IL94634A - Compounds to delay transplant rejection in mammals using rapamycin and a chemotherapeutic agent - Google Patents

Compounds to delay transplant rejection in mammals using rapamycin and a chemotherapeutic agent

Info

Publication number: IL94634A
Authority: IL; Israel
Prior art keywords: rapamycin; transplant rejection; day; amount; administered
Prior art date: 1989-06-06

Application number

IL9463490A

Other languages

English (en)

Hebrew (he)

Other versions

IL94634A0 (en

Original Assignee

Calne Roy

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1989-06-06

Filing date

1990-06-06

Publication date

1996-03-31

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23425763&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL94634(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1990-06-06 Application filed by Calne Roy filed Critical Calne Roy

1991-04-15 Publication of IL94634A0 publication Critical patent/IL94634A0/xx

1996-03-31 Publication of IL94634A publication Critical patent/IL94634A/en

Links

QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 title claims abstract description 89
ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 title claims abstract description 87
229960002930 sirolimus Drugs 0.000 title claims abstract description 87
206010052779 Transplant rejections Diseases 0.000 title claims abstract description 66
230000002401 inhibitory effect Effects 0.000 title claims abstract description 38
241000124008 Mammalia Species 0.000 title claims abstract description 28
239000002246 antineoplastic agent Substances 0.000 title claims abstract description 17
229940127089 cytotoxic agent Drugs 0.000 title claims abstract description 16
239000000203 mixture Substances 0.000 title claims description 27
210000000056 organ Anatomy 0.000 claims abstract description 29
PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims abstract description 16
108010036949 Cyclosporine Proteins 0.000 claims abstract description 16
229930105110 Cyclosporin A Natural products 0.000 claims abstract description 15
QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims abstract description 15
229960001265 ciclosporin Drugs 0.000 claims abstract description 15
QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims abstract description 15
230000005764 inhibitory process Effects 0.000 claims abstract description 14
229930182912 cyclosporin Natural products 0.000 claims abstract description 12
LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 claims abstract description 10
239000003246 corticosteroid Substances 0.000 claims abstract description 10
229960002170 azathioprine Drugs 0.000 claims abstract description 9
229960001334 corticosteroids Drugs 0.000 claims abstract description 9
239000003814 drug Substances 0.000 claims description 19
238000004519 manufacturing process Methods 0.000 claims description 5
239000003112 inhibitor Substances 0.000 claims description 3
239000006186 oral dosage form Substances 0.000 claims 6
239000006201 parenteral dosage form Substances 0.000 claims 6
238000000034 method Methods 0.000 abstract description 4
210000001519 tissue Anatomy 0.000 description 21
241001465754 Metazoa Species 0.000 description 12
241000700159 Rattus Species 0.000 description 11
230000004083 survival effect Effects 0.000 description 9
229940079593 drug Drugs 0.000 description 8
230000000694 effects Effects 0.000 description 8
230000001506 immunosuppresive effect Effects 0.000 description 8
241000282887 Suidae Species 0.000 description 7
231100000331 toxic Toxicity 0.000 description 7
230000002588 toxic effect Effects 0.000 description 7
238000002054 transplantation Methods 0.000 description 7
206010047115 Vasculitis Diseases 0.000 description 6
239000003795 chemical substances by application Substances 0.000 description 6
150000001875 compounds Chemical class 0.000 description 6
239000003018 immunosuppressive agent Substances 0.000 description 6
229940002612 prodrug Drugs 0.000 description 6
239000000651 prodrug Substances 0.000 description 6
241000282472 Canis lupus familiaris Species 0.000 description 5
241000282414 Homo sapiens Species 0.000 description 5
239000004006 olive oil Substances 0.000 description 5
235000008390 olive oil Nutrition 0.000 description 5
231100000419 toxicity Toxicity 0.000 description 5
230000001988 toxicity Effects 0.000 description 5
DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 4
210000002216 heart Anatomy 0.000 description 4
229940125721 immunosuppressive agent Drugs 0.000 description 4
238000002360 preparation method Methods 0.000 description 4
238000002560 therapeutic procedure Methods 0.000 description 4
206010029155 Nephropathy toxic Diseases 0.000 description 3
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
230000015572 biosynthetic process Effects 0.000 description 3
238000010562 histological examination Methods 0.000 description 3
230000007694 nephrotoxicity Effects 0.000 description 3
231100000417 nephrotoxicity Toxicity 0.000 description 3
241000894007 species Species 0.000 description 3
206010062016 Immunosuppression Diseases 0.000 description 2
108010002350 Interleukin-2 Proteins 0.000 description 2
208000029523 Interstitial Lung disease Diseases 0.000 description 2
108700018351 Major Histocompatibility Complex Proteins 0.000 description 2
241000187391 Streptomyces hygroscopicus Species 0.000 description 2
208000025865 Ulcer Diseases 0.000 description 2
230000001154 acute effect Effects 0.000 description 2
230000000843 anti-fungal effect Effects 0.000 description 2
230000000781 anti-lymphocytic effect Effects 0.000 description 2
229940121375 antifungal agent Drugs 0.000 description 2
210000001072 colon Anatomy 0.000 description 2
229940109239 creatinine Drugs 0.000 description 2
239000006185 dispersion Substances 0.000 description 2
-1 e.g. Substances 0.000 description 2
210000001035 gastrointestinal tract Anatomy 0.000 description 2
230000028993 immune response Effects 0.000 description 2
229960003444 immunosuppressant agent Drugs 0.000 description 2
210000003734 kidney Anatomy 0.000 description 2
230000000670 limiting effect Effects 0.000 description 2
206010025482 malaise Diseases 0.000 description 2
238000002559 palpation Methods 0.000 description 2
230000002980 postoperative effect Effects 0.000 description 2
230000020382 suppression by virus of host antigen processing and presentation of peptide antigen via MHC class I Effects 0.000 description 2
238000011287 therapeutic dose Methods 0.000 description 2
206010043554 thrombocytopenia Diseases 0.000 description 2
231100000041 toxicology testing Toxicity 0.000 description 2
230000036269 ulceration Effects 0.000 description 2
DHMQDGOQFOQNFH-UHFFFAOYSA-M Aminoacetate Chemical compound NCC([O-])=O DHMQDGOQFOQNFH-UHFFFAOYSA-M 0.000 description 1
FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 description 1
FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 1
208000014311 Cushing syndrome Diseases 0.000 description 1
206010012735 Diarrhoea Diseases 0.000 description 1
208000009386 Experimental Arthritis Diseases 0.000 description 1
YPINZEGNLULHHT-UHFFFAOYSA-N Fujimycin Natural products COC1CC(CCC1O)C=C(/C)C2OC(=O)C3CCCCCN3C(=O)C(=O)C4(O)OC(C(CC4C)OC)C(OC)C(C)CC(=CC(CC=C)C(=O)CC(O)C2C)C YPINZEGNLULHHT-UHFFFAOYSA-N 0.000 description 1
206010061216 Infarction Diseases 0.000 description 1
108010074338 Lymphokines Proteins 0.000 description 1
102000008072 Lymphokines Human genes 0.000 description 1
FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 description 1
241001529936 Murinae Species 0.000 description 1
206010030113 Oedema Diseases 0.000 description 1
241000282520 Papio Species 0.000 description 1
206010035664 Pneumonia Diseases 0.000 description 1
206010035742 Pneumonitis Diseases 0.000 description 1
241000288906 Primates Species 0.000 description 1
XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
206010037596 Pyelonephritis Diseases 0.000 description 1
208000001647 Renal Insufficiency Diseases 0.000 description 1
241001655322 Streptomycetales Species 0.000 description 1
230000006044 T cell activation Effects 0.000 description 1
210000001744 T-lymphocyte Anatomy 0.000 description 1
150000001298 alcohols Chemical class 0.000 description 1
230000000172 allergic effect Effects 0.000 description 1
208000022531 anorexia Diseases 0.000 description 1
230000000259 anti-tumor effect Effects 0.000 description 1
239000000427 antigen Substances 0.000 description 1
108091007433 antigens Proteins 0.000 description 1
102000036639 antigens Human genes 0.000 description 1
239000007864 aqueous solution Substances 0.000 description 1
208000010668 atopic eczema Diseases 0.000 description 1
210000003719 b-lymphocyte Anatomy 0.000 description 1
230000008901 benefit Effects 0.000 description 1
230000003115 biocidal effect Effects 0.000 description 1
230000000903 blocking effect Effects 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000001185 bone marrow Anatomy 0.000 description 1
239000007894 caplet Substances 0.000 description 1
239000002775 capsule Substances 0.000 description 1
230000000747 cardiac effect Effects 0.000 description 1
210000004027 cell Anatomy 0.000 description 1
229940044683 chemotherapy drug Drugs 0.000 description 1
206010009887 colitis Diseases 0.000 description 1
239000013256 coordination polymer Substances 0.000 description 1
206010061428 decreased appetite Diseases 0.000 description 1
230000003247 decreasing effect Effects 0.000 description 1
230000000881 depressing effect Effects 0.000 description 1
206010012601 diabetes mellitus Diseases 0.000 description 1
238000002651 drug therapy Methods 0.000 description 1
206010014599 encephalitis Diseases 0.000 description 1
238000002474 experimental method Methods 0.000 description 1
230000002538 fungal effect Effects 0.000 description 1
210000000987 immune system Anatomy 0.000 description 1
230000001861 immunosuppressant effect Effects 0.000 description 1
229940073062 imuran Drugs 0.000 description 1
230000007574 infarction Effects 0.000 description 1
230000001524 infective effect Effects 0.000 description 1
238000010255 intramuscular injection Methods 0.000 description 1
239000007927 intramuscular injection Substances 0.000 description 1
201000006370 kidney failure Diseases 0.000 description 1
201000002364 leukopenia Diseases 0.000 description 1
231100001022 leukopenia Toxicity 0.000 description 1
210000004185 liver Anatomy 0.000 description 1
208000020442 loss of weight Diseases 0.000 description 1
210000004072 lung Anatomy 0.000 description 1
210000004698 lymphocyte Anatomy 0.000 description 1
210000003563 lymphoid tissue Anatomy 0.000 description 1
239000003120 macrolide antibiotic agent Substances 0.000 description 1
230000007246 mechanism Effects 0.000 description 1
238000007799 mixed lymphocyte reaction assay Methods 0.000 description 1
238000012544 monitoring process Methods 0.000 description 1
238000013059 nephrectomy Methods 0.000 description 1
239000003921 oil Substances 0.000 description 1
235000019198 oils Nutrition 0.000 description 1
210000000496 pancreas Anatomy 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
229920000053 polysorbate 80 Polymers 0.000 description 1
229940068968 polysorbate 80 Drugs 0.000 description 1
239000000843 powder Substances 0.000 description 1
201000009395 primary hyperaldosteronism Diseases 0.000 description 1
230000002035 prolonged effect Effects 0.000 description 1
230000002829 reductive effect Effects 0.000 description 1
238000011160 research Methods 0.000 description 1
230000004044 response Effects 0.000 description 1
229940063122 sandimmune Drugs 0.000 description 1
210000003491 skin Anatomy 0.000 description 1
229940087854 solu-medrol Drugs 0.000 description 1
239000000243 solution Substances 0.000 description 1
210000000952 spleen Anatomy 0.000 description 1
239000004094 surface-active agent Substances 0.000 description 1
238000001356 surgical procedure Methods 0.000 description 1
239000000725 suspension Substances 0.000 description 1
230000009885 systemic effect Effects 0.000 description 1
239000003826 tablet Substances 0.000 description 1
229960001967 tacrolimus Drugs 0.000 description 1
238000012360 testing method Methods 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
208000016261 weight loss Diseases 0.000 description 1
230000004580 weight loss Effects 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Landscapes

Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Epidemiology (AREA)
Immunology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Gastroenterology & Hepatology (AREA)
Transplantation (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Materials For Medical Uses (AREA)
Medicines Containing Material From Animals Or Micro-Organisms (AREA)

IL9463490A 1989-06-06 1990-06-06 Compounds to delay transplant rejection in mammals using rapamycin and a chemotherapeutic agent IL94634A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US07/362,354 US5100899A (en)	1989-06-06	1989-06-06	Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof

Publications (2)

Publication Number	Publication Date
IL94634A0 IL94634A0 (en)	1991-04-15
IL94634A true IL94634A (en)	1996-03-31

Family

ID=23425763

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL9463490A IL94634A (en)	1989-06-06	1990-06-06	Compounds to delay transplant rejection in mammals using rapamycin and a chemotherapeutic agent

Country Status (18)

Country	Link
US (5)	US5100899A (de)
EP (1)	EP0401747B1 (de)
JP (1)	JP2969150B2 (de)
KR (1)	KR0160957B1 (de)
AT (1)	ATE135215T1 (de)
AU (1)	AU638253B2 (de)
CA (1)	CA2018287C (de)
DE (2)	DE69025803T2 (de)
DK (1)	DK0401747T3 (de)
ES (1)	ES2085299T3 (de)
GR (1)	GR3019792T3 (de)
HK (1)	HK1005704A1 (de)
HU (1)	HU206974B (de)
IL (1)	IL94634A (de)
LU (1)	LU90831I2 (de)
MX (1)	MX173183B (de)
NL (1)	NL300056I2 (de)
SG (1)	SG44632A1 (de)

Families Citing this family (178)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JPH04230389A (ja) *	1990-07-16	1992-08-19	American Home Prod Corp	ラパマイシン誘導体
US5378696A (en) *	1990-09-19	1995-01-03	American Home Products Corporation	Rapamycin esters
US5221670A (en) *	1990-09-19	1993-06-22	American Home Products Corporation	Rapamycin esters
US5358944A (en) *	1990-09-19	1994-10-25	American Home Products Corporation	Rapamycin esters for treating transplantation rejection
US5078999A (en) *	1991-02-22	1992-01-07	American Home Products Corporation	Method of treating systemic lupus erythematosus
US5321009A (en) *	1991-04-03	1994-06-14	American Home Products Corporation	Method of treating diabetes
IL101353A0 (en) *	1991-04-03	1992-11-15	American Home Prod	Pharmaceutical compositions for treating diabetes
US5514686A (en) *	1991-04-26	1996-05-07	Fujisawa Pharmaceutical Co., Ltd.	Use of macrolide compounds for eye diseases
US5138051A (en) *	1991-08-07	1992-08-11	American Home Products Corporation	Rapamycin analogs as immunosuppressants and antifungals
US5776943A (en) *	1991-05-14	1998-07-07	American Home Products Corporation	Rapamycin metabolites
WO1992021341A1 (en) *	1991-05-31	1992-12-10	Pfizer Inc.	Use of rapamycin prodrugs as immunosuppressant agents
ZA924953B (en) *	1991-07-25	1993-04-28	Univ Louisville Res Found	Method of treating ocular inflammation
DE4127737A1 (de) *	1991-08-22	1993-02-25	Hoechst Ag	Arzneimittel zur behandlung von abstossungsreaktionen bei organverpflanzungen
US6133301A (en) *	1991-08-22	2000-10-17	Aventis Pharma Deutschland Gmbh	Pharmaceuticals for the treatment of rejection reactions in organ transplantations
US5164399A (en) *	1991-11-18	1992-11-17	American Home Products Corporation	Rapamycin pyrazoles
GB9125660D0 (en) *	1991-12-03	1992-01-29	Smithkline Beecham Plc	Novel compound
US5516781A (en) *	1992-01-09	1996-05-14	American Home Products Corporation	Method of treating restenosis with rapamycin
US5221740A (en) *	1992-01-16	1993-06-22	American Home Products Corporation	Oxepane isomers of rapamycin useful as immunosuppressive agents
US5801144A (en) *	1992-01-28	1998-09-01	Karpas; Abraham	Use of a compound for the manufacture of a medicament for the treatment of HIV infection
US5262424A (en) *	1992-02-18	1993-11-16	American Home Products Corporation	Composition of sulfonylcarbamates of rapamycin and method of treating diseases requiring immunosuppression therewith
US5177203A (en) *	1992-03-05	1993-01-05	American Home Products Corporation	Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
DK0562853T3 (da)	1992-03-27	1996-07-01	American Home Prod	29-Demethoxyrapamycin til fremkaldelse af immunsuppression
US5288711A (en) *	1992-04-28	1994-02-22	American Home Products Corporation	Method of treating hyperproliferative vascular disease
JP2741285B2 (ja) *	1992-05-22	1998-04-15	千寿製薬株式会社	緑内障治療剤
US5874082A (en) *	1992-07-09	1999-02-23	Chiron Corporation	Humanized anti-CD40 monoclonal antibodies and fragments capable of blocking B cell proliferation
US5747034A (en) *	1992-07-09	1998-05-05	Chiron Corporation	Methods and materials for the induction of T cell anergy
US5397703A (en) *	1992-07-09	1995-03-14	Cetus Oncology Corporation	Method for generation of antibodies to cell surface molecules
US5256790A (en) *	1992-08-13	1993-10-26	American Home Products Corporation	27-hydroxyrapamycin and derivatives thereof
CA2106034A1 (en) *	1992-09-24	1994-03-25	Ralph J. Russo	21-norrapamycin
US5480989A (en) *	1992-10-13	1996-01-02	American Home Products Corporation	Carbamates of rapamycin
US5489680A (en) *	1992-10-13	1996-02-06	American Home Products Corporation	Carbamates of rapamycin
US5480988A (en) *	1992-10-13	1996-01-02	American Home Products Corporation	Carbamates of rapamycin
US5302584A (en) *	1992-10-13	1994-04-12	American Home Products Corporation	Carbamates of rapamycin
US5434260A (en) *	1992-10-13	1995-07-18	American Home Products Corporation	Carbamates of rapamycin
US5262423A (en) *	1992-10-29	1993-11-16	American Home Products Corporation	Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents
US5260300A (en) *	1992-11-19	1993-11-09	American Home Products Corporation	Rapamycin carbonate esters as immuno-suppressant agents
US5482945A (en) *	1992-12-22	1996-01-09	American Home Products Corporation	Innovative technique for immunosuppression involving administration of rapamycin loaded formed blood elements
US5349060A (en) *	1993-01-07	1994-09-20	American Home Products Corporation	Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents
US5252579A (en) *	1993-02-16	1993-10-12	American Home Products Corporation	Macrocyclic immunomodulators
US7279561B1 (en) *	1993-04-23	2007-10-09	Wyeth	Anti-rapamycin monoclonal antibodies
DE69435044T2 (de)	1993-04-23	2008-09-18	Wyeth	Rapamycin - Konjugate und Antikörper
US5504091A (en) *	1993-04-23	1996-04-02	American Home Products Corporation	Biotin esters of rapamycin
AT408520B (de) *	1993-05-27	2001-12-27	Novartis Erfind Verwalt Gmbh	Galenische formulierungen
CH686761A5 (de) *	1993-05-27	1996-06-28	Sandoz Ag	Galenische Formulierungen.
US6106834A (en) *	1993-06-02	2000-08-22	Research Corporation Technologies, Inc.	Use of anti-CD45 leukocyte antigen antibodies for immunomodulation
US6024957A (en) *	1993-06-02	2000-02-15	Research Corporation Technologies, Inc.	Immunomodulators and methods for the prevention and reversal of organ transplant rejection using same
WO1994028897A2 (en) *	1993-06-07	1994-12-22	The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services	Use of an mhc class i suppressor drug for the treatment of autoimmune diseases and transplantation rejection
US20020099067A1 (en) *	1993-07-08	2002-07-25	Ulrich Posanski	Pharmaceutical compositions for sparingly soluble therapeutic agents
US5387680A (en) *	1993-08-10	1995-02-07	American Home Products Corporation	C-22 ring stabilized rapamycin derivatives
US5616588A (en) *	1993-09-30	1997-04-01	American Home Products Corporation	Rapamycin formulation for IV injection
AU688782B2 (en) *	1993-09-30	1998-03-19	Wyeth	Rapamycin formulations for oral administration
US5516770A (en) *	1993-09-30	1996-05-14	American Home Products Corporation	Rapamycin formulation for IV injection
US5536729A (en) *	1993-09-30	1996-07-16	American Home Products Corporation	Rapamycin formulations for oral administration
IL111004A (en) *	1993-09-30	1998-06-15	American Home Prod	Oral formulations of rapamycin
US5378836A (en) *	1993-10-08	1995-01-03	American Home Products Corporation	Rapamycin oximes and hydrazones
US5373014A (en) *	1993-10-08	1994-12-13	American Home Products Corporation	Rapamycin oximes
US5391730A (en) *	1993-10-08	1995-02-21	American Home Products Corporation	Phosphorylcarbamates of rapamycin and oxime derivatives thereof
WO1995011992A1 (en) *	1993-10-27	1995-05-04	The Regents Of The University Of California	Antiviral compounds
US5385908A (en) *	1993-11-22	1995-01-31	American Home Products Corporation	Hindered esters of rapamycin
US5385910A (en) *	1993-11-22	1995-01-31	American Home Products Corporation	Gem-distributed esters of rapamycin
US5385909A (en) *	1993-11-22	1995-01-31	American Home Products Corporation	Heterocyclic esters of rapamycin
US5389639A (en) *	1993-12-29	1995-02-14	American Home Products Company	Amino alkanoic esters of rapamycin
US5525610A (en) *	1994-03-31	1996-06-11	American Home Products Corporation	42-Epi-rapamycin and pharmaceutical compositions thereof
US5898029A (en) *	1994-04-12	1999-04-27	The John Hopkins University	Direct influences on nerve growth of agents that interact with immunophilins in combination with neurotrophic factors
US5362718A (en) *	1994-04-18	1994-11-08	American Home Products Corporation	Rapamycin hydroxyesters
US5463048A (en) *	1994-06-14	1995-10-31	American Home Products Corporation	Rapamycin amidino carbamates
US5798386A (en) *	1994-08-03	1998-08-25	Cell Therapeutics, Inc.	Angiogenic lipid formulations
US5756453A (en) *	1994-08-03	1998-05-26	Cell Therapeutics, Inc.	Use of angiogenic lipids for vascularizing tissue
WO1996006847A1 (en) *	1994-08-31	1996-03-07	Pfizer Inc.	Process for preparing demethylrapamycins
US5491231A (en) *	1994-11-28	1996-02-13	American Home Products Corporation	Hindered N-oxide esters of rapamycin
US5563145A (en) *	1994-12-07	1996-10-08	American Home Products Corporation	Rapamycin 42-oximes and hydroxylamines
US5561138A (en) *	1994-12-13	1996-10-01	American Home Products Corporation	Method of treating anemia
US5496832A (en) *	1995-03-09	1996-03-05	American Home Products Corporation	Method of treating cardiac inflammatory disease
BE1009856A5 (fr)	1995-07-14	1997-10-07	Sandoz Sa	Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule.
JP3089350B2 (ja) *	1995-11-20	2000-09-18	ギルフォードファーマシューティカルズインコーポレイテッド	シクロフィリンロタマーゼ活性の阻害剤
US5780462A (en)	1995-12-27	1998-07-14	American Home Products Corporation	Water soluble rapamycin esters
JP2000506170A (ja) *	1996-03-05	2000-05-23	メデイノックス，インコーポレイテッド	酸化窒素スキャベンジャーを用いる複合治療方法とそのために有用な組成物
EP1208847B8 (de)	1996-07-30	2007-02-14	Novartis AG	Pharmazeutische zusammensetzungen zur behandlung der transplantatabstossung sowie der autoimmun- oder entzündlichen zustände
US5922730A (en) *	1996-09-09	1999-07-13	American Home Products Corporation	Alkylated rapamycin derivatives
US5989591A (en) *	1997-03-14	1999-11-23	American Home Products Corporation	Rapamycin formulations for oral administration
US5985325A (en) *	1997-06-13	1999-11-16	American Home Products Corporation	Rapamycin formulations for oral administration
IT1293795B1 (it) *	1997-07-28	1999-03-10	Angelini Ricerche Spa	Farmaco attivo nel ridurre la produzione di proteina mcp-1
FR2770526B1 (fr)	1997-11-04	2000-01-14	Atochem Elf Sa	Dispersions aqueuses stables a base de polymeres hydrosolubles contenant un dispersant cationique comportant des motifs hydrophobes
WO1999050388A1 (en) *	1998-03-27	1999-10-07	Chong Kun Dang Corporation	Streptomyces sp. producing tautomycetin and immunosuppressant comprising tautomycetin as active ingredient
US6096731A (en) *	1998-06-24	2000-08-01	Institute For Drug Research, Inc.	Method for preventing tissue damage associated with graft-versus-host or host-versus-graft disease following transplantation
US6015809A (en) *	1998-08-17	2000-01-18	American Home Products Corporation	Photocyclized rapamycin
US6297024B1 (en)	1998-10-15	2001-10-02	Cell Activation, Inc.	Methods for assessing complement activation
US6235494B1 (en)	1999-02-08	2001-05-22	The Scripps Research Institute	Substrates for assessing mannan-binding protein-associated serine protease activity and methods using the substrates
US6331547B1 (en)	1999-08-18	2001-12-18	American Home Products Corporation	Water soluble SDZ RAD esters
US6790228B2 (en)	1999-12-23	2004-09-14	Advanced Cardiovascular Systems, Inc.	Coating for implantable devices and a method of forming the same
US20070032853A1 (en)	2002-03-27	2007-02-08	Hossainy Syed F	40-O-(2-hydroxy)ethyl-rapamycin coated stent
US7807211B2 (en)	1999-09-03	2010-10-05	Advanced Cardiovascular Systems, Inc.	Thermal treatment of an implantable medical device
WO2001017953A1 (en)	1999-09-08	2001-03-15	Guilford Pharmaceuticals Inc.	Non-peptidic cyclophilin binding compounds and their use
CN100494182C (zh)	2000-05-12	2009-06-03	基酶有限公司	肿瘤坏死α因子信号的调节因子
US6670355B2 (en) *	2000-06-16	2003-12-30	Wyeth	Method of treating cardiovascular disease
US20020086857A1 (en) *	2000-09-15	2002-07-04	Mcdonald George B.	Method of long-term treatment of graft-versus-host disease using topical active corticosterioids
US20100184732A1 (en) *	2000-09-15	2010-07-22	Mcdonald George	Method of long-term treatment of graft-versus-host disease using topical active corticosteroids
EP1319008B1 (de)	2000-09-19	2008-10-15	Wyeth	Wasserlösliche rapamycin-ester
US6399625B1 (en)	2000-09-27	2002-06-04	Wyeth	1-oxorapamycins
US6399626B1 (en)	2000-10-02	2002-06-04	Wyeth	Hydroxyesters of 7-desmethylrapamycin
JP4202127B2 (ja)	2000-10-02	2008-12-24	ノバルティスバクシンズアンドダイアグノスティックス，インコーポレーテッド	アンタゴニスト抗ｃｄ４０抗体を用いるｂ細胞悪性腫瘍の治療方法
US6440991B1 (en)	2000-10-02	2002-08-27	Wyeth	Ethers of 7-desmethlrapamycin
TWI286074B (en)	2000-11-15	2007-09-01	Wyeth Corp	Pharmaceutical composition containing CCI-779 as an antineoplastic agent
JP2004532187A (ja)	2001-01-25	2004-10-21	ギルフォードファーマシュウティカルズインコーポレイテッド	三置換カルボサイクリックサイクロフィリン結合化合物とその用途
TWI296196B (en) *	2001-04-06	2008-05-01	Wyeth Corp	Antineoplastic combinations
TWI233359B (en) *	2001-04-06	2005-06-01	Wyeth Corp	Pharmaceutical composition for treating neoplasm
US6593362B2 (en)	2001-05-21	2003-07-15	Guilford Pharmaceuticals Inc.	Non-peptidic cyclophilin binding compounds and their use
ZA200603888B (en) *	2001-06-01	2007-05-30	Wyeth Corp	Antineoplastic combinations
UA77200C2 (en)	2001-08-07	2006-11-15	Wyeth Corp	Antineoplastic combination of cci-779 and bkb-569
MXPA04001523A (es)	2001-08-22	2004-05-31	Wyeth Corp	Dialdehidos de rapamicina.
BR0211986A (pt)	2001-08-22	2004-09-28	Wyeth Corp	29-enóis de rapamicina
US6641611B2 (en)	2001-11-26	2003-11-04	Swaminathan Jayaraman	Therapeutic coating for an intravascular implant
US20040137066A1 (en) *	2001-11-26	2004-07-15	Swaminathan Jayaraman	Rationally designed therapeutic intravascular implant coating
US20030153536A1 (en) *	2001-10-25	2003-08-14	Mitchell Glass	Compounds and methods of treating transplant rejection
US6939376B2 (en) *	2001-11-05	2005-09-06	Sun Biomedical, Ltd.	Drug-delivery endovascular stent and method for treating restenosis
US7682387B2 (en)	2002-04-24	2010-03-23	Biosensors International Group, Ltd.	Drug-delivery endovascular stent and method for treating restenosis
US20040024450A1 (en) *	2002-04-24	2004-02-05	Sun Biomedical, Ltd.	Drug-delivery endovascular stent and method for treating restenosis
AU2003247483A1 (en) *	2002-05-30	2003-12-31	The Children's Hospital Of Philadelphia	Methods for treatment of acute lymphocytic leukemia
NZ537829A (en)	2002-07-30	2006-09-29	Wyeth Corp	Parenteral formulations containing a rapamycin hydroxyester
DE60324609D1 (de) *	2002-09-17	2008-12-18	Wyeth Corp	GRANULIERTE FORMULIERUNG DES RAPAMYCINESTERS CCl-779
US8163726B2 (en) *	2002-09-18	2012-04-24	University Of Pennsylvania	Method of inhibiting choroidal neovascularization
ATE493980T1 (de)	2002-11-21	2011-01-15	Genzyme Corp	Verwendung eines diamidderivats zur verhinderung der chronischen transplantatabstossung
AU2003291143A1 (en)	2002-11-21	2004-06-18	Genzyme Corporation	Combination of diamide derivatives and immunosuppressive agents for induction of immune tolerance
AR042938A1 (es) *	2003-02-06	2005-07-06	Wyeth Corp	Uso del cci-779 en el tratamiento de la fibrosis hepatica
UA83484C2 (uk) *	2003-03-05	2008-07-25	Уайт	Спосіб лікування раку грудей комбінацією похідного рапаміцину і інгібітора ароматази - летрозолу, фармацевтична композиція
ATE352301T1 (de) *	2003-04-22	2007-02-15	Wyeth Corp	Antineoplastische zusammensetzungen
US7160867B2 (en) *	2003-05-16	2007-01-09	Isotechnika, Inc.	Rapamycin carbohydrate derivatives
US20050118344A1 (en)	2003-12-01	2005-06-02	Pacetti Stephen D.	Temperature controlled crimping
CA2539324A1 (en) *	2003-09-18	2005-03-31	Macusight, Inc.	Transscleral delivery
US7901451B2 (en) *	2004-09-24	2011-03-08	Biosensors International Group, Ltd.	Drug-delivery endovascular stent and method for treating restenosis
BRPI0516308A2 (pt) *	2004-10-04	2010-06-15	Qlt Usa Inc	composição fluida, métodos de tratamento de uma doença ou disfunção, métodos de liberação local ou sistêmica de um agente biológico, implantes, método de formação de um implante, kit de agente biológico e usos de uma composição fluida
US8313763B2 (en) *	2004-10-04	2012-11-20	Tolmar Therapeutics, Inc.	Sustained delivery formulations of rapamycin compounds
US20060084672A1 (en) *	2004-10-20	2006-04-20	The Hospital For Sick Children	Method for modification of y-secretase activity through inhibition of Fkbp13
US8021849B2 (en)	2004-11-05	2011-09-20	Siemens Healthcare Diagnostics Inc.	Methods and kits for the determination of sirolimus in a sample
JP4974903B2 (ja)	2005-02-09	2012-07-11	参天製薬株式会社	疾患または状態を処置するための液体処方物
US8663639B2 (en) *	2005-02-09	2014-03-04	Santen Pharmaceutical Co., Ltd.	Formulations for treating ocular diseases and conditions
KR20070121754A (ko) *	2005-03-21	2007-12-27	마커사이트, 인코포레이티드	질환 또는 상태의 치료를 위한 약물 송달 시스템
US7189582B2 (en)	2005-04-27	2007-03-13	Dade Behring Inc.	Compositions and methods for detection of sirolimus
JPWO2007037544A1 (ja) *	2005-09-30	2009-04-16	国立大学法人京都大学	制御性ｔ細胞の製造を向上させる薬剤のスクリーニング方法の開発、及び免疫抑制性のマクロライド系抗生剤を用いる制御性ｔ細胞の製造方法
WO2007092620A2 (en)	2006-02-09	2007-08-16	Macusight, Inc.	Stable formulations, and methods of their preparation and use
PL2001466T3 (pl)	2006-03-23	2016-06-30	Santen Pharmaceutical Co Ltd	Rapamycyna w małej dawce do leczenia chorób związanych z przepuszczalnością naczyń
US7943775B2 (en) *	2006-06-21	2011-05-17	The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services	Small molecules for imaging protein-protein interactions
WO2008022256A2 (en) *	2006-08-16	2008-02-21	Blagosklonny Mikhail V	Methods and compositions for preventing or treating age-related diseases
US8067055B2 (en) *	2006-10-20	2011-11-29	Biosensors International Group, Ltd.	Drug-delivery endovascular stent and method of use
US20080097591A1 (en)	2006-10-20	2008-04-24	Biosensors International Group	Drug-delivery endovascular stent and method of use
US20080103584A1 (en) *	2006-10-25	2008-05-01	Biosensors International Group	Temporal Intraluminal Stent, Methods of Making and Using
US20080306098A1 (en) *	2006-11-06	2008-12-11	Mutz Mitchell W	Pharmacokinetics of protease inhibitors and other drugs
EP1938800A1 (de)	2006-12-06	2008-07-02	Ranbaxy Laboratories Limited	Sirolimus-Nanodispersion
US20090054334A1 (en) *	2007-05-23	2009-02-26	Mutz Mitchell W	Combinatorial improvement of bifunctional drug properties
US20090053245A1 (en) *	2007-05-29	2009-02-26	Mutz Mitchell W	Pharmacokinetics and Efficacy of Anti-Angiogenic Drugs and Drugs Treating Diseases of the Blood
US20090068266A1 (en) *	2007-09-11	2009-03-12	Raheja Praveen	Sirolimus having specific particle size and pharmaceutical compositions thereof
US20090130210A1 (en) *	2007-09-11	2009-05-21	Raheja Praveen	Pharmaceutical compositions of sirolimus
KR100930167B1 (ko) *	2007-09-19	2009-12-07	삼성전기주식회사	초광각 광학계
WO2009055042A1 (en) *	2007-10-24	2009-04-30	Amplyx Pharmaceuticals, Inc.	Enhancing the efficacy of anti-infective therapeutics
EP2365802B1 (de)	2008-11-11	2017-08-02	The Board of Regents,The University of Texas System	Mikrokapseln von rapamycin und deren verwendung zur behandlung von krebs
US20100268187A1 (en) *	2009-04-17	2010-10-21	Ranbaxy Laboratories Limited	Packaging for sirolimus and composition thereof
US8716307B2 (en)	2009-05-13	2014-05-06	The Trustees Of The University Of Pennsylvania	Combination antineoplastic therapy
EP2451969A2 (de)	2009-07-07	2012-05-16	University Of Southern California	Biomarker für die frühe diagnose von autoimmunerkrankungen
HUE052213T2 (hu)	2009-11-06	2021-04-28	Univ Leland Stanford Junior	Grafitkilökõdés nem invazív diagnosztizálása szervátültetett betegekben
US9283211B1 (en)	2009-11-11	2016-03-15	Rapamycin Holdings, Llc	Oral rapamycin preparation and use for stomatitis
KR101267813B1 (ko)	2009-12-30	2013-06-04	주식회사 삼양바이오팜	향상된 수용해도를 갖는 라파마이신 함유 고분자나노입자 주사제형 조성물 및 그 제조방법, 및 방사선 요법과 병용하기 위한 항암 조성물
US9687523B2 (en) *	2010-02-04	2017-06-27	University Of Southern California	Compositions and methods for the treatment of sjörgren's syndrome
WO2011128910A2 (en)	2010-03-02	2011-10-20	Rpg Life Sciences Limited	A drug delivery solid dosage formulation of sirolimus
WO2011135580A2 (en)	2010-04-28	2011-11-03	Cadila Healthcare Limited	Pharmaceutical compositions of sirolimus
US9606117B2 (en)	2011-01-13	2017-03-28	University Of Southern California	Bioassay for the early detection of autoimmune diseases
EP2594260A1 (de)	2011-11-18	2013-05-22	LEK Pharmaceuticals d.d.	Feststoffpräparate mit Sirolimus mit erwünschter Bioverfügbarkeit und Herstellungsverfahren dafür
US9365880B2 (en)	2012-04-12	2016-06-14	Natco Pharma Limited	Fermentation process for the production of rapamycin
EP2705856A1 (de)	2012-09-07	2014-03-12	Deutsches Zentrum für Neurodegenerative Erkrankungen e.V.	Verbindungen zur Behandlung von neurodegenerativen Erkrankungen
US20150290176A1 (en)	2012-10-12	2015-10-15	The Board Of Regents Of The University Of Texas System	Use of mtor inhibitors to treat vascular cognitive impairment
EP2968281B1 (de)	2013-03-13	2020-08-05	The Board of Regents of The University of Texas System	Mtor-hemmer zur vorbeugung von darmpolypenwachstum
US9700544B2 (en)	2013-12-31	2017-07-11	Neal K Vail	Oral rapamycin nanoparticle preparations
AU2014373683B2 (en)	2013-12-31	2020-05-07	Rapamycin Holdings, Llc	Oral rapamycin nanoparticle preparations and use
US10765665B2 (en)	2015-11-24	2020-09-08	Melin Jeffrey	Composition comprising combination of rapamycin and an activator of AMP kinase and use thereof for treating diseases
US11066416B2 (en)	2016-02-04	2021-07-20	The Johns Hopkins University	Rapafucin derivative compounds and methods of use thereof
CA3013783A1 (en)	2016-02-04	2017-08-10	The Johns Hopkins University	Rapaglutins, novel inhibitors of glut and use thereof
US10774110B2 (en) *	2016-02-04	2020-09-15	The Johns Hopkins University	Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
KR20190025635A (ko)	2016-06-30	2019-03-11	듀렉트 코퍼레이션	데포 제형
US10682340B2 (en)	2016-06-30	2020-06-16	Durect Corporation	Depot formulations

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ZA737247B (en) *	1972-09-29	1975-04-30	Ayerst Mckenna & Harrison	Rapamycin and process of preparation
US3993749A (en) *	1974-04-12	1976-11-23	Ayerst Mckenna And Harrison Ltd.	Rapamycin and process of preparation
US4316688A (en) *	1980-01-02	1982-02-23	Milton Roskelley	Reinforcing removable post pocket tie-down
US4316885A (en) *	1980-08-25	1982-02-23	Ayerst, Mckenna And Harrison, Inc.	Acyl derivatives of rapamycin
US4650803A (en) *	1985-12-06	1987-03-17	University Of Kansas	Prodrugs of rapamycin

1989
- 1989-06-06 US US07/362,354 patent/US5100899A/en not_active Expired - Lifetime
1990
- 1990-06-04 MX MX021007A patent/MX173183B/es unknown
- 1990-06-05 EP EP90110612A patent/EP0401747B1/de not_active Expired - Lifetime
- 1990-06-05 DE DE69025803T patent/DE69025803T2/de not_active Expired - Lifetime
- 1990-06-05 CA CA002018287A patent/CA2018287C/en not_active Expired - Lifetime
- 1990-06-05 KR KR1019900008274A patent/KR0160957B1/ko not_active Expired - Lifetime
- 1990-06-05 AT AT90110612T patent/ATE135215T1/de active
- 1990-06-05 ES ES90110612T patent/ES2085299T3/es not_active Expired - Lifetime
- 1990-06-05 SG SG1996004582A patent/SG44632A1/en unknown
- 1990-06-05 AU AU56865/90A patent/AU638253B2/en not_active Expired
- 1990-06-05 DK DK90110612T patent/DK0401747T3/da active
- 1990-06-05 DE DE2001199045 patent/DE10199045I2/de active Active
- 1990-06-05 HU HU903487A patent/HU206974B/hu active Protection Beyond IP Right Term
- 1990-06-06 IL IL9463490A patent/IL94634A/en active Protection Beyond IP Right Term
- 1990-06-06 JP JP2146408A patent/JP2969150B2/ja not_active Expired - Lifetime
1991
- 1991-07-31 US US07/738,960 patent/US5212155A/en not_active Expired - Lifetime
1993
- 1993-01-26 US US08/009,570 patent/US5308847A/en not_active Expired - Lifetime
1994
- 1994-02-07 US US08/192,648 patent/US5403833A/en not_active Expired - Lifetime
1995
- 1995-01-24 US US08/377,163 patent/US5461058A/en not_active Expired - Lifetime
1996
- 1996-04-29 GR GR960401172T patent/GR3019792T3/el unknown
1998
- 1998-06-04 HK HK98104904A patent/HK1005704A1/en not_active IP Right Cessation
2001
- 2001-09-10 NL NL300056C patent/NL300056I2/nl unknown
- 2001-09-11 LU LU90831C patent/LU90831I2/fr unknown

Also Published As

Publication number	Publication date
JP2969150B2 (ja)	1999-11-02
EP0401747B1 (de)	1996-03-13
DE10199045I1 (de)	2003-06-05
US5403833A (en)	1995-04-04
EP0401747A3 (de)	1991-07-03
JPH0373158A (ja)	1991-03-28
EP0401747A2 (de)	1990-12-12
CA2018287C (en)	2001-11-20
KR910000169A (ko)	1991-01-29
MX173183B (es)	1994-02-07
DE10199045I2 (de)	2006-07-13
US5212155A (en)	1993-05-18
LU90831I2 (fr)	2001-11-12
ES2085299T3 (es)	1996-06-01
US5461058A (en)	1995-10-24
HUT54047A (en)	1991-01-28
NL300056I1 (nl)	2001-12-01
HU903487D0 (en)	1990-12-28
DE69025803T2 (de)	1996-07-25
GR3019792T3 (en)	1996-07-31
DK0401747T3 (da)	2004-03-08
CA2018287A1 (en)	1990-12-06
NL300056I2 (nl)	2002-04-02
IL94634A0 (en)	1991-04-15
HK1005704A1 (en)	1999-01-22
KR0160957B1 (ko)	1998-12-01
HU206974B (en)	1993-03-01
AU5686590A (en)	1991-01-31
US5100899A (en)	1992-03-31
ATE135215T1 (de)	1996-03-15
AU638253B2 (en)	1993-06-24
DE69025803D1 (de)	1996-04-18
SG44632A1 (en)	1997-12-19
US5308847A (en)	1994-05-03

Legal Events

Date	Code	Title
1996-08-04	FF	Patent granted
1996-10-31	FF	Patent granted
1997-03-18	KB	Patent renewed
2004-03-28	PEL	Intention of commissioner to extend period of protection
2004-07-25	KB	Patent renewed
2005-01-24	EXTP	Application for extension order is pending
2011-12-29	EXTN	Extension order renewed
2012-12-31	EXTN	Extension order renewed
2014-01-30	EXTN	Extension order renewed
2014-07-31	EXTP	Application for extension order is pending

Publication	Publication Date	Title
US5100899A (en)	1992-03-31	Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof
HK1005704B (en)	1999-01-22	Use of rapamycin and derivatives and prodrugs thereof in the manufacture of a medicament for inhibiting transplant rejection in mammals
JP4149905B2 (ja)	2008-09-17	サイクロスポリンａおよび４０−ｏ−（２−ヒドロキシエチル）−ラパマイシンを含む移植拒絶、自己免疫疾患または炎症性状態の処置用医薬組成物
Olsen et al.	1994	Rapamycin inhibits corneal allograft rejection and neovascularization
Hausen et al.	1999	Suppression of acute rejection in allogeneic rat lung transplantation: a study of the efficacy and pharmacokinetics of rapamycin derivative (SDZ RAD) used alone and in combination with a microemulsion formulation of cyclosporine
US8435520B2 (en)	2013-05-07	Combinations of immunosuppressive agents for the treatment or prevention of graft rejections
Kahan	2004	Sirolimus-based immunosuppression: present state of the art
KR100215167B1 (ko)	1999-08-16	면역 억제 조성물
DAVIES et al.	1993	Effect of a short course of rapamycin, cyclosporin A, and donor-specific transfusion on rat cardiac allograft survival
IE83399B1 (en)		Use of rapamycin and derivatives and prodrugs thereof in the manufacture of a medicament for inhibiting transplant rejection in mammals
KR20100126386A (ko)	2010-12-01	철 킬레이터 및 면역억제제의 조합물 및 이의 용도
MACDONALD et al.	2000	Management strategies for nephrotoxicity
US20080089894A1 (en)	2008-04-17	Transplant tolerance by costimulation blockade and T-cell activation-induced apoptosis
Kahan	2001	Sirolimus
Chen et al.	2015	Historical remarks of immunosuppressive therapy in organ transplantation
PROFILE	1999	AY 22989, NSC 226080, NSC 606698, Rapamycin, Rapamune®
Surgeon	1997	NEW IMMUNOSUPPRESSIVE DRUGS IN ORGAN TRANSPLANTATION
Rapamycin	1999	SDZ RAD
Watanabe et al.	1997	The synergistic effect of bactobolamine and tacrolimus on in vitro and in vivo experiments
Trofe et al.	2008	Pharmacotherapeutic Options in Solid Organ Transplantation
Mota	2000	Immunosuppression in kidney transplantation: A review and a personal approach
PT95230B (pt)	1997-09-30	Utilizacao de rapamicina e/ou dos seus derivados e/ou dos seus derivados e/ou pre-farmacos na producao de composicoes farmaceuticas para inibicao da rejeicao de transplantes de orgaos ou tecidos em mamiferos.
AU1550202A (en)	2002-03-21	Graft survival prolongation with porphyrins
MXPA06004707A (en)	2007-04-20	Cci-779 for treating mantle cell lymphoma