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1. 发明授权

US07005417B1 Echinocandin derivatives, method for preparing same and use as antifungal agents 失效
标题翻译：棘白菌素衍生物，其制备方法和用作抗真菌剂
公开(公告)号：US07005417B1
公开(公告)日：2006-02-28
申请号：US10009407
申请日：2000-06-08
申请人： Alain Corbier , Patrick Fauveau , Nathalie Pietre-Dischamp , Laurent Schio , Pascale Vicat
发明人： Alain Corbier , Patrick Fauveau , Nathalie Pietre-Dischamp , Laurent Schio , Pascale Vicat
IPC分类号： A61K38/12
CPC分类号： C07K7/56 , A61K38/00
摘要： A subject of the invention is the compounds of formula (I): in which either R1 and R2=H, OH, alkyl optionally substituted, or NR1 form with the carbon carrying NR1R2 a double bond and R2 is XRa, X being O, NH OR N-alkyl and Ra being H, alkyl optionally substituted, or R2 is e-N═C(—N-d)-N(f)-g R3=H, OH, CH3 R4=H, OH R=chain containing up to 30 carbon atoms, optionally containing one or more heteroatoms, one or more heterocycles, T=H, CH3, CH2CONH2, CH2C≡N, (CH2)2NH2, (CH2)2Nalk+X− Y=H, OH, Halogen, OSO3H W=H, OH Z=H or CH3. The products have of the antifungal properties.
摘要翻译：本发明的主题是式（I）的化合物：<化学式id =“CHEM-US-00001”num =“000

2. 发明申请

US20060035820A1 New derivatives of echinocandine, their preparation process and their use as antifungals 失效
标题翻译：棘皮菌素的新衍生物，其制备方法及其作为抗真菌剂的用途
公开(公告)号：US20060035820A1
公开(公告)日：2006-02-16
申请号：US11225627
申请日：2005-09-13
申请人： Patrick Fauveau , Stephen Hawser , Gilles Lebourg , Laurent Schio
发明人： Patrick Fauveau , Stephen Hawser , Gilles Lebourg , Laurent Schio
IPC分类号： A61K38/12 , C07K5/12
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b—C≡N radical or R1 and R2 together with the nitrogen which carries-them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear,. branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
摘要翻译：本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4，氢或羟基R：代表线性。支链或环状链T：氢，甲基，CH 2 CONH 2，CH 2C≡N，a（CH 2） / SUB 2）或（CH 2）2 N 2 O 2 N 2 O 2 N 2 N 2 O 2 X，卤素和烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH，Z：H，CH 3 。式（I）化合物具有抗真菌性质。

3. 发明授权

US07192920B2 Derivatives of echinocandine, their preparation process and their use as antifungals 失效
标题翻译：棘皮棘酸衍生物，其制备方法及其作为抗真菌剂的用途
公开(公告)号：US07192920B2
公开(公告)日：2007-03-20
申请号：US11225627
申请日：2005-09-13
申请人： Patrick Fauveau , Stephen Hawser , Gilles Lebourg , Laurent Schio
发明人： Patrick Fauveau , Stephen Hawser , Gilles Lebourg , Laurent Schio
IPC分类号： A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C≡N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
摘要翻译：本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮一起形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4：氢或羟基R：表示直链，支链或环状的链T：氢，甲基，CH 2 CONH 2，CH 2C≡N （CH 2）2 NH 2或（CH 2 CH 2）2，或（CH 2）2 卤素，烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH， Z：H，CH 3。式（I）化合物具有抗真菌性质。

4. 发明授权

US07160983B2 Echinocandin derivatives, their method of preparation and their application as anti-fungal agents 失效
标题翻译：棘白菌素衍生物，其制备方法及其作为抗真菌剂的应用
公开(公告)号：US07160983B2
公开(公告)日：2007-01-09
申请号：US10666072
申请日：2003-09-19
申请人： Olivier Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
发明人： Olivier Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
IPC分类号： C07K7/50
CPC分类号： A01N43/90 , A61K38/00 , C07D487/18 , C07K7/56
摘要： Compound of the formula wherein R2 is —CH2—CH2—NH2, R3 is —CH3, R4 is —OH, R is Z is methyl and salts thereof which are useful as antifungal agents.
摘要翻译：下式的化合物其中R 2是-CH 2 -CH 2 -NH 2，其中R 1，R 2， 3是-CH 3，R 4是-OH，R是Z是甲基，其盐可用作抗真菌剂。

5. 发明授权

US06677429B1 Echinocandin derivatives, preparation method and application as anti-fungal agents 失效
标题翻译：棘白菌素衍生物，制备方法和应用作为抗真菌剂
公开(公告)号：US06677429B1
公开(公告)日：2004-01-13
申请号：US09581451
申请日：2000-07-24
申请人： Olivier Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
发明人： Olivier Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
IPC分类号： A61K3812
CPC分类号： A01N43/90 , A61K38/00 , C07D487/18 , C07K7/56
摘要： A compound of Formula I in which R1 and R2=H, OH, alkyl optionally substituted, or NR1 forms with the carbon bearing NR1R2 a double bond and R2 is Xra, X being O, NH or N-alkyl and Ra being H, alkyl optionally substituted; R=a chain containing up to 10 carbon atoms, optionally comprising one or several heteroatoms, one or several heterocycles; T=H, CH2, CH2CONH2, CH2C≡, (CH2)2NH2; Y=H, OH, halogen; W=H, OH; Z=H or CH3; said products have antifungal properties.
摘要翻译：其中R 1和R 2 = H，OH，任选取代的烷基，或NR 1与含NR 1 R 2的碳形成双键的式I化合物，R 2为Xra，X为O，NH或N-烷基，R a为H，烷基任选取代; R =含有至多10个碳原子的链，任选地包含一个或几个杂原子，一个或几个杂环; T = H，CH 2，CH 2 CONH 2，CH 2 C =，（CH 2）2 NH 2; Y = H，OH，卤素; W = H，OH; Z = H或CH 3; 所述产品具有抗真菌性质。

6. 发明授权

US07285619B2 Echinocandin derivatives, their method of preparation and their application as anti-fungal agents 失效
标题翻译：棘白菌素衍生物，其制备方法及其作为抗真菌剂的应用
公开(公告)号：US07285619B2
公开(公告)日：2007-10-23
申请号：US11165458
申请日：2005-06-23
申请人： Olivier Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
发明人： Olivier Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
IPC分类号： C07K7/50
CPC分类号： A01N43/90 , A61K38/00 , C07D487/18 , C07K7/56
摘要： Compounds of the formula wherein the substituents are as defined in the application useful as antifungal agents.
摘要翻译：下式的化合物，其中取代基如本申请中所定义，可用作抗真菌剂。

7. 发明授权

US07022669B1 Echinocandin derivatives, method for preparing same and application as antifungal agents 失效
标题翻译：棘白菌素衍生物，其制备方法和作为抗真菌剂的应用
公开(公告)号：US07022669B1
公开(公告)日：2006-04-04
申请号：US10018073
申请日：2000-06-08
申请人： Patrick Fauveau , Stephen Hawser , Gilles Lebourg , Laurent Schio
发明人： Patrick Fauveau , Stephen Hawser , Gilles Lebourg , Laurent Schio
IPC分类号： A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , Y10S930/27
摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C≡N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
摘要翻译：本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮一起形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4：氢或羟基R：表示直链，支链或环状的链T：氢，甲基，CH 2 CONH 2，CH 2C≡N （CH 2）2 NH 2或（CH 2 CH 2）2，或（CH 2）2 卤素，烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH， Z：H，CH 3。式（I）的化合物具有抗真菌性质。

8. 发明申请

US20050267019A1 Echinocandin derivatives, their method of preparation and their application as anti-fungal agents 失效
标题翻译：棘白菌素衍生物，其制备方法及其作为抗真菌剂的应用
公开(公告)号：US20050267019A1
公开(公告)日：2005-12-01
申请号：US11165458
申请日：2005-06-23
申请人： Oliver Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
发明人： Oliver Courtin , Patrick Fauveau , Astrid Markus , Dominique Melon Manguer , Jean-Marc Michel , Laurent Schio
IPC分类号： A61K38/04 , A61K38/00 , A61K38/12 , A61P31/10 , C07D487/18 , C07K5/12 , C07K7/56
CPC分类号： A01N43/90 , A61K38/00 , C07D487/18 , C07K7/56
摘要： Compounds of the formula wherein the substituents are as defined in the application useful as antifungal agents.
摘要翻译：下式的化合物，其中取代基如本申请中所定义，可用作抗真菌剂。

9. 发明授权

US5141952A Heterocyclic dicarboxylic acids 失效
标题翻译：杂环二羧酸
公开(公告)号：US5141952A
公开(公告)日：1992-08-25
申请号：US716950
申请日：1991-06-18
申请人： Constantin Agouridas , Patrick Fauveau
发明人： Constantin Agouridas , Patrick Fauveau
IPC分类号： A61K31/35 , A61K31/351 , A61K31/445 , A61K39/39 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07D211/18 , C07D211/60 , C07D211/78 , C07D309/08 , C07D309/10 , C07D309/28
CPC分类号： C07D309/10 , C07D211/18 , C07D211/60
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines represent a possible endo or exo double bond, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R'.sub.2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of --OH, hydrogen, ##STR3## and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.
摘要翻译：选自下式的化合物的化合物，其中虚线表示可能的内端或外双键，R 1和R 2分别选自氢，1至8个碳原子的烷基 2至8个碳原子的烯基和炔基，6至14个碳原子的芳基，7至18个碳原子的芳烷基和1至8个碳原子的烷基或6至14个碳原子的芳基， X是-O-或-NR-，R选自-OH，氢，IMA和-COOR'，R'是氢或1至8个碳原子的烷基，Y选自由氢，1至8个碳原子的烷基和2至8个碳原子的烯基和炔基组成，全部任选被至少一个卤素或-OH取代，条件是如果Y是-OH，X不是-NH- 及其无毒，药学上可接受的具有抗菌和免疫学特性的酸或碱的加成盐。

10. 发明授权

US4493836A 9-Oxalysergic acid derivatives and uses thereof 失效
标题翻译： 9-氧肉桂酸衍生物及其用途
公开(公告)号：US4493836A
公开(公告)日：1985-01-15
申请号：US493355
申请日：1983-05-10
申请人： Lucien Nedelec , Andre Pierdet , Patrick Fauveau
发明人： Lucien Nedelec , Andre Pierdet , Patrick Fauveau
IPC分类号： A61K31/535 , A61P9/12 , A61P43/00 , C07D209/00 , C07D209/90 , C07D265/00 , C07D498/06 , C07D498/04
CPC分类号： C07D209/90
摘要： Novel derivatives of 9-oxalysergic acid of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of --CH.sub.2 OH, alkylthiomethyl with 1 to 4 alkyl carbon atoms, --CH.sub.2 CN, --COOH, --COOAlk and ##STR2## Alk is alkyl of 1 to 5 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.5 is alkyl of 1 to 5 carbon atoms or R.sub.4 and R.sub.5 together with the nitrogen form a saturated heterocycle optionally containing another heteroatom and their non-toxic, pharmaceutically acceptable acid addition salts having essentially dopaminergic agonist activity, inhibiting activity of prolactin secretion, serotoninergic activity and antihypertensive activity and their preparation.
摘要翻译：其中R选自氢和1至4个碳原子的烷基，其中R选自氢，氯和溴，R2选自下列化学式的9-氧代戊酸的新型衍生物：其中R选自氢，由氢，1-4个碳原子的烷基，7-12个碳原子的芳烷基和4-7个碳原子的环烷基烷基组成的组中，R3选自-CH2OH，具有1-4个烷基碳原子的烷硫基甲基，-CH 2 CN，-COOH，-COOAlk和Alk是1至5个碳原子的烷基，R 4选自氢和1至5个碳原子的烷基，R 5是1至5个碳原子的烷基或R 4和R 5与氮一起形成任选地含有另外的杂原子的饱和杂环及其无毒的药学上可接受的酸加成盐，其具有基本上多巴胺能激动剂活性，抑制催乳素分泌的活性，血清素能活性和抗高血压随行活动及其准备。

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