The Additional Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/61)
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Patent number: 6693116Abstract: The present application relates to compounds of the formula wherein R1 is hydrogen, halogen or lower alkoxy; R2 is hydrogen or is —C(O)-lower alkyl or —C(O)-phenyl, wherein the phenyl ring is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl, or is —C(O)-furanyl or —C(O)-thiophenyl, wherein the rings are unsubstituted or substituted by halogen; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases associated with the adenosine A2 receptor.Type: GrantFiled: September 18, 2002Date of Patent: February 17, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
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Patent number: 6689790Abstract: A compound of formula wherein R1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH2)n—C(O)NRaRb, —(CH2)n,-heteroaryl, —(CH2)n-aryl, —(CH2)n—CN, —(CH2)n—O-lower alkyl or —(CH2)n-cycloalkyl, or R′ and R″ form together with the N-atom a five or six-membered non-aromatic ring, containing no or one additional heteroatom selected from the group consiting of O and S, and said ring being unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, —C(O)NRaRb and —(CH2)n—O-lower alkyl, and RaRb are independently from each other hydrogen or lower alkyl; R2 is aryl or heteroaryl, unsubstituted or substituted by lower alkyl or halogen; and n is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 7, 2002Date of Patent: February 10, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
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Patent number: 6664252Abstract: This invention pertains to compounds having the structure: wherein NR1R2 is a substituted or unsubstituted 4-8 membered ring; wherein R3 is a substituted or unsubstituted four to six membered ring; wherein R5 is H, alkyl, substituted alkyl, aryl, arylalkyl, amino, substituted aryl; wherein R6 is H, alkyl, substituted alkyl, or cycloalkyl; with the proviso that NR1R2 is not 3-acetamido piperadino, 3-hydroxy pyrrolidino, 3-methyloxy carbonylmethyl pyrolidino, or 3-aminocarbonylmethyl pyrrolidino; with the proviso that NR1R2 is 3-hydroxymethyl piperadino only when R3 is 4-pyridyl; which specifically inhibit the adenosine A2a receptor and the use of these compounds to treat a disease associated with A2a adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.Type: GrantFiled: December 1, 2000Date of Patent: December 16, 2003Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo L. Castelhano, Bryan McKibben, David J. Witter
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Patent number: 6635762Abstract: Novel pyrrolo[2,3-d]pyrimidine compounds useful as inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 as well as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases are described.Type: GrantFiled: June 17, 1999Date of Patent: October 21, 2003Assignee: Pfizer Inc.Inventors: Todd A. Blumenkopf, Mark E. Flanagan, Matthew F. Brown, Paul S. Changelian
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Patent number: 6635771Abstract: Compounds of the formula in which R, R′, R7-R11, X, n1 and n3 are as defined herein. These compounds are useful as intermediates for preparing pharmaceutical compounds having pharmacological activity as chemical inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes.Type: GrantFiled: November 22, 2002Date of Patent: October 21, 2003Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Patent number: 6630475Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of ParkinsoType: GrantFiled: May 24, 2001Date of Patent: October 7, 2003Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil
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Patent number: 6627628Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).Type: GrantFiled: May 17, 2001Date of Patent: September 30, 2003Assignee: Aventis Pharma Deutschland, GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
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Patent number: 6624171Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.Type: GrantFiled: August 28, 2001Date of Patent: September 23, 2003Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
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Patent number: 6617329Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.Type: GrantFiled: August 23, 2001Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Patent number: 6600038Abstract: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.Type: GrantFiled: August 30, 2001Date of Patent: July 29, 2003Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Kazuyuki Tomisawa
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Patent number: 6599917Abstract: The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them.Type: GrantFiled: March 19, 2002Date of Patent: July 29, 2003Assignee: Eisai Co., Ltd.Inventors: Toshimi Okada, Nobuyuki Kurusu, Keigo Tanaka, Kazuki Miyazaki, Daisuke Shinmyo, Hiroyuki Sugumi, Hironori Ikuta, Hironobu Hiyoshi, Takao Saeki, Mamoru Yanagimachi, Masashi Ito
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Patent number: 6593338Abstract: 3-Substituted 2,7-naphthyridine derivatives of formula (1) are described: wherein L1 and L1 is each a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; Ar2 is an optionally substituted aromatic or heteroaromatic linking group; R16 is the group —L3(Alk2)tL4R20 in which L3 and L4 which may be the same or different is each a covalent bond or a linker atom or group, t is zero or the integer 1, Alk2 is an optionally substituted aliphatic or heteroaliphatic chain and R20 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof.Type: GrantFiled: November 27, 2001Date of Patent: July 15, 2003Assignee: Celltech R&D LimitedInventors: John Clifford Head, Catherine McKay, John Robert Porter
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Patent number: 6583146Abstract: Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.Type: GrantFiled: July 12, 2001Date of Patent: June 24, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Naoyuki Kanzaki, Seiji Miwatashi
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Patent number: 6579868Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, —CH═CH— or —C≡C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.Type: GrantFiled: July 5, 2000Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Nagata, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi
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Patent number: 6548509Abstract: This invention encompasses compounds of the formula wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: March 23, 2001Date of Patent: April 15, 2003Assignee: Neurogen CorporationInventor: Jun Yuan
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Patent number: 6514988Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, pplycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.Type: GrantFiled: September 29, 2000Date of Patent: February 4, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuo Choh, Koichi Kato, Shuji Hinuma
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Patent number: 6509338Abstract: The present invention describes novel pyrazolo[1,5-a]triazines of formula: wherein R3 is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.Type: GrantFiled: June 14, 1999Date of Patent: January 21, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard Eric Olson, William Eric Frietze
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Patent number: 6506772Abstract: Substituted [1,2,4]triazolo[1,5a]pyridine derivatives and pharmaceutically active salts thereof with activity as adenosine receptor ligands are disclosed. These compounds are useful for treatment of diseases responsive to modulation of the adenosine receptor.Type: GrantFiled: November 30, 2001Date of Patent: January 14, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Brodbeck, Matthias Heinrich Nettekoven
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Patent number: 6476030Abstract: Compounds according to Formula (I): or a salt or prodrug thereof, have good affinity as ligands for the alpha2 and/or alpha3 subunit of the human GABAA receptor and are useful for treatment of disorders of the central nervous system, including anxiety and convulsions.Type: GrantFiled: June 8, 2001Date of Patent: November 5, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Andrew Mitchinson, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
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Patent number: 6476022Abstract: This invention provides novel oxathiepino[6,5-b]dihydropyridines. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.Type: GrantFiled: June 23, 2000Date of Patent: November 5, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John H. Dodd, James R. Henry, Kenneth C. Rupert, James L. Bullington, Daniel A. Hall
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Patent number: 6472404Abstract: The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are hydroxyethylamine tripeptide mimetics which act as inhibitors of the HIV aspartyl protease, an essential enzyme in the replicative life cycle of HIV. Consequently, the compounds of this invention may be advantageously used in the treatment of HIV infection, either alone or in combination with other inhibitors of HIV viral replication or with pharmacoenhancers such as cytochrome P450 inhibitors.Type: GrantFiled: November 20, 2001Date of Patent: October 29, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Armstrong Martin, Sally Redshaw, Steven Swallow, Gareth John Thomas
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Patent number: 6458790Abstract: Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: March 20, 2001Date of Patent: October 1, 2002Assignee: Merck & Co., Inc.Inventors: Brenda L. Palucki, Khaled J. Barakat, Liangqin Guo, Yingjie Lai, Ravi P. Nargund, Min K. Park, Patrick G. Pollard, Iyassu K. Sebhat, Zhixiong Ye
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Patent number: 6455534Abstract: Described are compounds and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: where: one of A or E is nitrogen, with remaining atoms carbon; X=O, S, NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms). Other terms are described in the specification.Type: GrantFiled: April 2, 2001Date of Patent: September 24, 2002Assignee: Warner-Lambert CompanyInventors: Alexander James Bridges, William Alexander Denny, David Fry, Alan Kraker, Robert Frederick Meyer, Gordon William Rewcastle, Andrew Mark Thompson
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Patent number: 6444666Abstract: A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.Type: GrantFiled: August 27, 1998Date of Patent: September 3, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
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Patent number: 6420365Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.Type: GrantFiled: January 17, 2001Date of Patent: July 16, 2002Assignee: Neurogen CorporationInventors: John M. Peterson, Alan Hutchison, Kenneth Shaw, Kevin Hodgetts, George D. Maynard, Richard Lew
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Patent number: 6407114Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.Type: GrantFiled: October 22, 1999Date of Patent: June 18, 2002Assignee: Pfizer Inc.Inventors: Mark Edward Bunnage, John Paul Mathias, Stephen Derek Albert Street, Anthony Wood
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Publication number: 20020010335Abstract: This invention relates to a process for preparing compounds of the Formula I, 1Type: ApplicationFiled: August 3, 2001Publication date: January 24, 2002Inventors: Charles K. Chiu, David A. Griffith
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Publication number: 20020010170Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: March 16, 2001Publication date: January 24, 2002Inventors: Francesco Salituro, Guy Bemis, Huai Gao, Ghotas Evindar
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Patent number: 6326379Abstract: Compounds of the formulas are useful as inhibitors of cGMP PDE, especially type V.Type: GrantFiled: September 10, 1999Date of Patent: December 4, 2001Assignee: Bristol-Myers Squibb Co.Inventors: John E. Macor, Guixue Yu
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Patent number: 6316444Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.Type: GrantFiled: June 26, 2000Date of Patent: November 13, 2001Assignee: Merck & Co., Inc.Inventors: Julianne A. Hunt, Sander G. Mills, Peter J. Sinclair, Dennis M. Zaller
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Patent number: 6313124Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: January 28, 1998Date of Patent: November 6, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 6306872Abstract: The present invention relates to 6-substituted 1,2,4a,5a,8a,8b-hexahydro- and 1,2,3,4,4a,5a,8a,8b-octahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyrid-8(7H)-one derivatives of the general formula (I) and their salts in which the radicals R1, R2, R3, R4, B and A are each as defined in the description, to processes for their preparation and to their use for controlling endoparasites.Type: GrantFiled: November 10, 1999Date of Patent: October 23, 2001Assignee: Bayer AktiengesellschaftInventors: Peter Jeschke, Achim Harder, Norbert Mencke, Georg von Samson-Himmelstjerna
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Patent number: 6303597Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.Type: GrantFiled: June 26, 2000Date of Patent: October 16, 2001Assignee: Merck Sharp & Dohme LimitedInventors: William Robert Carling, Kevin William Moore, Leslie Joseph Street
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Patent number: 6297235Abstract: A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alky, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.Type: GrantFiled: November 12, 1998Date of Patent: October 2, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
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Patent number: 6291454Abstract: This invention provides novel dithiepino[6,5-b]pyridines of the following formulae. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthinatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.Type: GrantFiled: May 30, 2000Date of Patent: September 18, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: James L. Bullington, John H. Dodd, Daniel A. Hall
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Patent number: 6268369Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: July 31, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
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Patent number: 6265410Abstract: Described are compositions and a method of inhibiting epidermal growth factor receptor tyrosine kinase by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of Formula II: where: any two continguous positions in positions A-E taken together can be a single heteroatom selected from the group consisting of nitrogen, oxygen or sulfur, in which case the other two remaining atoms must be carbon; the remaining substituents are disclosed in the specificationType: GrantFiled: November 13, 1998Date of Patent: July 24, 2001Assignee: Warner-Lambert CompanyInventors: Alexander James Bridges, William Alexander Denny, David Fry, Alan Kraker, Robert Frederick Meyer, Gordon William Rewcastle, Andrew Mark Thompson
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Patent number: 6258809Abstract: Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: wherein R1, R13, X, Y, Z, G and Q are as defined herein.Type: GrantFiled: March 3, 2000Date of Patent: July 10, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
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Patent number: 6255305Abstract: Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.Type: GrantFiled: November 10, 1998Date of Patent: July 3, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street
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Patent number: 6245779Abstract: The present invention provides a naphthyridine derivative represented by the formula (1) wherein A is lower alkylene; R1 is H or an electron pair “-”; R2 is optionally substituted phenyl; when R1 is an electron pair “-”, R3 is a group represented by (wherein R4 and R5 each represent lower alkyl, etc.); when R1 is H, R3 is a group —S—R6 (wherein R6 is lower alkyl, etc.); and R7 is H or lower alkyl; and also provides an analgesic composition containing the above derivative as an active ingredient.Type: GrantFiled: December 9, 1999Date of Patent: June 12, 2001Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Tadao Shibutani, Yasuo Shoji, Takashi Okamura, Tsuneo Yasuda, Takeshi Iwamoto
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Patent number: 6211187Abstract: This invention encompasses compounds of the formula wherein Ar represents a mono- , di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists or human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: October 22, 1999Date of Patent: April 3, 2001Assignee: Neurogen CorporationInventor: Jun Yuan
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Patent number: 6200972Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: GrantFiled: February 23, 1998Date of Patent: March 13, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Jia-He Li, Gregory S. Hamilton
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Patent number: 6191131Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: January 28, 1998Date of Patent: February 20, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Patent number: 6187788Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.Type: GrantFiled: October 1, 1998Date of Patent: February 13, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuo Choh, Koichi Kato, Shuji Hinuma
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6140325Abstract: Thienopyrimidine derivatives are disclosed. Also disclosed are methods for the production and use of these compounds.Type: GrantFiled: September 30, 1996Date of Patent: October 31, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuo Choh, Tetsuya Ohtaki, Toshifumi Watanabe
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Patent number: 6124306Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; andR.sub.6 is --S--C.sub.1-6 alkyl (preferably --SCH.sub.3);The compounds of Formula I are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: September 21, 1998Date of Patent: September 26, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Joel Morris, Wade J. Adams, Janice M. Friis, Donn G. Wishka
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Patent number: 6117876Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.Type: GrantFiled: April 8, 1998Date of Patent: September 12, 2000Assignee: American Cyanamid CompanyInventors: Klaus-Juergen Pees, Guido Albert
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Patent number: 6013654Abstract: The present invention relates to imidazo[1,2-a]pyridine compounds of formula I which are dopamine D-4 antagonists and useful as anti-psychotic agents.Type: GrantFiled: December 30, 1998Date of Patent: January 11, 2000Assignee: Pharmacia & Upjohn CompanyInventor: Ruth Elizabeth TenBrink