Abstract: The transgenic animal of this invention can be used as an animal model for renal disease, bone disease, joint disease, pulmonary disease, hyperlipidemia, arteriosclerosis, cardiac disease, diabetes, obesity, digestive organ disease, infectious disease, allergic disease, endocrine disease, dementia or cancer, or complications thereof; and provides a nonhuman transgenic mammal for the unraveling of the mechanisms of said diseases, explorations for the development of therapeutic modalities for the diseases, and the screening of candidate therapeutic drugs.
Abstract: The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.
Abstract: 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:
Grant
Filed:
June 21, 1999
Date of Patent:
October 30, 2001
Assignee:
Takeda Chemical Industries, Ltd.
Inventors:
Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
Abstract: A solid preparation which comprises (i) a pharmaceutically active ingredient, (ii) one or more water-soluble sugar alcohols 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.
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 syndrome, multilocular ovary syndrome, pimples etc. or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.
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
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.
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.
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
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.
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.
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
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.