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1. 发明授权

US06787650B1 Urea compounds, process for producing the same and use thereof 失效
标题翻译：尿素化合物，其制造方法及其用途
公开(公告)号：US06787650B1
公开(公告)日：2004-09-07
申请号：US10089961
申请日：2002-04-05
申请人： Osamu Kurasawa , Shinichi Imamura , Shohei Hashiguchi , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba
发明人： Osamu Kurasawa , Shinichi Imamura , Shohei Hashiguchi , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba
IPC分类号： C07D41700
CPC分类号： C07D211/14
摘要： A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.
摘要翻译：下式的化合物：其中R 1为可被取代的烃基; R 2为可被取代的环状烃基或可被取代的杂环基; R 3为卤素原子，可以被取代的氨基甲酰基，可以被取代的氨磺酰基，可以被取代的酰基，可以被取代的C1-4烷基，可被取代的C1-4烷氧基，氨基其可以被取代，硝基或氰基; R 4是氢原子或羟基; n是0或1; 和p为0或1至4];或其盐具有有效的CCR5拮抗活性，并且可有利地用作抑制人外周血单核细胞的HIV感染的药物，特别是用于治疗或预防AIDS。

2. 发明授权

US07348324B2 Cyclic amine compounds as CCR5 antagonists 有权
标题翻译：环胺化合物作为CCR5拮抗剂
公开(公告)号：US07348324B2
公开(公告)日：2008-03-25
申请号：US10273111
申请日：2002-10-18
申请人： Shinichi Imamura , Shohei Hashiguchi , Taeko Hattori , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba , Yoshihiro Sugihara
发明人： Shinichi Imamura , Shohei Hashiguchi , Taeko Hattori , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba , Yoshihiro Sugihara
IPC分类号： A61P31/18 , A61K31/535 , A61K31/4965 , A61K31/44 , A61K31/47 , C07D413/00 , C07D241/00 , C07D211/00
CPC分类号： C07D401/12 , C07D211/58 , C07D211/62 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/14
摘要： A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y− (R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).
摘要翻译：式（I）化合物（其中R 1为氢原子，可被取代的烃基，可被取代的非芳香族杂环基，R 2 O 2 >可以被取代的烃基，可以被取代的非芳族杂环基，或者R 1和R 2可以彼此结合形成A至形成可以被取代的杂环基; A是N或N + - - - - - - - （R 5） SUP>为烃基; Y为 - 抗衡阴离子）; R 3为可被取代的环状烃基或可被取代的杂环基; n 为0或1; R 4为氢原子，可被取代的烃基，可被取代的杂环基，可被取代的烷氧基，可被取代的芳氧基，或可以被取代的氨基，E是可以是二价脂族烃基被除氧基以外的基团取代; G 1是一个键，CO或SO 2; G 2是CO，SO 2，NHCO，CONH或OCO; J为次甲基或氮原子; 并且Q和R中的每一个是可被取代的键或二价C 1-3烷基脂族烃; 条件是当G 2 O是OCO时J为次甲基，当另一个为键并且Q和R各自不被氧代基取代时，Q和R中的一个不为键，当G 1是一个键时）或其盐具有强的CCR5拮抗活性，并且可以有利地用于治疗或预防人类各种HIV感染性疾病（如艾滋病）。

3. 发明授权

US06562978B1 Cyclic amine compounds as CCR5 antagonists 有权
标题翻译：环胺化合物作为CCR5拮抗剂
公开(公告)号：US06562978B1
公开(公告)日：2003-05-13
申请号：US10089374
申请日：2002-03-29
申请人： Shinichi Imamura , Shohei Hashiguchi , Taeko Hattori , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba , Yoshihiro Sugihara
发明人： Shinichi Imamura , Shohei Hashiguchi , Taeko Hattori , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba , Yoshihiro Sugihara
IPC分类号： C07D21128
CPC分类号： C07D401/12 , C07D211/58 , C07D211/62 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/14
摘要： A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y−(R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).
摘要翻译：式（I）的化合物（其中R 1为氢原子，可被取代的烃基，可被取代的非芳族杂环基，R 2为可被取代的烃基，非芳香族杂环基或者R 1和R 2可以与A相互结合形成可被取代的杂环基; A是N或-N + -R 5 .Y-（R 5是烃基; Y-是抗衡阴离子）; R3是可以被取代的环状烃基或可以被取代的杂环基; n是0或1; R4是氢原子，可以被取代的烃基，可以被取代的杂环基，可被取代的烷氧基，可被取代的芳氧基或可被取代的氨基，E是可被除氧以外的基团取代的二价脂族烃基; G 1是键，CO 或SO 2; G2是CO，SO 2，NHCO，CONH或OCO; J是次甲基或硝基原子 Q和R分别为可以被取代的键或二价C 1-3脂族烃; 条件是当G2是OCO时J是次甲基，当另一个是键时Q和R中的一个不是键，并且当G 1是键时，Q和R各自不被氧代基取代）或其盐具有有效的CCR5拮抗活性，可有利地用于治疗或预防人类各种HIV感染性疾病（如艾滋病）。

4. 发明授权

US06627651B1 Cyclic compounds and uses thereof 失效
标题翻译：环状化合物及其用途
公开(公告)号：US06627651B1
公开(公告)日：2003-09-30
申请号：US09980773
申请日：2001-11-02
申请人： Mitsuru Shiraishi , Masanori Baba , Masaki Seto , Naoyuki Kanzaki , Osamu Nishimura
发明人： Mitsuru Shiraishi , Masanori Baba , Masaki Seto , Naoyuki Kanzaki , Osamu Nishimura
IPC分类号： A61K3138
CPC分类号： C07D405/12 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/44 , A61K31/4709 , A61K31/4725 , A61K31/661 , C07D217/06 , C07D309/08 , C07D313/08 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07F9/65517
摘要： Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1 is an optionally substituted five- or six-membered ring group; X1 is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1 and E4 are each optionally substituted carbon or the like; E2 and E3 are each oxygen or the like; and a and b are each a single bond or a double bond); X2 is a divalent group constituting a straight chain moiety; Z1 is a divalent cyclic group or the like; Z2 is a free valency or the like; and R2 is optionally substituted amino or the like.
摘要翻译：通式（1）的化合物或其盐，表现出对HIV感染性疾病的预防和治疗作用，其中R 1为任选取代的五元或六元环基团; X 1是自由价或类似物; W是由e表示的二价基团。例如通式（2）（其中A和B各自为任选取代的五至七元环; E1和E4各自为任选取代的碳等; E2和E3各自为氧等; 和b各自为单键或双键）; X 2是构成直链部分的二价基团; Z 1是二价的环状基团等; Z 2是自由价或类似物; 和R 2是任选取代的氨基等。

5. 发明授权

US06172061B2 Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative 失效
公开(公告)号：US06172061B2
公开(公告)日：2001-01-09
申请号：US09213377
申请日：1998-12-17
申请人： Osamu Nishimura , Masanori Baba , Hidekazu Sawada , Naoyuki Kanzaki , Ken-ichi Kuroshima , Mitsuru Shiraishi , Yoshio Aramaki
发明人： Osamu Nishimura , Masanori Baba , Hidekazu Sawada , Naoyuki Kanzaki , Ken-ichi Kuroshima , Mitsuru Shiraishi , Yoshio Aramaki
IPC分类号： A62K31351
CPC分类号： C07D407/12 , A61K31/335 , A61K31/351 , A61K31/452 , A61K31/4523 , A61K31/5377 , A61K31/665 , A61K31/67 , A61K45/06 , C07C233/62 , C07C2602/12 , C07D309/14 , C07D313/08 , C07D337/08
摘要： This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; 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, etc., or a salt thereof.

6. 发明授权

US06268354B1 Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative 失效
标题翻译：用于拮抗含有酰苯胺衍生物的CCR5的药物组合物
公开(公告)号：US06268354B1
公开(公告)日：2001-07-31
申请号：US09661320
申请日：2000-09-13
申请人： Osamu Nishimura , Masanori Baba , Hidekazu Sawada , Naoyuki Kanzaki , Ken-ichi Kuroshima , Mitsuru Shiraishi , Yoshio Aramaki
发明人： Osamu Nishimura , Masanori Baba , Hidekazu Sawada , Naoyuki Kanzaki , Ken-ichi Kuroshima , Mitsuru Shiraishi , Yoshio Aramaki
IPC分类号： A61K31165
CPC分类号： C07D407/12 , A61K31/335 , A61K31/351 , A61K31/452 , A61K31/4523 , A61K31/5377 , A61K31/665 , A61K31/67 , A61K45/06 , C07C233/62 , C07C2602/12 , C07D309/14 , C07D313/08 , C07D337/08
摘要： This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; 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, etc., or a salt thereof.
摘要翻译：本发明提供用于拮抗CCR5的药物组合物，其包含下式化合物：其中R 1为任选取代的5至6元环; W是下式的二价基团：其中环A是任选取代的5至6元芳环，X是任选取代的C，N或O原子，并且环B是任选取代的5-至7 记忆环 Z是化学键或二价基团; R2是（1）其中氮原子可以形成季铵等的任选取代的氨基或其盐。

7. 发明授权

US06235771B1 Anilide derivative, production and use thereof 失效
标题翻译：苯胺衍生物，生产和使用
公开(公告)号：US06235771B1
公开(公告)日：2001-05-22
申请号：US09463924
申请日：2000-03-27
申请人： Mitsuru Shiraishi , Masanori Baba , Masaki Seto , Naoyuki Kanzaki , Osamu Nishimura
发明人： Mitsuru Shiraishi , Masanori Baba , Masaki Seto , Naoyuki Kanzaki , Osamu Nishimura
IPC分类号： A61K3138
CPC分类号： C07D335/06 , A61K31/495 , A61K31/52 , A61K31/535 , A61K31/55 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K45/06 , C07D337/08 , C07D409/12 , C07D409/14 , C07F9/655372 , C07F9/65539 , A61K2300/00
摘要： 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 cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.
摘要翻译：本发明提供下式化合物：其中R 1为任选取代的5至6元环; 环A是任选取代的6至7元环; 环B是任选取代的苯环; n为1或2的整数; Z是化学键或二价基团; R2是（1）其中氮原子可以形成季铵的任选取代的氨基，（2）可以含有硫原子或氧原子作为构成原子的环的任选取代的含氮杂环基，其中氮原子可以形成季铵，（3）通过硫原子结合的基团或（4）下式的基团：其中k为0或1，当k为0时，磷原子可以形成鏻; R 5和R 6各自独立地为任选取代的烃基，任选取代的羟基或任选取代的氨基，并且R 5和R 6可以彼此结合形成环状基团以及相邻的磷原子或其盐，其可用于拮抗CCR5以及用于预防和治疗HIV感染性疾病。

8. 发明授权

US06376536B1 Quaternary ammonium salts and their use 失效
标题翻译：季铵盐及其用途
公开(公告)号：US06376536B1
公开(公告)日：2002-04-23
申请号：US09580270
申请日：2000-05-26
申请人： Mitsuru Shiraishi , Masanori Baba , Yoshio Aramaki , Osamu Nishimura , Naoyuki Kanzaki
发明人： Mitsuru Shiraishi , Masanori Baba , Yoshio Aramaki , Osamu Nishimura , Naoyuki Kanzaki
IPC分类号： A61K31351
CPC分类号： C07D407/12 , A61K31/335 , A61K31/351 , A61K31/452 , A61K31/4523 , A61K31/5377 , A61K31/665 , A61K31/67 , A61K45/06 , C07C233/62 , C07C2602/12 , C07D309/14 , C07D313/08 , C07D337/08 , C07D407/14
摘要： This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: wherein R1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is —CH2—, —S— or —O—; and R2, R3 and R4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.
摘要翻译：本发明提供一种拮抗CCR5的化合物，所述化合物由下式表示：其中R 1为任选取代的苯基或任选取代的噻吩基; Y是-CH 2 - ， - S-或-O-; R2，R3和R4独立地为任选取代的脂族烃基或任意取代的脂环族杂环基，对于HIV的感染性疾病的预防和治疗是有效的。

9. 发明授权

US6096780A Quaternary ammonium salts and their use 失效
标题翻译：季铵盐及其用途
公开(公告)号：US6096780A
公开(公告)日：2000-08-01
申请号：US377040
申请日：1999-08-19
申请人： Mitsuru Shiraishi , Masanori Baba , Yoshio Aramaki , Osamu Nishimura , Naoyuki Kanzaki
发明人： Mitsuru Shiraishi , Masanori Baba , Yoshio Aramaki , Osamu Nishimura , Naoyuki Kanzaki
IPC分类号： C07D313/08 , A61K31/00 , A61K31/167 , A61K31/335 , A61K31/351 , A61K31/452 , A61K31/4523 , A61K31/5377 , A61K31/55 , A61K31/665 , A61K31/67 , A61K31/76 , A61K45/06 , A61P31/00 , A61P31/12 , C07C233/62 , C07D309/14 , C07D337/08 , C07D407/12 , A61K31/38 , A61K31/165 , C07D313/00 , C07D337/12
CPC分类号： C07D407/12 , A61K31/335 , A61K31/351 , A61K31/452 , A61K31/4523 , A61K31/5377 , A61K31/665 , A61K31/67 , A61K45/06 , C07C233/62 , C07D309/14 , C07D313/08 , C07D337/08 , C07D407/14 , C07C2102/12
摘要： This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: ##STR1## wherein R.sup.1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is --CH.sub.2 --, --S-- or --O--; and R.sup.2, R.sup.3 and R.sup.4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.
摘要翻译：本发明提供一种拮抗CCR5的化合物，所述化合物由下式表示：其中R 1为任选取代的苯基或任选取代的噻吩基; Y是-CH 2 - ， - S-或-O-; R2，R3和R4独立地为任选取代的脂族烃基或任意取代的脂环族杂环基，对于HIV的感染性疾病的预防和治疗是有效的。

10. 发明授权

US06936602B1 Benzazepine derivatives, process for the preparation of the same and uses thereof 失效
标题翻译：苯并氮杂衍生物，其制备方法及其用途
公开(公告)号：US06936602B1
公开(公告)日：2005-08-30
申请号：US10018321
申请日：2000-06-15
申请人： Mitsuru Shiraishi , Masanori Baba , Yoshio Aramaki , Naoyuki Kanzaki , Osamu Nishimura
发明人： Mitsuru Shiraishi , Masanori Baba , Yoshio Aramaki , Naoyuki Kanzaki , Osamu Nishimura
IPC分类号： A61P31/18 , A61P43/00 , C07D223/16 , C07D405/12 , A61K31/55 , A61P31/00
CPC分类号： C07D223/16 , C07D405/12
摘要： Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.
摘要翻译：具有CCR5拮抗作用并对HIV感染发挥预防和治疗作用的通式（I）的化合物或其盐：其中R 1是5至6元芳环，其带有由以下通式表示的取代基：RZ 1 - ZZ 2 - （其中R 1是氢或任选取代的烃基; X是任选取代的亚烷基 ; Z 1和Z 2各自为杂原子），并且可以进一步被取代，其中R任选地与芳环键合形成另一个环; Y是任选取代的亚氨基; R 2和R 3各自为任选取代的脂族烃基或任选取代的杂脂环基团。

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