AR106018A1 - Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos - Google Patents

Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos

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Publication number
AR106018A1
AR106018A1 ARP160102593A ARP160102593A AR106018A1 AR 106018 A1 AR106018 A1 AR 106018A1 AR P160102593 A ARP160102593 A AR P160102593A AR P160102593 A ARP160102593 A AR P160102593A AR 106018 A1 AR106018 A1 AR 106018A1
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AR
Argentina
Prior art keywords
4alkyl
independently selected
6alkyl
halogen
cyano
Prior art date
Application number
ARP160102593A
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English (en)
Inventor
Allan Wiles Jason
S Phadke Avinash
Deshpande Milind
Agarwal Atul
Wang Xiangzhu
Chen Dawei
Hashimoto Akihiro
Pais Godwin
Rao GADHACHANDA Venkat
Wang Qiuping
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Achillion Pharmaceuticals Inc
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Publication date
Application filed by Achillion Pharmaceuticals Inc filed Critical Achillion Pharmaceuticals Inc
Publication of AR106018A1 publication Critical patent/AR106018A1/es

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Abstract

La presente se relaciona con compuestos de la fórmula (1) o sales farmacéuticamente aceptables de los mismos, donde: Q¹ es C(R¹R¹’); Q² es C(R²R²’); Q³ es C(R³R³’); X¹ es N y X² es CH; R¹, R¹’, R², R²’, R³ y R³’ se seleccionan independientemente entre hidrógeno, halógeno, hidroxilo, nitro, ciano, amino, C₁₋₆alquilo, C₂₋₆alquenilo, C₁₋₆alcoxi, C₂₋₆alquinilo, C₂₋₆alcanoilo, C₁₋₆tioalquilo, -C(O)OR⁹, -OC(O)R⁹, -NR⁹C(O)R¹⁰, -C(O)NR⁹R¹⁰, -OC(O)NR⁹R¹⁰, -NR⁹C(O)OR¹⁰, C₁₋₂haloalquilo, y C₁₋₂haloalcoxi; R⁹ y R¹⁰ se seleccionan independientemente, cada vez que aparecen, entre hidrógeno, C₁₋₆alquilo, (C₃₋₇cicloalquil)C₀₋₄alquilo, -C₀₋₄alquil(C₃₋₇cicloalquilo), y -O-C₀₋₄alquil(C₃₋₇cicloalquilo); o R¹ y R² se toman juntos para formar un anillo carbocíclico de 3 miembros; o R² y R³ se toman juntos para formar un anillo carbocíclico de 3 a 6 miembros; A es un grupo seleccionado entre los compuestos de fórmula (3) y (4); R⁵ y R⁶ se seleccionan independientemente entre -CHO, -C(O)NH₂, -C(O)NH(CH₃), C₂₋₆alcanoilo, hidrógeno, hidroxilo, halógeno, ciano, nitro, -COOH, -SO₂NH₂, vinilo, C₁₋₆alquilo, C₂₋₆alquenilo, C₁₋₆alcoxi, -C₀₋₄alquil(C₃₋₇cicloalquilo), -C(O)C₀₋₄alquil(C₃₋₇cicloalquilo), -P(O)(OR⁹)₂, -OC(O)R⁹, -C(O)OR⁹, -C(O)N(CH₂CH₂R⁹)(R¹⁰), -NR⁹C(O)R¹⁰, fenilo, y heteroarilo de 5 a 6 miembros; R⁸ y R⁸’ se seleccionan independientemente entre hidrógeno, halógeno, hidroxilo, C₁₋₆alquilo, -C₀₋₄alquil(C₃₋₇cicloalquilo), C₁₋₆alcoxi, y (C₁₋₄alquilamino)C₀₋₂alquilo; o R⁸ y R⁸’ se toman juntos para formar un grupo oxo; o R⁸ y R⁸’ se pueden tomar junto con el átomo de carbono al cual están unidos para formar un anillo carbocíclico de 3 miembros; X¹¹ es N o CR¹¹; X¹² es CR¹²; X¹³ es CR¹³; X¹⁴ es N o CR¹⁴; uno de R¹² y R¹³ se selecciona entre R³¹, y el otro de R¹² y R¹³ se selecciona entre R³²; R³¹ se selecciona entre hidrógeno, halógeno, hidroxilo, nitro, ciano, amino, -COOH, C₁₋₂haloalquilo, C₁₋₂haloalcoxi, C₁₋₆alquilo, -C₀₋₄alquil(C₃₋₇cicloalquilo), C₂₋₆alquenilo, C₂₋₆alcanoilo, C₁₋₆alcoxi, C₂₋₆alqueniloxi, -C(O)OR⁹, C₁₋₆tioalquilo, -C₀₋₄alquilo-NR⁹R¹⁰, -C(O)NR⁹R¹⁰, -SO₂R⁹, -SO₂NR⁹R¹⁰, -OC(O)R⁹, y -C(NR⁹)NR⁹R¹⁰, en donde cada R³¹ distinto de hidrógeno, halógeno, hidroxilo, nitro, ciano, C₁₋₂haloalquilo, y C₁₋₂haloalcoxi no está sustituido o está sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, nitro, ciano, amino, -COOH, -CONH₂, C₁₋₂haloalquilo, y C₁₋₂haloalcoxi, y cada R³¹ también está sustituido opcionalmente con un sustituyente seleccionado entre fenilo y heterociclo de 4 a 7 miembros que contiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O y S; en donde el fenilo o heterociclo de 4 a 7 miembros no está sustituido o está sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, nitro, ciano, C₁₋₆alquilo, C₂₋₆alquenilo, C₂₋₆alcanoilo, C₁₋₆alcoxi, (mono y di-C₁₋₆alquilamino)C₀₋₄alquilo, C₁₋₆alquiléster, -(C₀₋₄alquil)(C₃₋₇cicloalquilo), C₁₋₂haloalquilo, y C₁₋₂haloalcoxi; R³² se selecciona entre: (i) un arilo seleccionado entre el grupo que consiste en fenilo y naftilo; o (ii) un heterociclo de 5 a 6 miembros saturado o insaturado que tiene 1, 2 ó 3 heteroátomos independientemente seleccionado entre N, O ó S, en donde el heterociclo es unido a través de un átomo de carbono en el anillo heterocíclico a un átomo de carbono del anillo A; o (iii) un heteroarilo seleccionado entre el grupo que consiste en piridinilo, pirimidinilo, pirazolilo, pirazinilo, furilo, tienilo, isoxazolilo, tiazolilo, oxadiazolilo, oxazolilo, isotiazol, quinolinilo, isoquinolinilo, benzofuranilo, cinolinilo, indolizinilo, flalazinilo, piridazinilo, triazinilo, pteridinilo, tiadiazolilo, furazanilo, benzofurazanilo, benzotiofenilo, benzotiazolilo, benzooxazolilo, quinazolinilo, quinoxalinilo, naftiridinilo, tetrahidrofuranilo y furopiridilo; en donde cada R³² puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados entre halógeno, hidroxilo, amino, ciano, -CHO, -COOH, -CONH₂, C₁₋₆alquilo, C₂₋₆alquenilo, C₂₋₆alquinilo, -C₁₋₆alcoxi, C₂₋₆alcanoilo, C₁₋₆alquiléster, (mono y di-C₁₋₆alquilamino)C₀₋₂alquilo, C₁₋₂haloalquilo, hidroxi-C₁₋₆alquilo, éster, carbamato, urea, sulfonamida, -C₁₋₆alquil(heterociclo), C₁₋₆alquil(heteroarilo), -C₁₋₆alquil(C₃₋₇cicloalquilo), O-C₁₋₆alquil(C₃₋₇cicloalquilo), B(OH)₂, fosfato, fosfonato y C₁₋₂haloalcoxi; R¹¹ y R¹⁴ se seleccionan independientemente, cada vez que aparecen, entre hidrógeno, halógeno, hidroxilo, nitro, ciano, -O(PO)(OR⁹)₂, -(PO)(OR⁹)₂, C₁₋₆alquilo, C₂₋₆alquenilo, C₂₋₆alquinilo, C₂₋₆alcanoilo, C₁₋₆alcoxi, C₁₋₆tioalquilo, -C₀₋₄alquil(mono y di-C₁₋₆alquilamino), -C₀₋₄alquil(C₃₋₇cicloalquilo), -C₀₋₄alcoxi(C₃₋₇cicloalquilo), C₁₋₂haloalquilo, y C₁₋₂haloalcoxi; R²¹ y R²² se seleccionan independientemente, cada vez que aparecen, entre hidrógeno, hidroxilo, ciano, amino, C₁₋₆alquilo, C₁₋₆haloalquilo, C₁₋₆alcoxi, (C₃₋₇cicloalquil)C₀₋₄alquilo, (fenil)C₀₋₄alquilo, -C₁₋₄alquil-OC(O)OC₁₋₆alquilo, -C₁₋₄alquil-OC(O)C₁₋₆alquilo, -C₁₋₄alquil-C(O)OC₁₋₆alquilo, (heterocicloalquilo de 4 a 7 miembros)C₀₋₄alquilo que tiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O y S, y (heterociclo aromático o insaturado de 5 o 6 miembros)C₀₋₄alquilo que tiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O y S; R²³ se selecciona independientemente, cada vez que aparece, entre C₁₋₆alquilo, C₁₋₆haloalquilo, (aril)C₀₋₄alquilo, (C₃₋₇cicloalquil)C₀₋₄alquilo, (fenil)C₀₋₄alquilo, (heterocicloalquilo de 4 a 7 miembros)C₀₋₄alquilo que tiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O y S, y (heterociclo aromático o insaturado de 5 ó 6 miembros)C₀₋₄alquilo que tiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O y S; R²⁴ y R²⁵ se toman junto con el átomo de nitrógeno al cual están unidos para formar un grupo heterocicloalquilo monocíclico de 4 a 7 miembros, o un grupo heterocíclico bicíclico de 6 a 10 miembros que tiene anillos fusionados, espiro o en puente; L es un compuesto de fórmula (4); R¹⁷ es hidrógeno, C₁₋₆alquilo, o -C₀₋₄alquil(C₃₋₇cicloalquilo); R¹⁸ y R¹⁸’ se seleccionan independientemente entre hidrógeno, halógeno, hidroximetilo, y metilo; m es 0, 1, 2 ó 3; B es un grupo carbocíclico monocíclico o bicíclico; un grupo carbocíclico-oxi monocíclico o bicíclico; un grupo heterocíclico monocíclico, bicíclico o tricíclico que tiene 1, 2, 3, ó 4 heteroátomos independientemente seleccionados entre N, O y S, y entre 4 a 7 átomos en el anillo por anillo; C₂₋₆alquenilo; C₂₋₆alquinilo; -(C₀₋₄alquil)(arilo); -(C₀₋₄alquil)(heteroarilo); o -(C₀₋₄alquil)(bifenilo), y B no está sustituido o está sustituido con uno o más sustituyentes seleccionados independientemente entre R³³ y R³⁴, y 0 ó 1 sustituyente seleccionado entre R³⁵ y R³⁶; R³³ se selecciona independientemente entre halógeno, hidroxilo, -COOH, ciano, C₁₋₆alquilo, C₂₋₆alcanoilo, C₁₋₆alcoxi, -C₀₋₄alquilo-NR⁹R¹⁰, -SO₂R⁹, C₁₋₂haloalquilo, y C₁₋₂haloalcoxi; R³⁴ se selecciona independientemente entre nitro, C₁₋₆alquenilo, C₂₋₆alquinilo, C₁₋₆tioalquilo, -JC₃₋₇cicloalquilo, -B(OH)₂, -JC(O)NR⁹R²³, -JOSO₂OR²¹, -C(O)(CH₂)₁₋₄S(O)R²¹, -O(CH₂)₁₋₄S(O)NR²¹R²², -JOP(O)(OR²¹)(OR²²), -JP(O)(OR²¹)(OR²²), -JOP(O)(OR²¹)R²², -JP(O)(OR²¹)R²², -JOP(O)R²¹R²², -JP(O)R²¹R²², -JSP(O)(OR²¹)(OR²²), -JSP(O)(OR²¹)(R²²), -JSP(O)(R²¹)(R²²), -JNR⁹P(O)(NHR²¹)(NHR²²), -JNR⁹P(O)(OR²¹)(NHR²²), -JNR⁹P(O)(OR²¹)(OR²²), -JC(S)R²¹, -JNR²¹SO₂R²², -JNR⁹S(O)NR¹⁰R²², -JNR⁹SO₂NR¹⁰R²², -JSO₂NR⁹COR²², -JSO₂NR⁹CONR²¹R²², JNR²¹SO₂R²², -JC(O)NR²¹SO₂R²², -JC(NH₂)NR²², -JC(NH₂)NR⁹S(O)₂R²², -JOC(O)NR²¹R²², -JNR²¹C(O)OR²², -JNR²¹OC(O)R²², -(CH₂)₁₋₄C₍O₎NR²¹R²², -JC(O)NR²⁴R²⁵, -JNR⁹C(O)R²¹, -JC(O)R²¹, -JNR⁹C(O)NR¹⁰R²², -CCR²¹, -(CH₂)₁₋₄OC(O)R²¹, y -JC(O)OR²³; en donde cada R³⁴ puede no estar sustituido o estar sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, nitro, ciano, amino, oxo, -B(OH)₂, -Si(CH₃)₃, -COOH, -CONH₂, -P(O)(OH)₂, C₁₋₆alquilo, -C₀₋₄alquil(C₃₋₇cicloalquilo), C₁₋₆alcoxi, -C₀₋₂alquil(mono y di-C₁₋₄alquilamino), C₁₋₆alquiléster, C₁₋₄alquilamino, C₁₋₄hidroxiloalquilo, C₁₋₂haloalquilo, y C₁₋₂haloalcoxi; R³⁵ se selecciona independientemente entre naftilo, naftiloxi, indanilo, (heterocicloalquilo de 4 a 7 miembros)C₀₋₄alquilo que contiene 1 ó 2 heteroátomos seleccionados entre N, O y S, y heterociclo bicíclico que contiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O y S, y que contiene 4 a 7 átomos en cada anillo; en donde cada R³⁵ no está sustituido o está sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, nitro, ciano, C₁₋₆alquilo, C₂₋₆alquenilo, C₂₋₆alcanoilo, C₁₋₆alcoxi, (mono y di-C₁₋₆alquilamino)C₀₋₄alquilo, C₁₋₆alquiléster, -C₀₋₄alquil(C₃₋₇cicloalquilo), -SO₂R⁹, C₁₋₂haloalquilo, y C₁₋₂haloalcoxi; R³⁶ se selecciona independientemente entre tetrazolilo, (fenil)C₀₋₂alquilo, (fenil)C₁₋₂alcoxi, fenoxi, y heteroarilo de 5 ó 6 miembros que contiene 1, 2 ó 3 heteroátomos independientemente seleccionados entre N, O, B y S, en donde cada R³⁶ no está sustituido o está sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, nitro, ciano, C₁₋₆alquilo, C₂₋₆alquenilo, C₂₋₆alcanoilo, C₁₋₆alcoxi, (mono- y di-C₁₋₆alquilamino)C₀₋₄alquilo, C₁₋₆alquiléster, -C₀₋₄alquil(C₃₋₇cicloalquilo), -SO₂R⁹, -OSi(CH₃)₂C(CH₃)₃, -Si(CH₃)₂C(CH₃)₃, C₁₋₂haloalquilo, -S(O)₂R²¹, y C₁₋₂haloalcoxi; y J se selecciona independientemente, cada vez que aparece, entre un enlace covalente, C₁₋₄alquileno, -OC₁₋₄alquileno, C₂₋₄alquenileno, y C₂₋₄alquinileno.
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Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2015223068B2 (en) 2014-02-25 2020-07-30 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders
AR106018A1 (es) 2015-08-26 2017-12-06 Achillion Pharmaceuticals Inc Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos
WO2017035409A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders
WO2017035357A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Phosphonate compounds for treatment of medical disorders
AR105809A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos para el tratamiento de trastornos médicos
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
WO2017035361A1 (en) * 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for the treatment of medical disorders
AR105808A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos de amida para el tratamiento de trastornos médicos
WO2017035408A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Compounds for treatment of immune and inflammatory disorders
WO2017035355A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Ether compounds for treatment of medical disorders
WO2017035351A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of medical disorders
WO2017035401A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amide compounds for treatment of immune and inflammatory disorders
CA3007922A1 (en) * 2015-12-11 2017-06-15 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
EP3589287B1 (en) 2017-03-01 2022-09-14 Achillion Pharmaceuticals, Inc. Macrocyclic compounds for treatment of medical disorders
WO2018160891A1 (en) 2017-03-01 2018-09-07 Achillion Pharmaceutical, Inc. Pharmaceutical compounds for treatment of medical disorders
AU2018227849B2 (en) * 2017-03-01 2022-04-28 Achillion Pharmaceuticals, Inc. Aryl, heteroary, and heterocyclic pharmaceutical compounds for treatment of medical disorders
WO2018229543A2 (en) * 2017-06-14 2018-12-20 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
WO2019028284A1 (en) * 2017-08-02 2019-02-07 Achillion Pharmaceuticals, Inc. THERAPEUTIC REGIMES FOR THE TREATMENT OF NOCTURNAL PAROXYSTIC HEMOGLOBINURIA
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
GB201806022D0 (en) 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
JP2021529833A (ja) 2018-07-03 2021-11-04 アイエフエム デュー インコーポレイテッド Ｓｔｉｎｇ活性に関連する状態を治療するための化合物および組成物
US20230022157A1 (en) * 2018-08-20 2023-01-26 Achillion Pharmaceuticals, Inc. Pharmaceutical compounds for the treatment of complement factor d medical disorders
WO2020051532A2 (en) 2018-09-06 2020-03-12 Achillion Pharmaceuticals, Inc. Macrocyclic compounds for the treatment of medical disorders
EP3847174A4 (en) 2018-09-06 2022-06-15 Achillion Pharmaceuticals, Inc. MORPHIC FORMS OF COMPLEMENT D FACTOR INHIBITORS
AU2019346464A1 (en) 2018-09-25 2021-04-08 Achillion Pharmaceuticals, Inc. Morphic forms of complement factor D inhibitors
WO2020109343A1 (en) 2018-11-29 2020-06-04 F. Hoffmann-La Roche Ag Combination therapy for treatment of macular degeneration
BR112021011727A2 (pt) * 2018-12-17 2021-08-31 Achillion Pharmaceuticals, Inc Dosagem direcionada para o tratamento de distúrbios mediados do complemento
WO2021067801A1 (en) * 2019-10-03 2021-04-08 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
WO2021183555A1 (en) * 2020-03-10 2021-09-16 Achillion Pharmaceuticals, Inc. Ocular drug depot for complement-mediated disorders
WO2022047128A2 (en) * 2020-08-28 2022-03-03 Alexion Pharmaceuticals, Inc. Method for treating complement mediated disorders caused by betacoronaviruses
CN112375027B (zh) * 2020-12-07 2023-03-31 中国药科大学 吲哚磺酰胺类衍生物及其医药用途
US11478484B2 (en) * 2021-03-26 2022-10-25 Consortium “Ukrindustry” Method for preparing a liposomal composition comprising latanoprost, and the pharmacologically active liposomal composition for ophthalmotherapy prepared by this method
WO2023023227A1 (en) 2021-08-20 2023-02-23 Alexion Pharmaceuticals, Inc. Methods for treating sickle cell disease or beta thalassemia using complement alternative pathway inhibitors
WO2023069301A1 (en) * 2021-10-18 2023-04-27 Alexion Pharmaceuticals, Inc. Use of complement factor d inhibitor for treatment of lupus nephritis and immunoglobulin a nephropathy
CN114437043B (zh) * 2022-02-02 2023-06-16 浙江乐普药业股份有限公司 一种抗新冠药物Nirmatrelvir的制备方法
WO2024008121A1 (zh) * 2022-07-06 2024-01-11 南京明德新药研发有限公司 二氟取代的氮杂双环化合物及其应用

Family Cites Families (238)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB929405A (en) 1958-12-22 1963-06-19 Upjohn Co Processes for the encapsulation of particles
GB929401A (en) 1958-12-22 1963-06-19 Upjohn Co Encapsulated emulsions and processes for their preparation
GB969808A (en) 1962-06-08 1964-09-16 Boots Pure Drug Co Ltd Anthelmintic compositions and compounds
IT1148784B (it) 1980-04-09 1986-12-03 Eurand Spa Procedimento per la preparazione di microcapsule in un veicolo liquido
US4946929A (en) 1983-03-22 1990-08-07 Massachusetts Institute Of Technology Bioerodible articles useful as implants and prostheses having predictable degradation rates
US4794000A (en) 1987-01-08 1988-12-27 Synthetic Blood Corporation Coacervate-based oral delivery system for medically useful compositions
US4638045A (en) 1985-02-19 1987-01-20 Massachusetts Institute Of Technology Non-peptide polyamino acid bioerodible polymers
US4806621A (en) 1986-01-21 1989-02-21 Massachusetts Institute Of Technology Biocompatible, bioerodible, hydrophobic, implantable polyimino carbonate article
US5804178A (en) 1986-11-20 1998-09-08 Massachusetts Institute Of Technology Implantation of cell-matrix structure adjacent mesentery, omentum or peritoneum tissue
CA1340581C (en) 1986-11-20 1999-06-08 Joseph P. Vacanti Chimeric neomorphogenesis of organs by controlled cellular implantation using artificial matrices
US5736372A (en) 1986-11-20 1998-04-07 Massachusetts Institute Of Technology Biodegradable synthetic polymeric fibrous matrix containing chondrocyte for in vivo production of a cartilaginous structure
US5019379A (en) 1987-07-31 1991-05-28 Massachusetts Institute Of Technology Unsaturated polyanhydrides
JP2528706B2 (ja) 1988-05-30 1996-08-28 ゼリア新薬工業株式会社 ジヒドロピリジン化合物の製剤組成物
GB8819110D0 (en) 1988-08-11 1988-09-14 Norsk Hydro As Antihypertensive drug & method for production
US5010167A (en) 1989-03-31 1991-04-23 Massachusetts Institute Of Technology Poly(amide-and imide-co-anhydride) for biological application
US5019400A (en) 1989-05-01 1991-05-28 Enzytech, Inc. Very low temperature casting of controlled release microspheres
US5013557A (en) 1989-10-03 1991-05-07 Warner-Lambert Company Taste masking compositions comprising spray dried microcapsules containing sucralfate and methods for preparing same
KR0182801B1 (ko) 1991-04-16 1999-05-01 아만 히데아키 고체 분산체의 제조방법
TW209174B (es) 1991-04-19 1993-07-11 Takeda Pharm Industry Co Ltd
GB9206757D0 (en) 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
AU4198793A (en) 1992-07-24 1994-01-27 Takeda Chemical Industries Ltd. Microparticle preparation and production thereof
US5399665A (en) 1992-11-05 1995-03-21 Massachusetts Institute Of Technology Biodegradable polymers for cell transplantation
US5512600A (en) 1993-01-15 1996-04-30 Massachusetts Institute Of Technology Preparation of bonded fiber structures for cell implantation
US5514378A (en) 1993-02-01 1996-05-07 Massachusetts Institute Of Technology Biocompatible polymer membranes and methods of preparation of three dimensional membrane structures
US5565215A (en) 1993-07-23 1996-10-15 Massachusettes Institute Of Technology Biodegradable injectable particles for imaging
US5543158A (en) 1993-07-23 1996-08-06 Massachusetts Institute Of Technology Biodegradable injectable nanoparticles
GB9322014D0 (en) 1993-10-26 1993-12-15 Co Ordinated Drug Dev Improvements in and relating to carrier particles for use in dry powder inhalers
SE9401108D0 (sv) 1994-03-31 1994-03-31 Leiras Oy Ophthalmic composition I
SE9401109D0 (sv) 1994-03-31 1994-03-31 Leiras Oy Opthalmic composition II
US6074642A (en) 1994-05-02 2000-06-13 Alexion Pharmaceuticals, Inc. Use of antibodies specific to human complement component C5 for the treatment of glomerulonephritis
GB9412273D0 (en) 1994-06-18 1994-08-10 Univ Nottingham Administration means
US6007845A (en) 1994-07-22 1999-12-28 Massachusetts Institute Of Technology Nanoparticles and microparticles of non-linear hydrophilic-hydrophobic multiblock copolymers
US5716404A (en) 1994-12-16 1998-02-10 Massachusetts Institute Of Technology Breast tissue engineering
KR100424931B1 (ko) 1994-12-19 2004-07-05 다이이찌 세이야꾸 가부시기가이샤 서방성입상제제및그제조방법
GB9501841D0 (en) 1995-01-31 1995-03-22 Co Ordinated Drug Dev Improvements in and relating to carrier particles for use in dry powder inhalers
US6413539B1 (en) 1996-10-31 2002-07-02 Poly-Med, Inc. Hydrogel-forming, self-solvating absorbable polyester copolymers, and methods for use thereof
US6123727A (en) 1995-05-01 2000-09-26 Massachusetts Institute Of Technology Tissue engineered tendons and ligaments
GB9515182D0 (en) 1995-07-24 1995-09-20 Co Ordinated Drug Dev Improvements in and relating to powders for use in dry powder inhalers
JP3938938B2 (ja) 1995-07-26 2007-06-27 協和醗酵工業株式会社 キサンチン誘導体の固体分散体または固体分散体製剤
US6095148A (en) 1995-11-03 2000-08-01 Children's Medical Center Corporation Neuronal stimulation using electrically conducting polymers
US5902599A (en) 1996-02-20 1999-05-11 Massachusetts Institute Of Technology Biodegradable polymer networks for use in orthopedic and dental applications
WO1998000170A1 (en) 1996-07-01 1998-01-08 Universiteit Utrecht Hydrolysable hydrogels for controlled release
US6395302B1 (en) 1996-11-19 2002-05-28 Octoplus B.V. Method for the preparation of microspheres which contain colloidal systems
EP0842657A1 (en) 1996-11-19 1998-05-20 OctoPlus B.V. Microspheres for controlled release and processes to prepare these microspheres
AU7808198A (en) 1997-06-03 1998-12-21 Biocryst Pharmaceuticals, Inc. Novel compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation
US5837752A (en) 1997-07-17 1998-11-17 Massachusetts Institute Of Technology Semi-interpenetrating polymer networks
ES2287971T3 (es) 1997-08-11 2007-12-16 Pfizer Products Inc. Dispersiones farmaceuticas solidas con biodisponibilidad incrementada.
US6506577B1 (en) 1998-03-19 2003-01-14 The Regents Of The University Of California Synthesis and crosslinking of catechol containing copolypeptides
US6632922B1 (en) 1998-03-19 2003-10-14 The Regents Of The University Of California Methods and compositions for controlled polypeptide synthesis
US6686446B2 (en) 1998-03-19 2004-02-03 The Regents Of The University Of California Methods and compositions for controlled polypeptide synthesis
CA2325638A1 (en) 1998-03-26 1999-09-30 Hideki Yamada Amide derivatives and nociceptin antagonists
KR100818845B1 (ko) 1998-09-09 2008-04-01 메타베이시스 테라퓨틱스, 인크. 신규한 프럭토스 1,6-비스포스파타제의 헤테로방향족 억제제
GB9827145D0 (en) 1998-12-09 1999-02-03 Co Ordinated Drug Dev Improvements in or relating to powders
US6287588B1 (en) 1999-04-29 2001-09-11 Macromed, Inc. Agent delivering system comprised of microparticle and biodegradable gel with an improved releasing profile and methods of use thereof
AU6868900A (en) 1999-09-03 2001-04-10 Ajinomoto Co., Inc. Novel processes for preparing oxazepine derivatives
GB9927011D0 (en) 1999-11-16 2000-01-12 Advanced Phytonics Ltd Method for the production of particles
EP1239844B1 (en) 1999-12-20 2005-06-08 Nicholas J. Kerkhof Process for producing nanometer particles by fluid bed spray-drying
AP2002002552A0 (en) 1999-12-23 2002-06-30 Pfizer Prod Inc Pharmaceutical compositions providing enhanced drug concentrations.
EP1242055B1 (en) 1999-12-23 2008-04-23 Pfizer Products Inc. Hydrogel-driven drug dosage form
EP1267946A4 (en) 2000-02-28 2008-07-02 Genesegues Inc SYSTEM AND METHOD FOR ENCAPSULATING NANOCAPSULES
AU2001244713A1 (en) 2000-04-03 2001-10-15 Santen Pharmaceutical Co. Ltd. Transporters and drug delivery system by using the same
GB0009468D0 (en) 2000-04-17 2000-06-07 Vectura Ltd Improvements in or relating to formulations for use in inhaler devices
GB0009469D0 (en) 2000-04-17 2000-06-07 Vectura Ltd Improvements in or relating to formalities for use in inhaler devices
US6589549B2 (en) 2000-04-27 2003-07-08 Macromed, Incorporated Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles
US6495164B1 (en) 2000-05-25 2002-12-17 Alkermes Controlled Therapeutics, Inc. I Preparation of injectable suspensions having improved injectability
ATE378039T1 (de) 2000-06-27 2007-11-15 Vectura Ltd Herstellungsverfahren für partikel zur verwendung in einer arzneizusammensetzung
GB2364919A (en) 2000-07-21 2002-02-13 Cambridge Consultants Inhalers
GB0021024D0 (en) 2000-08-29 2000-10-11 Glaxo Group Ltd Inhalation device
EP2316490A3 (en) 2000-10-31 2012-02-01 PR Pharmaceuticals, Inc. Methods and compositions for enhanced delivery of bioactive molecules
US8580306B2 (en) 2000-11-30 2013-11-12 Vectura Limited Particles for use in a pharmaceutical composition
WO2003020797A1 (en) 2001-08-30 2003-03-13 The Regents Of The University Of California Transition metal initiators for controlled poly (beta-peptide) synthesis from beta-lactam monomers
GB0122318D0 (en) 2001-09-14 2001-11-07 Novartis Ag Organic compounds
US7528165B2 (en) * 2001-12-13 2009-05-05 National Health Research Institutes Indole compounds
BR0307516A (pt) 2002-02-01 2004-12-07 Pfizer Prod Inc Formas de dosagem de liberação imediata contendo dispersões de uma droga sólida
EP1546150B1 (en) 2002-07-16 2009-03-04 Amura Therapeutics Limited Pyrrole derivatives as inhibitors of cyteine proteases
AU2003302084A1 (en) 2002-11-15 2004-06-15 Bristol-Myers Squibb Company Open chain prolyl urea-related modulators of androgen receptor function
US7431026B2 (en) * 2003-04-22 2008-10-07 Avalon Advanced Products, Inc Paintball refillers and method for making and using same
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
US20050009910A1 (en) 2003-07-10 2005-01-13 Allergan, Inc. Delivery of an active drug to the posterior part of the eye via subconjunctival or periocular delivery of a prodrug
EP1663180A1 (en) 2003-09-15 2006-06-07 Vectura Limited Pharmaceutical compositions for treating premature ejaculation by pulmonary inhalation
JP2007505932A (ja) 2003-09-18 2007-03-15 マクサイト， インコーポレイテッド 経強膜送達
CN1997691B (zh) 2003-09-23 2011-07-20 北卡罗来纳大学查珀尔希尔分校 光固化的全氟聚醚用作微流体器件中的新材料
SE0302665D0 (sv) 2003-10-07 2003-10-07 Astrazeneca Ab Novel Process
WO2005044186A2 (en) 2003-10-28 2005-05-19 Glaxo Group Limited Inhalable pharmaceutical formulations employing desiccating agents and methods of administering the same
EP1704585B1 (en) 2003-12-19 2017-03-15 The University Of North Carolina At Chapel Hill Methods for fabricating isolated micro- and nano- structures using soft or imprint lithography
EP1713514B1 (en) 2004-01-28 2021-11-24 Johns Hopkins University Drugs and gene carrier particles that rapidly move through mucous barriers
ES2432112T3 (es) 2004-02-10 2013-11-29 The Regents Of The University Of Colorado, A Body Corporate Inhibición del factor B, de la vía alternativa del complemento y métodos relacionados
EP1727811B1 (en) 2004-03-24 2014-11-12 Shire Orphan Therapies GmbH New compounds for the inhibition of angiogenesis and use of thereof
GB0407627D0 (en) 2004-04-02 2004-05-05 Vectura Ltd Corkscrew pump
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
ES2246694B1 (es) 2004-04-29 2007-05-01 Instituto Cientifico Y Tecnologico De Navarra, S.A. Nanoparticulas pegiladas.
US20050244469A1 (en) 2004-04-30 2005-11-03 Allergan, Inc. Extended therapeutic effect ocular implant treatments
US7771742B2 (en) 2004-04-30 2010-08-10 Allergan, Inc. Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods
US8512738B2 (en) 2004-04-30 2013-08-20 Allergan, Inc. Biodegradable intravitreal tyrosine kinase implants
WO2006012373A2 (en) 2004-07-20 2006-02-02 Critical Therapeutics, Inc. Combination therapies of hmgb and complement inhibitors against inflammation
PL370285A1 (pl) 2004-09-23 2006-04-03 Glaxosmithkline Pharmaceuticals Spółka Akcyjna Inhalator proszkowy
PT1855652E (pt) 2005-01-28 2016-01-26 Bend Res Inc Secagem de partículas contendo fármacos
EP1844078B1 (en) 2005-02-03 2016-09-28 Bend Research, Inc Pharmaceutical compositions with enhanced performance
US8663639B2 (en) 2005-02-09 2014-03-04 Santen Pharmaceutical Co., Ltd. Formulations for treating ocular diseases and conditions
BRPI0608152A2 (pt) 2005-02-09 2009-11-10 Macusight Inc formulações para tratamento ocular
MX2007016039A (es) 2005-06-17 2008-10-27 Univ North Carolina Metodos, sistemas y materiales de fabricacion de nanoparticulas.
EP1922364A4 (en) 2005-08-09 2010-04-21 Univ North Carolina METHODS AND MATERIALS FOR MANUFACTURING MICROFLUIDIC DEVICES
US20070071756A1 (en) 2005-09-26 2007-03-29 Peyman Gholam A Delivery of an agent to ameliorate inflammation
US20070178133A1 (en) 2005-11-09 2007-08-02 Liquidia Technologies, Inc. Medical device, materials, and methods
JP2009521493A (ja) 2005-12-23 2009-06-04 アルコン，インコーポレイテッド 眼への受容体チロシンキナーゼ阻害（ＲＴＫｉ）化合物の送達のための医薬製剤
US8944804B2 (en) 2006-01-04 2015-02-03 Liquidia Technologies, Inc. Nanostructured surfaces for biomedical/biomaterial applications and processes thereof
US8663674B2 (en) 2006-01-13 2014-03-04 Surmodics, Inc. Microparticle containing matrices for drug delivery
PL2001466T3 (pl) 2006-03-23 2016-06-30 Santen Pharmaceutical Co Ltd Rapamycyna w małej dawce do leczenia chorób związanych z przepuszczalnością naczyń
US20080166411A1 (en) 2006-04-10 2008-07-10 Pfizer Inc Injectable Depot Formulations And Methods For Providing Sustained Release Of Poorly Soluble Drugs Comprising Nanoparticles
WO2007133808A2 (en) 2006-05-15 2007-11-22 Liquidia Technologies, Inc. Nano-particles for cosmetic applications
SI2041156T1 (sl) * 2006-07-13 2014-04-30 Achillion Pharmacetuticals, Inc. Peptidi 4-amino-4-oksobutanoila kot inhibitorji virusne replikacije
US8465775B2 (en) 2006-07-27 2013-06-18 The University Of North Carolina At Chapel Hill Nanoparticle fabrication methods, systems, and materials for fabricating artificial red blood cells
GB0617480D0 (en) 2006-09-06 2006-10-18 Univ Sheffield Novel nanoparticles
ATE498393T1 (de) 2006-09-08 2011-03-15 Univ Johns Hopkins Zusammensetzungen zur transportintensivierung durch die schleimhaut
US9022970B2 (en) 2006-10-16 2015-05-05 Alcon Research, Ltd. Ophthalmic injection device including dosage control device
EP2108642A1 (en) 2006-10-17 2009-10-14 Kyowa Hakko Kirin Co., Ltd. Jak inhibitor
BRPI0718696A2 (pt) 2006-11-09 2013-12-31 Alcon Res Ltd Matriz de polímero insolúvel em água para liberação de fármaco.
WO2008100304A2 (en) 2006-11-15 2008-08-21 The University Of North Carolina At Chapel Hill Polymer particle composite having high fidelity order, size, and shape particles
ES2397292T3 (es) * 2007-01-15 2013-03-06 Santen Pharmaceutical Co., Ltd Nuevo derivado de indol que tiene actividad inhibidora de cinasa I B
CN105770878A (zh) 2007-10-12 2016-07-20 麻省理工学院 疫苗纳米技术
WO2009091826A2 (en) 2008-01-14 2009-07-23 The Board Of Regents Of The University Of Texas System Compositions and methods related to a human cd19-specific chimeric antigen receptor (h-car)
WO2009100176A2 (en) 2008-02-07 2009-08-13 Abbott Laboratories Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor
CA2720250C (en) 2008-04-04 2018-01-23 Forsight Labs, Llc Therapeutic device for pain management and vision
WO2009132206A1 (en) 2008-04-25 2009-10-29 Liquidia Technologies, Inc. Compositions and methods for intracellular delivery and release of cargo
CN102112118A (zh) 2008-04-25 2011-06-29 北卡罗来纳-查佩尔山大学 特别用于非湿润模型的颗粒复制的可降解化合物及其使用方法
WO2010009087A1 (en) 2008-07-15 2010-01-21 Eyegate Pharmaceuticals, Inc. Iontophoretic delivery of a controlled-release formulation in the eye
NZ591956A (en) 2008-10-08 2012-11-30 Astrazeneca Ab Inhalation device where an airtight medicament containing cavity is closed by a seperating element opened by inhalation
BRPI0923282B1 (pt) 2008-12-05 2019-09-03 Liquidia Tech Inc método para a produção de materiais padronizados
WO2010088548A1 (en) 2009-01-29 2010-08-05 Forsight Labs, Llc Posterior segment drug delivery
US8623395B2 (en) 2010-01-29 2014-01-07 Forsight Vision4, Inc. Implantable therapeutic device
US20120052041A1 (en) 2009-02-04 2012-03-01 The Brigham And Women's Hospital, Inc. Polymeric nanoparticles with enhanced drug-loading and methods of use thereof
JP5969212B2 (ja) 2009-02-10 2016-08-17 シヴィダ・ユーエス・インコーポレイテッドＰｓｉｖｉｄａ Ｕｓ，Ｉｎｃ． 眼用トロカール組立体
WO2010099321A1 (en) 2009-02-26 2010-09-02 The University Of North Carolina At Chapel Hill Interventional drug delivery system and associated methods
US10952965B2 (en) 2009-05-15 2021-03-23 Baxter International Inc. Compositions and methods for drug delivery
CN102596097B (zh) 2009-06-03 2015-05-20 弗赛特实验室有限责任公司 一种眼***件
JP5656996B2 (ja) 2009-07-13 2015-01-21 ザ ユニバーシティ オブ ノース キャロライナ アット チャペル ヒル 工学的に作製されたエアロゾル粒子、およびそれに関連した方法
TWI492769B (zh) 2009-09-23 2015-07-21 Alcon Res Ltd 可注射的水性眼用組成物及其使用之方法
US8410139B2 (en) * 2009-10-07 2013-04-02 Bristol-Myers Squibb Company Prodrugs of a piperidinyl derivative as modulators of chemokine receptor activity
WO2011046204A1 (ja) 2009-10-16 2011-04-21 持田製薬株式会社 非アルコール性脂肪肝炎関連マーカー
WO2011050365A1 (en) 2009-10-23 2011-04-28 Forsight Labs, Llc Conformable therapeutic shield for vision and pain
EP3260092A1 (en) 2009-10-23 2017-12-27 Nexisvision, Inc. Corneal denervation for treatment of ocular pain
TWI478730B (zh) 2009-12-03 2015-04-01 Alcon Res Ltd 眼科乳劑
US8889193B2 (en) 2010-02-25 2014-11-18 The Johns Hopkins University Sustained delivery of therapeutic agents to an eye compartment
US20130071349A1 (en) 2010-03-02 2013-03-21 Allergan, Inc. Biodegradable polymers for lowering intraocular pressure
CN102939282B (zh) 2010-04-16 2015-12-02 Ac免疫有限公司 用于治疗与淀粉状蛋白或淀粉状蛋白样蛋白有关的疾病的化合物
WO2011140203A2 (en) 2010-05-05 2011-11-10 Alcon Research, Ltd. Stabilized ophthalmic galactomannan formulations
US8999312B2 (en) 2010-06-02 2015-04-07 Alcon Research, Ltd. Use of PBO-PEO-PBO block copolymers in ophthalmic compositions
CA2807508A1 (en) 2010-08-05 2012-02-09 Forsight Vision4, Inc. Subconjunctival implant for posterior segment drug delivery
SI2600812T1 (sl) 2010-08-05 2021-12-31 ForSight Vision4, Inc., Naprava za zdravljenje očesa
WO2012019139A1 (en) 2010-08-05 2012-02-09 Forsight Vision4, Inc. Combined drug delivery methods and apparatus
EP3861969A1 (en) 2010-08-05 2021-08-11 ForSight Vision4, Inc. Injector apparatus for drug delivery
US9084976B2 (en) 2010-09-03 2015-07-21 Bend Research, Inc. Spray-drying apparatus and methods of using the same
US10307372B2 (en) 2010-09-10 2019-06-04 The Johns Hopkins University Rapid diffusion of large polymeric nanoparticles in the mammalian brain
US20120121718A1 (en) 2010-11-05 2012-05-17 The Johns Hopkins University Compositions and methods relating to reduced mucoadhesion
WO2012065006A2 (en) 2010-11-11 2012-05-18 Forsight Vision4, Inc. Methods and apparatus to determine porous structures for drug delivery
TW201304822A (zh) 2010-11-15 2013-02-01 Vectura Ltd 組成物及用途
US20140031769A1 (en) 2010-11-19 2014-01-30 Forsight Vision4, Inc. Therapeutic agent formulations for implanted devices
ES2647664T3 (es) * 2011-01-04 2017-12-26 Novartis Ag Compuestos de indol o análogos de los mismos útiles para el tratamiento de la degeneración macular relacionada con la edad (AMD)
WO2012109363A2 (en) 2011-02-08 2012-08-16 The Johns Hopkins University Mucus penetrating gene carriers
WO2012145801A1 (en) 2011-04-29 2012-11-01 Jagat Rakesh Kanwar Nanoparticle
US9060938B2 (en) 2011-05-10 2015-06-23 Bend Research, Inc. Pharmaceutical compositions of active agents and cationic dextran polymer derivatives
US8691750B2 (en) 2011-05-17 2014-04-08 Axolabs Gmbh Lipids and compositions for intracellular delivery of biologically active compounds
MX349079B (es) * 2011-05-27 2017-07-07 Achillion Pharmaceuticals Inc Alifanos, ciclofanos, heterafanos, heterofanos, hetero-heterafanos y metalocenos sustituidos utiles para tratar infecciones por el vhc.
CN103929961A (zh) 2011-06-20 2014-07-16 美国阿尔茨海默病研究所公司 化合物及其治疗应用
MX363606B (es) 2011-06-22 2019-03-28 Apellis Pharmaceuticals Inc Uso de inhibidores del complemento en trastornos crónicos.
EP2739252A4 (en) 2011-08-05 2015-08-12 Forsight Vision4 Inc SMALL MOLECULE ADMINISTRATION USING AN IMPLANTABLE THERAPEUTIC DEVICE
KR102071083B1 (ko) 2011-09-14 2020-01-29 포사이트 비젼5, 인크. 안내 삽입물 장치 및 방법
GB201115874D0 (en) 2011-09-14 2011-10-26 Astrazeneca Ab Inhaler
LT2755600T (lt) 2011-09-16 2021-04-26 Forsight Vision4, Inc. Skysčio pakeitimo aparatas
US20150037428A1 (en) 2011-11-29 2015-02-05 The University Of North Carolina At Chapel Hill Geometrically engineered particles and methods for modulating macrophage or immune responses
EP2790733B1 (en) 2011-12-14 2019-10-30 The Johns Hopkins University Nanoparticles with enhanced mucosal penetration or decreased inflammation
EP2724741B1 (en) 2012-10-26 2017-06-14 Vectura GmbH Inhalation device for use in aerosol therapy
SI2797652T1 (sl) 2011-12-27 2019-03-29 Vectura Gmbh Inhalacijska naprava s sistemom za povratno informacijo
RU2598627C2 (ru) 2012-01-19 2016-09-27 Дзе Джонс Хопкинс Юниверсити Композиции на основе наночастиц с улучшенным проникновением через слизистые оболочки
WO2013116061A1 (en) 2012-02-03 2013-08-08 Forsight Vision4, Inc. Insertion and removal methods and apparatus for therapeutic devices
AU2013229447B2 (en) 2012-03-09 2017-04-13 Vectura Gmbh Mixing channel for an inhalation device and inhalation device
AU2013232300B2 (en) 2012-03-16 2015-12-17 The Johns Hopkins University Non-linear multiblock copolymer-drug conjugates for the delivery of active agents
CN104363924B (zh) 2012-03-16 2018-04-17 约翰霍普金斯大学 用于递送hif‑1抑制剂的控制释放调配物
US20140107025A1 (en) 2012-04-16 2014-04-17 Jade Therapeutics, Llc Ocular drug delivery system
US9827191B2 (en) 2012-05-03 2017-11-28 The Johns Hopkins University Compositions and methods for ophthalmic and/or other applications
WO2013166436A1 (en) 2012-05-03 2013-11-07 Kala Pharmaceuticals, Inc. Pharmaceutical nanoparticles showing improved mucosal transport
EP4008355A1 (en) 2012-05-03 2022-06-08 Kala Pharmaceuticals, Inc. Pharmaceutical nanoparticles showing improved mucosal transport
EP3808339A1 (en) 2012-05-03 2021-04-21 Kala Pharmaceuticals, Inc. Pharmaceutical nanoparticles showing improved mucosal transport
PE20150623A1 (es) 2012-05-04 2015-05-17 Novartis Ag Moduladores de la ruta del complemento y usos de los mismos
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
AU2013256008B2 (en) 2012-05-04 2016-02-25 The Johns Hopkins University Lipid-based drug carriers for rapid penetration through mucus linings
KR102339315B1 (ko) * 2012-06-18 2021-12-15 오메로스 코포레이션 다양한 질환 및 장애의 치료를 위해 masp-1 및/또는 masp-2 및/또는 masp-3를 억제하는 조성물 및 방법
EP2864322B1 (en) 2012-06-20 2016-04-27 Novartis AG Complement pathway modulators and uses thereof
ES2647124T3 (es) * 2012-06-28 2017-12-19 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la ruta del complemento
US9464081B2 (en) 2012-06-28 2016-10-11 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
WO2014002053A1 (en) 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
JP6214647B2 (ja) * 2012-06-28 2017-10-18 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
CA2876993A1 (en) * 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
JP6273274B2 (ja) 2012-06-28 2018-01-31 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
WO2014005150A1 (en) 2012-06-29 2014-01-03 Novartis Ag Crystalline forms of l-(2-((lr,3s,5r)-3-( (2 -fluoro-3 - (trifluoromethoxy) phenyl) carbamoyl) - 2 -azabicycl o [3.1.0] hexan- 2 -yl) - 2 -oxoethyl) - 5 -methyl - 1h - pyrazolo [3, 4 -c] pyridine - 3 - carboxami de and salts thereof
WO2014002059A1 (en) 2012-06-29 2014-01-03 Novartis Ag CRYSTALLINE FORMS OF 1-(2-((1R,3S,5R)-3-(((R)-1-(3-chloro-2-fluorophenyl)ethyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1Hpyrazolo[3,4-c]pyridine-3-carboxamide
EP2872503B1 (en) 2012-07-12 2018-06-20 Novartis AG Complement pathway modulators and uses thereof
ES1077714Y (es) 2012-07-31 2012-12-20 Gutierrez Jose Ramon Perez Envase de madera
PE20150776A1 (es) 2012-09-10 2015-05-21 Hoffmann La Roche 6-aminoacido-heteroarildihidropirimidinas para el tratamiento y profilaxis de la infeccion del virus de la hepatitis b
SG11201502008WA (en) 2012-09-17 2015-04-29 Bind Therapeutics Inc Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using same
AU2013317899A1 (en) 2012-09-20 2015-05-07 Akina, Inc. Biodegradable microcapsules containing filling material
CA2888808C (en) 2012-10-26 2021-11-09 Forsight Vision5, Inc. Ophthalmic system for sustained release of drug to eye
US9773428B2 (en) 2012-12-11 2017-09-26 Fluidity Software, Inc. Computerized system and method for teaching, learning, and assessing step by step solutions to stem problems
AU2014209350B8 (en) 2013-01-23 2019-04-18 Department Of Veterans Affairs (Us) Targeting constructs based on natural antibodies and uses thereof
EP2968113B8 (en) 2013-03-14 2020-10-28 Forsight Vision4, Inc. Systems for sustained intraocular delivery of low solubility compounds from a port delivery system implant
CA2907681C (en) 2013-03-28 2022-11-22 Forsight Vision4, Inc. Ophthalmic implant for delivering therapeutic substances
KR20150139899A (ko) 2013-04-01 2015-12-14 알러간, 인코포레이티드 지속적인 안구내 방출을 위한 마이크로스피어 약물 전달 시스템
JO3425B1 (ar) 2013-07-15 2019-10-20 Novartis Ag مشتقات البابيريدينيل-اندول واستخدامها كعامل متمم لمثبطات b
JP2016169161A (ja) 2013-07-19 2016-09-23 大日本住友製薬株式会社 新規イミダゾピリジン化合物
CN105813578A (zh) 2013-10-15 2016-07-27 弗赛特影像5股份有限公司 用于增加或减少粘液的制剂和方法
CN105849090A (zh) 2013-10-30 2016-08-10 诺华股份有限公司 2-苄基-苯并咪唑补体因子b抑制剂及其用途
JP6546194B2 (ja) 2013-12-06 2019-07-17 アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ 眼性状態を処置するための前房内インプラント
AU2015223068B2 (en) * 2014-02-25 2020-07-30 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders
WO2017035413A2 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of immune and inflammatory disorders
AR105808A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos de amida para el tratamiento de trastornos médicos
AR105809A1 (es) 2015-08-26 2017-11-08 Achillion Pharmaceuticals Inc Compuestos para el tratamiento de trastornos médicos
WO2017035418A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for treatment of immune and inflammatory disorders
WO2017035411A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Ether compounds for treatment of immune and inflammatory disorders
WO2017035357A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Phosphonate compounds for treatment of medical disorders
WO2017035362A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Use of complement pathway inhibitor compounds to mitigate adoptive t-cell therapy associated adverse immune responses
AR106018A1 (es) 2015-08-26 2017-12-06 Achillion Pharmaceuticals Inc Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos
WO2017035352A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Carbamate, ester, and ketone compounds for treatment of medical disorders
WO2017035401A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amide compounds for treatment of immune and inflammatory disorders
WO2017035348A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Alkyne compounds for treatment of medical disorders
WO2017035361A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Disubstituted compounds for the treatment of medical disorders
WO2017035409A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders
WO2017035417A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Phosphonate compounds for treatment of immune and inflammatory disorders
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
WO2017035415A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Alkyne compounds for treatment of immune and inflammatory disorders
WO2017035355A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Ether compounds for treatment of medical disorders
WO2017035408A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Compounds for treatment of immune and inflammatory disorders
WO2017035351A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of medical disorders
CA3007922A1 (en) 2015-12-11 2017-06-15 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
TW202222786A (zh) 2016-02-01 2022-06-16 美商百歐克斯製藥公司 苯并吡唑化合物及其類似物
CN112280762B (zh) * 2020-11-13 2022-11-01 中山俊凯生物技术开发有限公司 一种烟酰胺核糖激酶突变体及其编码基因和应用
CN113832125B (zh) * 2021-10-19 2023-09-26 中山百灵生物技术股份有限公司 一种烟酰胺核糖激酶突变体及其编码基因和应用
CN114107160A (zh) * 2021-12-27 2022-03-01 浙江工业大学 一种烟酰胺核糖激酶基因工程菌及其应用
CN114606213B (zh) * 2022-01-28 2024-05-03 浙江工业大学 一种多聚磷酸激酶突变体、工程菌及其应用

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