The Polycyclo Ring System Is Bicyclo-carbocyclic Patents (Class 546/205)
  • Patent number: 6329399
    Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: December 11, 2001
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Takao Itoh, Takuji Nakashima, Akira Nozawa, Kouji Yokoyama, Hiroyuki Takimoto, Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima
  • Patent number: 6323217
    Abstract: A compound of formula (I): wherein: R1 represents hydrogen or alkyl, R2a and R2b represent a group selected from hydrogen, halogen, alkyl, hydroxy, alkoxy, trihaloalkyl, cyano, nitro, amino, alkylamino and dialkylamino, R3 represents hydrogen or hydroxy, X represents oxygen or methylene, V represents an alkylene chain that is optionally unsaturated and optionally substituted, U represents a bond or an alkylene chain, W represents a group selected from aryl and heteroaryl, each of those groups being optionally substituted by one or more identical or different groups, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: November 27, 2001
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Catherine Thollon, Marie-Pierre Bourguignon
  • Patent number: 6319921
    Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: November 20, 2001
    Assignee: Boerhinger Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
  • Patent number: 6316470
    Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: November 13, 2001
    Assignee: Neurogen Corporation
    Inventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
  • Patent number: 6303593
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: October 16, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Christopher Forbes, Shouwu Miao, William H. Parsons, Kathleen Rupprecht, Frank Kayser
  • Patent number: 6303620
    Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
    Type: Grant
    Filed: May 6, 1999
    Date of Patent: October 16, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Michael Ankersen
  • Patent number: 6291478
    Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.
    Type: Grant
    Filed: March 13, 2000
    Date of Patent: September 18, 2001
    Assignee: L'Oreal
    Inventors: Jean-Baptiste Galey, Maria Dalko
  • Publication number: 20010021715
    Abstract: Compounds of general formula (I) 1
    Type: Application
    Filed: January 18, 2001
    Publication date: September 13, 2001
    Applicant: Astra Pharma Inc.
    Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
  • Patent number: 6288234
    Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 11, 2001
    Assignee: Advanced Medicine, Inc.
    Inventor: John H. Griffin
  • Patent number: 6288085
    Abstract: The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: September 11, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Duncan Robertson Rae, Samuel George Gibson
  • Patent number: 6288123
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: September 11, 2001
    Assignee: Cambridge NeuroSciences, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: 6277866
    Abstract: The present invention provides a novel compound useful as a medicament, an acetylcholinesterase inhibitor, and an agent for preventing, treating and improving various kinds of senile dementia, Alzheimer-type senile dementia, cerebrovascular dementia or attention deficit hyperactivity disorder, namely, 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanone)-2-yl]methylpiperidine represented by the following formula: or a pharmaceutically acceptable salt thereof, and a process for producing the same.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: August 21, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshio Takeuchi, Norio Shibata, Emiko Suzuki, Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto
  • Publication number: 20010012848
    Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
    Type: Application
    Filed: December 19, 2000
    Publication date: August 9, 2001
    Inventors: Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, Bret Eugene Huff, Charles Howard Mitch, Michael Alexander Staszak, John Stanley Ward
  • Patent number: 6268363
    Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: July 31, 2001
    Assignee: 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
  • Patent number: 6262060
    Abstract: The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes, obesity or inflammation utilizing them.
    Type: Grant
    Filed: November 27, 2000
    Date of Patent: July 17, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Manuel Bedoya-Zurita, Juan Antonio Diaz Martin, Marc Daumas
  • Patent number: 6251918
    Abstract: The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of formula (I).
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: June 26, 2001
    Assignee: Warner-Lambert Company
    Inventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
  • Publication number: 20010004669
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: January 10, 2001
    Publication date: June 21, 2001
    Inventors: Bertrand L. Chenard, John E. Macor, Barbara E. Segelstein
  • Patent number: 6242438
    Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: June 5, 2001
    Assignee: Pfizer Inc.
    Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
  • Patent number: 6242432
    Abstract: Compounds or compositions containing compounds of the formula A-(X1—NO2)to or salts thereof, for the preparation of antithrombotic medications wherein “to” is the integer 1 or 2X1 is an alkylene connecting bridge and “A” is the residue of timolol or analapril.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: June 5, 2001
    Assignee: Nicox S.A.
    Inventor: Piero del Soldato
  • Patent number: 6221866
    Abstract: in which R(1) to R(8) have the meanings stated in the claims, act on the Kv1.5 potassium channel, and inhibit a potassium current, referred to as “ultra-rapidly activating delayed rectifier,” in the human atrium. They are therefore very particularly suitable as novel antiarrhythmic active substances, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g., atrial fibrillation or atrial flutter.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: April 24, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Uwe Gerlach, Hans Ulrich Stilz, Hans-Jochen Lang
  • Patent number: 6211364
    Abstract: The present invention provides intermediate for the preparation of indane-like compounds which are useful for the modulation of a muscarinic receptor.
    Type: Grant
    Filed: June 10, 1999
    Date of Patent: April 3, 2001
    Assignee: Eli Lilly and Company
    Inventors: Bret E Huff, Michael A Staszak, John S Ward
  • Patent number: 6197791
    Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: March 6, 2001
    Assignee: American Cyanamid Company
    Inventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Jannie Lea Baker, Jeremy Ian Levin
  • Patent number: 6187792
    Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: March 5, 1998
    Date of Patent: February 13, 2001
    Assignee: Astra Pharma Inc.
    Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
  • Patent number: 6180818
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: November 3, 1999
    Date of Patent: January 30, 2001
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6177448
    Abstract: The present invention relates to novel pyridine derivatives and compositions comprising them useful in the treatment of disease states mediated by the chemokine Interleukin-8.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: January 23, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine L. Widdowson, John Gerald Gleason
  • Patent number: 6174924
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 16, 2001
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: 6166006
    Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.
    Type: Grant
    Filed: December 17, 1998
    Date of Patent: December 26, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
  • Patent number: 6153625
    Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen, halogen, alkyl, alkenyl, alkynyl, hydroxy, alkoxy, trihaloalkyl, or any pair may form a heterocycle,R.sub.5 represents hydrogen, alkyl, or arylalkyl,R.sub.6 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, or trihaloalkyl,A, together with the carbons of the phenyl, represents a heterocycle,their isomers and addition pharmaceutically-acceptable acid or base salts thereof, and medicinal products containing the same which are useful in the treatment of pathologies in which 5HT.sub.1B receptors are involved.
    Type: Grant
    Filed: August 13, 1999
    Date of Patent: November 28, 2000
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi
  • Patent number: 6143791
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 7, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Hu Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: 6124361
    Abstract: The present invention relates to compounds of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and psychiatric disorders.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: September 26, 2000
    Assignee: Pfizer Inc
    Inventor: Bertrand L. Chenard
  • Patent number: 6121325
    Abstract: The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: September 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Meng Hsin Chen, Gregori J. Morriello, Ravi Nargund, Arthur A. Patchett, Lihu Yang
  • Patent number: 6114570
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: September 5, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6107345
    Abstract: A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: August 22, 2000
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Aimee Dessinges, Jean-Christophe Harmange, Mark Millan, Adrian Newman-Tancredi, Mauricette Brocco
  • Patent number: 6083943
    Abstract: A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: July 4, 2000
    Assignee: Pfizer Inc
    Inventors: Masaya Ikunaka, Yuji Shishido, Masami Nakane
  • Patent number: 6063927
    Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: May 16, 2000
    Assignee: SmithKline Beecham plc
    Inventors: Andrew Simon Craig, Alan David Jones, Deirdre O'Keeffe, Neal Ward
  • Patent number: 6048877
    Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: April 11, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
  • Patent number: 6031099
    Abstract: Piperidine compounds having the general formula (I), ##STR1## wherein R.sup.1 is (a) a group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, phenyl, cycloalkylalkyl, cycloalkenylalkyl, phenylalkyl or diphenylalkyl linked to the piperidyl N-atom through an at least 2-membered spacer group; or (b) a group having general formula (II), ##STR2## wherein X is CHR.sup.10, O, S, SO, SO.sub.2 or NR.sup.10, Z.sup.1 is CH.sub.2, O, or S; Z.sup.2 and Z.sup.3 are independently (CH.sub.2).sub.n, n being 0 or 1, O or S or Z.sup.1 and Z.sup.2 may together represent a group --CH.dbd.CH--; or when Z.sup.3 is (CH.sub.2).sub.n wherein n is 0, Z.sup.1 and Z.sup.2 may together represent a 3-membered divalent group; show potent sigma receptor activity. Furthermore they show effect in animal models indicative of anxiolytic properties.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 29, 2000
    Assignee: H. Lundbeck A/S
    Inventors: Ejner K. Moltzen, Jens Kristian Perregaard
  • Patent number: 6022971
    Abstract: 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: Grant
    Filed: January 26, 1998
    Date of Patent: February 8, 2000
    Assignee: Pfizer Inc
    Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
  • Patent number: 6013656
    Abstract: New 2-(arylalkenyl)azacycloalkane derivatives which are ligands for sigma receptors, of the formula (I) ##STR1## in which: Ar is aryl or heteroaryl, optionally mono- to trisubstituted,m has the value 1 or 2,n has the value 1 to 3,R is phenyl, or cycloalkyl containing 3 to 7 carbon atoms,their isomers and their addition salts.Medicinal drugs which are antipsychotic agents and are useful in gastroenterology.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: January 11, 2000
    Assignee: Warner-Lambert Company
    Inventors: Alain Pierre Calvet, Henry Jacobelli, Jean-Louis Junien, Pierre Riviere, Fran.cedilla.ois-Joseph Roman
  • Patent number: 6013814
    Abstract: The present invention relates to novel 1.alpha.-hydroxy vitamin D derivatives in which the 17-position side chain carries an azide or optionally substituted 1,2,3-triazole group, including compounds of general formula (I) where R.sup.1 represents a methyl group having .alpha.- or .beta.-configuration; W represents a valence bond or a C.sub.1-5 alkylene group; X represents azide or an optionally substituted triazole group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcaemic effect.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: January 11, 2000
    Assignee: Research Institute for Medicine and Chemistry, Inc.
    Inventors: Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal, Gaddam Subba Reddy
  • Patent number: 5998441
    Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O--or --S--;or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of estrogen.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: December 7, 1999
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5998401
    Abstract: A class of substituted phenoxy naphthalene compounds of the structure: ##STR1## where n is 2 or 3; R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl; R.sup.2 is is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl, or halo; and R.sup.3 is 1-piperidinyl, 1-pyrollidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; are useful in the treatment of pathological conditions associated with post-menopause including osteoporosis, endometriosis, uterine fibroid disease, cardiovascular disease (particularly hyperlipidemia), and hormonally-dependent cancers (particularly breast and uterine cancer).
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: December 7, 1999
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5994370
    Abstract: The present invention provides a class of substituted indene compounds and their pharmaceutically acceptable salts which possess selective estrogen receptor modulator (SERM) activity and are thus useful in the treatment of osteoporosis and cardiovascular disease, particularly hyperlipidemia in women. The compounds possess the structure ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.2 is hydrogen, hydroxy, halo, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexa-methyleneimino, and n is 2 or 3. The dashed line bond between the carbon atoms at positions 1 and 2 of the indene nucleus represent an optional double bond with the proviso that when the double bond is absent, the parenthetic hydroxy group at position 1 is present and vice versa.
    Type: Grant
    Filed: April 22, 1998
    Date of Patent: November 30, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Charles David Jones, Pamela Ann Pennington
  • Patent number: 5985895
    Abstract: The invention relates to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z-Y entity represents an N--CH.sub.2, C.dbd.CH or CH--CH.sub.2 group;R.sup.1 represents a hydrogen, fluorine, bromine or iodine atom or a hydroxyl, methoxy, nitrile or nitro group;R.sup.2 represents a hydrogen or bromine atom or a hydroxyl, methoxy, nitrile or nitro group;the R.sub.1 and R.sub.2 substituents both being situated on the same ring of the naphthamide unit or each being situated on one of the rings;R.sup.3 and R.sup.4 can be identical or different and each independently represent a hydrogen or chlorine atom or a methoxy or methyl group or an electron-withdrawing group.The invention also relates to their therapeutic applications as partial agonists of the dopamine D.sub.3 receptor.The invention applies more particularly to the treatment of neuropsychiatric conditions involving the dopamine D.sub.
    Type: Grant
    Filed: June 26, 1998
    Date of Patent: November 16, 1999
    Assignees: Institut National De La Sante et De La Recherche Medicale-INSERM, Societe Civile Bioprojet
    Inventors: Camille-Georges Wermuth, Andre Mann, Fabrice Garrido, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Pierre Sokoloff
  • Patent number: 5977141
    Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: November 2, 1999
    Assignee: Warner-Lambert Company
    Inventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
  • Patent number: 5972964
    Abstract: Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: October 26, 1999
    Assignee: H. Lundbeck A/S
    Inventor: Jens Perregaard
  • Patent number: 5968923
    Abstract: 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: Grant
    Filed: February 10, 1997
    Date of Patent: October 19, 1999
    Assignee: Pfizer Inc.
    Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Sandra Dora Meadows, Donald Stuart Middleton
  • Patent number: 5968954
    Abstract: New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are as defined in the description, in the form of a racemic mixture and in the form of optical isomers, and physiologically-tolerable acid addition salts thereof. The products of the invention are useful as medicaments and exhibit selective binding affinity for the 5HT.sub.1B receptors.
    Type: Grant
    Filed: February 26, 1998
    Date of Patent: October 19, 1999
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert
  • Patent number: 5965575
    Abstract: New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful in the treatment of disorders involving the serotininergic system.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: October 12, 1999
    Assignee: Adir Et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert, Valerie Audinot
  • Patent number: 5965562
    Abstract: The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl-amino)-piperi dines of the formula ##STR1## wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts thereof, to the use thereof, to processes for the preparation thereof and to pharmaceutical compositions comprising a compound according to the invention or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: October 12, 1999
    Assignee: Novartis Corporation
    Inventors: Silvio Ofner, Siem Jacob Veenstra, Walter Schilling