Patents Assigned to Daiichi Pharmaceutical Co., LTD
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Patent number: 6596898Abstract: A process for preparing compounds represented by the following general formula (I) wherein X represents chlorine atom, bromine atom, or iodine atom, and R includes alkoxy group and amino group which comprises the step of allowing a compound represented by the formula: CH2═CXF react with a compound represented by the formula: N2CHCOR in the presence of a catalyst containing a metal atom such as a transition metal of group 8 together with chiral carboxylic-type or amide-type ligands to preferentially obtain a stereoisomer of the compound of the general formula (I) wherein the stereochemical configuration at the 1-position is S-configurationType: GrantFiled: February 27, 1998Date of Patent: July 22, 2003Assignees: Daiichi Pharmaceutical Co., Ltd., Sumitomo Chemical Co., Ltd.Inventors: Tsutomu Ebata, Toshifumi Akiba, Takanobu Ikeya, Ryuhei Wakita, Mikio Sasaki
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Patent number: 6596754Abstract: The present invention relates to a preventive and/or therapeutic drug for hypercytokinemia, liver diseases, and syndromes caused by the aggravation of sepsis, containing an anti-thrombin agent and/or a thrombin production inhibitor as an active ingredient. The present invention is applicable to prevention of or therapy for diseases such as sepsis, severe sepsis, septic shock, and multiple organ dysfunction syndrome. More particularly, the present invention is useful for an emergency medical service, for treatment of injury caused by a traffic accident, burns, heat attacks, or severe infective diseases. In addition, the present invention is useful for prevention and treatment for hypercytokinemia and liver diseases.Type: GrantFiled: March 2, 2001Date of Patent: July 22, 2003Assignee: Daiichi Pharmaceuticals Co., Ltd.Inventors: Tsuyoshi Hara, Kazuko Fujiwara
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Publication number: 20030130340Abstract: The present invention relates to novel benzothiophene derivatives represnted by the following formula (I) or salts thereof, inhibitors of steroid 17&agr;-hydroxylase and/or C17-20 lyase, and pharmaceutical compositions containing the benzothiophene derivative or the salt.Type: ApplicationFiled: November 18, 2002Publication date: July 10, 2003Applicant: Daiichi Pharmaceutical Co. Ltd.Inventors: Shin?apos;ichi Shimada, Shin Nomoto, Masayuki Okue, Ken?apos;ichi Kimura, Junji Nakamura, Yoshikazu Ikeda, Takeko Takada
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Patent number: 6586604Abstract: The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases.Type: GrantFiled: June 8, 2001Date of Patent: July 1, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Kenichi Kimura, Rie Miyauchi, Hitoshi Ohki, Katsuhiro Kawakami
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Patent number: 6573260Abstract: This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I), its salts and hydrates thereof: {R1 and R2: hydrogen, alkyl; n: 1 to 4; Q: following structure (Ia): [R3: alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl, alkylamino; R4: hydrogen, alkylthio; R5: hydrogen, amino, hydroxyl, thiol, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; X1: halogen, hydrogen, A1: nitrogen, structure of formula (II): (X2: hydrogen, amino, halogen, cyano, halogenomethyl, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; R4 and R3 or X2 and R3 may together form a cyclic structure; Y: hydrogen, various ester forming groups]}.Type: GrantFiled: May 24, 2001Date of Patent: June 3, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Rie Miyauchi, Toshiyuki Takeda, Isao Hayakawa
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Patent number: 6573377Abstract: This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G1 are condensed tricyclic heterocyclic rings or salts thereof, and a compound represented by the following formula (Ib) having various substituents or salts thereof.Type: GrantFiled: January 24, 2001Date of Patent: June 3, 2003Assignee: Daiichi Pharmaceuticals Co., Ltd.Inventors: Akio Ejima, Satoru Ohsuki, Hitoshi Ohki, Hiroyuki Naito, Chie Makino
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Publication number: 20030092720Abstract: A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): 1Type: ApplicationFiled: April 26, 2001Publication date: May 15, 2003Applicant: DAIICHI PHARMACEUTICAL CO., LTDInventors: Kiyoshi Nakayama, Masami Ohtsuka, Haruko Kawato, William Watkins, Jason Zhang, Monica Palme, Aesop Cho
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Patent number: 6559157Abstract: Dihydronaphthalene compounds have excellent 17&agr;-hydroxylase/C17-20-lyase inhibiting activity, thromboxan A2 synthesis inhibiting activity, and aromatase inhibiting activity and are thereby are useful as preventive and/or therapeutic agents for various male sex hormone- and female sex hormone-dependent diseases such as prostate cancer, prostatomegaly, masculinization, breast cancer, mastopathy, uterine cancer, endometriosis, and ovarian cancer, as well as myocardial infarction, angina pectoris, and bronchial asthma.Type: GrantFiled: May 25, 2001Date of Patent: May 6, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Rolf Wolfgang Hartmann, Bertil Wachall, Makoto Yoshihama, Masamichi Nakakoshi, Shin Nomoto, Yoshikazu Ikeda
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Publication number: 20030082134Abstract: The present invention provides an agent for preventing and/or treating cachexia comprising T-CF-II as an effective ingredient. An agent for preventing and treating cachexia caused by cancer, acquired immunodeficient syndrome (AIDS), cardiac diseases, infectious disease, shock, burn, endotoxinemia, organ inflammation, surgery, diabetes, collagen diseases, radiotherapy, chemotherapy is provided by the present invention.Type: ApplicationFiled: October 9, 2002Publication date: May 1, 2003Applicant: Daiichi Pharmaceutical Co., Ltd.Inventors: Masamichi Kojiro, Hirohisa Yano, Akihiro Iemura
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Publication number: 20030078249Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed.Type: ApplicationFiled: December 28, 2001Publication date: April 24, 2003Applicant: Daiichi Pharmaceutical Co., LTD.Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
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Patent number: 6552018Abstract: The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.Type: GrantFiled: October 17, 2000Date of Patent: April 22, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Akio Ejima, Satoru Ohsuki, Hitoshi Ohki, Hiroyuki Naito
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Patent number: 6552197Abstract: Disclosed are a process for the preparation of a compound represented by the formula (1), which comprises treating a compound represented by the formula (2) with methanesulfonic acid and then subjecting the thus-treated compound to recrystallization; and Compound (1) so obtained. This Compound (1) is free of hygroscopicity, excellent in filterability and solubility and easy in handling. Furthermore, according to the preparation process of the present invention, an unnecessary isomer can be converted into the target one and separation of the target isomer can be conducted easily.Type: GrantFiled: June 11, 2001Date of Patent: April 22, 2003Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Shinji Kamihara, Kazuaki Kanai, Shigeru Noguchi, Hirofumi Terasawa, Hiroaki Kitaoka
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Publication number: 20030073117Abstract: A novel mechanosensitive channel protein derived from mouse or humans which is expressed specifically in the kidney and has the function of non-selectively transporting cation into cells in response to a mechanical stimulus; a DNA encoding these proteins; a method of screening cation channel activity activators or inhibitors with these proteins; and antibodies to these proteins. The above-described proteins are useful as a diagnostic agent or a therapeutic agent for diseases based on abnormalities in the cation channel, such as hypertension or diabetes, or as a tool for screening chemicals for preventing and/or treating these diseases.Type: ApplicationFiled: August 23, 2002Publication date: April 17, 2003Applicant: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Suzuki, Ken?apos;ichi Ishibashi
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Patent number: 6545151Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: January 16, 2001Date of Patent: April 8, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Publication number: 20030050471Abstract: Antibiotics RK-1061s having a novel chemical structure and a method of production thereof.Type: ApplicationFiled: August 5, 2002Publication date: March 13, 2003Applicant: Daiichi Pharmaceutical Co., Ltd.Inventors: Ken-Ichi Kimura, Yoshikazu Ikeda, Shinobu Kagami, Hidetoshi Takahashi, Kousaku Takahashi, Makoto Yoshihama, Makoto Ubukata, Kiyoshi Isono
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Patent number: 6525042Abstract: Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1 is hydrogen, hydroxyl, nitro or the like; R2 and R3 are each independently hydrogen, halogeno or the like; R4 and R5 are each dependently hydrogen, halogeno or the like; Q1 is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2 is a single bond, oxygen or the like; Q3 is, e.g., a group represented by formula (a): T1 is carbonyl or the like; and X1 and X2 are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.Type: GrantFiled: March 28, 2000Date of Patent: February 25, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Syozo Kobayashi, Satoshi Komoriya, Masayuki Ito, Tsutomu Nagata, Akiyoshi Mochizuki, Noriyasu Haginoya, Takayasu Nagahara, Haruhiko Horino
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Patent number: 6515142Abstract: A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1 represents a protective group for a nitrogen atom; R2 represents a methanesulfonyl group or p-toluenesulfonyl group; R1 represents a hydrogen atom, an aralkyl group, or an alkyl group having 1 to 6 carbon atoms; and X represents a halogen atom. The above process is useful as an industrial process for preparing intermediates of anticoagulant aromatic amidine derivatives described in Japanese Patent Application Laid-Open (kokai) No. 208946/1993.Type: GrantFiled: November 7, 2001Date of Patent: February 4, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Yukio Yokoyama, Tatsuya Kobayashi, Takeo Koyama
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Patent number: 6504029Abstract: Disclosed are a process for the preparation of a compound represented by the formula (1), which comprises treating a compound represented by the formula (2) with methanesulfonic acid and then subjecting the thus-treated compound to recrystallization; and Compound (1) so obtained. This Compound (1) is free of hygroscopicity, excellent in filterability and solubility and easy in handling. Furthermore, according to the preparation process of the present invention, an unnecessary isomer can be converted into the target one and separation of the target isomer can be conducted easily.Type: GrantFiled: July 13, 1995Date of Patent: January 7, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shinji Kamihara, Kazuaki Kanai, Shigeru Noguchi, Hirofumi Terasawa, Hiroaki Kitaoka
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Patent number: 6498139Abstract: The present invention provides methods of inhibiting or sequestering 14-3-3 protein from binding to the insulin receptor substrate −1 or −2 by administering a substance which inhibits the interaction of these two proteins.Type: GrantFiled: March 29, 2000Date of Patent: December 24, 2002Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Yoshio Yazaki, Tomoichiro Asano, Hideo Kubo, Akira Kanda
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Publication number: 20020193591Abstract: The present invention provides a process for producing intermediates of antibacterial agents in accordance with the following steps and intermediates in the production thereof.Type: ApplicationFiled: July 11, 2002Publication date: December 19, 2002Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Makoto Takemura, Hisashi Takahashi