Piperazine Ring Patents (Class 544/121)
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Patent number: 6395731Abstract: The invention relates to heterocyclic derivatives of formula (I) and (Ia), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.Type: GrantFiled: December 20, 2000Date of Patent: May 28, 2002Assignee: Astrazeneca ABInventors: Nowak Thorsten, John Preston, John W Rayner, Michael J Smithers, Andrew Stocker
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Patent number: 6387899Abstract: The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CONR6R7, CN, CF3, OH, C1-C6 alkoxy, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceuType: GrantFiled: October 21, 1998Date of Patent: May 14, 2002Assignee: AstraZeneca ABInventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
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Patent number: 6384030Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; is 1, 2 or 3; Y is O, S or NR2; R1 represents hydrogen, aryl, Het1, or an optionally substituted C1-6alkyl; each R2 independently represents hydrogen or C1-6alkyl; or in case R1 and R2 are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R3 independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het1 represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het2 is the same as Het1 and may also be piperazinylType: GrantFiled: November 9, 2000Date of Patent: May 7, 2002Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Jan Heeres, Frank Christopher Odds
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Patent number: 6380186Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: October 8, 1999Date of Patent: April 30, 2002Assignee: Pfizer INCInventor: Harry Ralph Howard
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Patent number: 6362188Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.Type: GrantFiled: December 16, 1999Date of Patent: March 26, 2002Assignee: Schering CorporationInventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Patent number: 6352987Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.Type: GrantFiled: February 26, 2001Date of Patent: March 5, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
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Patent number: 6344456Abstract: The invention concerns compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein. Said compounds are useful in therapy as antithrombotic agents.Type: GrantFiled: January 10, 2001Date of Patent: February 5, 2002Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Patent number: 6340682Abstract: The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C═C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is or and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.Type: GrantFiled: February 23, 1999Date of Patent: January 22, 2002Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Mototsugu Kabeya, Hiromichi Shigyo, Masami Shiratsuchi, Yukio Hattori, Hiroshi Nakao, Takao Nagoya, Seiichi Sato, Soichi Oda, Makoto Suda, Manabu Shibasaki
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Patent number: 6335337Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp iib/iiia platelet receptors, and which can be used therapeutically as antithrombotic agents.Type: GrantFiled: January 9, 2001Date of Patent: January 1, 2002Assignee: Laboratoire L. LafonInventors: Christophe Yue, Marguerite Henry, Thierry Giboulot, Brigitte Lesur
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Patent number: 6333324Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 26, 1999Date of Patent: December 25, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masahiro Neya, Hitoshi Yamazaki, Natsuko Kayakiri, Kentaro Sato, Teruo Oku
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Patent number: 6326371Abstract: The present invention relates to a method for treating a patient suffering from a mental disorder, comprising administering to the patient an effective 5-HT1A agonistic and 5-HT2 antagonistic amount of a compound having the formula (I): or a pharmacologically active salt thereof.Type: GrantFiled: October 4, 1996Date of Patent: December 4, 2001Assignee: Pharmacia AktiebolagInventors: Lisbeth Abramo, Torbjörn Lundstedt, Curt Nordvi, Knut Gunnar Olsson, Martin Brodszki
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Publication number: 20010046993Abstract: This invention provides a compound of the formula (I): 1Type: ApplicationFiled: December 7, 2000Publication date: November 29, 2001Inventors: Takafumi Ikeda, Mitsuhiro Kawamura, Noriaki Murase, Seiji Nukui, Yuji Shishido, Makato Kawai, Yoshiyuki Okumura
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Patent number: 6316617Abstract: This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: August 8, 2000Date of Patent: November 13, 2001Assignee: Neurogen CorporationInventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
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Patent number: 6313118Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salType: GrantFiled: October 21, 1998Date of Patent: November 6, 2001Assignee: Astra AktiebolagInventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
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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: 6306860Abstract: Anti-viral agents of formula (1) have been identified. Their preparation method is described. These 2,5-pyridinedicarboxylic acid derivatives or their pharmaceutically acceptable salts are useful in countering the proliferation of viruses such as hepatitis B virus and human immunodeficiency virus.Type: GrantFiled: November 7, 2000Date of Patent: October 23, 2001Assignee: Dong Wha Pharm. Inc. Co., Ltd.Inventors: Sung Joon Yoon, Sang Wook Lee, Hyeong Su Sim, Yong Kyun Park, Wang Yong Yang, Jong Woo Kim, Jae Jin Han, Je In Yoon, Sang Jin Park, Hee Jeoung Park, Dong Hyuk Sin, Hwan Bong Chang
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Patent number: 6291458Abstract: The present invention relates to pharmaceutically acceptable salts of the compound of formula I or solvates of said salt in which the compound of formula I is as the (R)-enantiomer, the (S)-enantiomer or the racemate, a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: GrantFiled: July 21, 2000Date of Patent: September 18, 2001Assignee: AstraZeneca ABInventors: Stefan Berg, Daniel Sohn
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Patent number: 6288059Abstract: A compound of formula (I), a pharmaceutically acceptable salt or ester or other derivative thereof: R1 is optionally substituted cycloalkyl or optionally substituted saturated heterocyclic group. R2 is optionally substituted aryl or optionally substituted heteroaryl. A is methylene, carbonyl or sulfonyl. B is a single bond, alkylene or alkenylene. D is oxygen or sulfur. G is alkylene or alkenylene. L is —N(R3)— or —C(R4)(R5)—. R3 is optionally substituted aryl or optionally substituted heteroaryl. R4 is H, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl or optionally substituted saturated heterocyclic group. R5 is alkyl optionally substituted with amino, amino, optionally substituted acylamino, OH, optionally substituted hydroxyalkyl, alkoxy or —CO—R6. R6 is alkyl, alkoxy or amine residue. R4 together with R5 forms a cycloalkane ring, cycloalkene ring, or saturated heterocyclic ring. R7 is alkyl.Type: GrantFiled: June 5, 2000Date of Patent: September 11, 2001Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Takeshi Yamaguchi
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Patent number: 6281210Abstract: The present invention provides a compound of formula I which have potent activities against gram positive and gram-negative bacteria.Type: GrantFiled: December 6, 2000Date of Patent: August 28, 2001Assignee: Pharmacia & Upjohn CompanyInventor: Jackson B. Hester, Jr.
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Patent number: 6277854Abstract: The invention relates to compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, R8, Y, A, B, X, a, b, c, d, v, and w are as described herein. The compounds of formula (1.0) are useful for inhibiting tumor growth.Type: GrantFiled: July 13, 1999Date of Patent: August 21, 2001Assignee: Schering CorporationInventors: F. George Njoroge, Ronald J. Doll, Stacy W. Remiszewski
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Patent number: 6262052Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 26, 1999Date of Patent: July 17, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
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Patent number: 6228857Abstract: The present invention relates to pharmaceutically acceptable salts of the compound of formula I or solvates of said salt in which the compound of formula I is as the (R)-enantiomer, the (S)-enantiomer or the racemate, a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: GrantFiled: July 21, 2000Date of Patent: May 8, 2001Assignee: AstraZeneca ABInventors: Stefan Berg, Daniel Sohn
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Patent number: 6225309Abstract: The invention concerns compounds of formula (I), wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and 1-C)alkyl; M1 is a group of formula: NR2—L1—T1R3, in which R2 and R3 together form a (1-4C)alylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)rL2—T3R5 in which R is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.Type: GrantFiled: August 9, 1999Date of Patent: May 1, 2001Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
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Patent number: 6221858Abstract: Use of a compound of formula (I) and the pharmaceutically acceptable acid addition salts thereof, wherein R1 is either halogen or hydrogen and R2 is halogen; X is CH2, O or S; R3 and R4 are the same or different and selected from hydrogen or lower alkyl; n is 2 or 3; A is selected from the pyrimidyl- or pyridyl-groups (a), (b) or (c) wherein R5, R6 and R7 are as defined in the description; for the manufacture of a medicament for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug or substance of abuse or for treatment thereof.Type: GrantFiled: November 5, 1998Date of Patent: April 24, 2001Assignee: Pharmacia & Upjohn ABInventor: Anders Björk
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Patent number: 6207665Abstract: This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: GrantFiled: June 9, 1998Date of Patent: March 27, 2001Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Guo Ping Wei, Wei Xu, Wei Zheng
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Patent number: 6204268Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: March 20, 2001Assignee: COR Therapeutics, INCInventors: Robert M. Scarborough, Bing-Yan Zhu, Ting Su
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6194413Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: May 12, 1998Date of Patent: February 27, 2001Assignee: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
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Patent number: 6140330Abstract: A thiazole compound of the formula: ##STR1## wherein T is lower alkylene; u is 0 or 1; R.sup.1 and R.sup.2 are the same or different and are each H, or lower alkyl, etc.; R.sup.3 is ##STR2## R.sup.4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca.sup.2+ /phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.Type: GrantFiled: March 24, 1998Date of Patent: October 31, 2000Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Toyoki Mori, Michiaki Tominaga, Fujio Tabusa, Kazuyoshi Nagami, Kaoru Abe, Kenji Nakaya, Isao Takemura, Tomoichi Shinohara, Yoshihisa Tanada, Takahito Yamauchi
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Patent number: 6133265Abstract: Amido, amino and sulfonamide substituted benzylamine derivatives useful in treating eating disorders have the formula ##STR1## where X.sub.1, X.sub.2, and X.sub.3, independently represent substituents of formula ##STR2## D=H, lower straight or branched chain alkyl having 1-6 carbon atoms, a methylene unit incorporated into a ring connected with G as in the cases of pyrrolidine, pyrrolidone, piperidine, and piperidone;E=O or H.sub.2 ;O=0 or 1;G=straight or branched chain lower alkyl having 1-6 carbon atoms, aryl, aryl substituted with halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, heteroaryl--selected from the group consisting of 2-, 3-, or 4-pyridyl, 2-pyrazyl, 2-, or 3-thienyl, 2-pyrazinyl, 2-, 3-, or 4-quinolyl, 1-, 3-, or 4-isoquinolyl, 2-quinoxalyl, 3-, or 4-cinnolyl, said heteroaryl substituted with halogen, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms;and A, T and R.sub.1 -R.sub.Type: GrantFiled: July 18, 1997Date of Patent: October 17, 2000Assignee: Neurogen CorporationInventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
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Patent number: 6130220Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: October 10, 2000Assignees: Syntex (USA) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker
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N-((phenyl, benzodioxinyl or N-heteroarylpiperazinyl)alkyl)-N-(N-heteroaryl)substituted carboxamides
Patent number: 6127357Abstract: Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formula A is C.sub.2-4 alkylene chain optionally substituted by lower alkyl, Z is oxygen or sulphur, R is hydrogen or lower alkyl, R.sup.1 is a mono or bicyclic aryl or heteroaryl radical, R.sup.2 is a mono or bicyclic heteroaryl radical and R.sup.3 is hydrogen or a specified radical such as lower alkyl, cycloalkyl, aryl, heteroaryl or optionally substituted amino.Type: GrantFiled: May 11, 1995Date of Patent: October 3, 2000Assignee: John Wyeth & Brother, Ltd.Inventors: Ian Anthony Cliffe, Howard Langham Mansell -
Patent number: 6124283Abstract: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula ##STR1## wherein X is N or CH;Y is NR.sub.2 CH.sub.2, CH.sub.2 --NR.sub.2, NR.sub.2 --CO, CO--NR.sub.2 or NR.sub.2 SO.sub.2 ;R.sub.1 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or (CH.sub.2).sub.n -aryl,where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted;n is 0-4;as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.Type: GrantFiled: April 25, 1997Date of Patent: September 26, 2000Assignee: Astra AktiebolagInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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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: 6103719Abstract: The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R.sup.3 or CH--R.sup.4,Y=CH.sub.2 or (CH.sub.2).sub.2,Z=O or H.sub.2 ;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: May 27, 1999Date of Patent: August 15, 2000Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck
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Patent number: 6100262Abstract: The present invention concerns novel (2-morpholinylmethyl)benzamide derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sup.2 is hydrogen, halo or C.sub.1-6 alkylsulfonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is a radical of formula R.sup.4 --C(.dbd.O)--Alk-- (a); R.sup.5 --C(.dbd.O)--N(R.sup.6)--Alk-- (b); or R.sup.7 --C(.dbd.O)--O--Alk-- (c); wherein each Alk is independently C.sub.1-12 alkanediyl; R.sup.4 is hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.5 and R.sup.7 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.6 is hydrogen or C.sub.Type: GrantFiled: September 22, 1999Date of Patent: August 8, 2000Assignee: Janssen Pharmaceutica, NV.Inventors: Marie-Louise Hendrickx, Kurt Godfried Cornelius Emile Van Daele, Peter Jules Victor Van Daele, Glenn Kurt Ludo Van Daele, Frans Maria Alfons Van den Keybus, Marc Gustaaf Celine Verdonck
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Patent number: 6087357Abstract: This application is a 371 of PCT/JP96/03641 filed Dec. 12, 1996.Type: GrantFiled: June 18, 1998Date of Patent: July 11, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Takashi Manabe, Nobukiyo Konishi, Kazuhiko Take, Norihiro Igari, Shinji Shigenaga, Hiroshi Matsuda, Tadashi Terasaka
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6030946Abstract: Cysteine protease inhibitors are provided.Type: GrantFiled: June 3, 1996Date of Patent: February 29, 2000Assignee: Axys Pharmaceuticals, Inc.Inventors: Jeffrey L. Klaus, David Rasnick, James T. Palmer, Elaine Yee-Lin Kuo
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Patent number: 6022971Abstract: The present invention provides compounds of the formula (I): ##STR1## 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 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.sup.1 is phenyl, benzyl, 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 trifluoromethyl;R.sup.2 represents various groups;X is C.sub.1 -C.sub.4 alkylene; andX.sup.1 is a direct link or C.sub.1 -C.sub.6 alkylene.Type: GrantFiled: January 26, 1998Date of Patent: February 8, 2000Assignee: Pfizer IncInventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 5985873Abstract: This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: July 18, 1997Date of Patent: November 16, 1999Assignee: Neurogen CorporationInventors: Charles A. Blum, Alan Hutchison, John M. Peterson
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Patent number: 5981537Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sup.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; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: May 9, 1996Date of Patent: November 9, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Fritz Reusser, Gary J. Cleek, Irene W. Althaus
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Patent number: 5977113Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 2, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5968938Abstract: This invention relates to certain novel piperazine compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.Type: GrantFiled: May 29, 1998Date of Patent: October 19, 1999Assignee: Merck & Co., Inc.Inventors: Peter D. Williams, Michelle A. Sparks, Ian Bell, James P. Guare, Jr., Roger M. Freidinger
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Patent number: 5945534Abstract: Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## in which X is alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding pyrazinecarboxylic acid derivatives, catalyzed by optically active rhodium complexes. The compounds of the formula I are intermediates for the preparation of pharmaceutical active substances, for example, HIV protease inhibitors.Type: GrantFiled: April 14, 1997Date of Patent: August 31, 1999Assignee: Lonza AGInventor: Rudolf Fuchs
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Patent number: 5939413Abstract: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or Tachykinin-mediated diseases in human beings or animals.Type: GrantFiled: November 24, 1997Date of Patent: August 17, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Takashi Manabe, Nobukiyo Konishi, Shinji Shigenaga, Kenji Murano, Hiroshi Matsuda, Hiroshi Miyake
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Patent number: 5935955Abstract: A piperazinedione of general formula (I): ##STR1## wherein R.sup.1 is selected from hydrogen;a group of formula --(NH).sub.t --COR.sup.3 wherein t is 0 or 1 and R.sup.3 is an organic substituent as defined herein;a group of formula (D): ##STR2## and a group of formula (E): ##STR3## and the pharmaceutically acceptable salts thereof are useful as modulators of multi-drug resistance.Type: GrantFiled: August 29, 1997Date of Patent: August 10, 1999Assignee: Xenova LimitedInventors: Philip A. Ashworth, Sukhjit Hunjan, Ian A. Pretswell, Harnish Ryder, Stephen J. Brocchini
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Patent number: 5935958Abstract: Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetyl-cholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.Type: GrantFiled: June 26, 1997Date of Patent: August 10, 1999Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Derek B. Lowe, Wei K. Chang, Sundeep Dugar
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Patent number: 5929077Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected b ##STR1## its enantiomers, diastereomers, and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: October 17, 1997Date of Patent: July 27, 1999Inventor: Katerina Leftheris
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler