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141. 发明申请

US20030220268A1 New phenylalanine derivatives 有权
标题翻译：新型苯丙氨酸衍生物
公开(公告)号：US20030220268A1
公开(公告)日：2003-11-27
申请号：US10300856
申请日：2002-11-21
申请人： AJINOMOTO CO. INC
发明人： Shingo Makino , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
IPC分类号： A61K038/05 , A61K031/517 , A61K031/513 , C07D43/02 , C07K005/04 , C07D239/54
CPC分类号： C07D239/22 , C07D239/54 , C07D239/78 , C07D239/80 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D265/26 , C07D285/16 , C07D285/24 , C07D401/12 , C07D471/04 , C07D475/02 , C07D487/04 , Y02P20/582
摘要： Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to null4 integrin. They are used as therapeutic agents for various diseases concerning null4 integrin. 1
摘要翻译：指定的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗活性。它们被用作关于α4整联蛋白的各种疾病的治疗剂。

142. 发明授权

US06605604B1 Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them 失效
标题翻译：抑制金属蛋白酶的羧酸和异羟肟酸化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US06605604B1
公开(公告)日：2003-08-12
申请号：US09720850
申请日：2000-12-26
申请人： Patrick Casara , Anne Marie Chollet , Thierry Le Diguarher , Ghanem Atassi , Jacqueline Bonnet , Alain Pierre , Massimo Sabatini , Gordon Tucker , Nicolas Guilbaud
发明人： Patrick Casara , Anne Marie Chollet , Thierry Le Diguarher , Ghanem Atassi , Jacqueline Bonnet , Alain Pierre , Massimo Sabatini , Gordon Tucker , Nicolas Guilbaud
IPC分类号： C07D20948
CPC分类号： C07D209/48 , C07C233/82 , C07C259/10 , C07C311/29 , C07D231/22 , C07D237/32 , C07D239/96 , C07D253/08 , C07D275/06 , C07D403/12 , C07D409/12 , C07D471/04
摘要： The invention concerns a compound of formula (I) wherein: n is equal to 0 or 1; R1, R2, R3, R4 represent a hydrogen or an alkyl group, or R1 and R3 together form a cycloalkyl group; R5 represents a hydrogen, an alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, hetereoalkylalkyl, hetereocycloalkyl, hetereocycloalkylalkyl group (all optionally substituted), or a —CO—R6 group; and R6 represents R7 or OR7 or NR7R8, with R7 representing an aryl, arylalkyl, heteroaryl or heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl group (all optionally substituted), and R8 representing an alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl (all optionally substituted); or R5 and R6 form with the nitrogen atom and the Z group bearing them a saturated monocyclic, bicyclic or tricyclic group, partially unsaturated or unsaturated, with 5 to 16 chain links containing 1 to 7 heteroatoms and optionally substituted; R10 represents a hydrogen atom or a hydroxy group, and in the latter case R1, R2, R3, R4 are independently selected among hydrogen and alkyl; Z represents a hydroxy, alkoxy, alkenyloxy, benzyloxy group or a NH—OR group; X represents a sulphur, a SO, SO2 group (in those cases where R3 and R4 are different from an alkyl) or a group —CO—O— (in which case R1 and R3 form a cycloalkyl group), or X represents an oxygen atom; W represents a W1—(A)p or W1—B—W2—(A)p group wherein W1 and W2 represent an aryl or heteroaryl group, A is a standard substituent of aromatic cycles, B a bond, an oxygen or an alkylene, alkenylene, alkynylene group, and p is an integer ranging between 0 and 5; T1 and T2 represent a bond or an alkylene, alkenylene, or alkynylene group. The invention is useful for preparing medicines.
摘要翻译：本发明涉及式（I）的化合物，其中：n等于0或1; R1，R2，R3，R4表示氢或烷基，或R1和R3一起形成环烷基; R5代表氢，烷基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基烷基，杂三环烷基，杂三环烷基烷基（全部任意取代）或-CO-R 6基团; 并且R 6表示R 7或OR 7或NR 7 R 8，其中R 7表示芳基，芳基烷基，杂芳基或杂芳基烷基，杂环烷基，杂环烷基烷基（全部被取代），R 8表示烷基，芳基，芳基烷基，杂芳基或杂芳基烷基（全部被取代）或R 5和R 6与氮原子一起形成，Z基团带有饱和的单环，双环或三环基团，部分不饱和或不饱和的，具有5至16个含有1至7个杂原子和任选取代的链节; R 10表示氢原子或羟基，在后一种情况下，R 1，R 2，R 3，R 4独立地选自氢和烷基; Z表示羟基，烷氧基，烯氧基，苄氧基或NH-OR基; X表示硫，SO，SO 2基（在那些R3和R4不同于烷基的情况下）或基团-CO-O-（在这种情况下，R1和R3形成环烷基），或X表示氧原子; W表示W1-（A）p或W1-B-W2-（A）p基团，其中W1和W2表示芳基或杂芳基，A是芳族环的标准取代基，B a键，氧或亚烷基亚烯基，亚炔基，p为0〜5的整数。 T1和T2表示键或亚烷基，亚烯基或亚炔基。本发明可用于制备药物。

143. 发明授权

US06420427B1 Aminobutyric acid derivatives 失效
标题翻译：氨基丁酸衍生物
公开(公告)号：US06420427B1
公开(公告)日：2002-07-16
申请号：US09529056
申请日：2000-04-07
申请人： Kanji Takahashi , Tsuneyuki Sugiura
发明人： Kanji Takahashi , Tsuneyuki Sugiura
IPC分类号： A01N3718
CPC分类号： C07D207/327 , C07B2200/07 , C07B2200/09 , C07C233/47 , C07C233/63 , C07C233/83 , C07C235/06 , C07C235/16 , C07C235/42 , C07C235/52 , C07C237/22 , C07C243/34 , C07C255/41 , C07C255/57 , C07C259/06 , C07C259/08 , C07C271/22 , C07C311/21 , C07C323/42 , C07C323/60 , C07C327/30 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2603/74 , C07D207/34 , C07D207/40 , C07D207/46 , C07D209/18 , C07D209/42 , C07D211/14 , C07D211/46 , C07D211/62 , C07D213/54 , C07D213/56 , C07D213/68 , C07D213/70 , C07D213/81 , C07D215/14 , C07D231/12 , C07D233/56 , C07D233/74 , C07D249/08 , C07D253/08 , C07D263/57 , C07D277/62 , C07D295/13 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/84 , C07D309/12 , C07D333/16 , C07D333/38 , C07D333/44 , C07D333/60 , C07D405/12 , C07F7/1804
摘要： An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.
摘要翻译：式（I）的氨基丁酸衍生物（其中所有符号如说明书中所定义）及其盐。式（I）化合物对基质金属蛋白酶具有抑制活性，可用于预防和/或治疗疾病，例如类风湿病，关节炎，异常骨吸收，骨质疏松症，牙周炎，间质性肾炎，动脉硬化，肺气肿，肝硬化，角膜损伤，肿瘤细胞侵袭或生长的转移，自身免疫疾病（例如克罗恩病，干燥综合征），血管迁移或白细胞浸润引起的疾病，动脉化，多发性硬化，主动脉瘤，子宫内膜异位症。

144. 发明申请

US20020042418A1 Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acides 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US20020042418A1
公开(公告)日：2002-04-11
申请号：US09845392
申请日：2001-04-30
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K031/53 , A61K031/517 , A61K031/502 , A61K031/47
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: 1 wherein r is 0-2, T is selected from 2 and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

145. 发明授权

US5932577A Substituted oxobutyric acids as matrix metalloprotease inhibitors 失效
标题翻译：取代的氧代丁酸作为基质金属蛋白酶抑制剂
公开(公告)号：US5932577A
公开(公告)日：1999-08-03
申请号：US857053
申请日：1997-05-15
申请人： Brian R. Dixon , Jinshan Chen , Michael C. VanZandt , David R. Brittelli
发明人： Brian R. Dixon , Jinshan Chen , Michael C. VanZandt , David R. Brittelli
IPC分类号： C07C59/90 , C07D209/48 , C07D253/08 , A61K31/53 , C07C65/32 , C07D251/00
CPC分类号： C07D209/48 , C07C59/90 , C07D253/08
摘要： The present invention provides pharmaceutical compositions and methods for treating certain conditions associated with matrix metalloproteases comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metalloprotease, resulting in achievement of the desired effect. The compounds of the present invention are either of the generalized formula: ##STR1## wherein y is 0, 2, or, 3, r is 0-6, Z is (CH.sub.2).sub.7 or (CH.sub.2).sub.e --C.sub.6 H.sub.4 --(CH.sub.2).sub.f, wherein e is 0-1 and f is 0-5, and R.sup.15 is --H, --Cl, --OMe or ##STR2## wherein n is 0-4, R.sup.17 is C.sub.2 H.sub.5, alkyl, benzyl, and R.sup.16 is ##STR3## wherein t is 0-2, x is 0-4, and R.sup.4 is one of the following: halide, alkyl of 1-6 carbons, OR, NR.sub.2, NO.sub.2 (R=H or alkyl of 1-6 carbons).
摘要翻译：本发明提供用于治疗与基质金属蛋白酶相关的某些病症的药物组合物和方法，其包括给予一定量的有效抑制至少一种基质金属蛋白酶活性的本发明化合物或组合物，从而达到预期的效果。本发明的化合物是以下通式：其中y是0,1或3，r是0-6，Z是（CH2）7或（CH2）e-C6H4-（CH2）f，其中 e为0-1，f为0-5，R15为-H，-Cl，-OMe或其中n为0-4，R17为C2H5，烷基，苄基，R16为其中t为0-2，x 是0-4，R4是以下之一：卤化物，1-6个碳的烷基，OR，NR2，NO2（R = H或1-6个碳原子的烷基）。

146. 发明授权

US5925637A Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US5925637A
公开(公告)日：1999-07-20
申请号：US856693
申请日：1997-05-15
申请人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32 , C07D253/08 , C07C63/64 , C07D253/10
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，溃疡性溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

147. 发明授权

US4552878A Benzo- and thieno-triazine-1,2,3 ones-4 失效
标题翻译：苯并 - 噻吩并三嗪-1,2,3,4-四酮
公开(公告)号：US4552878A
公开(公告)日：1985-11-12
申请号：US534173
申请日：1983-09-19
申请人： Gerard Ferrand , Herve Dumas , Michel Bayssat , Jean-Claude Depin
发明人： Gerard Ferrand , Herve Dumas , Michel Bayssat , Jean-Claude Depin
IPC分类号： A61K31/53 , A61P25/24 , A61P25/26 , C07D253/08 , C07D495/04 , C07D403/06
CPC分类号： C07D253/08 , C07D495/04
摘要： This invention relates to benzo- and thieno-triazine-1,2,3 ones-4 represented by the formula ##STR1## in which m is 2, 3 or 4, X is the vinylene group --CH.dbd.CH-- or a sulfur atom; R.sub.1 and R.sub.2 can be alike or different and are hydrogen, halogen, a lower alkyl radical, lower alkoxy radical or trifluoromethyl radical; when X is --CH--CH-- n is 0, 1 or 2 and R is hydrogen, halogen, a lower alkyl radical, lower alkoxy radical or nitro group; when X is a sulfur atom, R is hydrogen or constitutes a --CH.sub.2 --.sub.4 chain between the two open positions of the thiophenic ring. The compounds are useful as antidepressant drugs.
摘要翻译：本发明涉及由式“IMAGE”表示的苯并 - 噻吩并三嗪-1,2,3,4-四烷基，其中m为2,3或4，X为亚乙烯基-CH = CH-或硫原子 ; R 1和R 2可以相同或不同，为氢，卤素，低级烷基，低级烷氧基或三氟甲基; 当X是-CH-CH- n是0,1或2且R是氢时，卤素，低级烷基，低级烷氧基或硝基; 当X是硫原子时，R是氢或在噻吩环的两个开放位置之间构成-CH2-4链。该化合物可用作抗抑郁药物。

148. 发明授权

US4520023A 3-(3-Iodopropargyl)-benzo-1,2,3-triazin-4-ones, and their use in microbicidal agents 失效
标题翻译： 3-（3-碘代炔丙基） - 苯并-1,2,3-三嗪-4-酮，以及它们在杀微生物剂中的用途
公开(公告)号：US4520023A
公开(公告)日：1985-05-28
申请号：US549338
申请日：1983-11-04
申请人： Hans-Georg Schmitt , Wilfried Palus , Hermann Genth
发明人： Hans-Georg Schmitt , Wilfried Palus , Hermann Genth
IPC分类号： C07D251/34 , A01N43/64 , A01N43/707 , C07D253/08 , A61K31/53
CPC分类号： C07D253/08
摘要： The new 3-(3-iodopropargyl)-benzo-1,2,3-triazin-4-ones can be prepared by reacting benzo-1,2,3-triazin-4-ones with a propargyl compound. The new compounds can be used as active compounds in microbicidal agents.
摘要翻译：新的3-（3-碘炔丙基） - 苯并-1,2,3-三嗪-4-酮可以通过苯并-1,2,3-三嗪-4-酮与炔丙基化合物反应来制备。新化合物可用作杀菌剂中的活性化合物。

149. 发明授权

US4138557A 2-Equivalent yellow couplers 失效
标题翻译： 2-等效黄色耦合器
公开(公告)号：US4138557A
公开(公告)日：1979-02-06
申请号：US777168
申请日：1977-03-14
申请人： Immo Boie , Gunter Renner , Friedrich-Wilhelm Kunitz
发明人： Immo Boie , Gunter Renner , Friedrich-Wilhelm Kunitz
IPC分类号： C07D215/22 , C07D237/16 , C07D237/32 , C07D239/36 , C07D239/54 , C07D239/90 , C07D239/96 , C07D241/20 , C07D241/44 , C07D251/30 , C07D253/08 , G03C7/305 , C07C103/20 , C07C97/16 , C07C103/74
CPC分类号： C07D215/22 , C07D237/16 , C07D237/32 , C07D239/36 , C07D239/54 , C07D239/90 , C07D239/96 , C07D241/20 , C07D241/44 , C07D251/30 , C07D253/08 , G03C7/30535
摘要： 2-Equivalent yellow couplers for the production of yellow dye images in color photographic silver halide materials have as splittable group a nitrogen-containing 6-membered heteroaromatic ring which is linked by the said nitrogen atom to the coupling position of the coupler molecule, contains a carbonyl group adjacent said nitrogen, and also contains one or two additional nitrogens as well as a fused-on aromatic carbocyclic ring. When the heteroaromatic ring contains two additional nitrogens, all three nitrogens are vicinal; when it contains only one additional nitrogen, the splittable group is a 1,3-quinazolinone-4 having at least one carboxy, lower-aliphatic-alcohols-esterified carboxy, nitro, methyl or chloro substituent.
摘要翻译：用于在彩色照相卤化银材料中生产黄色染料图像的2-等效的黄色成色剂具有可分离的基团，由所述氮原子连接到成色剂分子的偶联位置的含氮6元杂芳环包含邻近所述氮的羰基，并且还含有一个或两个另外的氮以及稠合的芳族碳环。当杂芳环含有两个另外的氮时，所有三个氮都是邻位的; 当仅含有一个另外的氮时，可裂解基团是具有至少一个羧基，低级 - 脂族 - 醇 - 酯化的羧基，硝基，甲基或氯取代基的1,3-喹唑啉酮-4。

150. 发明授权

US3794726A Inhibiting aggressive behavior with 1,2,3-benzotriazin-(3h)-one 失效
标题翻译：用1,2,3-苄氧基 - （3H） - 酮抑制剧烈的行为
公开(公告)号：US3794726A
公开(公告)日：1974-02-26
申请号：US3794726D
申请日：1972-08-21
申请人： UNIROYAL INC
发明人： ARIYAN Z
IPC分类号： A61K31/53 , C07D253/08 , A61K27/00
CPC分类号： C07D253/08 , A61K31/53
摘要： 1,2,3-benzotriazin-4(3H)-one is useful as an anti-aggression agent.
摘要翻译： 1,2,3-苯并三嗪-4（3H） - 酮可用作抗侵袭剂。

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