Tetrazoles (including Hydrogenated) Patents (Class 548/250)
-
Publication number: 20110237633Abstract: The present invention provides compounds and pharmaceutically acceptable compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which hepatocyte growth factor/scatter factor (HGF/SF) or the activities thereof, or agonists or antagonists thereof, have a therapeutically useful role.Type: ApplicationFiled: December 11, 2009Publication date: September 29, 2011Inventors: Bijoy Panicker, Lambertus J.W.M. Oehlen, Itzhak G. Goldberg
-
Patent number: 8017635Abstract: Certain novel phenylalkyl substituted azole derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B, D, E, G, a, b, c, d, and R through R11, inclusively, are folly described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: May 24, 2006Date of Patent: September 13, 2011Assignee: FMC CorporationInventors: John W. Lyga, Frank Zawacki, Larry Y. Zhang
-
Patent number: 8008505Abstract: This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.Type: GrantFiled: September 21, 2009Date of Patent: August 30, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
-
Patent number: 8003805Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 28, 2010Date of Patent: August 23, 2011Assignee: Array BioPharma Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
-
Patent number: 8003801Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.Type: GrantFiled: November 9, 2006Date of Patent: August 23, 2011Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
-
Publication number: 20110201640Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:Type: ApplicationFiled: August 6, 2009Publication date: August 18, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
-
Publication number: 20110184187Abstract: The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.Type: ApplicationFiled: April 7, 2011Publication date: July 28, 2011Inventor: Gottfried Sedelmeier
-
Patent number: 7981914Abstract: Compounds of the formula: wherein R1, R2, Ar1, Ar2, and n are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.Type: GrantFiled: October 1, 2008Date of Patent: July 19, 2011Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Todd Richard Elworthy, Hans Maag, Sunil Sahdeo
-
Patent number: 7964625Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds, the bis(1-aryl-5-tetrazolyl)methanes, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.Type: GrantFiled: September 29, 2006Date of Patent: June 21, 2011Assignee: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TnoInventors: Frank Henri Johan Schuren, Henricus Matheus Wilhelmus Maria Thijssen, Roy Christiaan Montijn
-
Patent number: 7956054Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: July 2, 2010Date of Patent: June 7, 2011Assignee: Theravance, Inc.Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
-
Patent number: 7956216Abstract: Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.Type: GrantFiled: December 21, 2006Date of Patent: June 7, 2011Assignee: The Walter and Eliza Hall Institute of Medical ResearchInventors: Guillaume Laurent Lessene, Jonathan Baell
-
Patent number: 7947664Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5; Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: January 8, 2009Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent R. Whitehead
-
Patent number: 7947696Abstract: Novel phenylquinazoline derivatives of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: April 24, 2006Date of Patent: May 24, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller
-
Patent number: 7943779Abstract: The present invention relates to an improved process for the manufacture of olmesartan and pharmaceutically acceptable salts and esters thereof as an active ingredient of a medicament for the treatment of hypertension and related diseases and conditions.Type: GrantFiled: July 27, 2006Date of Patent: May 17, 2011Assignee: KRKAInventors: Silvo Zupancic, Anica Pecavar, Miha Vrbinc, Renata Osolnik
-
Patent number: 7943788Abstract: A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); a pharmaceutically acceptable salt thereof, or a prodrug thereof.Type: GrantFiled: January 31, 2005Date of Patent: May 17, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Sumihiro Nomura, Eiji Kawanishi, Kiichiro Ueta
-
Patent number: 7932279Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.Type: GrantFiled: October 14, 2008Date of Patent: April 26, 2011Assignee: ArQule, Inc.Inventors: Rui-Yang Yang, Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Rocio Palma, Neil Westlund
-
Patent number: 7923566Abstract: The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.Type: GrantFiled: December 21, 2005Date of Patent: April 12, 2011Assignee: Suven Life Sciences LimitedInventors: Arava Veera Reddy, Siripalli Udaya Bhaskara Rao, Chinnapillai Rajendiran, Venkateswarlu Jasti
-
Patent number: 7919071Abstract: The present invention relates to a contrast agent of Formula I V-L-Z Formula I where V is a non-peptidic vector having affinity for the Angiotensin II receptor, L is a bond, a spacer or a linker moiety and Z represents a moiety detectable in an in vivo imaging procedure of a human or animal body.Type: GrantFiled: January 9, 2004Date of Patent: April 5, 2011Assignee: GE Healthcare ASInventors: Magne Solbakken, Torgrim Engell, Harry John Wadsworth, Colin M. Archer
-
Patent number: 7915402Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: April 20, 2009Date of Patent: March 29, 2011Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
-
Patent number: 7906546Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: GrantFiled: May 6, 2010Date of Patent: March 15, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
-
Patent number: 7906501Abstract: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.Type: GrantFiled: April 27, 2005Date of Patent: March 15, 2011Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, Lucio Claudio Rovati
-
Patent number: 7897331Abstract: Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkylammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring.Type: GrantFiled: June 16, 2010Date of Patent: March 1, 2011Assignee: Bayer HealthCare LLCInventors: James P. Albarella, Steven W. Felman, John J. Landi, Karen L. Marfurt
-
Patent number: 7884212Abstract: The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid.Type: GrantFiled: September 29, 2006Date of Patent: February 8, 2011Inventor: Silvo Zupancic
-
Patent number: 7880015Abstract: The present invention provides a method for the preparation of N-(1-oxopentyl)-N-[[2?-(1H-tetra-zol-5-yl)[1,1?-biphenyl]-4-yl]methyl]-L-valine (Valsartan) which comprises; treating N-[[2?-(1-triphenylmethyl-tetra-zol-5-yl)biphenyl-4-yl]methyl]-L-valine methyl ester (X) with oxalic acid or its hydrates in a solvent to produce N-[[2?-(1-triph-enylmethyl-tetrazol-5-yl)biphenyl-4-yl]methy]-L-valine methyl ester oxalate (Xa) and treating the compound (Xa) with a base in a solvent followed by reacting with valeryl chloride in presence of base in a solvent to produce N-[[2?-(1-triphenylmethyl-tetra-zol-5-yl)[1,1?biphenyl]-4-yl]methyl]-N-valeryl-L-valine methyl ester (XI), de-protecting the compound (XI) using anhydrous acidic conditions to produce N-(1-oxopentyl)-N-[[2?-(1-H-tetrazol-5-yl)[1,1?biphenyl]-4-yl]methyl-L-valine methyl ester (V) followed by treating with base in a solvent to produce Valsartan.Type: GrantFiled: June 29, 2007Date of Patent: February 1, 2011Assignee: Aurobindo Pharma Ltd.Inventors: Sankar Reddy Budidet, Senthil Kumar Natarajan, Venkata Kishore Gowrabathina, Ramesh Dandala, Sivakumaran Meenakshisunderam
-
Patent number: 7880014Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5-; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: December 11, 2007Date of Patent: February 1, 2011Assignees: Merck Sharp & Dohme Corp., NiCox S.A.Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali, Chris Franklin, Nicoletta Almirante, Laura Storoni, Silvia Stefanini
-
Patent number: 7875647Abstract: A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: GrantFiled: September 28, 2007Date of Patent: January 25, 2011Assignee: Green Cross CorporationInventors: Jinhwa Lee, Jeong Min Kim, Chong-Hwan Jonathan Chang, Suk Ho Lee, Hee Jeong Seo, Suk Youn Kang, Kwang-Seop Song, Jong Yup Kim, Min-ah Kim, Sung-han Lee, Kwang-Woo Ahn, Myung Eun Jung, Ji-Hyun Park
-
Patent number: 7875641Abstract: The present invention relates to sesquihydrate hydrochloride salt of irbesartan and pharmaceutical compositions comprising the same.Type: GrantFiled: July 29, 2005Date of Patent: January 25, 2011Assignee: KRKA Tovarna Zdravil, D.D., Novo MestoInventors: Silvo Zupancic, Matej Smrkolj, Renata Jaske
-
Publication number: 20110015403Abstract: The novel process for iodinating substituted azoles, especially for iodinating substituted 1H-tetrazoles and substituted 1H-triazoles, affords the desired compounds in high purity and with good yield.Type: ApplicationFiled: January 12, 2007Publication date: January 20, 2011Inventor: Erasmus Vogl
-
Patent number: 7851494Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: July 2, 2007Date of Patent: December 14, 2010Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. von Borstel, Kirvin L. Hodge, Michael K. Bamat, Stephen D. Wolpe
-
Patent number: 7842708Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: October 5, 2009Date of Patent: November 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
-
Patent number: 7838683Abstract: Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4?-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.Type: GrantFiled: May 4, 2007Date of Patent: November 23, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Gennady Nisnevich, Igor Rukhman, Boris Pertsikov, Julia Kaftanov, Ben-Zion Dolitzky
-
Publication number: 20100292286Abstract: The invention provides the crystalline imidazole-5-carboxylic acid derivative (I, the chemical name: 2-butyl-4-chloro-1-[2?-(1H-tetrazol-5-yl) 1,1?-biphenyl-methyl]-imidazole-5-carboxylic acid, 1-[(isopropoxy)-carbonyloxy] methyl ester), its preparation method and uses thereof.Type: ApplicationFiled: October 10, 2008Publication date: November 18, 2010Inventors: Jianhui Guo, Dong An
-
Patent number: 7834042Abstract: A compound having the structure (Formula I), wherein Y is —Y1—Y2—Y3—Y4—Y5—; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.Type: GrantFiled: December 11, 2007Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali
-
Patent number: 7833330Abstract: Embodiments of the present subject matter provide a compound and material that may be used as a lead-free primary explosive. An embodiment of the present subject matter provides the compound copper(I) nitrotetrazolate. Certain embodiments of the present subject matter provide methods for preparing lead-free primary explosives. The method includes: providing cuprous salt; providing water; providing 5-nitrotetrazolate salt; combining the cuprous salt, water and 5-nitrotetrazolate salt to form a mixture; and heating the mixture. The method may also include providing cuprous chloride and providing sodium 5-nitrotetrazolate. Certain embodiments of the present subject matter also provide methods for preparing copper(I) nitrotetrazolate. The method includes: providing cuprous salt; providing water; providing 5-nitrotetrazolate salt; combining the cuprous salt, water and 5-nitrotetrazolate salt to form a mixture; and heating the mixture.Type: GrantFiled: February 20, 2007Date of Patent: November 16, 2010Assignee: Pacific Scientific Energetic Materials CompanyInventors: John W. Fronabarger, Michael D. Williams, William B. Sanborn
-
Patent number: 7834041Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: September 5, 2008Date of Patent: November 16, 2010Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Vivek Sasikumar
-
Publication number: 20100286215Abstract: There is provided compounds of formula (I): wherein Y, ring A, D1, D2, D3, L1, Y1, L2, Y2, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: September 3, 2008Publication date: November 11, 2010Inventors: Benjamin Pelcman, Peter Nilsson, Martins Katkevics
-
Patent number: 7824710Abstract: Described is a new crystalline Form A of Andolast disodium salt, triclinic, displaying a thermal event at 98-112° C. and melting with decomposition at about 400° C. (DSC). Andolast disodium Form A is a not hygroscopic solid, surprisingly stable to several humidity conditions in a temperature range acceptable for ordinary storage conditions. In addition its stability allows both chemical manufacturing and pharmaceutical manufacturing process consistency and reproducibility under conditions more viable and less expensive when compared to those used for highly hygroscopic solids.Type: GrantFiled: February 23, 2007Date of Patent: November 2, 2010Assignee: Rottapharm S.p.A.Inventors: Antonio Giordani, Antonino Santoro, Paolo Senin, Matteo Ghirri, Francesco Makovec, Paola Gilotta, Walter Peris, Lucio Claudio Rovati
-
Patent number: 7820825Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: GrantFiled: March 14, 2007Date of Patent: October 26, 2010Assignee: Wyeth LLCInventors: Derek Cecil Cole, Magda Asselin, Joseph Raymond Stock, Albert Jean Robichaud, Ji-In Kim, William Ronald Solvibile, Jonathan Laird Gross
-
Patent number: 7816562Abstract: The invention is amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate anion wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms, and a cationic counter ion.Type: GrantFiled: October 6, 2006Date of Patent: October 19, 2010Assignee: Dow Global Technologies Inc.Inventors: Shaoguang Feng, Gary L. Jialanella, Peter Nickias, Toni Ristoski
-
Patent number: 7807701Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.Type: GrantFiled: November 13, 2007Date of Patent: October 5, 2010Assignee: Japan Tobacco Inc.Inventors: Kimiya Maeda, Hironobu Nagamori, Hiroshi Nakamura, Hisashi Shinkai, Yasunori Suzuki, Daisuke Takahashi, Toshio Taniguchi
-
Patent number: 7807702Abstract: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: GrantFiled: November 21, 2006Date of Patent: October 5, 2010Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Scott Eugene Conner, Philip-Arthur Hipskind, Allie Edward Tripp, Guoxin Zhu
-
Patent number: 7795255Abstract: Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.Type: GrantFiled: January 5, 2006Date of Patent: September 14, 2010Assignee: InSight Biopharmaceuticals Ltd.Inventors: Joel M. Van Gelder, Joseph Y. Klein, Yochai Basel, Anat Reizelman, Susanna Tchilibon, Orly Mouallem
-
Patent number: 7790770Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: GrantFiled: November 13, 2006Date of Patent: September 7, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Heather Finlay, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
-
Patent number: 7781437Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: October 10, 2006Date of Patent: August 24, 2010Assignee: Schering CorporationInventors: Seong Heon Kim, Bandarpalle B. Shankar, Joseph A. Kozlowski, Stuart B. Rosenblum, Neng-Yang Shih
-
Publication number: 20100204199Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: ApplicationFiled: April 14, 2010Publication date: August 12, 2010Inventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
-
Patent number: 7772285Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.Type: GrantFiled: November 13, 2002Date of Patent: August 10, 2010Assignee: Toyama Chemical Co., Ltd.Inventors: Hisaaki Chaki, Hironori Kotsubo, Tadashi Tanaka, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
-
Publication number: 20100197562Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: February 11, 2008Publication date: August 5, 2010Applicants: SCHERING CORPORATION AND PHARMACOPEIA, LLC, PHARMACOPEIA, INC.Inventors: Manuel De lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie L. Ciesla, Chia-yu Huang, Bo Liang
-
Patent number: 7767822Abstract: Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkylammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring. Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkyl ammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring, e.g. the compounds of the general formula shown below. Formula (A-)a.Type: GrantFiled: January 13, 2006Date of Patent: August 3, 2010Assignee: Bayer Healthcare LLCInventors: James P. Albarella, Steven W. Felman, John J. Landi, Karen L. Marfurt
-
Patent number: 7763610Abstract: The present invention relates to a compound of formula (I) (wherein all symbols have the same meanings as described hereinbefore). The compound antagonizes cysLT2 and therefore, it is useful as an agent for the prevention and/or treatment of respiratory diseases such as bronchial asthma, bronchial asthma, chronic obstructive pulmonary disease, pneumonectasia, chronic bronchitis, pneumonia (e.g. interstitial pneumonitis etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), and the like, or as an expectorant or antitussives.Type: GrantFiled: August 31, 2004Date of Patent: July 27, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Jun Takeuchi, Satoshi Itadani, Yoshisuke Nakayama, Tadashi Tatsumi, Shinya Takahashi, Manabu Fujita
-
Publication number: 20100179203Abstract: This invention relates to novel pyrazole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: June 27, 2008Publication date: July 15, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen, David Spencer Jones