The Additional Hetero Ring Is Bonded Directly To A Ring Carbon Of The Bicyclo Ring System Patents (Class 548/466)
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Patent number: 6521657Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: October 30, 2001Date of Patent: February 18, 2003Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6518429Abstract: The present invention relates to novel imidazole derivatives which show an inhibitory activity against farnesyl transferase, pharmaceutically acceptable salts or isomers thereof and pharmaceutical compositions comprising such imidazole derivatives. More particularly, the present invention relates to intermediate compounds which are used in the preparation of the imidazole derivatives of the invention. Related processes also are disclosed.Type: GrantFiled: March 20, 2001Date of Patent: February 11, 2003Assignee: LG Chemical, Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6492374Abstract: The present invention relates to benzofuran derivatives having general Formula (I) wherein A is selected from (1), (2), (3), (4) wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.Type: GrantFiled: June 4, 2001Date of Patent: December 10, 2002Assignee: H. Lundbeck A/SInventors: Kim Andersen, Mario Rottländer, Klaus Peter Bøgesø, Henrik Pedersen, Thomas Ruhland, Robert Dancer
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3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3&bgr;
Patent number: 6479490Abstract: This invention relates to inhibitors of glycogen synthase kinase-3&bgr;, methods of treating diseases characterized by an excess of Th2 cytokines, and to 3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives of Formula (I): that are inhibitors of glycogen synthase kinase -3&bgr;, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: July 27, 2001Date of Patent: November 12, 2002Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Andrew Grupe, Gary Allen Peltz -
Patent number: 6444615Abstract: This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In particular, the present invention pertains to 2-thioxo-4,5-imidazolidinediones or 2,4,5-imidazolidinetriones wherein a 2,4,5,6-tetrasubstituted phenyl ring is linked to the heterocyclic ring.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Dow AgroSciences LLCInventors: Bin Li, Ying Man, Zongjian Zhang, Adam Chi-Tung Hsu
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Patent number: 6409956Abstract: An injection-molding process using warp-free pigment compositions including diaryldiketopyrrolo[3,4-C]pyrroles to improve the dimensional stability of the injection molded product by decreasing warping wherein the constituents of the formulation being injection molded are added into an injection molding machine in ready-premixed form or simultaneously as individual components. Preferred pigments are quinacridone pigments, disazo condensation pigments, isoindolinone pigments and pyrrolo[3,4-C]pyrrole pigments with pyrrolo[3,4-C]pyrrole pigments being especially preferred.Type: GrantFiled: April 20, 1999Date of Patent: June 25, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Franck Rey Flandrin, Guo-Hua Hu, Philippe Bugnon, Zhimin Hao
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Patent number: 6395766Abstract: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.Type: GrantFiled: November 6, 2000Date of Patent: May 28, 2002Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Helen Jane Bryant, Mark Stuart Chambers, Neil Roy Curtis
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Publication number: 20020058817Abstract: The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.Type: ApplicationFiled: March 1, 2001Publication date: May 16, 2002Inventors: Samuel J. Danishefsky, Shawn J. Stachel, Chul Bom Lee, Mark D. Chappell, Zhicai Wu
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Patent number: 6387923Abstract: Compounds represented by the formula: wherein A is selected from the group consisting of W is NH2 or H; and each X, Y and Z is individually selected from the group consisting of OH, H and halogen provided at least one of X and Y is H; tautomers, or pharmaceutically acceptable salts thereof; are provided. Compounds of the present invention are useful as inhibitors of PNP and of T-cell proliferation. Compounds of the present invention are useful for treating Cancer. Method for preparing the compounds of the present invention are also provided.Type: GrantFiled: March 22, 2001Date of Patent: May 14, 2002Assignee: Biocryst Pharmacueticals, Inc.Inventors: Philip E. Morris, Jr., John A. Montgomery, Yarlagadda S. Babu
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Publication number: 20020052397Abstract: This invention relates to inhibitors of glycogen synthase kinase-3&bgr;, methods of treating diseases characterized by an excess of Th2 cytokines, and to 3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives of Formula (I): 1Type: ApplicationFiled: July 27, 2001Publication date: May 2, 2002Inventors: Leyi Gong, Andrew Grupe, Gary Allen Peltz
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Patent number: 6358993Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 22, 1999Date of Patent: March 19, 2002Assignee: CeNes Pharmaceuticals, Inc.Inventors: N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant
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Patent number: 6353008Abstract: The present invention provides the compounds of the following formula (I): and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of formula (I).Type: GrantFiled: November 28, 2000Date of Patent: March 5, 2002Assignee: Eli Lilly and CompanyInventors: Larry Wayne Hertel, Yao-Chang Xu
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Patent number: 6344468Abstract: The present invention relates to substituted isoindolone derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for these, and also pharmaceutical preparations which comprise compounds of the formula I.Type: GrantFiled: October 6, 2000Date of Patent: February 5, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel, Viola Groehn
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Patent number: 6307056Abstract: Disclosed are 4-aryloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, as well as methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis, using said compounds.Type: GrantFiled: December 15, 1999Date of Patent: October 23, 2001Assignee: Hoffman-La Roche Inc.Inventors: Wendy Lea Corbett, Kin-Chun Luk, Paige E. Mahaney
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Patent number: 6268391Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.Type: GrantFiled: April 7, 2000Date of Patent: July 31, 2001Assignee: Glaxo Wellcome Inc.Inventors: Scott Howard Dickerson, Philip Anthony Harris, Robert Neil Hunter, III, David Kendall Jung, Karen Elizabeth Lackey, Robert Walton McNutt, Jr., Michael Robert Peel, James Marvin Veal
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Patent number: 6255306Abstract: The present invention relates to compounds of the formulaType: GrantFiled: August 11, 1998Date of Patent: July 3, 2001Inventor: John E. Macor
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Patent number: 6242438Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.Type: GrantFiled: June 1, 1998Date of Patent: June 5, 2001Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 6180643Abstract: The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. In particular, the compounds of the invention are useful for the prophylaxis and treatment of diseases or conditions involving inflammation. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of inflammation and other maladies, such as pain and diabetes, using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: June 8, 1999Date of Patent: January 30, 2001Assignee: Amgen Inc.Inventors: Jeffery A. Zablocki, Eugene Tarlton, Jr., James P. Rizzi, Nathan B. Mantlo
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Patent number: 6140347Abstract: A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: October 14, 1998Date of Patent: October 31, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Andrew Madin, Joseph George Neduvelil, Graham Andrew Showell, Leslie Joseph Street, Monique Bodil Van Niel
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Patent number: 6133452Abstract: The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is very efficient and robust macrocyclization methodology.Type: GrantFiled: January 21, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventors: Margaret Mary Faul, Leonard Larry Winneroski, Jr.
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Patent number: 6130239Abstract: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.Type: GrantFiled: December 15, 1999Date of Patent: October 10, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Yi Chen, Wendy Lea Corbett, Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk, Paige E. Mahaney, Steven Gregory Mischke
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Patent number: 6096887Abstract: The present invention encompasses structures of the formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## W represents substituted or unsubstituted heteroaryl; X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxy, nitro, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; and n is 1,2,3, or 4,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. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: February 25, 1998Date of Patent: August 1, 2000Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Patent number: 6063804Abstract: Compounds of formula (I): ##STR1## wherein: R represents hydrogen, alkyl, optionally-substituted amino, or linear or branched (C.sub.1 -C.sub.6)-acyl,R.sub.1 and R.sub.2, which may be identical or different, each represents independently of the other aryl, heteroaryl, or (C.sub.5 -C.sub.7)-cycloalkyl, or one of those groups optionally substituted,A, together with the atoms in common with the pyrrole, represents saturated or unsaturated, monocyclic or bicyclic (C.sub.3 -C.sub.12)-cycloalkyl, or a saturated heterocycle having 5 to 7 ring members and containing one or two nitrogen, or 7-oxabicyclo[2.2.1]heptane, or one of those groups optionally substituted,their isomers, and also addition salts thereof with a pharmaceutically-acceptable acid or base, pharmaceutical compositions thereof, and use thereof as medicaments.Type: GrantFiled: November 25, 1998Date of Patent: May 16, 2000Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Bernard Portevin, Jacqueline Bonnet, Charles Tordjman
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Patent number: 6060473Abstract: 7-Azabicyclo[2.2.1]-heptane and -heptene derivatives are disclosed that can be administered to a mammal, including a human, to treat disorders associated with a decrease or increase in cholinergic activity.Type: GrantFiled: August 20, 1996Date of Patent: May 9, 2000Assignee: UCB S.A. - DTBInventors: T. Y. Shen, W. Dean Harman, Dao Fei Huang, Javier Gonzalez
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Patent number: 6046138Abstract: An indole derivative having the formula (I) or (II) and root formation inducing agents wherein these indole derivatives are an effective ingredient: ##STR1## wherein, R does not exist or represents a C.sub.1 to C.sub.4 alkylene group.Type: GrantFiled: March 10, 1998Date of Patent: April 4, 2000Assignee: Shiseido Company, Ltd.Inventors: Mineyuki Yokoyama, Shoko Yamaguchi, Seiichi Yoshida, Okihiko Sakamoto, Kiyotaka Kojima
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Patent number: 6037475Abstract: The present invention provides a method for synthesizing indolylmaleimides by reacting an activated maleimide preferably with an optionally substituted organometalic-3-indole in the presence of a transition metal catalyst.Type: GrantFiled: February 11, 1999Date of Patent: March 14, 2000Assignee: Eli Lilly & CompanyInventors: Margaret M. Faul, Michael R. Jirousek, John H. McDonald, III, David Andrew Neel
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Patent number: 5998438Abstract: Described herein are compounds selective for a 5-HT.sub.1D -like receptor, which have the general formula: ##STR1## wherein A is selected from a six-membered, non-aromatic, optionally substituted carbocycle and a six-membered, non-aromatic, optionally substituted heterocycle having one or two heteroatoms selected from O, S, SO, SO.sub.2 and N.sup.4 ;R.sup.1 is selected from H and OH;n is 0 or 1 as permited by chemical structure;R.sup.2 is selected from CR.sup.5 CR.sup.6 CH.sub.2 NR.sup.7 R.sup.8 or a group of formula II, III or IV: ##STR2## R.sup.3 is selected from H and benzoyl; R.sup.4 is selected from H, loweralkyl, benzyl, loweralkylcarbonyl, loweralkylaminocarbonyl, loweralkylaminothiocarbonyl, loweralkanoyl, loweralkylaminoimide and loweralkoxy-substituted loweralkylene;R.sup.5 and R.sup.6 are independently selected from H, loweralkoxy and hydroxy;R.sup.7 and R.sup.8 are independently selected from H and loweralkyl or R.sup.7 and R.sup.Type: GrantFiled: November 21, 1997Date of Patent: December 7, 1999Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Abdelmalik Slassi, Louise Edwards, Qingchang Meng, Sumanas Rakhit
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Patent number: 5968923Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, COOH, --COO(C.sub.1 -C.sub.4 alkyl), C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro (C.sub.1 -C.sub.4) alkyl and fluoro (C.sub.1 -C.sub.4) Alkoxy; R.sub.1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluormethyl; R.sup.2 is --CO.sub.2 H, --CONR.sup.3 R.sup.4, --CONR.sup.5 (C.sub.3 -C.sub.7 cycloalkyl), --NR.sup.5 (C.sub.2 -C.sub.5 alkanoyl), --NR.sup.Type: GrantFiled: February 10, 1997Date of Patent: October 19, 1999Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Sandra Dora Meadows, Donald Stuart Middleton
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Patent number: 5958943Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid variety and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1996Date of Patent: September 28, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5929094Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.Type: GrantFiled: October 22, 1997Date of Patent: July 27, 1999Assignee: Merck & Co., Inc.Inventors: Philippe Durette, Ihor Kopka, Malcolm MacCoss, Sander Mills
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Patent number: 5919946Abstract: The present invention provides a method for synthesizing indolylmaleimides by reacting an activated maleimide preferably with an optionally substituted organometallic-3-indole in the presence of a transition metal catalyst.Type: GrantFiled: March 20, 1997Date of Patent: July 6, 1999Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, John H. McDonald, III, David Neel
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Patent number: 5891901Abstract: Compounds of the formula ##STR1## wherein R is alkyl, alkylthio or hydroxy, as well as, pharmaceutically acceptable salts of compounds of formula I are antiproliferative agents useful in the treatment of cancer.Type: GrantFiled: July 24, 1997Date of Patent: April 6, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Urvashi Hooda Dhingra, Donna Mary Huryn, Dennis Dalton Keith, Giuseppe Federico Weber
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Patent number: 5865857Abstract: A dye of Formula (1): ##STR1## wherein: D is a group of Formula (2): ##STR2## or a group of Formula (3): ##STR3## or a group of Formula (4): ##STR4## The variables are defined in the disclosures. The dyes and dye mixtures produce blue to green shades on synthetic textile materials such as polyester which have good build up and good light- and wet-fastness.Type: GrantFiled: June 19, 1997Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: Denise Cavanagh, Mark Robert James, Barry Huston Meyrick, Paul Wight
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Patent number: 5859261Abstract: The present invention provides a method for synthesizing indolylmaleimides by reacting an activated maleimide preferably with an optionally substituted organometallic-3-indole in the presence of a transition metal catalyst.Type: GrantFiled: December 19, 1997Date of Patent: January 12, 1999Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, John H. McDonald, III, David Andrew Neel
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Patent number: 5856517Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.1' are independently alkyl, aryl, alkenyl or alkynyl;R.sup.2 and R.sup.2' are independently hydrogen or alkyl;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are ##STR2## CH.sub.2 OR.sup.10, CHO, CH.sub.2 NR.sup.11 R.sup.12, hydrogen, halogen, cyano, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, aralkyloxy, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl, provided that at least one of R.sup.4, R.sup.5, R.sup.6 or R.sup.7 is cyano, ##STR3## CH.sub.2 OR.sup.10, CH.sub.2 NR.sup.11 R.sup.12, or CHO ; R.sup.8 is alkyl, aralkyl or aryl;R.sup.10 is hydrogen, alkyl, aralkyl or aryl;R.sup.11 and R.sup.Type: GrantFiled: July 24, 1997Date of Patent: January 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Donna Mary Huryn, Dennis Dalton Keith
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Patent number: 5808094Abstract: A process for the preparation of mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formula ##STR1## by heating a corresponding mixture in solid form to the temperature range from 220.degree. to 380.degree. C.A and B are, for example, each a group of formula ##STR2## wherein R.sub.1 and R.sub.2 are each independently hydrogen, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, phenyl or --CN,G is --O--, --NR.sub.7 --, --N.dbd.N-- or --SO.sub.2 --,R.sub.3 and R.sub.4 are hydrogen, and R.sub.7 is hydrogen, methyl or ethyl.The mixed crystals and solid solutions obtained are excellently suited for pigmenting high molecular weight material.Type: GrantFiled: July 22, 1997Date of Patent: September 15, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
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Patent number: 5808064Abstract: We have found that 2-unsubstituted indoles of structural formula (IV) can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline (I) and an acyl silane derivative (II), followed by deprotection of the silyl protecting groups. ##STR1## The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride. When applied to 5-triazolyl substituted indoles, the present process also eliminates the tendency of triazolyl polymerization in the Fischer indole synthesis.Type: GrantFiled: August 7, 1997Date of Patent: September 15, 1998Assignee: Merck & Co., Inc.Inventors: Cheng-Yi Chen, Robert D. Larsen
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Patent number: 5773612Abstract: A compound of formula II' ##STR1## in whichR.sub.I is an ethoxy group or a chlorine atom;R.sub.II is hydrogen, a chlorine atom or a methyl group;R.sub.III is a chlorophenyl group or a methoxyphenyl group;R.sub.IV is an amino group, a group NR.sub.9 R.sub.10 or NR.sub.9 R.sub.XI, or a piperazin-1-yl radical substituted in the 4-position by a (C.sub.2 -C.sub.10)alkylene group substituted by an amino group which is free or carries a protective group;R.sub.10 is (CH.sub.2).sub.p R.sub.35 or a (C.sub.2 -C.sub.10)alkylene group substituted by R.sub.21 ;R.sub.XI is a (C.sub.1 -C.sub.12)alkyl group or a group .omega.-R.sub.32 R.sub.33 N(C.sub.1 -C.sub.4)-alkylcarbonyl; andR.sub.21 is R.sub.36 ; a group OR.sub.37 ; a group NR.sub.32 R.sub.33 ; a cyano group; a group S(C.sub.1 -C.sub.7)alkyl; a group SO(C.sub.1 -C.sub.7)alkyl; or a group SO.sub.2 (C.sub.1 -C.sub.7)alkyl;R.sub.35 is a piperid-4-yl group which is unsubstituted or substituted in the 1-position by a (C.sub.1 -C.sub.7)alkoxycarbonyl group or by a (C.sub.Type: GrantFiled: April 30, 1996Date of Patent: June 30, 1998Assignee: SanofiInventors: Jean Wagnon, Bernard Tonnerre, Alain Di Malta, Richard Roux, Marie-Sophie Amiel, Claudine Serradeil-Legal
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Patent number: 5770742Abstract: 5-Thiophene-substituted tryptamine analogs are provided, which exhibit selectivity towards 5-HT.sub.D1 receptors and consequently show potential in alleviation of the symptoms of migraine. The analogs are represented by the following general chemical formula: ##STR1## in which X represents H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or halogen, at the 4- or 5-position of the thiophene nucleus; Y represents a direct bond or a C.sub.1 -C.sub.3 alkylene group optionally substituted with hydroxyl: and Z represents amino, mono- or di-N-lower alkyl-substituted amino, or optionally N-lower alkyl-substituted pyrrolidine.Type: GrantFiled: May 16, 1996Date of Patent: June 23, 1998Assignee: Allelix Biopharmaceuticals Inc.Inventors: Qingchang Meng, Abdelmalik Slassi, Sumanas Rakhit
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Patent number: 5750702Abstract: The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl;X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxy, nitro, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; andn is 1, 2, 3, or 4,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. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: July 16, 1996Date of Patent: May 12, 1998Assignee: Neurogen CorporationInventors: Pamela Albaugh, Alan Hutchison
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Patent number: 5736564Abstract: The present invention relates to dihydroisoindole compounds, pharmaceutical compositions containing these compounds, and their use as endothelin receptor antagonists.Type: GrantFiled: December 12, 1996Date of Patent: April 7, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Robert Gene Franz, M. Amparo Lago, Aiming Gao
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Patent number: 5726063Abstract: A colorimetric assay of enaldehydes or of malonic dialdehyde as lipid peroxidation indices in an aqueous medium includinga) addition to the medium of a reagent of a compound of general formula I and their optional addition salts with organic or inorganic bases or with organic or inorganic acids. ##STR1## in which formula: A and C, which may be identical or different, each represent H, ##STR2## wherein A and C cannot simultaneously represent H, with:R.sup.1 =H; alkyl; aralkyl; aryl substituted on the aryl ring; alkyl sulfonate Y.sup.+ ; alkyl phosphonate, Y.sup.+ ; or alkyl carboxylate, Y.sup.+ ;R.sup.2 =H; --OR.sup.4 ; F; Cl; Br; I; --NO.sub.2 ; SO.sub.3.sup.31 Y.sup.+ ; --CN; --COOR.sup.4 ; or --CONR.sup.5 R.sup.6 ;R.sup.3 =H; --OR.sup.4 ; --NR.sup.5 R.sup.6 ; --SR.sup.4 ; F; Cl; Br; I; --NO.sub.2 ; --SO.sub.3 --Y.sup.+ ; --CN; --COR.sup.5 ; --COOR.sup.4 ; or --CONR.sup.5 R.sup.6 ;R.sup.4 =H; alkyl; aralkyl; or aryl substituted on the aryl ring;R.sup.Type: GrantFiled: August 23, 1996Date of Patent: March 10, 1998Assignee: Oxis Isle of Man, LimitedInventors: Dominique Gerard-Monnier, Irene Erdelmeier, Jean Chaudiere, Jean-Claude Yadan
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Patent number: 5708169Abstract: The present invention provides for new 5-amidomethyl, .alpha.,.beta.-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with zero (0) to two(2) halogen atoms and substituted in the para position with, e.g., piperazinyl, thiomorpholinyl (and corresponding sulfoxide and sulfone), thiazolidinyl (and sulfoxide and sulfone), morpholinyl, azetidinyl, pyrrolidinyl, piperidinyl, pyrrolyl, azepinyl, troponyl, 3,7-diazabicyclo?3.3.0!octan-3-yl, bridged thiazinyl or bridged oxazinyl moieties. In those cases where a ring nitrogen is present, then this is substituted to form an amide, formamide, sulfonamide, urethane, or alkylated with a wide variety of moieties.Type: GrantFiled: September 5, 1996Date of Patent: January 13, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Jackson B. Hester, Jr., Steven Joseph Brickner, Michael Robert Barbachyn, Douglas K. Hutchinson, Dana Scott Toops
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Patent number: 5693824Abstract: A process for the preparation of mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formula ##STR1## by heating a corresponding mixture in solid form to the temperature range from 220.degree. to 380.degree. C.A and B are, for example, each a group of formula ##STR2## wherein R.sub.1 and R.sub.2 are each independently hydrogen, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, phenyl or --CN, G is --O--, --NR.sub.7 --, --N.dbd.N-- or --SO.sub.2 --, R.sub.3 and R.sub.4 are hydrogen, and R.sub.7 is hydrogen, methyl or ethyl.The mixed crystals and solid solutions obtained are excellently suited for pigmenting high molecular weight material.Type: GrantFiled: September 12, 1996Date of Patent: December 2, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
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Patent number: 5691373Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.Type: GrantFiled: February 6, 1995Date of Patent: November 25, 1997Assignee: Warner-Lambert CompanyInventors: Kent Alan Berryman, Annette Marian Doherty, Jeremy John Edmunds, William Chester Patt, Mark Stephen Plummer, Joseph Thomas Repine
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Patent number: 5672618Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: May 25, 1995Date of Patent: September 30, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Michael Paal, Theo Schotten, Wolfgang Stenzel
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Patent number: 5668152Abstract: The present invention discloses compounds that are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.Type: GrantFiled: May 25, 1995Date of Patent: September 16, 1997Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., John H. McDonald, III, Gerd Ruhter, Theo Schotten
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Patent number: 5665723Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##Type: GrantFiled: June 2, 1995Date of Patent: September 9, 1997Assignee: Merck & Co., Inc.Inventors: George D. Hartman, John H. Hutchinson, Wasyl Halczenko
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Patent number: 5660598Abstract: A dye of Formula (1): ##STR1## wherein: D is a group of Formula (2): ##STR2## or a group of Formula (3): ##STR3## or a group of Formula (4): ##STR4## The variables are defined in the specification. The dyes and dye mixtures produce blue to green shades on synthetic textile materials such as polyester which have good build up and good light- and wet-fastness.Type: GrantFiled: May 3, 1995Date of Patent: August 26, 1997Assignee: Zeneca LimitedInventors: Denise Cavanagh, Mark Robert James, Barry Huston Meyrick, Paul Wight
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Patent number: RE36736Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Y have the signficance given in the description, are useful in the control or prevention of inflammatory, immunological, bronchopulmonary or cardiovascular disorders.Type: GrantFiled: January 27, 1998Date of Patent: June 13, 2000Assignee: Hoffman-La Roche Inc.Inventors: Peter D. Davis, Christopher H. Hill, Geoffrey Lawton