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81. 发明授权

US07273856B2 Linear basic compounds having NK-2 antagonist activity and formulations thereof 有权
标题翻译：具有NK-2拮抗剂活性的线性碱性化合物及其制剂
公开(公告)号：US07273856B2
公开(公告)日：2007-09-25
申请号：US10494077
申请日：2002-10-28
申请人： Alessandro Sisto , Valerio Caciagli , Maria Altamura , Alessandro Giolitti , Valentina Fedi , Antonio Guidi , Danilo Giannotti , Nicholas Harmat , Rossano Nannicini , Franco Pasqui , Carlo Alberto Maggi
发明人： Alessandro Sisto , Valerio Caciagli , Maria Altamura , Alessandro Giolitti , Valentina Fedi , Antonio Guidi , Danilo Giannotti , Nicholas Harmat , Rossano Nannicini , Franco Pasqui , Carlo Alberto Maggi
IPC分类号： A61K31/455 , A61K31/535 , C07D265/30 , C07D211/82 , C07D207/00
CPC分类号： C07D409/12 , A61K38/00 , C07D333/70 , C07K5/06026 , C07K5/06034 , C07K5/06078
摘要： Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I)
摘要翻译：本文描述的是通式（I）的化合物，其通常用作速激肽拮抗剂，特别是神经激肽A; 和包含式（I）化合物的药物制剂，

82. 发明申请

US20070203338A1 Novel carboxylic acid derivatives, their preparation and use 失效
标题翻译：新型羧酸衍生物，其制备和用途
公开(公告)号：US20070203338A1
公开(公告)日：2007-08-30
申请号：US11789630
申请日：2007-04-25
申请人： Hartmut Riechers , Dagmar Klinge , Wilhelm Amberg , Andreas Kling , Stefan Muller , Ernst Baumann , Joachim Rheinheimer , Uwe Vogelbacher , Wolfgang Wernet , Liliane Unger , Manfred Raschack
发明人： Hartmut Riechers , Dagmar Klinge , Wilhelm Amberg , Andreas Kling , Stefan Muller , Ernst Baumann , Joachim Rheinheimer , Uwe Vogelbacher , Wolfgang Wernet , Liliane Unger , Manfred Raschack
IPC分类号： C07D251/22 , C07D207/00 , C07D233/22 , C07D303/48 , C07D257/06 , C07D239/24
CPC分类号： C07D495/04 , C07D239/34 , C07D239/48 , C07D239/52 , C07D239/60 , C07D239/70 , C07D239/96 , C07D251/20 , C07D251/26 , C07D251/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/04 , C07D491/048
摘要： Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
摘要翻译：其中R-R 6，X，Y和Z具有说明书中所述含义及其制备的羧酸衍生物。新型化合物适用于控制疾病。

83. 发明授权

US07256191B2 Materials and methods for the treatment of depression 失效
标题翻译：治疗抑郁症的材料和方法
公开(公告)号：US07256191B2
公开(公告)日：2007-08-14
申请号：US10931586
申请日：2004-08-31
申请人： Pascal Druzgala
发明人： Pascal Druzgala
IPC分类号： A06K31/535 , A61K31/24 , C07D207/00 , C07D207/04 , C07D211/18 , C07D265/28 , C07D229/00
CPC分类号： C07C251/58 , A61K31/165 , A61K31/192 , A61K31/215 , A61K31/221 , A61K31/277 , A61K31/4015
摘要： The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.
摘要翻译：本发明提供了易于被代谢药物解毒系统代谢的化合物。特别地，教导了被设计为在化合物的结构内包括酯的氟伏沙明类似物。还提供了治疗抑郁症和情感障碍（例如强迫症）的方法。还教导了氟伏沙明类似物的药物组合物。

84. 发明授权

US07250444B2 Pyrrole-based HMG-CoA reductase inhibitors 失效
标题翻译：基于吡咯的HMG-CoA还原酶抑制剂
公开(公告)号：US07250444B2
公开(公告)日：2007-07-31
申请号：US10862844
申请日：2004-06-07
申请人： Robert Michael Kennedy , William Keun-Chan Park , Bruce David Roth , Yuntao Song , Bharat K. Trivedi
发明人： Robert Michael Kennedy , William Keun-Chan Park , Bruce David Roth , Yuntao Song , Bharat K. Trivedi
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C04B35/632 , C07C303/40 , C07C311/13 , C07D207/33 , C07D207/34 , C07D207/36 , C07D319/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.
摘要翻译：提供了可用作低胆固醇血症和降血脂化合物的HMGCo-A还原酶抑制剂化合物。还提供了化合物的药物组合物。还提供了制备方法和使用该化合物的方法。

85. 发明授权

US07244758B2 N-type calcium channel blockers 失效
标题翻译： N型钙通道阻滞剂
公开(公告)号：US07244758B2
公开(公告)日：2007-07-17
申请号：US10856921
申请日：2004-05-28
申请人： Hassan Pajouhesh , Terrance P. Snutch , Hossein Pajouhesh , Yanbing Ding
发明人： Hassan Pajouhesh , Terrance P. Snutch , Hossein Pajouhesh , Yanbing Ding
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/09
摘要： Compounds that are derivatives of 3-aminomethyl-pyrrolidine generally containing at least one benzhydril moiety are useful in treating conditions which benefit from blocking calcium ion channels.
摘要翻译：通常含有至少一个二苯甲基部分的3-氨基甲基吡咯烷的衍生物的化合物可用于治疗受阻于钙离子通道的病症。

86. 发明授权

US07241897B2 Process for preparing cyanine dye labeling reagents 有权
标题翻译：制备花青染料标记试剂的方法
公开(公告)号：US07241897B2
公开(公告)日：2007-07-10
申请号：US10761906
申请日：2004-01-21
申请人： Jannis G. Stavrianopoulos , Elazar Rabbam
发明人： Jannis G. Stavrianopoulos , Elazar Rabbam
IPC分类号： C07D293/00 , C07D291/00 , C07D207/00 , C09B5/00 , C09B7/02 , G01N33/53 , C07H21/02 , C07H19/04
CPC分类号： C07H21/00 , C09B23/02 , C09B47/00 , C09B57/00 , Y10S436/80
摘要： This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.
摘要翻译：本发明提供标记试剂，标记的靶标和制备标记试剂的方法。标记试剂可以采用花青染料，呫吨染料，卟啉染料，香豆素染料或复合染料的形式。这些标记试剂可用于标记探针或靶标，包括核酸和蛋白质。这些试剂可用于基于蛋白质和基于核酸探针的测定。它们也适用于实时检测过程。

87. 发明授权

US07226938B2 Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US07226938B2
公开(公告)日：2007-06-05
申请号：US10656059
申请日：2003-09-05
申请人： Hui Cai , Nicholas I. Carruthers , Curt A. Dvorak , James P. Edwards , Annette K. Kwok , Jianmei Wei
发明人： Hui Cai , Nicholas I. Carruthers , Curt A. Dvorak , James P. Edwards , Annette K. Kwok , Jianmei Wei
IPC分类号： C07D207/00 , C07D333/02 , A61K31/41 , A01N43/64
CPC分类号： C07D491/04 , C07D495/04
摘要： Certain thienopyrrolyl and furanopyrrolyl compounds are disclosed as useful to treat or prevent disorders and conditions mediated by the histamine H4 receptor, including allergic rhinitis.
摘要翻译：公开了某些噻吩并吡喃基和呋喃并吡咯基化合物可用于治疗或预防由组胺H 4受体介导的病症和病症，包括过敏性鼻炎。

88. 发明授权

US07189754B2 Pyrrolidine ester derivatives with oxytocin modulating activity 有权
标题翻译：吡咯烷酯衍生物与催产素调节活性
公开(公告)号：US07189754B2
公开(公告)日：2007-03-13
申请号：US10471290
申请日：2002-03-19
申请人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
发明人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D401/10 , A61K31/401 , C07D207/22 , C07D403/10
摘要： The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1–C6-alkyl, C2–C6-alkenyl, C2–C6-alkynyl, aryl, heteroaryl, 3–8-membered cycloalkyl, acyl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1–2 further cycloalkyl or aryl or heteroaryl group
摘要翻译：本发明涉及式（I）的吡咯烷酯用于治疗和/或预防早产，早产和痛经的用途。特别地，本发明涉及式（I）的吡咯烷酯的用途，特别是拮抗催产素受体。本发明还涉及新的吡咯烷酯。 X选自CR 6，S 6，S 6，N 6，R 6，R 6， 7 ; R选自包含C 1 -C 6 -C 6烷基，C 2 -C 6 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，饱和或不饱和的3-8元环烷基，其可以含有1-3个选自N，O，S，芳基，杂芳基的杂原子 C 1 -C 6 - 烷基芳基，C 1 -C 6 - 烷基杂芳基，C 1 -C 6 - 烷基芳基，C 1 -C 6 - R 1选自由C 1 -C 6 - C 6 - 烷基，C 2 - （C 1 -C 6）烷基组成的组或由C 1 -C 6 - C 6 - 烯基，C 2 -C 6 - 炔基，芳基，杂芳基，3-8元环烷基，酰基，C

89. 发明授权

US07160877B2 Aliphatic nitrogen-containing 5-membered ring compound 失效
标题翻译：脂肪族含氮五元环化合物
公开(公告)号：US07160877B2
公开(公告)日：2007-01-09
申请号：US10872442
申请日：2004-06-22
申请人： Kosuke Yasuda , Hiroshi Morimoto , Saburo Kawanami , Masataka Hikota , Takeshi Matsumoto , Kenji Arakawa
发明人： Kosuke Yasuda , Hiroshi Morimoto , Saburo Kawanami , Masataka Hikota , Takeshi Matsumoto , Kenji Arakawa
IPC分类号： A61K31/55 , C07D207/00
CPC分类号： C07D207/404 , A61K31/40 , A61K31/425 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/5375 , C07D207/16 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
摘要翻译：本发明提供由式[I]表示的脂族含氮的5元环化合物：其中A表示-CH 2 - 或-S-，R 1， SUP>表示氢原子，低级烷基，羟基低级烷基或低级烷氧基低级烷基，X表示-N（R 3 O） - ， - O-或-CO-，其中R 3表示氢原子或低级烷基，R 2表示（1）可被取代的环状基团，或（2）可以被取代的环状基团，或取代或其药学上可接受的盐，制备上述化合物的方法和包含上述化合物作为有效成分的药物组合物。

90. 发明授权

US07122666B2 Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses 失效
标题翻译：杂芳基取代的吡咯衍生物，其制备及其治疗用途
公开(公告)号：US07122666B2
公开(公告)日：2006-10-17
申请号：US10354648
申请日：2003-01-30
申请人： Tomio Kimura , Akira Nakao , Nobuyuki Ohkawa , Takayoshi Nagasaki , Takanori Yamazaki
发明人： Tomio Kimura , Akira Nakao , Nobuyuki Ohkawa , Takayoshi Nagasaki , Takanori Yamazaki
IPC分类号： C07D207/00 , C07D209/00
CPC分类号： C07D451/02 , C07D401/04 , C07D401/14 , C07D453/02 , C07D455/02 , C07D471/04 , C07D487/04
摘要： Compounds having activity against production of an inflammatory cytokine of formula (I)′: A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is (IIa)′, (IIb)′ or (IIc)′: m′ is 1; E′ is nitrogen; D′ is >C(R5′)—, R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′ is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′ is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′ is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.
摘要翻译：具有抗式产生式（I）的炎性细胞因子的活性化合物的化合物：A'是吡咯; R 1是苯基或萘基; R 2是吡啶基或嘧啶基; （IIa）'，（IIb）'或（IIc）'：m'为1; E'是氮; D'是> C（R 5'） - ，R 5'是氢，取代基α'或取代基β'; B'是含氮5元杂环; R 4'是1至3个取代基α'，取代基β'和取代基γ'的取代基; R 1'和R 3'连接到与R 2'连接的吡咯原子相邻的吡咯的两个原子上; 取代基α'是羟基，硝基，氰基，卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或-NR a R b B。 R a，O和R b'是氢，烷基，烯基，炔基，芳烷基或烷基磺酰基，或者R a'和R“ b'与氮原子形成杂环基; 取代基β'是烷基，烯基，炔基，芳烷基或环烷基; 取代基γ'是氧代，羟基亚氨基，烷氧基亚氨基，亚烷基，亚烷基二氧基，烷基亚磺酰基，烷基磺酰基，芳基，芳氧基，亚烷基或芳亚烷基。

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