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1. 发明授权

US4734417A Lipid- and cholesterol-reducing derivatives of halo-biphenyl primary alcohols 失效
标题翻译：卤代联苯基伯醇的脂质和胆固醇降低衍生物
公开(公告)号：US4734417A
公开(公告)日：1988-03-29
申请号：US882586
申请日：1986-07-07
申请人： Henri Cousse , Andre Delhon , Jean-Pierre Rieu , Gilbert Mouzin
发明人： Henri Cousse , Andre Delhon , Jean-Pierre Rieu , Gilbert Mouzin
IPC分类号： A61K31/075 , A61K31/135 , A61K31/215 , A61K31/22 , A61K31/415 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/495 , A61P3/06 , A61P9/10 , C07C41/00 , C07C43/174 , C07C67/00 , C07C69/145 , C07C213/00 , C07C217/10 , C07C227/00 , C07C227/18 , C07C229/12 , C07D213/30 , C07D213/80 , C07D233/60 , C07D295/15 , C07D295/20 , C07D521/00 , C07D295/00
CPC分类号： C07D213/30 , C07C43/1742 , C07D213/80 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/15 , Y10S514/80
摘要： The invention relates to new derivatives of biphenyl primary alcohols, their preparation and use as medicaments useful in the treatment and prevention of atherosclerotic disorders. The new derivatives have the general formula ##STR1## in which X represents a halogen atom, and more particularly chlorine, bromine or fluorine in ortho or meta position,R represents an alkyl, amino alkyl, pyridyl alkyl or acyl radical and more particularly ##STR2## and acetyl.
摘要翻译：本发明涉及联苯基伯醇的新衍生物，它们的制备和用途可用作治疗和预防动脉粥样硬化性疾病的药物。新衍生物具有通式“IMAGE”，其中X表示卤素原子，更特别是邻位或间位的氯，溴或氟，R表示烷基，氨基烷基，吡啶基烷基或酰基，更具体地说，IMAGE > + TR 和乙酰基。

2. 发明授权

US4008323A Method of reducing cholesterol using certain aromatic keto acids 失效
标题翻译：使用某些芳香族酮酸降低胆固醇的方法
公开(公告)号：US4008323A
公开(公告)日：1977-02-15
申请号：US560344
申请日：1975-03-21
申请人： Henri Cousse , Gilbert Mouzin , Jean-Pierre Rieu , Andre Delhon
发明人： Henri Cousse , Gilbert Mouzin , Jean-Pierre Rieu , Andre Delhon
IPC分类号： C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90 , C07D295/185 , A61K31/495 , A61K31/19 , A61K31/205 , A61K31/235
CPC分类号： C07D295/185 , C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90
摘要： This invention relates to new chemical compounds useful as drugs, as well as to pharmaceutical compositions containing the same. This application claims their hypocholesterolemic use.The new products are aromatic keto acid compounds with antiinflammatory as well as analgetic and hypocholesteremic acitvity and having the general formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, phenyl, halophenyl, alkyl, phenoxy, or substituted phenoxy.R.sub.2 is hydrogen or alkoxy. R.sub.1 and R.sub.2 may form a ring, for instance: phenyl or cyclohexyl. R.sub.3 is always other than hydrogen, being either methyl (CH.sub.3) or methylene.When R.sub.3 is CH.sub.3, a double bond is present between the A and B carbons. When R.sub.3 is a methylene connected by a double bond to the B carbon, there can be only a single bond between the A and B carbons. The remaining valences of the A carbon atom are satisfied by hydrogen atoms.R.sub.4 may be OH, alkoxy, ##STR2## The drugs containing these active principles are useful in the prevention and treatment of inflammatory syndromes, pain, and conditions involving excess chloresterol.
摘要翻译：本发明涉及可用作药物的新化合物，以及含有该化合物的药物组合物。本申请要求其低胆固醇血症用途。

3. 发明授权

US4714789A Halo-biphenyl tertiary alcohols useful in therapy in the treatment of atherosclerosis 失效
标题翻译：用于治疗动脉粥样硬化的卤代联苯三醇
公开(公告)号：US4714789A
公开(公告)日：1987-12-22
申请号：US884959
申请日：1986-07-14
申请人： Henri Cousse , Andre Delhon , Jean-Pierre Rieu , Jean-Francois Patoiseau
发明人： Henri Cousse , Andre Delhon , Jean-Pierre Rieu , Jean-Francois Patoiseau
IPC分类号： C07C29/40 , A61K31/045 , A61P3/04 , A61P3/06 , A61P9/10 , C07C27/00 , C07C33/46 , C07C67/00 , C07C33/34
CPC分类号： C07C33/46
摘要： The invention concerns halo-biphenyl tertiary alcohols of the general formula: ##STR1## in which: X is chlorine or bromine in ortho or meta position.R and R.sub.1, which may be identical or different, represent an alkyl group of low molecular weight having from 1 to 4 carbon atoms, inclusive.These new derivatives are useful as medicaments, particularly in the treatment of atherosclerosis and obesity.
摘要翻译：本发明涉及以下通式的卤代 - 联苯叔醇：其中：X是邻位或间位的氯或溴。 R和R 1可以相同或不同，表示具有1-4个碳原子的低分子量烷基。这些新衍生物可用作药物，特别是用于治疗动脉粥样硬化和肥胖症。

4. 发明授权

US4605654A 2-(arylalkyloxymethyl)morpholines and the central nervous system compositions 失效
标题翻译： 2-（芳基烷氧基甲基）吗啉和中枢神经系统组成
公开(公告)号：US4605654A
公开(公告)日：1986-08-12
申请号：US809698
申请日：1985-12-17
申请人： Henri Cousse , Gilbert Mouzin , Jean-Pierre Rieu , Mike Briley , Antoine Stenger
发明人： Henri Cousse , Gilbert Mouzin , Jean-Pierre Rieu , Mike Briley , Antoine Stenger
IPC分类号： A61K31/535 , A61K31/5375 , A61P25/04 , A61P25/24 , A61P25/26 , C07D265/30 , C07D303/22 , C07D319/00 , C07D413/12 , C07D295/08
CPC分类号： C07D265/30 , C07D303/22 , C07D413/12
摘要： The present invention relates to new 2-(arylalkyloxymethyl)morpholine derivatives, the preparation thereof and their application as drugs which are useful in the treatment of disorders of the central nervous system.The 2-(arylalkyloxymethyl)morpholine derivatives according to the invention correspond to the general formula (I): ##STR1## in which: Ar denotes an aromatic group and more especially the following radicals: ##STR2## in the case where Ar denotes a phenyl radical and R denotes a hydrogen atom, an alkyl, alkoxy or halogen group, a trifluoromethyl radical, a nitro or amino group, a hydroxy group or an arylalkyloxy group.
摘要翻译：本发明涉及新的2-（芳基烷氧基甲基）吗啉衍生物，其制备方法及其作为可用于治疗中枢神经系统疾病的药物的应用。根据本发明的2-（芳基烷氧基甲基）吗啉衍生物对应于通式（I）：其中：Ar表示芳族基团，更特别是以下基团： + TR 在Ar表示苯基且R表示氢原子，烷基，烷氧基或卤素基，三氟甲基，硝基或氨基，羟基或芳基烷氧基的情况下。

5. 发明授权

US4058558A Aromatic keto acids and derivatives having analgetic, antiinflammatory, and hypocholesterolemizing action 失效
标题翻译：具有止痛，抗炎和低胆固醇作用的芳香酮酸和衍生物
公开(公告)号：US4058558A
公开(公告)日：1977-11-15
申请号：US560946
申请日：1975-03-21
申请人： Henri Cousse , Gilbert Mouzin , Jean-Pierre Rieu
发明人： Henri Cousse , Gilbert Mouzin , Jean-Pierre Rieu
IPC分类号： C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90 , C07D295/185 , C07C63/33 , A61K31/19
CPC分类号： C07D295/185 , C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90
摘要： This invention relates to new chemical compounds useful as drugs, as well as to pharmaceutical compositions containing the same.The new products are aromatic keto acid compounds with antiinflammatory as well as analgetic and hypocholesteremic activity and having the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, phenyl, halophenyl, phenoxy, or substituted phenoxy.R.sub.2 is hydrogen or alkoxy.R.sub.1 and R.sub.2 may form a ring, for instance: phenyl or cyclohexyl.R.sub.3 is always other than hydrogen, being either methyl (CH.sub.3) or methylene. When R.sub.3 is CH.sub.3, a double bond is present between the A and B carbons. When R.sub.3 is a methylene connected by a double bond to the B carbon, there can be only a single bond between the A and B carbons. The remaining valences of the A carbon atom are satisfied by hydrogen atoms.R.sub.4 may be OH, alkoxy, ##STR2##The drugs containing these active principles are useful in the prevention and treatment of inflammatory syndromes, pain, and conditions involving excess cholresterol.
摘要翻译：本发明涉及可用作药物的新化合物，以及含有该化合物的药物组合物。

6. 发明授权

US4510142A Derivatives of biphenyl alkyl carboxylates and their use as medicaments 失效
标题翻译：联苯烷基羧酸盐的衍生物及其作为药物的用途
公开(公告)号：US4510142A
公开(公告)日：1985-04-09
申请号：US433987
申请日：1982-10-12
申请人： Henry Cousse , Gilbert Mouzin , Jean-Pierre Tarayre , Jean-Pierre Rieu
发明人： Henry Cousse , Gilbert Mouzin , Jean-Pierre Tarayre , Jean-Pierre Rieu
IPC分类号： A61K31/215 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/451 , A61P25/04 , A61P29/00 , B01J27/00 , C07B61/00 , C07C67/00 , C07C231/00 , C07C231/12 , C07C235/16 , C07D211/16 , C07D213/75 , C07D295/185 , A61K31/495
CPC分类号： C07D213/75 , C07D211/16 , C07D295/185
摘要： This invention relates to new derivatives of biphenyl alkyl carboxylates, to a process for the preparation thereof and the use thereof as medicaments.The new derivatives according to the present invention correspond to general formula (I): ##STR1## wherein X represents a hydrogen atom or a halogen atom,R represents a hydrogen atom or an alkyl group, andR.sub.1 represents the following groups: ##STR2## These compounds will notably be used in the treatment of obstinate pains and inflammatory syndromes.
摘要翻译：本发明涉及联苯基羧酸烷基酯的新衍生物，其制备方法及其作为药物的用途。根据本发明的新衍生物对应于通式（I）：其中X表示氢原子或卤素原子，R表示氢原子或烷基，R1表示以下基团：这些化合物将特别用于治疗顽固性疼痛和炎性综合征。

7. 发明授权

US08946225B2 Derivatives of 2H pyridazin-3-ones, their preparation and their use as SCD-1 inhibitors 有权
标题翻译： 2H哒嗪-3-酮的衍生物，其制备及其作为SCD-1抑制剂的用途
公开(公告)号：US08946225B2
公开(公告)日：2015-02-03
申请号：US13388884
申请日：2010-08-05
申请人： Elisabeth Dupont-Passelaigue , Samuel Mialhe , Jean-Pierre Rieu , Didier Junquero , Karine Valeille
发明人： Elisabeth Dupont-Passelaigue , Samuel Mialhe , Jean-Pierre Rieu , Didier Junquero , Karine Valeille
IPC分类号： A61K31/50 , A61K31/501 , C07D237/02
CPC分类号： C07D237/22 , C07D401/12 , C07D403/12
摘要： The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: •either —(C═O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, •or —(C═O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.
摘要翻译：本发明涉及通式（I）的化合物，其特征在于（式1）其中特别地：-R 1表示一个或多个基团，例如三氟甲基，卤素如F，Cl， - 当n = m = 1时， W表示CH，Y表示氧，-U表示：• - （C = O）CH2NH-，并且在哒嗪酮的第4位分支，则R2表示H，•或 - （C = O）NH-，U为支链在哒嗪酮的位置（4），（5）或（6）中，R 2表示H，-R 3表示氢或甲基，加成盐与药学上可接受的碱和酸和不同的异构体，用作SCD-1酶抑制剂用于治疗肥胖，2型糖尿病和脂质疾病。

8. 发明授权

US5308844A Substituted 3-piperazinylalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones and their use in therapy 失效
标题翻译：取代的3-哌嗪基烷基-2,3-二氢-4H-1,3-苯并恶嗪-4-酮及其在治疗中的用途
公开(公告)号：US5308844A
公开(公告)日：1994-05-03
申请号：US925493
申请日：1992-08-05
申请人： Jean-Pierre Rieu , Dennis Bigg
发明人： Jean-Pierre Rieu , Dennis Bigg
IPC分类号： A61K31/535 , A61K31/536 , A61P3/04 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/24 , A61P25/26 , C07D265/22 , C07D413/12 , C07D295/10
CPC分类号： C07D413/10 , C07D265/22
摘要： The invention relates to novel substituted 3-piperazinylalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones of formula I ##STR1## their pharmaceutically acceptable inorganic or organic salts, optionally in their hydrated form, the racemates, the enantismers or their mixtures, their preparation and their use as medicaments as well as all the pharmaceutical compositions of I which are or are not combined with another active principle.
摘要翻译：本发明涉及式I的新的取代的3-哌嗪基烷基-2,3-二氢-4H-1,3-苯并恶嗪-4-酮其药学上可接受的无机或有机盐，任选以其水合形式，外消旋体，他们的制剂及其作为药物的用途以及I的所有药物组合物，或者不与其它活性成分组合。

9. 发明授权

US06531469B1 Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application 失效
标题翻译：取代的1-（4-哌啶基）-3-（芳基）异硫脲的制备及其治疗应用
公开(公告)号：US06531469B1
公开(公告)日：2003-03-11
申请号：US09889805
申请日：2001-07-20
申请人： Jean-Pierre Rieu , Jean-François Patoiseau , Gareth John , Bruno Legrand , Yvan Verscheure
发明人： Jean-Pierre Rieu , Jean-François Patoiseau , Gareth John , Bruno Legrand , Yvan Verscheure
IPC分类号： C07D41712
CPC分类号： C07D413/12 , C07D417/12
摘要： The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (1) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH2—CH(OH)—CH2— radical. R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R1 to R6, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively, and their pure, enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (1) and their possible hydrates.
摘要翻译：本发明涉及新型取代的N-苯并（噻唑/氧杂）嗪-2-基-1-芳基烷氧基烷基-4-哌啶胺及其制备及其治疗用途。本发明涉及式（1）的化合物，其中：X表示氧或硫原子; Y表示亚烷基，支链或不支链，含有2-6个碳原子或CH2-CH（OH）-CH2-基。 R表示氢，烷基，支链或不支链，含有1至7个碳原子; R 1至R 6相同或不同，表示氢，饱和或不饱和的烷基，支链或不含并且含有1至5个碳原子，饱和或不饱和烷氧基，支链或不具有1至5个碳原子，卤代，硝基，含有2〜3个碳原子的羟基，酰基或酰氧基，含1至5个碳原子的烷基氨基，三氟甲基或三氟甲氧基; n是1至6的整数，以及它们的纯的对映体或它们的混合物，式（1）化合物的治疗上可接受的矿物和有机盐及其可能的水合物。

10. 发明授权

US5385931A Sulfonamides derived from benzocyclic or benzoheterocyclic acids, their preparation and application in therapeutics 失效
标题翻译：衍生自苯环或苯并杂环酸的磺酰胺，其制备和在治疗中的应用
公开(公告)号：US5385931A
公开(公告)日：1995-01-31
申请号：US613842
申请日：1990-12-28
申请人： Dennis Bigg , Alain Duflos , Jean-Pierre Rieu
发明人： Dennis Bigg , Alain Duflos , Jean-Pierre Rieu
IPC分类号： A61K31/19 , A61K31/215 , A61K31/22 , A61K31/335 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/38 , A61K31/381 , A61P7/02 , C07C69/757 , C07C229/26 , C07C311/19 , C07D307/85 , C07D311/66 , C07D317/46 , C07D333/70 , C07D307/81 , C07D333/60
CPC分类号： C07D311/66 , C07C229/26 , C07C311/19 , C07C69/757 , C07D307/85 , C07D317/46 , C07D333/70 , C07C2102/08
摘要： The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.4 =H or Me; A represents a benzo-cyclic or benzo-heterocyclic divalent radical chosen from the following (a) to (j): ##STR3## and n can assume the values 1 to 4 inclusive; and the therapeutically acceptable organic or inorganic salts (R.sub.3 =H), the pure isomers or diastereoisomers or their mixture and all the pharmaceutical compositions of formula I with other active principles.The invention relates to the application of I as a medicament and the preparation processes.
摘要翻译： PCT No.PCT / FR90 / 00234 Sec。 371 1990年12月28日第 102（e）1990年12月28日日期PCT提交1990年4月4日PCT公布。 WO90 / 12007 PCT出版物日本1990年10月18日。本发明涉及苯并环或苯并杂环酸的新磺酰胺衍生物及其通式I的衍生物或具有1〜9个C的支链低级烷基; 未取代或被一个或多个基团取代的苯基：具有1-4个碳原子的直链或支链低级烷基，卤代，烷氧基，硝基，氨基，二烷基氨基或CF 3; 取代或未取代的萘; 硫代苯基; R1表示氢或直链或支链的低级烷基或苄基; R2表示氢，直链或支链的低级烷基，取代或未取代的苯基或芳烷基; R3表示氢或直链或支链的低级烷基（1-6）; -X-表示选自以下的二价官能团：-CH 2 - ; 其中R4 = H或Me; A表示选自以下（a）至（j）的苯并环或苯并杂环二价基团：（a）GE（e）图像（f）（h）（i）（j），n可以取值1〜4，和治疗上可接受的有机或无机盐（R3 = H），纯异构体或非对映异构体或其混合物以及具有其它活性成分的式I的所有药物组合物。本发明涉及I作为药物的应用及其制备方法。

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