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1. 发明授权

US06632807B1 (2R,4S)-(−)-[N-(4-diethoxyphosphorylmethyl)phenyl]-1,2,4,5- tetrahydro-4-methyl-7,8-methylenedioxy-5-oxo-3-benzothiepin-2-carboxamide 失效
标题翻译：（2R，4S） - （ - ） - [N-（4-二乙氧基磷酰基甲基）苯基] -1,2,4,5-四氢-4-甲基-7,8-亚甲二氧基-5-氧代-3-苯并噻吩并-2 甲酰胺
公开(公告)号：US06632807B1
公开(公告)日：2003-10-14
申请号：US09635067
申请日：2000-08-09
申请人： Takashi Sohda , Shigehisa Taketomi , Tsuneo Oda
发明人： Takashi Sohda , Shigehisa Taketomi , Tsuneo Oda
IPC分类号： A61K3167
CPC分类号： C07D495/04 , C07F9/6561 , C07F9/657181
摘要： This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.
摘要翻译：本发明涉及由下式表示的光学活性苯并硫代衍生物：其中R代表低级烷基; R <1 和R <2 独立地表示低级烷基，或者可以结合在一起形成环，其显示出优异的成骨促进作用并且可用作骨疾病的预防或治疗药物

2. 发明授权

US06346521B1 Optically active 2R, 4S benzothiepin isomer 失效
标题翻译：光学活性的2R，4S苯并硫代异构体
公开(公告)号：US06346521B1
公开(公告)日：2002-02-12
申请号：US08579731
申请日：1995-12-28
申请人： Takashi Sohda , Shigehisa Taketomi , Tsuneo Oda
发明人： Takashi Sohda , Shigehisa Taketomi , Tsuneo Oda
IPC分类号： A61K3167
CPC分类号： C07D495/04 , C07F9/6561 , C07F9/657181
摘要： This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.
摘要翻译：本发明涉及由下式表示的光学活性苯并硫代衍生物：其中R代表低级烷基; R1和R2独立地表示低级烷基，或者可以结合在一起形成环，其表现出优异的成骨促进作用，并且可用作骨疾病的预防或治疗药物。

3. 发明授权

US5434246A Parathyroid hormone derivatives 失效
标题翻译：甲状旁腺激素衍生物
公开(公告)号：US5434246A
公开(公告)日：1995-07-18
申请号：US033099
申请日：1993-03-16
申请人： Tsunehiko Fukuda , Shizue Nakagawa , Shigehisa Taketomi
发明人： Tsunehiko Fukuda , Shizue Nakagawa , Shigehisa Taketomi
IPC分类号： A61K38/00 , C07K14/635 , C07K14/00 , A61K38/23 , C07K4/00
CPC分类号： C07K14/635 , A61K38/00
摘要： Parathyroid hormone (PTH) derivatives represented by the general formula: ##STR1## or a salt thereof, wherein R.sub.1 represents Ser or a D-.alpha.-amino acid residue of 4 or less carbon atoms;R.sub.2 represents a tetrapeptide chain which contains at least one water-soluble .alpha.-amino acid residue;R.sub.3 represents a tripeptide chain which contains at least one water-soluble .alpha.-amino acid residue; andR.sub.4 represents an aromatic amino acid residue or an amide thereof,except that R.sub.1 is Ser when R.sub.2 is His-Leu-Asn-Ser, R.sub.3 is E-F-Gwherein E is Arg or His, F is Lys or His, G is Lys, Leu or Gln, are disclosed.The parathyroid hormone derivatives of the present invention are stable and have high biological activity, therefore they are useful as drugs for bone diseases and the like.
摘要翻译：由以下通式表示的甲状旁腺激素（PTH）衍生物或其盐，其中R1表示Ser或4个或更少碳原子的D-α-氨基酸残基; R2表示含有至少一个水溶性α-氨基酸残基的四肽链; R3表示含有至少一个水溶性α-氨基酸残基的三肽链; R4代表芳族氨基酸残基或酰胺，当R 2为His-Leu-Asn-Ser时，R1为Ser，R3为EFG，其中E为Arg或His，F为Lys或His，G为Lys，Leu 或Gln。本发明的甲状旁腺激素衍生物是稳定的并且具有高的生物活性，因此它们可用作骨疾病等药物。

4. 发明授权

US5376647A bisphosphonic acid derivatives, and useful as a bone resorption inhibitor 失效
标题翻译：双膦酸衍生物，可用作骨吸收抑制剂
公开(公告)号：US5376647A
公开(公告)日：1994-12-27
申请号：US3955
申请日：1993-01-19
申请人： Takashi Sohda , Iwao Yamazaki , Noriaki Kawamura , Shigehisa Taketomi
发明人： Takashi Sohda , Iwao Yamazaki , Noriaki Kawamura , Shigehisa Taketomi
IPC分类号： A61K31/66 , A61K31/663 , A61P19/08 , A61P19/10 , A61P29/00 , A61P43/00 , C07F9/38 , C07F9/40 , C07F9/58 , C07F9/6506 , C07F9/6512 , C07F9/6524 , C07F9/6539 , C07F9/6561 , A61K31/675
CPC分类号： C07F9/588 , C07F9/3873 , C07F9/405 , C07F9/65067 , C07F9/65127 , C07F9/6524 , C07F9/6539 , C07F9/6561
摘要： A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.
摘要翻译：通式（I）的双膦酸衍生物：其中A是任选取代的环状基团; R1是氢原子或低级烷酰基; R2，R3，R4和R5相同或不同，为氢原子或低级烷基; m为0,1或2; n为2〜10的整数，或其盐。还公开了其生产方法和含有通式（I）化合物或其盐的骨吸收抑制剂。

5. 发明申请

US20090186946A1 Genetically Modified Animal and Use Thereof 审中-公开
标题翻译：转基因动物及其使用
公开(公告)号：US20090186946A1
公开(公告)日：2009-07-23
申请号：US12306480
申请日：2007-06-26
申请人： Shigehisa Taketomi , Mayumi Nishida
发明人： Shigehisa Taketomi , Mayumi Nishida
IPC分类号： A61K31/137 , A01K67/00
CPC分类号： A01K67/0275 , A01K2217/05 , A01K2267/03
摘要： The present invention provides a non-human mammal deficient in the expression of the SLC-1 gene, having the characteristics of (1) a lower blood insulin level in glucose tolerance test, (2) increased insulin sensitivity, (3) higher resistance to obesity even on high fat diet, (4) a smaller white fat cell size, and (5) accentuated lipolysis, compared with the corresponding wild-type animal, or a portion of the body thereof. Also provided is an obesity and/or type II diabetes model non-human mammal that is deficient in the expression of the SLC-1 gene, having the characteristics of (1) elevated expression of adiponectin, (2) delayed onset of hyperglycemia, (3) a lower blood glycohemoglobin level, and (4) accentuated energy consumption, compared with the corresponding obesity and/or type II diabetes model non-human mammal wherein the expression of the gene is normal, or a portion of the body thereof.
摘要翻译：本发明提供了缺乏SLC-1基因表达的非人类哺乳动物，具有以下特征：（1）葡萄糖耐量试验中血糖水平越低，（2）胰岛素敏感性越高，（3）抗性越高肥胖甚至高脂肪饮食，（4）较小的白色脂肪细胞大小，和（5）与相应的野生动物相比，或其一部分体重增加的脂肪分解。还提供了缺乏SLC-1基因表达的肥胖和/或II型糖尿病模型，具有以下特征：（1）脂联素的表达升高，（2）高血糖迟发性发作（ 3）较低血糖血红蛋白水平，和（4）加强能量消耗，与基因表达正常或身体的一部分相应的肥胖和/或II型糖尿病模型非人哺乳动物相比较。

6. 发明授权

US06489351B1 Condensed 4,5,6,7-tetrahydrobenzo[C]thiophenes as enhancer for cell differentation induction factor action 失效
标题翻译：缩合的4,5,6,7-四氢苯并[C]噻吩作为细胞分化诱导因子作用的增强剂
公开(公告)号：US06489351B1
公开(公告)日：2002-12-03
申请号：US10105333
申请日：2002-03-26
申请人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
发明人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
IPC分类号： A61K311424
CPC分类号： C07D495/04 , C07D513/04 , C07F9/6561
摘要： A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
摘要翻译：由下式表示的化合物：其中X表示硫原子或氧原子; Y表示任选氧化的硫原子或氧原子; Z表示键或二价烃基; R1表示任选取代的烃基; R 2表示任选的酰胺化或酯化的羧基; 环A表示任选取代的芳族五元杂环; 或其盐。上述化合物具有细胞分化诱导因子作用增强活性和抗基质金属蛋白酶活性，并且其可用于预防和治疗骨疾病如骨质疏松症，骨折，骨关节炎和类风湿性关节炎，动脉硬化，癌转移以及基于神经变性的疾病。

7. 发明授权

US5852039A Pharmaceutical composition containing quinoline or quinazoline derivatives 失效
公开(公告)号：US5852039A
公开(公告)日：1998-12-22
申请号：US783079
申请日：1997-01-15
申请人： Takashi Sohda , Shigehisa Taketomi , Atsuo Baba
发明人： Takashi Sohda , Shigehisa Taketomi , Atsuo Baba
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/4741 , A61K31/4745 , A61K31/50 , A61K31/505 , A61K31/517 , C07D215/54 , C07D401/12 , C07D403/12 , C07D417/12 , C07D491/04 , C07D521/00 , C07D215/00 , C07D215/14
CPC分类号： C07D231/12 , A61K31/47 , A61K31/4709 , A61K31/4741 , A61K31/4745 , A61K31/50 , A61K31/505 , A61K31/517 , C07D215/54 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D417/12 , C07D491/04
摘要： The present invention provides a pharmaceutical composition for inhibiting bone resorption or for preventing or treating osteoporosis which comprises a quinoline or quinazoine derivative as an active ingredient.

8. 发明授权

US5580863A Benzopyran derivatives and their use 失效
标题翻译：苯并吡喃衍生物及其用途
公开(公告)号：US5580863A
公开(公告)日：1996-12-03
申请号：US242638
申请日：1994-05-13
申请人： Takashi Sohda , Shigehisa Taketomi , Tsuneo Oda
发明人： Takashi Sohda , Shigehisa Taketomi , Tsuneo Oda
IPC分类号： C07F9/655 , C07F9/6558 , C07F9/6571 , A61K31/665 , A61K31/675 , C07D311/24 , C07F9/38
CPC分类号： C07F9/65586 , C07F9/65522 , C07F9/657181
摘要： This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.
摘要翻译：本发明涉及由下式表示的化合物：其中B代表氢原子或低级烷基; 环A表示可具有一个或多个取代基的苯环; + E，ovs xxxxx + EE表示单键或双键; Q1表示由下式表示的基团：或被下式表示的基团取代的烃基，其中X表示键或具有1-4个原子的链长的间隔基作为直链部分，可能有一个或多个侧链; 无论相同或不同，R 1和R 2独立地表示氢原子或低级烷基，或可以结合在一起形成环; Q2表示氢原子，可以被取代的烃残基或可被取代的杂环残基; 或其盐。

9. 发明授权

US06025467A Parathyroid hormone derivatives and their use 失效
标题翻译：甲状旁腺激素衍生物及其用途
公开(公告)号：US06025467A
公开(公告)日：2000-02-15
申请号：US44536
申请日：1998-03-19
申请人： Tsunehiko Fukuda , Shizue Nakagawa , Junko Habashita , Shigehisa Taketomi
发明人： Tsunehiko Fukuda , Shizue Nakagawa , Junko Habashita , Shigehisa Taketomi
IPC分类号： A61K38/00 , C07K14/635 , C12N15/16 , C07K7/06 , A61K38/16
CPC分类号： C07K14/635 , A61K38/00
摘要： Disclosed is a parathyroid hormone (PTH) (1-34) derivative in which at least the amino acid residue at the 10-position is substituted by an acidic amino acid residue. The derivatives of the present invention showing potent cAMP-producing activity and bone formation activity, and thus are useful as therapeutic agents for bone diseases, etc.
摘要翻译：披露了至少10位的氨基酸残基被酸性氨基酸残基取代的甲状旁腺激素（PTH）（1-34）衍生物。本发明的衍生物显示出有效的cAMP生产活性和骨形成活性，因此可用作骨疾病等的治疗剂。

10. 发明授权

US5910492A Osteogenic promoting pharmaceutical composition 失效
标题翻译：成骨促进药物组成
公开(公告)号：US5910492A
公开(公告)日：1999-06-08
申请号：US719467
申请日：1996-09-25
申请人： Tetsuo Hoshino , Hiroya Muranishi , Shigehisa Taketomi , Susumu Iwasa
发明人： Tetsuo Hoshino , Hiroya Muranishi , Shigehisa Taketomi , Susumu Iwasa
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K47/26 , A61K47/36 , A61K31/67 , A61K31/66
CPC分类号： A61K31/683 , A61K9/0019 , A61K9/1647 , A61K47/26 , A61K47/36 , A61K9/2031
摘要： This invention provides a pharmaceutical composition comprising a non-peptide osteogenic promoting substance and a biodegradable polymer, which can be safely used as a prophylactic/therapeutic agent for various bone diseases (e.g., bone fractures).
摘要翻译：本发明提供了包含非肽成骨促进物质和生物可降解聚合物的药物组合物，其可以安全地用作各种骨疾病（例如骨折）的预防/治疗剂。

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