July 28, 1999Publication date: October 31, 2002Inventors: JAY R. LULY, YOSHISUKE NAKASATO, ETSUO OHSHIMA, HIROKI SONE, OSAMU KOTERA, GERALDINE C. B. HARRIMAN
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Stype 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
Publication number: 20020161231Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: 1Type: ApplicationFiled: April 10, 2002Publication date: October 31, 2002Applicant: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara -
Patent number: 6465481Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R4, R5a, R5b, R6, R9, X, A and B have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: GrantFiled: September 7, 2000Date of Patent: October 15, 2002Assignee: AstraZeneca ABInventors: Marianne Frantsi, Kurt-Jürgen Hoffmann, Gert Strandlund
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Publication number: 20020147207Abstract: The present invention relates compounds of the formula (I): 1Type: ApplicationFiled: April 1, 2002Publication date: October 10, 2002Inventors: Ian Thomas Huscroft, Janusz Jozef Kulagowski, Piotr Antoni Raubo
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Patent number: 6444819Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: October 11, 2001Date of Patent: September 3, 2002Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Salva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Publication number: 20020119973Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.Type: ApplicationFiled: July 28, 1999Publication date: August 29, 2002Inventors: JAY R. LULY, YOSHISUKE NAKASATO, ETSUO OHSHIMA, HIROKI SONE, OSAMU KOTERA, GERALDINE C.B. HARRIMAN
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Publication number: 20020103217Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: January 8, 2002Publication date: August 1, 2002Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Publication number: 20020099065Abstract: The invention related to novel 3, 5, and/or 6 swainsonine analogues, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.Type: ApplicationFiled: October 29, 2001Publication date: July 25, 2002Applicant: GlycoDesign Inc.Inventors: Rajan Shah, Jeremy Carver, Jose Marino-Albernas, Igor Tvaroska, Francois Daniel Tropper, James Dennis
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Patent number: 6420130Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.Type: GrantFiled: April 28, 1999Date of Patent: July 16, 2002Assignee: Aurora Biosciences CorporationInventors: Lewis R. Makings, Gregor Zlokarnik
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Patent number: 6410557Abstract: Novel dry skin remedies useful for treatment dry skin, containing as the active ingredient spiro [oxathiolane-quinuclidine] derivatives represented by general formula (I) or acid addition salts thereof, desirably cis-2-methylspiro [1,3-oxathiolane-5,3′-quinuclidine] hydrochloride. The remedies promote the secretion of sebaceous and sweat glands through oral or parenteral administration to treat dry skin, thus being useful as drugs.Type: GrantFiled: July 5, 2001Date of Patent: June 25, 2002Assignee: Daiichi Pharmaceutical Col, Ltd.Inventors: Keiji Hayashi, Hirohiko Arisawa, Hiroaki Masunaga
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Patent number: 6410505Abstract: A class of predominantly hydrophilic 1,8-naphthalimide dyes. The dye contains at least two 1,8-naphthalimide ring systems, joined by a spacer moiety. Each of the 1,8-naphthalimide ring system has a ring nitrogen atom and bears, at the 4 position, an amino nitrogen atom, carrying a hydrogen. The remaining unsatisfied valences, if present, of the ring nitrogen atoms or the amino nitrogen atoms, or all, are occupied by one or more alkyl substituents. Each of the 1,8-naphthalimide ring system is free of an azo substituent and is also free of a nucleofuge. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species can cause structural changes in lipid and any associated proteins and polypeptides, extra- or intra-cellular or transmembrane, leading to polymerization and crosslinking.Type: GrantFiled: June 28, 1999Date of Patent: June 25, 2002Assignee: Microbiomed Corp.Inventors: David E. Lewis, Ronald E. Utecht, Millard M. Judy, J. Lester Matthews
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Patent number: 6410548Abstract: Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 12, 2001Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Ravi P. Nargund, Zhixiong Ye, Brenda L. Palucki, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
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Publication number: 20020058813Abstract: Compounds of general structural formula I such as that shown in structural formula II 1Type: ApplicationFiled: June 29, 2001Publication date: May 16, 2002Inventors: Ying-Duo Gao, Douglas J. Macneil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6359135Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: April 9, 2001Date of Patent: March 19, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6352995Abstract: The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein n is 1 or 2 or 3, A is —O—, —S—, —CH—, —O—CH2—, or —CH2—O—; B is —O—, —S—, —CH2—, —0—CH2—, or —CH2—O—; and C is N, or —CR1—; D is N, or —CR2—; E is N, or —CR3—; and F is N, or —CR4—; wherein R1, R2, R3 and R4 each independently are selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6 membered heteroaryl group. The compounds of the invention are useful for the treatment of disorders or diseases responsive to the activity of nicotinic ACh receptor modulators.Type: GrantFiled: October 14, 1999Date of Patent: March 5, 2002Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldbaek Nielsen, Elsebet Nielsen
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Patent number: 6348472Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of spiroisoquinolinone derivatives of Formula I. As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.Type: GrantFiled: June 2, 2000Date of Patent: February 19, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Ildiko Antal, Leah M. Giupponi, Robert H. Stoffel, Marc A. Bruce
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Patent number: 6342459Abstract: The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which a further ring system is bonded to the f side of the naphthopyran. The inventive photochromic dyes generally have the general formula (I) wherein n, R1, R2, R3, X, B and B′ are defined as in claim 1. The inventive compounds are distinguished by good darkening and decolorizing properties and a very good service life.Type: GrantFiled: May 18, 2000Date of Patent: January 29, 2002Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Claudia Mann, Udo Weigand
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Patent number: 6329385Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1999Date of Patent: December 11, 2001Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
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Patent number: 6326375Abstract: Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents nitrogen; Y represents an optionally substituted imino or oxygen atom, which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.Type: GrantFiled: August 18, 2000Date of Patent: December 4, 2001Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
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Patent number: 6316437Abstract: Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing 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 can be achieved.Type: GrantFiled: September 27, 2000Date of Patent: November 13, 2001Assignee: Merck & Co., Inc.Inventor: Jacob M. Hoffman
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Patent number: 6313299Abstract: The present invention relates to quinolonecarboxylic acid derivatives having more excellent and broad antibacterial activities than the existing quinolone-series antibiotics. More specifically, it pertains to novel quinolonecarboxylic acid derivatives represented by following formula 1, which have a derivative of 7-[8-(alkoxyimino)-2,6-diazaspiro[3.4]oct-6-yl] as a substituent, and pharmaceutically acceptable salts and isomers thereof: Wherein, A is C—H, C—F, C—Cl, C—O—CH3 or N; Y is H or amino; R1 is cyclopropyl or 2,4-difluorophenyl; R2 is C1-4 alkyl; and R3 is H or C1-4 alkyl.Type: GrantFiled: December 23, 1999Date of Patent: November 6, 2001Assignee: Dong Wha Pharmaceutical Industrial Co., Ltd.Inventors: Sung-Joon Yoon, Yong-Ho Chung, Chi-Woo Lee, Yoon-Seok Oh, Nam-Doo Kim, Jae-Kyung Lim, Yoon-Ho Jin
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Patent number: 6303593Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Christopher Forbes, Shouwu Miao, William H. Parsons, Kathleen Rupprecht, Frank Kayser
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Patent number: 6294545Abstract: A compound of formula (I) wherein A is a bidentate group of the formula: XC═CY or XCH—CHY (wherein X and Y are independently hydrogen, hydroxy, acyloxy, alkoxy, cyano or halogen); and Ar is optionally substituted phenyl or optionally substituted heteroaryl; or an acid addition salt, quaternary ammonium salt or N-oxide derived therefrom; provided that when A is CH2—H2 then Ar is neither 5-chloropyrid-3-yl nor 5-trifluoromethylpyrid-3-yl; an insecticidal, acaricidal or nematicidal composition comprising an insecticidally, acaricidally or nematicidally effective amount of a compound of formula (I); a method of using a compound of formula (I) to combat or control insect, acarine or nematode pests; and processes for preparing a compound of said formula.Type: GrantFiled: May 12, 2000Date of Patent: September 25, 2001Assignee: Syngenta LimitedInventors: Christopher John Urch, Roger Salmon
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Patent number: 6294534Abstract: Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: June 10, 1999Date of Patent: September 25, 2001Assignee: Merck & Co., Inc.Inventors: Ravi P. Nargund, Brenda L. Palucki, Zhixiong Ye, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
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Patent number: 6288083Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: September 4, 1998Date of Patent: September 11, 2001Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
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Patent number: 6288084Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1999Date of Patent: September 11, 2001Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
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Patent number: 6277991Abstract: The present invention relates to the use of small organic compounds acting as opioid receptor ligands for the treatment of vasomotor disturbances. In particular the present invention relates to the use of triaza-spiro compounds of formula wherein R1, R2, R3, R4, R5, z and n are defined in the specification, for the treatment of migraine, non-insulin dependent diabetes mellitus (type II diabetes), sepsis, inflammation, incontinence and/or vasomotor disturbances, in particular the peripheral vasomotor effects known as hot flushes or hot flashes.Type: GrantFiled: May 13, 1999Date of Patent: August 21, 2001Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Brett Watson, Christain Thomsen
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Patent number: 6258469Abstract: The benzidine derivatives of the invention are symmetrical compounds of the following structure: in which: n=1, 2 or 3; R1=H, phenyl or 1-naphthyl, R2 and R3 together form a fused benzene ring, an a- or b-fused naphthalene ring or a fused 1,2,5-thiadiazole ring.Type: GrantFiled: August 17, 1999Date of Patent: July 10, 2001Assignee: Siemens AktiengesellschaftInventors: Andreas Kanitz, Jörg Schumann
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Patent number: 6251890Abstract: The present invention relates to carbapenem antibacterial agents of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 represents: in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.Type: GrantFiled: March 13, 2000Date of Patent: June 26, 2001Assignee: Merck & Co., Inc.Inventors: Timothy A. Blizzard, Ronald W. Ratcliffe, Jerry D. Morgan, II, Robert R. Wilkening
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Patent number: 6211369Abstract: Spiro compounds of the formula (I), where X1, X2, X3, X4 are identical or different and are —S—, —O—, —NR5—, —CR5═N— or —CR5═CH—, with the proviso that at least one of the groups X1-4 is different from —CR5═CH—, are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.Type: GrantFiled: January 3, 2000Date of Patent: April 3, 2001Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Josef Salbeck, Donald Lupo
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Patent number: 6211189Abstract: There are provided novel compounds of formula (I) wherein A represents an aromatic carbocyclic ring or a 5- or 6-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S; X represents —(CH2)n— wherein n represents zero or 1; and R1, R2 and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and tautomers thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: May 31, 2000Date of Patent: April 3, 2001Assignee: AstraZeneca UK LimitedInventors: Peter Hamley, Austen Pimm, Alan Tinker
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Patent number: 6184221Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.Type: GrantFiled: August 4, 1998Date of Patent: February 6, 2001Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann, Joachim Brendel
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Patent number: 6174940Abstract: The present invention relates to mixtures comprising the compound I in a proportion of 65-95% by weight, the compound II in a proportion of 5-35% by weight and the compound III in a proportion of 0-10% by weight wherein the substituents are as defined in the description, and to mixtures with other compounds. The mixtures are suitable for stabilizing organic material against the effect of light and heat.Type: GrantFiled: August 13, 1998Date of Patent: January 16, 2001Assignee: Clariant GmbHInventors: Thomas St{umlaut over (a)}hrfeldt, Mathias Mehrer, Matthias Z{umlaut over (a)}h, Gerhard Pfahler
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Patent number: 6166037Abstract: The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: August 27, 1998Date of Patent: December 26, 2000Assignee: Merck & Co., Inc.Inventors: Richard J. Budhu, Edward Holson, Jeffrey J. Hale, Christopher Lynch, Malcolm Maccoss, Scott C. Berk, Sander G. Mills, Christopher A. Willoughby
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Patent number: 6166034Abstract: Novel spiro piperdine derivatives of formula (I), in which P.sup.1, P.sup.2, R.sup.1, R.sup.2, R.sup.2 ', R.sup.3, m, A, E, G, X, Y, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 have the meanings defined in claim 1 are described, as well as their use for preparing medicaments which have 5HT1D receptor antagonist activity.Type: GrantFiled: May 8, 1998Date of Patent: December 26, 2000Assignee: SmithKline Beecham p. l. cInventor: Francis David King
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Patent number: 6130101Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.Type: GrantFiled: September 23, 1997Date of Patent: October 10, 2000Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Wai-Yee Leung, Richard P. Haugland
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Patent number: 6117874Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LTB.sub.4 antagonists. The compounds of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.Type: GrantFiled: February 1, 1999Date of Patent: September 12, 2000Assignee: Pfizer Inc.Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
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Patent number: 6117880Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are also orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostastin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. Further objects will become apparent from reading the following description.Type: GrantFiled: October 28, 1998Date of Patent: September 12, 2000Assignee: Merck & Co., Inc.Inventors: Liangquin Guo, Ralph T. Mosley, Alexander Pasternak, Arthur A. Patchett, Lihu Yang
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Patent number: 6114529Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R.sup.0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: ##STR2## wherein the symbols are as defined above.Type: GrantFiled: October 18, 1999Date of Patent: September 5, 2000Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 6110914Abstract: A compound of formula ##STR1## wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H.sub.2 or F.sub.2 ;A is N or C(R.sup.2); G is N or C(R.sup.3); D is N or C(R.sup.4);with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;R.sup.1 is hydrogen or C.sub.1 to C.sub.4 alkyl;R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.Type: GrantFiled: October 29, 1998Date of Patent: August 29, 2000Assignee: Astra AktiebolagInventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
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Patent number: 6057333Abstract: Discorhabdin compounds are derived from marine sponges of the genus Batzella or prepared by synthetic methods. These compounds, and pharmaceutical compositions containing them as active ingredients, are useful as immunomodulatory, antitumor agents, and/or caspase inhibitors.Type: GrantFiled: July 24, 1998Date of Patent: May 2, 2000Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Sarath P. Gunaskera, Peter J. McCarthy, Shirley A. Pomponi, Amy E. Wright, Ross E. Longley
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Patent number: 6046333Abstract: The present invention is directed to a novel convergent process for the preparation of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'- yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.Type: GrantFiled: October 21, 1997Date of Patent: April 4, 2000Assignee: Merck & Co., Inc.Inventors: Ilias Dorziotis, Ioannis Houpis, Audrey Molina, Ralph Volante
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Patent number: 6013652Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.Type: GrantFiled: December 4, 1997Date of Patent: January 11, 2000Assignee: Merck & Co., Inc.Inventors: Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Yuan-Ching P. Chiang, Patrick T. Dunn, Hiroo Koyama
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Patent number: 6013802Abstract: The present invention describes a family of fluorescent indicators for metal cations. The indicators are fluorophore conjugates of pyridyl-based metal ion chelators. The indicators are very sensitive detection as quantification reagents for a variety of metals, in a variety of oxidation states, even in the presence of high concentrations of Ca.sup.2+, Na.sup.+, or K.sup.+ or other ions, such as is found in seawater, making them highly useful for assaying physiological samples, biological samples, or environmental samples.Type: GrantFiled: February 7, 1997Date of Patent: January 11, 2000Assignee: Molecular Probes, Inc.Inventors: Brian Matthew Hoyland, Michael A. Kuhn, Richard P. Haugland
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Patent number: 6011150Abstract: There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.Type: GrantFiled: May 15, 1995Date of Patent: January 4, 2000Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kazuhiko Kondo
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Patent number: 6002000Abstract: Methods are disclosed for determining an analyte in a medium suspected of containing the analyte. One method comprises providing (1) combining a medium suspected of containing the analyte and a novel chemiluminescent compound, (2) combining a means for chemically activating the chemiluminescent compound; and (3) detecting the amount of luminescence generated by the chemiluminescent compound. The amount of luminescence generated is related to the amount of analyte in the medium. The chemiluminescent compound can be chemically activated by hydrogen peroxide. Compositions and kits are also disclosed.Type: GrantFiled: June 11, 1996Date of Patent: December 14, 1999Assignee: Dade Behring Marburg GmbHInventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
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Patent number: 5962462Abstract: The present invention is directed to spiro-substituted azacycles of the Formula 1: ##STR1## (wherein R.sub.1, l, m, Q, W, X, Y, and Z are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: December 12, 1997Date of Patent: October 5, 1999Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Malcolm Maccoss, Martin S. Springer
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Patent number: 5962469Abstract: The present invention is directed to novel cyclic nitrones and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in which radicals either damage or destroy tissues via oxidation, and pharmaceutical compositions containing these cyclic nitrones.Type: GrantFiled: November 26, 1997Date of Patent: October 5, 1999Assignee: Hoechst Marion Roussel Inc.Inventors: Craig E. Thomas, Thomas L. Fevig, Stephen M. Bowen, Robert A. Farr, Albert A. Carr, David A. Janowick
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Patent number: 5962465Abstract: The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.Type: GrantFiled: January 29, 1998Date of Patent: October 5, 1999Assignee: American Home Products CorporationInventors: Gary P. Stack, Richard E. Mewshaw, Byron A. Bravo, Young H. Kang