Patents Represented by Attorney Elaine M. Ramesh
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Patent number: 6653476Abstract: The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.Type: GrantFiled: August 22, 2002Date of Patent: November 25, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Atsuo Baba, Haruhiko Makino, Isao Aoki, Toshiaki Nagata
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Patent number: 6649643Abstract: Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.Type: GrantFiled: April 12, 2002Date of Patent: November 18, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6627630Abstract: A condensed pyridazine derivative which is useful as a pharmaceutical composition for preventing or treating allergic skin diseases such as contact dermatitis, pruritus, dried dermatitis, acute urticaria and prurigo.Type: GrantFiled: April 18, 2001Date of Patent: September 30, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuhiko Kawano, Hideaki Nagaya, Michiyo Gyoten, Yukio Hara, Motoki Ikeuchi
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Patent number: 6627651Abstract: Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1 is an optionally substituted five- or six-membered ring group; X1 is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1 and E4 are each optionally substituted carbon or the like; E2 and E3 are each oxygen or the like; and a and b are each a single bond or a double bond); X2 is a divalent group constituting a straight chain moiety; Z1 is a divalent cyclic group or the like; Z2 is a free valency or the like; and R2 is optionally substituted amino or the like.Type: GrantFiled: November 2, 2001Date of Patent: September 30, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Masaki Seto, Naoyuki Kanzaki, Osamu Nishimura
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Patent number: 6620825Abstract: A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.Type: GrantFiled: June 3, 2002Date of Patent: September 16, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Hiroyuki Kimura, Naoyuki Kanzaki
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Patent number: 6613805Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 16, 2001Date of Patent: September 2, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 6613887Abstract: The invention provides an ependymin-like protein derived from a mammal, or its partial peptide or its precursor protein, or a salt thereof; a signal peptide; a DNA coding for the protein, etc. a recombinant vector; a transformant; a method of producing the protein; a pharmaceutical composition comprising the protein, etc. or DNA, an antibody against the protein, etc.; and a method for screening and a screening kit for compounds promoting the function of the protein. The protein, its partial peptide or a salt thereof has physiological activities such as a nerve-extending or nerve-regenerating activity, a gliacyte stimulating activity, and so on. The protein, etc. or the DNA is useful as a therapeutic or prophylactic agent for Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis (ALS), dementia or cerebellar degeneration. The antibody against the protein, etc. can be used in the assay of the protein, etc. in a test sample. Furthermore, the protein, etc.Type: GrantFiled: February 25, 1999Date of Patent: September 2, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Kazuhiro Ogi, Haruo Onda
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Patent number: 6610694Abstract: A condensed pyridazine derivative which exhibits anti-allergic activity, anti-histaminic activity and/or eosinophil chemotaxis-inhibiting activity, anti-inflammatory activity, anti-PAF (platelet-activating factor) activity, and the like, and is useful as an agent for preventing or treating asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis, and the like.Type: GrantFiled: April 2, 2001Date of Patent: August 26, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuhiko Kawano, Hideaki Nagaya, Michiyo Gyoten
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Patent number: 6605629Abstract: A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, a thiol group which may optionally be substituted, or an amino group which may optionally be substituted; A represents an acyl group which may optionally be substituted, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, or a carboxyl group which may optionally be esterified or amidated; B represents an aromatic group which may optionally be substituted; X represents oxygen atom, sulfur atom, or nitrogen atom which may optionally be substituted; and Y represents a divalent hydrocarbon group or heterocyclic group, or a salt thereof; which is useful as an agent for preventing or treating neuropathy.Type: GrantFiled: June 29, 2001Date of Patent: August 12, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Katsuhito Murase
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Patent number: 6589547Abstract: The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.Type: GrantFiled: August 9, 2000Date of Patent: July 8, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasutaka Igari, Akira Saikawa, Yoshiyuki Inada, Shigeru Kamei
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Patent number: 6586004Abstract: A solid preparation which comprises (i) a pharmaceutically active ingredient, (ii) one or more water-soluble sugar alcohol selected from the group consisting of sorbitol, maltitol, reduced starch saccharide, xylitol, reduced palatinose and erythritol, and (iii) low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight; which exhibits excellent buccal disintegration and dissolution and also appropriate strength.Type: GrantFiled: March 7, 2001Date of Patent: July 1, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshihiro Shimizu, Masae Sugaya
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Patent number: 6583164Abstract: The composition of the present invention comprises a quaternized nitrogen-containing imidazole-1-yl or 1,2,4-triazole-1-yl compound wherein one of the nitrogen atoms constituting the azole ring is quaternized with a group eliminating in vivo and represented by the formula: wherein R1 represents a hydrocarbon or heterocyclic group which may be substituted, R2 represents a hydrogen atom or a lower alkyl group, and n is 0 or 1, and a saccharide, said compound being capable of being converted into an anti-fungal azole compound upon elimination of said group in vivo. The composition of the present invention is stable and usable particularly as a pharmaceutical preparation for an injection composition.Type: GrantFiled: March 19, 2001Date of Patent: June 24, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidetoshi Horibe, Yoko Nishida, Masao Nagao
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Patent number: 6573289Abstract: A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.Type: GrantFiled: October 18, 2000Date of Patent: June 3, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6566535Abstract: A process for preparing a compound represented by the following formula: wherein each symbol is as defined below, or a salt thereof, characterized by subjecting a compound represented by the following formula: wherein R1 is an electron-attracting group; R2, R3, R4, R5, R6 and R7 are each a hydrogen atom, a halogen atom, an optionally substituted amino group, an optionally substituted hydroxyl group, an optionally substituted thiol group, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group, provided that R6 and R7 may be united to form a ring; and R8 is a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, to a ring-closing reaction.Type: GrantFiled: November 7, 2001Date of Patent: May 20, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tatsuya Ito, Tomomi Ikemoto, Kiminori Tomimatsu
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Patent number: 6555565Abstract: An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.Type: GrantFiled: January 15, 2002Date of Patent: April 29, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Junji Matsui, Naoki Tarui, Yu Momose, Ken-ichi Naruo
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Patent number: 6552054Abstract: The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone derivatives for bone diseases and chondropathy: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 is a hydrogen atom or hydrocarbon group; R3 is a hydrogen atom, hydrocarbon group or halogen; n is an integer of 0-3; or a salt thereof.Type: GrantFiled: March 1, 2002Date of Patent: April 22, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Masahiro Kawase, Akira Mori
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Patent number: 6534496Abstract: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.Type: GrantFiled: October 7, 1999Date of Patent: March 18, 2003Assignee: Takeda Chemical Industries, Inc.Inventors: Yuji Ishihara, Yukio Fujisawa, Naoki Furuyama
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Patent number: 6531604Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 11, 2002Date of Patent: March 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Patent number: 6518257Abstract: To provide a composition having a steroid C17,20-lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the pophylaxis or treatment of prostatism and tumors such as beast cancer and the like.Type: GrantFiled: April 18, 2002Date of Patent: February 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Tomohiro Kaku, Masami Kusaka
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Patent number: 6500820Abstract: The present invention provides a composition for neurotrophic action which comprises a compound of the formula: wherein Ar is an optionally condensed phenyl group which may be substituted; n is an integer of 1 to 10; R is a hydrogen atom or a hydrocarbon group which may be substituted; and Y is an amino group which may be substituted or a nitrogen-containing saturated heterocyclic group which may be substituted; or a salt thereof, which compounds are useful for preventing and/or treating (1) neurodegenerative diseases (e.g. senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, Creutzfelt-Jakob disease, amyotrophic lateral sclerosis, diabetic neuropathy, etc.), (2) neuropathy in cerebrovascular diseases (e.g. impairment of cerebral blood flow based on cerebral infarction, cerebral hemorrhage, cerebral sclerosis, etc.), brain trauma, spinal cord injury, cerebritis sequela and cerebral palsy, (4) mental diseases (e.g.Type: GrantFiled: October 10, 2000Date of Patent: December 31, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Masaomi Miyamoto, Koki Kato, Yuji Ishihara