Patents Represented by Attorney Mark Chao
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Patent number: 6407116Abstract: A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or S; one of R1 and R2 represents a group represented by the formula: (wherein Ar1 and Ar2 represent an aromatic group optionally having substituents; Ar1 and Ar2 may form a condensed cyclic group optionally having substituents together with an adjacent carbon atom; ring B represents a nitrogen-containing heterocycle optionally having substituents; X and Y are a bond, O, S(O)p (p is an integer of 0 to 2), NR4 (R4 is H or a lower alkyl group) or a bivalent straight-chained lower hydrocarbon group, which may contain 1 to 3 hetero atoms, optionally having substituents; and R3 represents H, a hydroxy group optionally having substituents or an optionally esterified carboxyl group); and the other is a hydrogen atom, a cyano group or a hydrocarbon group optionally having substituents&rsqType: GrantFiled: February 25, 2000Date of Patent: June 18, 2002Assignee: Takeda Chemical Industries, Inc.Inventors: Masahiro Kajino, Shinji Morimoto, Atsuhiro Inaba, Hideaki Nagaya
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Patent number: 6407129Abstract: A quaternized nitrogen-containing imidazol-1-yl or 1,2,4-triazol-1-yl compound wherein one of the nitrogen atoms constituting an azole ring is quaternized with a substituent capable of being eliminated in vivo and the substituent can be eliminated in vivo to be converted into an antifungal azole compound, has an improved solubility in water, can advantageously be applied to injection, has an improved internal absorption and can be expected to have a good effect for the treatment or prevention of disease.Type: GrantFiled: September 20, 1999Date of Patent: June 18, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Katsumi Itoh, Tomoyuki Kitazaki, Kenji Okonogi
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Patent number: 6403595Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.Type: GrantFiled: August 3, 2000Date of Patent: June 11, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-ichi Terashita
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Patent number: 6399639Abstract: 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: March 7, 2000Date of Patent: June 4, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Junji Matsui, Naoki Tarui, Yu Momose, Ken-ichi Naruo
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Patent number: 6399103Abstract: A method of producing sustained-release microcapsules which comprises dispersing a physiologically active polypeptide into a solution of a biodegradable polymer and zinc oxide in an organic solvent, followed by removing the organic solvent; which provides a sustained-release preparation showing a high entrapment ratio of the physiologically active polypeptide and its constant high blood concentration levels over a long period of time.Type: GrantFiled: November 14, 2000Date of Patent: June 4, 2002Assignee: Takeda Chemical Industries, Inc.Inventors: Yutaka Yamagata, Masafumi Misaki, Susumu Iwasa
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Patent number: 6388022Abstract: The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO2X)m wherein  is a carrier, X is a leaving group, Y is a bond or spacer, Z is a bivalent group, when Z is a bivalent electron attractive group, W is an aromatic ring which may be substituted and when Z is a bivalent non-electron attractive group, W is an aromatic ring which is substituted by an electron attractive group and may be further substituted and m is 1 or 2, or a salt thereof, which is useful for synthesizing a novel organic compound.Type: GrantFiled: August 30, 1999Date of Patent: May 14, 2002Assignee: Takeda Chemical Industires, Ltd.Inventors: Katsunori Nagai, Tetsuo Miwa
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Patent number: 6387687Abstract: A microorganism having indolmycin-producing ability and tryptophan analogue resistance is provided, and indolmycin or its salt can be produced efficiently by cultivating such microorganism in a medium to produce and accumulate indolmycin or its salt in the culture broth followed by recovering a product.Type: GrantFiled: January 23, 2001Date of Patent: May 14, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiko Naotsuka, Motoo Izawa, Ken-ichiro Miyagawa
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Patent number: 6359134Abstract: The present invention provides compounds which specifically inhibit FXa, which are effective when orally administered and which are useful as a safe medicine for the prevention or treatment of diseases caused by thrombus or infarction.Type: GrantFiled: November 30, 1999Date of Patent: March 19, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Tawada, Fumio Ito, Norihiko Moriya, Zen-ichi Terashita
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Patent number: 6355672Abstract: 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 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Patent number: 6352982Abstract: The present invention provides a compound of the formula: wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; Z is an optionally substituted cyclic group or linear hydrocarbon group; R1 is a hydrogen atom, an optionally substituted hydrocarbon group or heterocyclic ring; R2 is an optionally substituted amino group; D is a bond or an optionally substituted divalent hydrocarbon group; E is a bond, —CON(Ra)—, —N(Ra)CO—, —N(Rb)CON(Rc)—, —N(Rd)COO—, —N(Re)SO2—, —COO—, —N(Rf)—, —O—, —S— —SO—, —SO2—, (in which Ra, Rb, Rc, Rd, Re and Rf are respectively a hydrogen atom or an optionally substituted hydrocarbon group); G is a bond or an optionally divalent substituted hydrocarbon group; L is a divalent group; ringType: GrantFiled: October 14, 1999Date of Patent: March 5, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroshi Mabuchi, Nobuhiro Suzuki, Takashi Miki
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Patent number: 6350749Abstract: The present invention is to provide a compound of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic heterocyclic ring, the ring B an optionally substituted 5- to 6-membered aromatic homocyclic ring or an optionally substituted 5- to 6-membered aromatic heterocyclic ring, R1 is a hydrogen atom, a hydroxy group or a lower alkyl group, and n is 0 or 1, or a salt thereof, which is effective for the prevention or treatment of ischemic cardiac disease, etc., and which is useful as an agent for preventing or treating ischemic cardiac disease, etc. such as myocardial infarction, arrhythmia, etc.Type: GrantFiled: August 8, 2000Date of Patent: February 26, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Shoji Fukumoto, Keiji Kusumoto
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Patent number: 6348485Abstract: The present invention provides a pharmaceutical composition for treating or preventing sleep disorders which comprises (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide in combination with at least one active component selected from zolpidem, zopiclone, triazolam and brotizolam.Type: GrantFiled: November 14, 2000Date of Patent: February 19, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Masaomi Miyamoto
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Patent number: 6344209Abstract: An apatite-coated solid composition which contains a biodegradable polymer and an apatite-coated solid composition which contains a biodegradable polymer and a medicinal substance have properties of sustained release and of osteoconductive activity.Type: GrantFiled: October 20, 1999Date of Patent: February 5, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Kazuhiro Saito, Tetsuo Hoshino
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Patent number: 6340686Abstract: A compound of the formula: wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula: wherein R5 is hydrogen or R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.Type: GrantFiled: May 16, 2000Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuhiro Suzuki, Nobuo Choh, Yoshi Nara
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Patent number: 6329403Abstract: A pharmaceutical composition which comprises an insulin sensitizer in combination with an anorectic, which is useful as an agent for preventing or treating diabetes.Type: GrantFiled: August 25, 1999Date of Patent: December 11, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Odaka, Masahiro Yamane
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Patent number: 6328994Abstract: An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 &mgr;m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.Type: GrantFiled: August 4, 1999Date of Patent: December 11, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshihiro Shimizu, Shuji Morimoto, Tetsuro Tabata
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Patent number: 6329388Abstract: The compounds of the present invention possess excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.Type: GrantFiled: December 14, 2000Date of Patent: December 11, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuo Choh, Nobuhiro Suzuki, Takashi Imada
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Patent number: 6329389Abstract: The present invention provides a compound of the formula: wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO2 or CO; Y represents a spacer having a main chain of 2 to 5 atoms; n represents an integer of 1 to 5; i) R1 and R2 each represents a hydrogen atom or a lower alkyl which may be substituted, ii) R1 and R2 form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, or iii) R1 or R2 together with —(CH2)n—N═ form, bonded to a component atom of Ring B, a spiro-ring which may be substituted; Ring A represents an aromatic ring which may be substituted; Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl, with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula: —NHCOR11 where R11 represents alkyl, alkoxyalkyl, alkylthioType: GrantFiled: November 19, 1999Date of Patent: December 11, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Nobuhiro Suzuki, Kaneyoshi Kato, Shiro Takekawa, Jun Terauchi, Satoshi Endo
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto