Patents Represented by Attorney, Agent or Law Firm Philippe Y. Riesen
  • Patent number: 6352982
    Abstract: 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; ring
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: March 5, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroshi Mabuchi, Nobuhiro Suzuki, Takashi Miki
  • Patent number: 6329389
    Abstract: 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, alkylthio
    Type: Grant
    Filed: November 19, 1999
    Date of Patent: December 11, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Nobuhiro Suzuki, Kaneyoshi Kato, Shiro Takekawa, Jun Terauchi, Satoshi Endo
  • Patent number: 6297379
    Abstract: A compound of formula (I) 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 (A) wherein R5 is hydrogen of 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: Grant
    Filed: April 26, 2000
    Date of Patent: October 2, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shuichi Furuya, Nobuhiro Suzuki, Nobuo Choh, Yoshi Nara
  • Patent number: 6265586
    Abstract: A process for producing indolmycin or a salt thereof which comprises reacting a compound of the formula: or a salt thereof with methylamine or a salt thereof, can be produced in an optically active form in a high yield and high quality, and is advantageous from the industrial point of view.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: July 24, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keiji Kamiyama, Yutaka Nakayama
  • Patent number: 6262267
    Abstract: The compound of the present invention possesses 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 sydrome, multilocular ovary sydrome, pimples etc, or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: July 17, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shuichi Furuya, Nobuo Choh, Nobuhiro Suzuki, Takashi Imada
  • Patent number: 6251926
    Abstract: This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.
    Type: Grant
    Filed: November 15, 1999
    Date of Patent: June 26, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
  • Patent number: 6248740
    Abstract: The present invention provides a compound represented by the formula: wherein Ar1 and Ar2 are independently an aromatic group which may be substituted, and Ar1 and Ar2 may form a condensed cyclic group with an adjacent carbon atom; ring B is a nitrogen-containing heterocycle which may be substituted; X and Y are the same or different and are independently a bond, an oxygen atom, S(O)p (p is an integer of 0 ot 2), NR4 wherein R4 is a hydrogen atom or a lower alkyl group, or a bivalent linear lower hydrocarbon group which may contain 1 to 3 hetero atoms and the bivalent linear lower hydrocarbon group may be substituted; A is a nitrogen atom or CR7 wherein R7 is a hydrogen atom, a halogen atom, a hydrocarbon which may be substituted, an acyl group or a hydroxy group which may be substituted; R1, R2 and R3 are the same or different and are independently a hydrogen atom, a halogen atom, a hydrocarbon group which may be substituted, an acyl group or a hydroxy group which may be substituted; R8 is
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: June 19, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yasuhiko Kawano, Hideaki Nagaya, Michiyo Gyoten
  • Patent number: 6248766
    Abstract: A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.
    Type: Grant
    Filed: March 9, 1999
    Date of Patent: June 19, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Masaki Setoh, Zen-ichi Terashita
  • Patent number: 6242600
    Abstract: The present invention provides compounds and medicines effective for prophylaxis and therapy of various diseases by controlling or inhibiting cell-adhesion. Especially, the compounds of this invention inhibit platelet aggregation action without remarkable elongation of hemorrhagic period and can be used as a safe and long-acting antithrombotic drug as compared with known substances showing the same activity. Compounds of this invention are piperazinones of the formula: wherein the ring A is a basic heterocyclic group; the ring B is a nitrogen containing heterocyclic group or a cyclic hydrocarbon group; Y is CH2; R1 is H, OH, NH2 or an hydrocarbon group which may be bound through CO, S, SO or SO2; R2 is H or a hydrocarbon group; R3 is an optionally esterified or amidated carboxyl group; and D is a lower alkyl group substituted with an optionally esterified carboxyl group; or a salt thereof.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: June 5, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Norikazu Tamura, Zen-ichi Terashita
  • Patent number: 6235771
    Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:  wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5 and R6 are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5 and R6 may bind to each other to form a cy
    Type: Grant
    Filed: March 27, 2000
    Date of Patent: May 22, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Masaki Seto, Naoyuki Kanzaki, Osamu Nishimura
  • Patent number: 6214838
    Abstract: A compound of the formula (I): wherein R is hydrogen or C2-6 alkanoyl; X is halogen; and ring A is benzene ring which is optionally substituted by 1 to 4 substituents selected from {circle around (1)} halogen, {circle around (2)} hydroxy, {circle around (3)} C1-6 alkoxy optionally substituted by halogen or phenyl, {circle around (4)} C1-6 alkylthio optionally substituted by halogen or phenyl, {circle around (5)} C1-6 alkyl optionally substituted by halogen, {circle around (6)} C2-6 alkanoylamino or {circle around (7)} carboxy optionally esterified by C1-6 alkyl, or a salt thereof; which can be used for preventing or treating inflammatory disease, arthritis, chronic rheumatoid arthritis, autoimmune diseases, or rejection after organ transplantation.
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: April 10, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba, Taihei Yamane
  • Patent number: 6197350
    Abstract: 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: Grant
    Filed: May 27, 1999
    Date of Patent: March 6, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yutaka Yamagata, Masafumi Misaki, Susumu Iwasa
  • Patent number: 6087384
    Abstract: 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 --NR.sup.3 -- where R.sup.3 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; R.sup.1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R.sup.1 ; 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: Grant
    Filed: March 15, 1999
    Date of Patent: July 11, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Junji Matsui, Naoki Tarui, Yu Momose, Ken-ichi Naruo
  • Patent number: 6022564
    Abstract: This invention provides a method for producing a microparticle which comprises pulverizing a solid preparation comprising a compound represented by the formula: ##STR1## wherein ring A is an optionally substituted benzene ring; R is a hydrogen atom or an optionally substituted hydrocarbon group; B is an optionally esterified or amidated carboxyl group; X is --CH(OH)-- or --CO--; k is 0 or 1; and n is 0, 1 or 2 or a pharmaceutically acceptable salt thereof and a biodegradable polymer of .alpha.-hydroxycarboxylic acid in the presence of a pulverizing auxiliary, which can provide microparticles which are less adhesive and involve less aggregation and are thus excellent in drug entrapment ratio and control of drug-release in a desired particle size.
    Type: Grant
    Filed: March 1, 1999
    Date of Patent: February 8, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Nobuyuki Takechi, Muneo Nonomura, Shigehiro Higuchi, Toshiharu Beppu
  • Patent number: 5324506
    Abstract: Disclosed are colored cosmetic compositions that, when applied to a person's skin (e.g., the lips or cheeks), hair or nails, exhibit exceptional brilliance and clarity of color, and a method of using those compositions to provide an aesthetically pleasing appearance to the skin, hair or nails. The compositions comprise (a) a pigment formed by incorporating a solvated dye into a resin, and (b) a cosmetic carrier having admixed therein the pigment in an amount effective to provide an attractive cosmetic effect to the composition when it is applied to a person's skin, hair, or nails. The methods of this invention comprise applying an effective amount of the foregoing composition to a person's skin (e.g., lips or cheeks), hair or nails.
    Type: Grant
    Filed: July 6, 1992
    Date of Patent: June 28, 1994
    Assignee: Estee Lauder, Inc.
    Inventors: Louis C. Calvo, David W. Peters
  • Patent number: 5143723
    Abstract: Disclosed are colored cosmetic compositions that, when applied to a person's skin (e.g., the lips or cheeks), hair or nails, exhibit exceptional brilliance and clarity of color, and a method of using those compositions to provide an aesthetically pleasing appearance to the skin, hair or nails. The compositions comprise: (a) a pigment formed by incorporating a solvated dye into a resin, and (b) a cosmetic carrier having admixed therein the pigment in an amount effective to provide an attractive cosmetic effect to the composition when it is applied to a person's skin, hair, or nails. The methods of this invention comprise applying an effective amount of the foregoing composition to a person's skin (e.g., lips or cheeks), hair or nails.
    Type: Grant
    Filed: March 5, 1990
    Date of Patent: September 1, 1992
    Assignee: Estee Lauder, Inc.
    Inventors: Luis C. Calvo, David W. Peters