Chalcogen Bonded Directly To Ring Carbon Of The Tricyclo Ring System Patents (Class 546/86)
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Patent number: 6964970Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar-C0-6alkyl; X is H, C1-4alkyl, OR?, SR?, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R?)2, CH2N(R?) 2, NO2, CF3, CO2R?, CON(R?)2, COR?, NR?C(O)R?, F, Cl, Br, I, or CF3S(O)r—; R? is H, C1-6alkyl or Ar-C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 5, 2003Date of Patent: November 15, 2005Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark Seefeld
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Patent number: 6933303Abstract: This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.Type: GrantFiled: October 18, 2002Date of Patent: August 23, 2005Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Rongyuan Xie, Ravindra R. Yarragunta, Tan Ren
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Patent number: 6916825Abstract: Compounds of the formula 1 in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.Type: GrantFiled: March 28, 2001Date of Patent: July 12, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Wilm Buhr
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Patent number: 6911543Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 1, 2002Date of Patent: June 28, 2005Assignee: Pfizer Inc.Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Steven Charles Reitz
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Patent number: 6908928Abstract: Crystalline monohydrate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.Type: GrantFiled: September 24, 2001Date of Patent: June 21, 2005Assignee: BI Pharma KG.Inventors: Rolf Banholzer, Peter Sieger, Christian Kulinna, Michael Trunk, Manfred Graulich, Peter Specht, Helmut Meissner, Andreas Mathes
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Patent number: 6890933Abstract: The present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.Type: GrantFiled: February 23, 2001Date of Patent: May 10, 2005Assignee: President and Fellows of Harvard CollegeInventors: Yan Feng, Tarun M. Kapoor, Thomas Mayer, Zoltan Maliga, Timothy J. Mitchison, Justin Yarrow
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Patent number: 6849640Abstract: The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: August 6, 2002Date of Patent: February 1, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Michael D. Ennis, Kristine E. Frank, Robert L. Hoffman, Jian-Min Fu
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Patent number: 6841555Abstract: The invention provides novel lavendamycin analogs having the following general formula: and quinoline-5,8-diones having the following formula: Methods of making and using and compositions containing these compounds are also disclosed.Type: GrantFiled: August 29, 2002Date of Patent: January 11, 2005Assignee: Ball State UniversityInventors: Mohammad Behforouz, Nancy C. Behforouz
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Patent number: 6770655Abstract: The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.Type: GrantFiled: January 21, 2003Date of Patent: August 3, 2004Assignee: Aryx TherapeuticsInventors: Xiaoming Zhang, Jurg R. Pfister, Cyrus Becker, Pascal Druzgala
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Patent number: 6720330Abstract: Compounds according to the formula A—Z—W as herein described, wherein A is selected from the groups consisting of: A′—(CH2)n—, A′—(CH2)nSO2—, and A′—(CH2)nCO—, where n is 0 to 4; and A′ is selected from (a) (C6-C10)aryl-, or (b) (C1-C9)heteroaryl-; which groups may be optionally substituted; and pharmaceutically acceptable salts, solvates or hydrates thereof; pharmaceutical compositions thereof; and methods useful to facilitate secretion of growth hormone(GH) in mammals.Type: GrantFiled: September 17, 2001Date of Patent: April 13, 2004Assignee: Pfizer Inc.Inventors: Bruce A. Hay, Bridget M. Cole, Anthony P. Ricketts
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Patent number: 6720331Abstract: A composition includes a substituted dihydro- or tetrahydro-&bgr;-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-&bgr;-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.Type: GrantFiled: April 3, 2002Date of Patent: April 13, 2004Assignees: National Sun Yat-sen University, National Yang-Ming UniversityInventors: Sheau Farn Yeh, Ya-Ching Shen
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Patent number: 6699865Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: January 2, 2003Date of Patent: March 2, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Hale, Xiaoling Xie, Jeremy Green, Jingrong Cao, Christopher Baker, Francois Maltais, James Janetka, Guy Bemis, Michael Mullican, Judith Straub, Qing Tang
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Patent number: 6686372Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective &bgr;3 receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: April 10, 2002Date of Patent: February 3, 2004Assignee: Eli Lilly and CompanyInventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
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Patent number: 6673781Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.Type: GrantFiled: February 1, 2002Date of Patent: January 6, 2004Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Masahiro Fuji, Tetsuo Okada, Makoto Adachi, Tomoyuki Ogawa
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Publication number: 20030158221Abstract: The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.Type: ApplicationFiled: January 21, 2003Publication date: August 21, 2003Inventors: Xiaming Zhang, Jurg R. Pfister, Cyrus Becker, Pascal Druzgala
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Patent number: 6608098Abstract: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.Type: GrantFiled: February 25, 2002Date of Patent: August 19, 2003Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Patent number: 6573272Abstract: Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar—C0-6alkyl; X is H, C1-4alkyl, OR′, SR′, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R′)2, CH2N(R′)2, NO2, CF3, CO2R′, CON(R′)2, COR′, NR′C(O)R′, F, Cl, Br, I, or CF3S(O)r—; R′ is H, C1-6alkyl or Ar—C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2001Date of Patent: June 3, 2003Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark Seefeld
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Patent number: 6528509Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: October 5, 2001Date of Patent: March 4, 2003Assignee: Vertex Pharmacuticals, IncorporatedInventors: Michael Hale, Xiaoling Xie, Jeremy Green, Jingrong Cao, Christopher Baker, Francois Maltais, James Janetka, Guy Bemis, Michael Mullican, Judith Straub, Qing Tang, Robert Mashal
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Patent number: 6528649Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein n, R1, R2, R3, W, Q, and X are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: May 29, 2001Date of Patent: March 4, 2003Assignee: Neurogen CorporationInventors: Guolin Cai, Kenneth Shaw
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Patent number: 6511987Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: GrantFiled: November 10, 2000Date of Patent: January 28, 2003Assignee: Neurogen CorporationInventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchinson
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Patent number: 6492364Abstract: Novel triazolo derivatives represented by the following formula and pharmaceutically acceptable salts thereof, as well as chemokine inhibitors containing the same as an effective component. These are useful as therapeutic agents for allergic diseases such as bronchial asthma and atopic dermatitis; therapeutic agents for inflammatory diseases such as chronic rheumatoid arthritis; therapeutic agents for autoimmune diseases such as ulcerative colitis and nephritis; and as anti-AIDS drugs.Type: GrantFiled: September 22, 2000Date of Patent: December 10, 2002Assignee: Toray Industries, Inc.Inventors: Toshiya Takahashi, Takayuki Imaoka, Noriko Mori, Masayuki Kaneko, Koh Tanida, Yuichi Torii
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Patent number: 6492358Abstract: The present invention relates to novel &bgr;-carboline derivatives of the general formula wherein all the variables are as described within the specification, useful as phosphodiesterase inhibitors. The present invention further relates to use of the described derivatives for the treatment of diseases and conditions related to PDE, for example male erectile dysfunction.Type: GrantFiled: May 2, 2001Date of Patent: December 10, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Zhihua Sui, Mark J. Macielag
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Patent number: 6451809Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof where R1-R4 and A are defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are, therefore, useful in the diagnosis and treatment of anxiety, Down Syndrome, depression, sleep, cognitive and seizure disorders, overdose with benzodiazepine drugs and for enhancement of alertness.Type: GrantFiled: January 16, 2001Date of Patent: September 17, 2002Assignee: Neurogen CorporationInventors: Bogumila Rachwal, Pamela Albaugh, Kenneth Shaw
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Patent number: 6380193Abstract: A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.Type: GrantFiled: September 1, 1998Date of Patent: April 30, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6372908Abstract: A method of preparing a catalyst having the elements and the proportions indicated by the following empirical formula: VSbmAaDdOx where A is one or more Ti, Sn, where Sn is always present D is one or more Li, Mg, Ca, Sr, Ba, Co, Fe, Cr, Ga, Ni, Zn, Ge, Nb, Zr, Mo, W, Cu, Te, Ta, Se, Bi, Ce, In, As, B, Al and Mn wherein m is 0.5 to 10 a is greater than zero to 10 d is zero to 10 x is determined by the oxidation state of the cations present, comprising making an aqueous slurry of a mixture of source batch materials comprising compounds of said elements to be included in the final catalyst, followed by drying and heat calcining the mixture to an active catalyst, wherein the source batch material for the tin is a solution which comprises SnO2.Type: GrantFiled: May 9, 2000Date of Patent: April 16, 2002Assignee: The Standard Oil CompanyInventors: James Frank Brazdil, Jr., Joseph Peter Bartek
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Patent number: 6358946Abstract: A C-6 ring-substituted pyrido[1,2-a]benzimidazole derivative of the formula: methods of preparation and pharmaceutical compositions containing a substituted pyrido[1,2-a]benzimidzole derivative as the active ingredient are disclosed. The substituted pyrido[1,2-a]benzimidazole derivatives are useful in the treatment of central nervous system disorders.Type: GrantFiled: July 20, 2000Date of Patent: March 19, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Allen B. Reitz, Samuel O. Nortey, Pauline Sanfilippo, Malcolm K. Scott
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Patent number: 6350757Abstract: A compound selected from those of formula (I): wherein: represents single or double bond, R1 represents hydrogen, alkyl, —R6-aryl, —R6-cycloalkyl, —R6-heterocycle, —CO2R7—, —COR8, or —CONHR8, wherein R6, R7, and R8 are as defined in the description, R2 represents cyano, mono- or di-alkylaminoalkylaminocarbonyl, —CO2R8, —CONHR8, —NR8R9, —NHCO2R7, or —COR8 wherein R7, R8, and R9 are as defined in the description, R3 and R4 together form (C3-C10)cycloalkyl, R5 represents hydrogen, alkyl, or arylalkyl, Ra, Rb, Rc, Rd, which may be identical or different, represent a group as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of CNS disorders.Type: GrantFiled: July 21, 2000Date of Patent: February 26, 2002Assignee: Les Laboratoires ServierInventors: Solo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Jean-Daniel Brion, Mark Millan, Anne Dekeyne, Jean Boutin
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Publication number: 20010011133Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: January 16, 2001Publication date: August 2, 2001Applicant: Neurogen Corporation.Inventors: Bogumila Rachwal, Pamela Albaugh, Kenneth Shaw
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Publication number: 20010009916Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: 1Type: ApplicationFiled: May 13, 1999Publication date: July 26, 2001Inventor: ARTHUR G. ROMERO
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Patent number: 6265228Abstract: Combinatorial chemical libraries of the Formula [S]—C(O)—L′—Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and —L′—Z is a linker/ligand residue. In these libraries, Z is and Y is —P(O)(OR6)(OR7), —CH(OH)—COR8, —CH,CH═CH2—CH2CH(OH)CH2OH, —CH2CHO, —CH2CH2OH, —CH2CH2OC(O)NHR26, —CH2CH2NR27R28, or The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.Type: GrantFiled: June 18, 1999Date of Patent: July 24, 2001Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Timothee Felix Herpin, Yvonne Class Shimshock, Cullen Lee Cavallaro
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Patent number: 6245775Abstract: Cycloakano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carbonylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.Type: GrantFiled: July 3, 1997Date of Patent: June 12, 2001Assignee: Bayer AktiengesellschaftInventors: Ulrich Müller, Richard Connell, Siegfried Goldmann, Rudi Grützmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
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Patent number: 6177569Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof where R1-R4 and A are defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are, therefore, useful in the diagnosis and treatment of anxiety, Down Syndrome, depression, sleep, cognitive and seizure disorders, overdose with benzodiazepine drugs and for enhancement of alertness.Type: GrantFiled: August 25, 1999Date of Patent: January 23, 2001Assignee: Neurogen CorporationInventors: Bogumila Rachwal, Pamela Albaugh, Kenneth Shaw
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Patent number: 6175014Abstract: The invention provides a process for the preparation of a compound of general formula (I): wherein Im represents an imidazolyl group of the formula: and R1 represents a hydrogen atom or a group as herein defined including —CO2R5, —COR5, —CONR5R6 or —SO2R5 wherein R5 and R6, which may be the same or different, are as herein defined with the proviso that R5 does not represent a hydrogen atom when R1 represents a group —CO2R5 or —SO2R5; one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6alkyl, C3-7cycloaklyl, C3-6alkenyl, phenyl or phenyl C1-3alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6alkyl group; and n represents 2 or 3; which comprises reacting a compound of formula (II) or a protected derivative thereof, with a compound of formula (III): HOCH2-Im (III) or a salt thereof in the presence of an acid at an elevatType: GrantFiled: October 18, 1993Date of Patent: January 16, 2001Assignee: Glaxo Group LimitedInventors: Ian Harold Coates, Alexander William Oxford, Peter Charles North, Thomas Miller, Anthony David Baxter, Kevin Ian Hammond
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Patent number: 6159985Abstract: The subject invention involves compounds having the structure: wherein the C.sub..alpha. --N.sub..beta. and C.sub.5 -C.sub.6 bonds are independently single or double bonds, R1 is selected from alkyl, aryl, and heterocycle; R2-R13 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable salts thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.Type: GrantFiled: September 21, 1999Date of Patent: December 12, 2000Assignee: The Procter & Gamble CompanyInventors: Song Liu, David Edward Portlock, Schwe Fang Pong
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Patent number: 6093723Abstract: This invention relates to 4-substituted .beta.-carbolines and .beta.-carboline analogs that inhibit Ca.sup.+2 influx and interleukin-2 (IL-2) production. The 4-substituted .beta.-carbolines and .beta.-carboline analogs of this invention are represented by formula (I): ##STR1## wherein Q, n, R, R', R" and R.sub.1 -R.sub.4 are as defined herein. This invention also relates to methods for producing .beta.-carbolines. Because of their selective immunomodulating properties, the compounds and pharmaceutical compositions of this invention are particularly well suited for preventing and treating immune disorders, including autoimmune disease, inflammatory disease, organ transplant rejection and other disorders associated with IL-2 mediated immune response.Type: GrantFiled: August 8, 1997Date of Patent: July 25, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Clara K Miao, Ian F. Potocki, Roger J. Snow, Karl D. Hargrave, Thomas P. Parks
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Patent number: 6075021Abstract: Compounds of general formula (I) ##STR1## in which the variables are as defined in the specification, their preparation and their application in therapeutics.Type: GrantFiled: April 7, 1999Date of Patent: June 13, 2000Assignee: SynthelaboInventors: Yannick Evanno, Mireille Sevrin, Christian Maloizel, Odette Legalloudec, Pascal George
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Patent number: 6066633Abstract: Compound of formula (I): ##STR1## in which: m represents an integer from 1 to 4 inclusive, and n and p an integer from 0 to 4 inclusive,X represents O, S or a single bond,R.sub.1 represent hydrogen or halogen, or alkyl, alkoxy, hydroxy, trihaloalkyl or trihaloalkoxy,R.sub.2, R.sub.3 and R.sub.4, which may be same or different, each represents hydrogen or alkyl,R.sub.5 represents hydrogen or halogen, or alkoxy, aryloxy or heteroaryloxy,R.sub.6, R.sub.7 and R.sub.8, which may be same or different, each represents hydrogen or alkyl, or together form, with the atoms carrying them respectively, an optionally substituted heterocycle,R.sub.9 represents SO.sub.3 H, --CO.sub.2 R.sub.10, --CO--NR.sub.11 R.sub.12, or --NR.sub.13 R.sub.14, wherein R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14 each represents hydrogen or alkyl or together (R.sub.11 /R.sub.12 ; R.sub.13 /R.sub.Type: GrantFiled: November 13, 1998Date of Patent: May 23, 2000Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Georges Remond, Joseph Paladino, Ghanem Atassi, Alain Pierre, Gordon Tucker, Jacqueline Bonnet, Massimo Sabatini
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Patent number: 6057325Abstract: This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.Type: GrantFiled: November 9, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutia, N.V.Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 6030983Abstract: The invention provides novel lavendamycin analogs having the following general formula: ##STR1## and quinoline-5,8-diones having the following formula: ##STR2## Methods of making and using and compositions containing these compounds are also disclosed.Type: GrantFiled: October 31, 1997Date of Patent: February 29, 2000Assignee: Ball State UniversityInventors: Mohammad Behforouz, Nancy C. Behforouz
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Patent number: 6020342Abstract: Compounds of the formula: ##STR1## which are useful as anti-ulcer agent are provided.Type: GrantFiled: October 21, 1997Date of Patent: February 1, 2000Assignee: Shinnippon Pharmaceutical, Inc.Inventors: Hironori Tanaka, Kazuyoshi Fukuzumi, Takeshi Togawa, Kimiko Banno, Toshihisa Ushiro, Masaaki Morii, Takafumi Nakatani
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Patent number: 6001847Abstract: A compound of formula ##STR1## and salts and solvates thereof, wherein R.sup.0, R.sup.1, and R.sup.2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.Type: GrantFiled: June 8, 1998Date of Patent: December 14, 1999Assignee: ICOS CorporationInventors: Alain Claude-Marie Daugan, Richard Frederic LaBaudiniere
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Patent number: 5958972Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: May 20, 1997Date of Patent: September 28, 1999Assignee: Warner-Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Joseph Armand Picard, Andrew David White, Qi-Zhuang Ye
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Patent number: 5952498Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido?1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido?1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.Type: GrantFiled: March 31, 1997Date of Patent: September 14, 1999Assignee: Bayer AktiengesellschaftInventors: Jan-Bernd Lenfers, Peter Fey, Paul Naab, Kai Van Laak
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Patent number: 5922731Abstract: A compound of the general formula 1; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: June 30, 1997Date of Patent: July 13, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Allen B. Reitz, Louis J. Fitzpatrick, Alfonzo D. Jordan, Pauline J. Sanfilippo
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Patent number: 5886004Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful 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: March 24, 1997Date of Patent: March 23, 1999Assignee: Eli Lilly and CompanyInventors: James E. Audia, David L. G. Nelson
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Patent number: 5880126Abstract: 9H-Pyrido?3,4-b!indole compounds have a pronounced leukotriene-B.sub.4 antagonistic action, and thus show a completely different spectrum of activity than known .beta.-carbolines.Type: GrantFiled: December 8, 1997Date of Patent: March 9, 1999Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Buchmann, Hartmut Rehwinkel, Frank Schneider, Wolfgang Frohlich, Claudia Giesen, Hartwig Hennekes
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Patent number: 5866587Abstract: Compound of formula (I): ##STR1## in which: m, n, which are identical or different, represent 0, 1 or 2,R.sub.1, R.sub.2, which are identical or different, represent hydrogen, optionally substituted alkyl, aryl, or form with the carbon atom carrying them carbonyl or (C.sub.3 -C.sub.7)cycloalkyl,R.sub.3 represents hydrogen, alkyl, hydroxyl or aryl,R.sub.4 represents any of the groups as defined in the description,X represents --SO.sub.2 --, --CO-- or --SO.sub.2 NH--,R.sub.5 represents optionally substituted alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl or heterocyclic,A represents an aryl ring or a heterocycle,its isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitors.Type: GrantFiled: April 25, 1997Date of Patent: February 2, 1999Assignee: Adir Et CompagnieInventors: Guillaume de Nanteuil, Joseph Paladino, Georges Remond, Ghanem Atassi, Alain Pierre, Gordon Tucker, Jacqueline Bonnet, Massimo Sabatini
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Patent number: 5861410Abstract: 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: April 9, 1997Date of Patent: January 19, 1999Assignee: 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: 5856334Abstract: Specified imidazoquinoline derivatives represented by the formula (I): ##STR1## where Q represents an optionally substituted phenyl, pyridyl or furyl group; Y represents either a hydrogen atom or, when taken together with Z, an oxygen atom and a methylene group; Z represents a hydrogen atom, a hydroxymethyl group, a carboxymethyl group, a 2-oxo-1-pyrrolidinyl group or the following formula (III):--A--R.sup.2 (III)(where A represents an oxygen atom, a sulfur atom or the group --NH--);or salts of such derivatives inhibit the increase of eosinophils and are useful as agents for preventing and/or treating diseases that manifest the increase of eosinophils.Type: GrantFiled: January 28, 1997Date of Patent: January 5, 1999Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidenori Mochizuki, Kazuo Kato, Ichiro Yamamoto, Kiyoshi Mizuguchi
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Patent number: RE38452Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 and R2 are independently hydrogen, C1-6 alkyl or R1 and R2 are joined to form pyrrolidine, piperidine, morpholine or imidazole. X is OCH3, SO2R3, SO2CF3 or CN where R3 is C1-6 alkyl or an Aryl; and Y is hydrogen, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2. These new compounds are suitable for treating anxiolytic disorder, schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure or treating migraine headaches in patients in need of such treatment.Type: GrantFiled: May 13, 1999Date of Patent: March 2, 2004Assignee: Pharmacia & Upjohn CompanyInventor: Arthur Glenn Romero