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1. 发明授权

US5378689A Peptides having renin inhibitory activity, their preparation and use 失效
标题翻译：具有肾素抑制活性的肽，其制备和用途
公开(公告)号：US5378689A
公开(公告)日：1995-01-03
申请号：US98746
申请日：1993-07-28
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Hidekuni Takahagi , Yasuteru Iijima , Tatsuo Kokubu , Kunio Hiwada
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Hidekuni Takahagi , Yasuteru Iijima , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： A61K31/425 , C07D277/30 , C07D413/06 , A61K37/02 , C07K5/08
CPC分类号： C07D277/30
摘要： Compounds of formula (I): ##STR1## [in which: R.sup.1 is heterocyclic group having 5 or 6 ring atoms, or --NR.sup.7 R.sup.8, where R.sup.7 is alkyl and R.sup.8 is optionally substituted phenyl, optionally substituted phenylalkyl or cycloalkyl; R.sup.2 is optionally substituted phenyl or naphthyl; R.sup.3 is thiazolyl; R.sup.4 is cyclohexyl or isopropyl; R.sup.5 is alkyl; and R.sup.6 is alkyl] and salts thereof have renin-inhibitory and, hence, hypotensive activities and are of value in the diagnosis and treatment of hypertension induced by failures in the renin-angiotensin system. They may be prepared by reacting together appropriate amino acids or derivatives thereof.
摘要翻译：式（I）化合物：其中：R 1为具有5或6个环原子的杂环基或-NR 7 R 8，其中R 7为烷基，R 8为任选取代的苯基，任选取代的苯基烷基或环烷基 R2是任选取代的苯基或萘基; R3是噻唑基; R4是环己基或异丙基; R5是烷基; 和R6是烷基]，其盐具有肾素抑制作用，因此具有降血压活性，并且在肾素 - 血管紧张素系统失败引起的高血压的诊断和治疗中具有价值。它们可以通过使合适的氨基酸或其衍生物一起反应来制备。

2. 发明授权

US5378690A New renin-inhibitory oligopeptides, their preparation and their use 失效
标题翻译：新的肾素抑制性寡肽，其制备及其应用
公开(公告)号：US5378690A
公开(公告)日：1995-01-03
申请号：US99776
申请日：1993-07-30
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Yasuteru Iijima , Hidekuni Takahagi , Hiroyuki Koike , Tatsuo Kokubu , Kunio Hiwada
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Yasuteru Iijima , Hidekuni Takahagi , Hiroyuki Koike , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： C07D233/54 , C07D261/08 , C07D277/30 , C07D295/13 , C07D295/185 , C07D333/24 , C07K5/02 , A61K37/02 , C07K5/08
CPC分类号： C07D233/64 , C07D261/08 , C07D277/30 , C07D295/13 , C07D295/185 , C07D333/24 , C07K5/0205 , C07K5/0227
摘要： Oligopeptides of formula (I): ##STR1## where R.sup.1 -R.sup.5 are various organic groups, and A represents a group of formula --NH-- or --(CH.sub.2).sub.n --, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.
摘要翻译：式（I）的寡肽：其中R 1 -R 5是各种有机基团，A表示式-NH-或 - （CH 2）n - 的基团，其中n表示整数 1〜3具有肾素抑制活性，特别适合于口服给药。它们可以通过使用常规肽合成反应来缩合其组分氨基酸或低级寡肽来制备。

3. 发明授权

US5364844A Renin-inhibitory oligopeptides, their preparation and use 失效
标题翻译：肾素抑制寡肽，其制备和用途
公开(公告)号：US5364844A
公开(公告)日：1994-11-15
申请号：US936883
申请日：1992-08-27
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Yasuteru Iijima , Hidekuni Takahagi , Tatsuo Kokubu , Kunio Hiwada
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Yasuteru Iijima , Hidekuni Takahagi , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： C07K5/02 , A61K37/02 , C07K5/06 , C07K5/08
CPC分类号： C07K5/0227 , C07K5/0207
摘要： Compounds of formula (I): ##STR1## A is a carbon-carbon bond or C.sub.1 -C.sub.3 alkylene; B is imino group or C.sub.1 -C.sub.2 alkylene; R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, heterocyclic or optionally substituted amino; R.sup.2 is optionally substituted phenyl or optionally substituted naphthyl; R.sup.3 is thiazolyl, isoxazolyl or imidazolyl; R.sup.4 is isopropyl or cyclohexyl; R.sup.5 and R.sup.6 are C.sub.1 -C.sub.4 alkyl, or, together with the carbon atom to which they are attached, C.sub.3 -C.sub.7 cycloalkyl; R.sup.7 is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl group; and R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl. These compounds have renin-inhibitory and, hence, hypotensive activities. The invention also provides a method for the treatment or prophylaxis of hypertension induced by failures in the renin-angiotensin system.
摘要翻译：式（I）的化合物：A是碳 - 碳键或C1-C3亚烷基; B是亚氨基或C 1 -C 2亚烷基; R1是C1-C4烷基，C1-C4烷氧基，杂环或任选取代的氨基; R2是任选取代的苯基或任选取代的萘基; R3是噻唑基，异恶唑基或咪唑基; R4是异丙基或环己基; R 5和R 6是C 1 -C 4烷基，或者与它们所连接的碳原子一起是C 3 -C 7环烷基; R7是氢，任选取代的C 1 -C 6烷基; 并且R 8是氢或C 1 -C 4烷基。这些化合物具有肾素抑制，因此具有降血压活性。本发明还提供了用于治疗或预防由肾素 - 血管紧张素系统中的失败引起的高血压的方法。

4. 发明授权

US4898862A 1,2,4-triazinone derivatives, their preparation and use 失效
标题翻译： 1,2,4-三嗪酮衍生物，其制备和用途
公开(公告)号：US4898862A
公开(公告)日：1990-02-06
申请号：US26290
申请日：1987-03-16
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Mitsuo Sugiyama , Fujio Saito , Hiroyuki Koike , Takeshi Oshima , Yasuo Simoji , Hitoshi Nagahori
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Mitsuo Sugiyama , Fujio Saito , Hiroyuki Koike , Takeshi Oshima , Yasuo Simoji , Hitoshi Nagahori
IPC分类号： C07D253/06 , C07D401/12 , C07D403/12
CPC分类号： C07D253/06 , C07D401/12 , C07D403/12
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 is hydrogen or alkl; R.sup.2 is a variety of groups or atoms; R.sup.3 is optionally substituted hydroxy or --(NH).sub.n --NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 are a variety of groups or atoms, preferably alkyl substituted by heterocyclic, and n is 0 or 1; Q is oxygen or sulfur; and A is a C.sub.1 -C.sub.6 alkylene group) have valuable cardiotionic activity and may be used for the treatment of cardiac disorders. They may be prepared from corresponding compounds containing a benzene ring with a group --QH at the 1-position and a group --CO--CHR.sup.1 --NH--COOR.sup.7 at the 4-position by ring closure and introduction of the group of formula --A--CO--R.sup.3 in any order.
摘要翻译：式（I）化合物：其中：R 1是氢或烷基; R 2是各种基团或基团; R 3是任选取代的羟基或 - （NH）n -NR 5 R 6，其中R 5和R 6 是各种基团或原子，优选被杂环取代的烷基，n为0或1; Q为氧或硫; A为C1-C6亚烷基）具有有价值的心血管活性，可用于治疗心脏疾病它们可以由相应的化合物制备，所述化合物含有1-环基团-QH的苯环和通过闭环在4-位上的-CO-CHR1-NH-COOR7基团，并引入式-A- CO-R3以任何顺序。

5. 发明授权

US4914093A Pyridazinone derivatives, their preparation and use 失效
标题翻译：哒嗪酮衍生物，其制备和用途
公开(公告)号：US4914093A
公开(公告)日：1990-04-03
申请号：US325112
申请日：1989-03-16
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Seiji Kumakura , Hiroyuki Koike , Shinsaku Kobayashi
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Seiji Kumakura , Hiroyuki Koike , Shinsaku Kobayashi
IPC分类号： A61K31/50 , A61P1/04 , A61P7/02 , A61P9/04 , A61P9/12 , C07D237/00 , C07D237/04 , C07D237/14 , C07D401/12 , C07D403/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D237/04 , C07D237/14 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Compounds of formula (I): ##STR1## (wherein Q is oxygen or sulfur, the dotted line is a single or double bond, A is alkylene, and R.sup.1 -R.sup.5 are a variety of atoms or organic groups)have excellent ability to potentiate myocardial contractivity and a variety of other properties, and can be used to treat cardiac disorders.
摘要翻译：式（I）化合物：其中Q为氧或硫，虚线为单键或双键，A为亚烷基，R1-R5为多种原子或有机基团）具有优异的增强心肌收缩力和多种其他特性的能力，可用于治疗心脏疾病。

6. 发明授权

US4421766A Method of preserving organic materials from fungal attack and a composition for use in such a method 失效
标题翻译：从真菌侵袭中保存有机材料的方法和用于这种方法的组合物
公开(公告)号：US4421766A
公开(公告)日：1983-12-20
申请号：US338141
申请日：1982-01-08
申请人： Yasuhiro Morisawa , Kiyoshi Konishi , Mitsuru Kataoka
发明人： Yasuhiro Morisawa , Kiyoshi Konishi , Mitsuru Kataoka
IPC分类号： A01N37/06 , A01N37/18 , A01N37/22 , B27K3/36 , B27K3/40 , C07C51/363 , C07C57/52 , C07C57/54 , C07C57/76 , A01N37/02
CPC分类号： C07C57/76 , A01N37/06 , A01N37/18 , A01N37/22 , C07C51/363 , C07C57/52 , C07C57/54 , B27K3/36 , B27K3/40
摘要： A variety of organic materials susceptible to fungal attack (especially wood and wood-based materials) can be protected from such attack and fungi growing on such materials can be eradicated by treating them, e.g. by applying to the surfaces or impregnating, with one or more compounds of formula (I): ##STR1## (wherein X represents a halogen atom and R represents a hydroxy group, an alkoxy gorup, a substituted or unsubstituted phenoxy group, an amino group, a mono- or di- alkylamino group, a phenylamino or benzylamino group which is unsubstituted or has one or two substituents on the benzene ring of the phenyl or benzyl moiety, or a 3-halo-2,3-diiodoallyloxy group). An anti-fungal composition contains one or more of these compounds in admixture with a carrier or adjuvant.
摘要翻译：可以保护易受真菌侵袭的各种有机材料（特别是木材和木质材料），免受这种攻击，并且可以通过对这些材料进行处理来消除在这些材料上生长的真菌。（I）（其中X表示卤素原子，R表示羟基，烷氧基羰基，取代或未取代的苯氧基，烷氧基羰基，取代或未取代的苯氧基，氨基，单或二烷基氨基，苯基氨基或苄基氨基，或苯基或苄基部分的苯环上未取代或具有一个或两个取代基，或3-卤代-2,3-二碘代乙酰氧基）。抗真菌组合物含有一种或多种这些化合物与载体或佐剂的混合物。

7. 发明授权

US4259350A Iodopropargyl derivatives, their use and preparation 失效
标题翻译：碘代炔丙基衍生物，其用途和制备方法
公开(公告)号：US4259350A
公开(公告)日：1981-03-31
申请号：US20165
申请日：1979-03-13
申请人： Yasuhiro Morisawa , Kiyoshi Konishi , Mitsuru Kataoka
发明人： Yasuhiro Morisawa , Kiyoshi Konishi , Mitsuru Kataoka
IPC分类号： A01N37/00 , A01N37/02 , A01N37/06 , A01N37/08 , A01N37/10 , A01N37/34 , A01N37/40 , A01N37/48 , A01N39/02 , A01N41/04 , A01N43/00 , A01N43/06 , A01N43/40 , A01N47/06 , A01N53/00 , A01N57/00 , A61K31/195 , B27K3/34 , C07C69/007 , C07C69/612 , C07C69/614 , C07C69/62 , C07C69/63 , C07C69/96 , C07C205/18 , C07C255/13 , C07C309/63 , C07C309/65 , C07C309/73 , C07C309/75 , C07D213/55 , C07D213/65 , C07D213/79 , C07D307/16 , C07D307/68 , C07D333/16 , C07D333/24 , C07D333/38 , A01N43/02
CPC分类号： C07D213/79 , A01N37/02 , A01N37/06 , A01N37/08 , A01N37/10 , A01N39/02 , A01N41/04 , A01N43/06 , A01N43/40 , A01N47/06 , A01N53/00 , C07C255/00 , C07C309/65 , C07C309/73 , C07C309/75 , C07C69/63 , C07C69/76 , C07C69/78 , C07C69/96 , C07D213/55 , C07D213/65 , C07D307/16 , C07D307/68 , C07D333/16 , C07D333/24 , C07D333/38
摘要： Iodopropargyl derivatives of formula:IC.tbd.CCH.sub.2 OR[wherein R represents an alkanoyl group (which may be unsubstituted or have one or more halogen, cyano, substituted or unsubstituted .alpha.-phenoxy or phenyl substituents) an alkenoyl group (optionally phenyl-substituted), a substituted or unsubstitutd alkoxycarbonyl group, a cycloalkanoyl group, a substituted or unsubstituted benzoyl group, a substituted or unsubstituted phenoxycarbonyl group, a substituted or unsubstituted benzyloxycarbonyl group, a heterocyclic carbonyl group, an alkylsulphonyl group, a substituted or unsubstituted benzenesulphonyl group, a naphthyloxycarbonyl group, an iodopropargyloxycarbonyl group, a substituted or unsubstituted cycloalkoxycarbonyl group, a heterocyclic methoxycarbonyl group, a 3-pyridyloxycarbonyl group (which may be unsubstituted or have one or more halogen substituents) or an alkenyloxycarbonyl group] are, except where R represents an acetyl or an unsubstituted benzoyl group, new compounds and are useful for the preservation of a variety or organic materials, including the protection of these materials against fungal or insect attack. The derivatives may be prepared by reacting 3-hydroxy-1-iodo-1-propyne with a compound of formula RX (in which R is as defined above and X represents a halogen atom) or, where R in the desired compound contains an oxycarbonyl group, reacting the 3-hydroxy-1-iodo-1-propyne with phosgene and then reacting the product with an appropriate hydroxy-containing compound.
摘要翻译：其中R表示烷酰基（其可以是未取代的或具有一个或多个卤素，氰基，取代或未取代的α-苯氧基或苯基取代基）烯酰基（任选被苯基取代的），一个取代或未取代的烷氧基羰基，环烷酰基，取代或未取代的苯甲酰基，取代或未取代的苯氧基羰基，取代或未取代的苄氧基羰基，杂环羰基，烷基磺酰基，取代或未取代的苯磺酰基，萘氧基羰基，碘代炔丙氧基羰基，取代或未取代的环烷氧基羰基，杂环甲氧基羰基，3-吡啶氧基羰基（其可以是未取代的或具有一个或多个卤素取代基）或烯氧基羰基]，其中R表示乙酰基或未取代的苯甲酰基，新化合物并且可用于保存各种或有机材料，包括保护这些材料免受真菌或昆虫的攻击。衍生物可以通过使3-羟基-1-碘-1-丙炔与式RX化合物（其中R如上定义并且X表示卤素原子）反应制备，或其中所需化合物中的R含有氧羰基将3-羟基-1-碘-1-丙炔与光气反应，然后使产物与合适的含羟基化合物反应。

8. 发明授权

US4098893A Pyridine derivatives and their use as anticoccidial agents 失效
标题翻译：吡啶衍生物及其用作抗焦虑剂
公开(公告)号：US4098893A
公开(公告)日：1978-07-04
申请号：US816215
申请日：1977-07-15
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Noritoshi Kitano , Toshiaki Matsuzawa
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Noritoshi Kitano , Toshiaki Matsuzawa
IPC分类号： C07D213/81 , C07D213/82 , C07D213/85 , A61K31/44 , C07D213/56
CPC分类号： C07D213/81 , C07D213/82 , C07D213/85
摘要： Pyridine derivatives having the formula ##STR1## wherein R.sub.1 is an alkyl group having 1 to 3 carbon atoms; R.sub.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R.sub.3 is hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 3 or 4 carbon atoms, an alkyl group having 1 or 2 carbon atoms and hydroxy as a substituent, an alkanoyl group having 1 to 18 carbon atoms, an alkenoyl group having 3 to 11 carbon atoms, an aromatic acyl group having 6 or 10 carbon atoms in the aromatic ring and optionally alkyl, alkoxy, acetylamino, cyano or halogen as a substituent, a heterocyclic acyl group, an alkylcarbamoyl group having 1 to 4 carbon atoms in the alkyl moiety, an allylcarbamoyl group or hydroxy group; n is an integer of 0 to 2 inclusive; and, when n is 2, R.sub.1 's may be the same or different; provided that when R.sub.2 is said alkyl group having 1 to 3 carbon atoms, R.sub.3 is said alkyl group having 1 to 4 carbon atoms.They are highly effective in the treatment of coccidiosis.

9. 发明授权

US4053608A Compositions and methods for the treatment of coccidiosis 失效
标题翻译：用于治疗结肠炎的组合物和方法
公开(公告)号：US4053608A
公开(公告)日：1977-10-11
申请号：US602574
申请日：1975-08-07
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Noritoshi Kitano , Toshiaki Matsuzawa
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Noritoshi Kitano , Toshiaki Matsuzawa
IPC分类号： C07D213/61 , C07D213/81 , C07D333/38 , C07D409/12 , A61K31/455 , A61K31/44
CPC分类号： C07D213/81
摘要： Anticoccidial compositions which comprise as active ingredient pyridine derivatives having the formula ##STR1## wherein R.sub.1 is hydrogen atom, a halomethyl group or methyl group;R.sub.2 is hydrogen atom or an alkyl group of 1-3 carbon atoms;R.sub.3 is hydrogen atom, an alkyl group of 1-3 carbon atoms, allyl group, an alkyl group having 2 or 3 carbon atoms and alkoxy of 1 or 2 carbon atoms as a substituent, an alkyl group having 1-3 carbon atoms and hydroxy as a substituent, an alkanoyl group of 1-18 carbon atoms, a haloacetyl group, an alkenoyl group of 3-11 carbon atoms, an aromatic acyl group, a heterocyclic acyl group, an N-alkylcarbamoyl group of 1-4 carbon atoms in the alkyl moiety or hydroxy group;Provided that when R.sub.2 is said alkyl group of 1-3 carbon atoms, R.sub.3 is said alkyl group of 1-3 carbon atoms and inorganic acid addition salts thereof.

10. 发明授权

US4094982A Pyridine sulfonamides and their use as anticoccidial agents 失效
标题翻译：吡啶磺酰亚胺及其作为抗焦虑剂
公开(公告)号：US4094982A
公开(公告)日：1978-06-13
申请号：US681154
申请日：1976-04-28
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Noritoshi Kitano , Toshiaki Mastuzawa
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Noritoshi Kitano , Toshiaki Mastuzawa
IPC分类号： C07D213/70 , C07D213/02 , A01N9/22
CPC分类号： C07D213/70
摘要： Pyridine derivatives having the formula ##STR1## wherein R.sub.1 represents hydrogen atom, amino group or a group ##STR2## in which R.sub.5 and R.sub.6 may be the same or different and each represents an alkyl group of 1 to 4 carbon atoms or R.sub.5 is hydrogen atom and R.sub.6 represents an alkyl group of 1 to 4 carbon atoms, an alkenyl group of 3 or 4 carbon atoms or a benzyl group optionally substituted with halogen, cyano, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms;R.sub.2 represents nitro group, amino group or an alkylamino group of 1 to 3 carbon atoms;R.sub.3 and R.sub.4 individually represent hydrogen atom, an alkyl group of 1 to 4 carbon atoms, an alkoxyalkyl group which has 1 to 4 carbon atoms in the alkoxy moiety and 2 to 4 carbon atoms in the alkyl moiety, an alkenyl group of 3 or 4 carbon atoms, an alkanoyl group of 1 to 18 carbon atoms or a benzyl group optionally substituted with halogen, cyano, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; provided that when R.sub.1 is hydrogen atom and R.sub.2 is nitro group, R.sub.3 and R.sub.4 may be the same or different and each represents said alkyl group or said alkoxyalkyl group or R.sub.3 is hydrogen atom and R.sub.4 is hydrogen atom, said alkyl group, said alkoxyalkyl group, said alkenyl group, said alkanoyl group or said benzyl group, when R.sub.1 is hydrogen atom and R.sub.2 is amino group or said alkylamino group, R.sub.3 and R.sub.4 individually is hydrogen atom or they may be the same or different and each represents said alkyl group, when R.sub.1 is amino group and R.sub.2 is nitro group, R.sub.3 and R.sub.4 may be the same or different and each represents said alkyl group or R.sub. 3 is hydrogen atom and R.sub.4 is said alkyl group or said alkenyl group, and when R.sub.1 is said group ##STR3## and R.sub.2 is nitro group, R.sub.3 and R.sub.4 are the same as defined above with respect to the R.sub.5 and R.sub.6.They are highly effective in the treatment of coccidiosis, especially that caused by the protozoa belonging to the species Eimeria tenella or E. necatrix.

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