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1. 发明申请

US20220395636A1 TRAINING DEVICES AND METHODS FOR SIMULATING INTRANASAL DRUG DELIVERY 有权
公开(公告)号：US20220395636A1
公开(公告)日：2022-12-15
申请号：US17773313
申请日：2020-10-30
申请人： JANSSEN PHARMACEUTICA, N.V.
发明人： William DAVIES , Ian SCRIMGEOUR , Nick FOLEY , Jimmy MOWER , Monica A. KAPIL
IPC分类号： A61M5/178
摘要： Various training devices and methods for simulating intranasal drug delivery are described. In one exemplary embodiment, a training device can include an outer sleeve, a locking sleeve coupled to the outer sleeve, a core sleeve coupled to the locking sleeve, and a plunger operatively coupled to the core sleeve. The plunger can be configured to selectively translate the core sleeve from an initial position to a first actuated position that indicates the release of a first simulated dose of a drug, and from the first actuated position to a second actuated position that indicates the release of a second simulated dose of the drug, in which the device does not contain the drug. The plunger can also be configured to rotate relative to the outer sleeve to reset the core sleeve to the initial position such that the core sleeve can be translated back to the first and second actuated positions.

2. 再颁专利

USRE48841E1 Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators 有权
公开(公告)号：USRE48841E1
公开(公告)日：2021-12-07
申请号：US16391791
申请日：2019-04-23
申请人： Janssen Pharmaceutica N.V.
发明人： Wenying Chai , Michael A. Letavic , Kiev S. Ly , Daniel J. Pippel , Dale A. Rudolph , Kathleen C. Sappey , Brad M. Savall , Chandravadan R. Shah , Brock T. Shireman , Akinola Soyode-Johnson , Emily M. Stocking , Devin M. Swanson
IPC分类号： C07D487/04 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/498 , A61K31/506 , A61K31/53 , A61K31/5377
摘要： Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

3. 发明授权

US09688696B2 Piperidine/piperazine derivatives 有权
公开(公告)号：US09688696B2
公开(公告)日：2017-06-27
申请号：US15292196
申请日：2016-10-13
申请人： Janssen Pharmaceutica NV
发明人： Jean-Pierre Andre Marc Bongartz , Lieven Meerpoel , Gustaaf Maria Boeckx , Guy Rosalia Eugeen Van Lommen , Christophe Francis Robert Nestor Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
IPC分类号： C07D239/26 , C07D239/42 , A61K31/496 , C07D513/04 , C07D231/12 , C07D249/08 , C07D249/12 , C07D271/06 , C07D487/04 , C07D271/107 , C07D401/10 , C07D271/10 , C07D401/04 , C07D401/12
CPC分类号： C07D513/04 , C07D231/12 , C07D239/26 , C07D239/42 , C07D249/08 , C07D249/12 , C07D271/06 , C07D271/10 , C07D271/107 , C07D401/04 , C07D401/10 , C07D401/12 , C07D487/04
摘要： The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

4. 发明授权

US09499567B2 Piperidine/piperazine derivatives 有权
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：US09499567B2
公开(公告)日：2016-11-22
申请号：US14803275
申请日：2015-07-20
申请人： Janssen Pharmaceutica NV
发明人： Jean-Pierre Andre Marc Bongartz , Lieven Meerpoel , Gustaaf Maria Boeckx , Guy Rosalia Eugeen Van Lommen , Christophe Francis Robert Nestor Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
IPC分类号： C07D231/12 , C07D249/08 , C07D271/06 , C07D271/10 , A61K31/496 , C07D513/04 , C07D239/26 , C07D239/42 , C07D249/12 , C07D487/04 , C07D271/107 , C07D401/10
CPC分类号： C07D513/04 , C07D231/12 , C07D239/26 , C07D239/42 , C07D249/08 , C07D249/12 , C07D271/06 , C07D271/10 , C07D271/107 , C07D401/04 , C07D401/10 , C07D401/12 , C07D487/04
摘要： The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
摘要翻译：本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

5. 发明授权

US09302987B2 Pyrrolidinyl derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
标题翻译：吡咯烷基衍生物作为11-β羟基类固醇脱氢酶抑制剂
公开(公告)号：US09302987B2
公开(公告)日：2016-04-05
申请号：US14656752
申请日：2015-03-13
申请人： Janssen Pharmaceutica N.V.
发明人： Libuse Jaroskova , Joannes Theodorus Maria Linders , Christophe Francis Robert Nestor Buyck , Louis Jozef Elisabeth Van Der Veken , Vladimir Dimtchev Dimitrov , Theo Teofanov Nikiforov
IPC分类号： C07D207/26 , C07D405/06 , C07D207/267 , C07D211/76
CPC分类号： C07D211/76 , C07D207/26 , C07D207/267 , C07D405/06
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2—C1-4alkyl-; R6 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1或2; L表示任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4烷基 - ，羟基-C 1-4烷基，羟基，C 1-3烷氧基或苯基-C 1-4烷基的取代基取代的C 1-3烷基接头。 M表示直接键或任选被一个或两个选自羟基，C 1-4烷基或C 1-4烷氧基的取代基取代的C 1-3烷基接头; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或可能的两个或三个选自羟基，Ar 1和卤素的取代基取代; 或者R 1和R 2与它们所连接的苯环一起形成萘基或1,3-苯并二恶唑基，其中所述萘基或1,3-苯并二恶唑基任选被卤素取代; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 4表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R5表示氢，C1-4烷基或Ar2-C1-4烷基 - ; R 6表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; Ar1和Ar2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基 - 或苯基-C 1-4烷基取代; 用作药物。

6. 发明授权

US09237749B2 Antimicrobial combinations of pyrion compounds with polyethyleneimines 有权
标题翻译：吡喃化合物与聚乙烯亚胺的抗菌组合
公开(公告)号：US09237749B2
公开(公告)日：2016-01-19
申请号：US13805013
申请日：2011-06-29
申请人： Dany Leopold Jozefien Bylemans , Miguel F. C. De Bolle
发明人： Dany Leopold Jozefien Bylemans , Miguel F. C. De Bolle
IPC分类号： A01N43/40 , A61K31/44 , A61L2/18 , B27K3/50 , C02F1/50 , A01N33/04 , A01N33/12 , A61K31/4412 , A61K31/785 , C10M161/00
CPC分类号： A01N43/40 , A01N33/04 , A61K31/44 , A61K31/4412 , A61K31/785 , A61L2/18 , B27K3/50 , C02F1/50 , C10M161/00 , C10M2215/221 , C10M2217/046 , C10M2219/09 , C10N2230/16 , C10N2240/40 , A01N33/12 , A01N2300/00 , A61K2300/00
摘要： The present invention relates to combinations of the pyrion compounds sodium pyrithione and 1-hydroxy-2-pyridinone, and polyethyleneimines (PEI) which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of a pyrion compound selected from sodium pyrithione and 1-hydroxy-2-pyridinone together with polyethyleneimines; in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, viruses, and the like.
摘要翻译：本发明涉及吡啶化合物吡啶硫酮钠和1-羟基-2-吡啶酮的组合以及提供改善的杀生物作用的聚乙烯亚胺（PEI）。更具体地，本发明涉及包含选自吡啶硫酮钠和1-羟基-2-吡啶酮与聚乙烯亚胺的吡啶化合物的组合的组合物; 以提供协同的杀生物效果。包含这些组合的组合物可用于保护任何生物或非生物材料，例如作物，植物，水果，种子，由木材，茅草等制成的物体，工程材料，可生物降解材料和织物，以防止由于微生物如细菌，真菌，酵母，藻类，病毒等的作用。

7. 发明授权

US09078896B2 Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase 有权
标题翻译：吡啶和嘧啶衍生物作为组蛋白脱乙酰酶的抑制剂
公开(公告)号：US09078896B2
公开(公告)日：2015-07-14
申请号：US14151970
申请日：2014-01-10
申请人： Janssen Pharmaceutica N.V.
发明人： Laurence Francoise Bernadette Marconnet-Decrane , Sandrine Francoise Dominique Gaurrand , Patrick René Angibaud
IPC分类号： C07D403/12 , A61K31/496 , C07D213/78 , C07D239/42 , C07D409/14 , A61K45/06 , C07D213/82
CPC分类号： A61K31/496 , A61K45/06 , C07D213/78 , C07D213/82 , C07D239/42 , C07D403/12 , C07D409/14 , Y02A50/411
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R1，R2，R3和X具有定义的含义，具有组蛋白脱乙酰酶抑制酶活性; 其制剂，含有它们的组合物及其作为药物的用途。

8. 发明授权

US09056850B2 Process for the preparation of compounds useful as inhibitors of SGLT 有权
公开(公告)号：US09056850B2
公开(公告)日：2015-06-16
申请号：US12578934
申请日：2009-10-14
申请人： Walter Ferdinand Maria Filliers , Rudy Laurent Maria Broeckx , Patrick Hubert J. Nieste , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Christopher Teleha
发明人： Walter Ferdinand Maria Filliers , Rudy Laurent Maria Broeckx , Patrick Hubert J. Nieste , Masanori Hatsuda , Masahiko Yoshinaga , Mitsuhiro Yada , Christopher Teleha
IPC分类号： C07D409/04 , C07D333/12 , C07D409/10
CPC分类号： C07D333/12 , C07D409/10 , C07H7/04 , C07H13/04
摘要： The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

9. 发明授权

US08927297B2 Methods to measure dissociation rates for ligands that form reversible covalent bonds 有权
标题翻译：测量形成可逆共价键的配体的解离速率的方法
公开(公告)号：US08927297B2
公开(公告)日：2015-01-06
申请号：US12850117
申请日：2010-08-04
申请人： Dionisios Rentzeperis , Marta Cristina Abad , Ludmila A. Barnakova , Frank A. Lewandowski , Cynthia M. Milligan
发明人： Dionisios Rentzeperis , Marta Cristina Abad , Ludmila A. Barnakova , Frank A. Lewandowski , Cynthia M. Milligan
IPC分类号： G01N33/53 , G01N33/68
CPC分类号： G01N33/6848 , G01N2333/723
摘要： The crystal structure of the ligand binding domain of ERR-α in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-α, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-α activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-α and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
摘要翻译：与ERR-α的Cys325形成可逆硫醚键的配体复合物中ERR-α的配体结合结构域的晶体结构，测量形成可逆共价键的配体的解离速率的方法，以及设计形成可逆共价键的配体的方法公开了用作ERR-α活性调节剂的可逆共价键。晶体结构和方法为调节ERR-α的活性提供了新的分子机制，为合理的药物设计提供依据，以获得有效的特异性配体，用作这种新药物靶标活性的调节剂。

10. 发明授权

US08853445B2 Process for the preparation of protected L-alanine derivatives 有权
公开(公告)号：US08853445B2
公开(公告)日：2014-10-07
申请号：US14162150
申请日：2014-01-23
申请人： Janssen Pharmaceutica, N.V.
发明人： Luigi Anzalone , Penina Feibush , Frank J. Villani
IPC分类号： C07C231/14 , C07C237/42 , C07C271/22 , C07C269/06
CPC分类号： C07C231/06 , C07C231/14 , C07C233/65 , C07C237/42 , C07C269/06 , C07C271/22
摘要： The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.

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